Identification

Name
Osimertinib
Accession Number
DB09330
Type
Small Molecule
Groups
Approved
Description

Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy.

Development of third-generation EGFR-TKIs, such as osimertinib, has been in response to altered tumour resistance patterns following treatment and toxic side effects that impact patient quality of life. Treatment with first-generation EGFR-TKIs (gefitinib and erlotinib) has been associated with the development of resistance through activating mutations in the EGFR gene. Second-generation EGFR-TKIs (afatinib and dacomitinib) were then developed to be more potent inhibitors, although their use is associated with increased toxicity through nonspecific targeting of wild-type EGFR. In contrast, third-generation inhibitors are specific for the gate-keeper T790M mutations which increases ATP binding activity to EGFR and result in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.

Structure
Thumb
Synonyms
  • Mereletinib
  • N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
External IDs
AZD 9291 / AZD-9291 / AZD9291
Product Ingredients
IngredientUNIICASInChI Key
Osimertinib mesylateRDL94R2A161421373-66-1FUKSNUHSJBTCFJ-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TagrissoTablet, film coated40 mgOralAstra Zeneca Ab2016-02-02Not applicableEu
TagrissoTablet80 mgOralAstra Zeneca2016-07-19Not applicableCanada
TagrissoTablet, film coated40 mgOralAstra Zeneca Ab2016-02-02Not applicableEu
TagrissoTablet, film coated80 1/1OralAstra Zeneca Lp2015-11-13Not applicableUs
TagrissoTablet40 mgOralAstra Zeneca2016-07-19Not applicableCanada
TagrissoTablet, film coated80 mgOralAstra Zeneca Ab2016-02-02Not applicableEu
TagrissoTablet, film coated40 1/1OralAstra Zeneca Lp2015-11-13Not applicableUs
TagrissoTablet, film coated80 mgOralAstra Zeneca Ab2016-02-02Not applicableEu
Categories
UNII
3C06JJ0Z2O
CAS number
1421373-65-0
Weight
Average: 499.619
Monoisotopic: 499.269573331
Chemical Formula
C28H33N7O2
InChI Key
DUYJMQONPNNFPI-UHFFFAOYSA-N
InChI
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
IUPAC Name
N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
SMILES
COC1=C(NC2=NC=CC(=N2)C2=CN(C)C3=C2C=CC=C3)C=C(NC(=O)C=C)C(=C1)N(C)CCN(C)C

Pharmacology

Indication

Osimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.

Structured Indications
Pharmacodynamics

A pharmacokinetic/pharmacodynamic analysis suggested a concentration-dependent QTc interval prolongation of 14 msec (upper bound of two-sided 90% CI: 16 msec) at a dose of osimertinib 80 mg.

Mechanism of action

Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs. As a third-generation tyrosine kinase inhibitor, osimertinib is specific for the gate-keeper T790M mutation which increases ATP binding activity to EGFR and results in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.

TargetActionsOrganism
AEpidermal growth factor receptor
inhibitor
Human
Absorption

The median time to Cmax was found to be 6 hours.

Volume of distribution

The mean volume of distribution at steady state is 986 L.

Protein binding

Plasma protein binding is likely high due to its physiochemical properties.

Metabolism

Osimertinib is metabolized to at least two pharmacologically active metabolites, AZ7550 and AZ5104, that circulate at approximately 10% of the concentration of the parent compound. Biochemical assays have shown that AZ7550 has similar potency and efficacy to osimertinib, while AZ5104 is more potent against mutant and wild-type EGFR. The main metabolic pathways are oxidation (predominantly by CYP3A) and dealkylation.

Route of elimination

Osimertinib is primarily eliminated through excretion in the feces (68%), to a lesser extent through urine (14%), while only 2% is excreted unchanged.

Half life

The population estimated mean half-life is 48 hours.

Clearance

Oral clearance is 14.2 L/hr.

Toxicity

Across clinical trials, interstitial lung disease (ILD)/pneumonitis occurred in 3.3% of treated patients with 0.5% of these being fatal. There is also a change of QTc interval prolongation; electrocardiogram and electrolytes should be monitored in patients with a history or predisposition for QTc prolongation. Cardiomyopathy occurred in 1.4% of patients, therefore left ventricular ejection fraction (LVEF) should be measured at baseline and then every 3 months during treatment. Osimertinib can cause embryo-fetal toxicity, requiring female patients to take effective birth control during therapy and for 6 weeks after final dose.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Osimertinib.Approved
AbirateroneThe serum concentration of Abiraterone can be increased when it is combined with Osimertinib.Approved
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Osimertinib.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Osimertinib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Osimertinib.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Osimertinib.Experimental
AdinazolamThe serum concentration of Adinazolam can be increased when it is combined with Osimertinib.Approved
AlbendazoleThe serum concentration of Albendazole can be increased when it is combined with Osimertinib.Approved, Vet Approved
AlclometasoneThe serum concentration of Alclometasone can be increased when it is combined with Osimertinib.Approved
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Osimertinib.Approved, Illicit
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Osimertinib.Approved, Investigational
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Osimertinib.Approved, Investigational
AllylestrenolThe serum concentration of Allylestrenol can be increased when it is combined with Osimertinib.Approved
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Osimertinib.Approved, Investigational
AlogliptinThe serum concentration of Alogliptin can be increased when it is combined with Osimertinib.Approved
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Osimertinib.Approved, Withdrawn
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Osimertinib.Approved, Investigational
AmbroxolThe serum concentration of Ambroxol can be increased when it is combined with Osimertinib.Approved, Investigational
AminophenazoneThe serum concentration of Aminophenazone can be increased when it is combined with Osimertinib.Approved, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Osimertinib.Approved
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Osimertinib.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Osimertinib.Approved
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Osimertinib.Approved
AmprenavirThe serum concentration of Amprenavir can be increased when it is combined with Osimertinib.Approved
AnagrelideThe serum concentration of Anagrelide can be decreased when it is combined with Osimertinib.Approved
AntipyrineThe serum concentration of Antipyrine can be increased when it is combined with Osimertinib.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Osimertinib.Approved
ApremilastThe serum concentration of Apremilast can be increased when it is combined with Osimertinib.Approved, Investigational
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Osimertinib.Approved, Investigational
ArgatrobanThe serum concentration of Argatroban can be increased when it is combined with Osimertinib.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Osimertinib.Approved, Investigational
ArtemetherThe serum concentration of Artemether can be increased when it is combined with Osimertinib.Approved
AsenapineThe serum concentration of Asenapine can be increased when it is combined with Osimertinib.Approved
AstemizoleThe serum concentration of Astemizole can be increased when it is combined with Osimertinib.Approved, Withdrawn
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Osimertinib.Approved, Investigational
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Osimertinib.Approved
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Osimertinib.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Osimertinib.Approved, Investigational
AzelastineThe serum concentration of Azelastine can be increased when it is combined with Osimertinib.Approved
AzithromycinThe serum concentration of Azithromycin can be increased when it is combined with Osimertinib.Approved
BanoxantroneThe serum concentration of Banoxantrone can be increased when it is combined with Osimertinib.Investigational
BedaquilineThe serum concentration of Bedaquiline can be increased when it is combined with Osimertinib.Approved
BendamustineThe serum concentration of Bendamustine can be decreased when it is combined with Osimertinib.Approved, Investigational
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Osimertinib.Approved, Illicit
Benzyl alcoholThe serum concentration of Benzyl alcohol can be increased when it is combined with Osimertinib.Approved
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Osimertinib.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Osimertinib.Approved, Investigational
BexaroteneThe serum concentration of Bexarotene can be increased when it is combined with Osimertinib.Approved, Investigational
BezafibrateThe serum concentration of Bezafibrate can be increased when it is combined with Osimertinib.Approved
BicalutamideThe serum concentration of Bicalutamide can be increased when it is combined with Osimertinib.Approved
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Osimertinib.Approved
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Osimertinib.Approved, Withdrawn
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Osimertinib.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Osimertinib.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Osimertinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Osimertinib.Approved
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Osimertinib.Approved
BrinzolamideThe serum concentration of Brinzolamide can be increased when it is combined with Osimertinib.Approved
BrivaracetamThe serum concentration of Brivaracetam can be increased when it is combined with Osimertinib.Approved, Investigational
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Osimertinib.Approved, Illicit
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Osimertinib.Approved, Investigational
BrompheniramineThe serum concentration of Brompheniramine can be increased when it is combined with Osimertinib.Approved
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Osimertinib.Approved
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Osimertinib.Approved, Investigational
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Bupropion can be increased when it is combined with Osimertinib.Approved
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Osimertinib.Approved, Investigational
BusulfanThe serum concentration of Busulfan can be increased when it is combined with Osimertinib.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Osimertinib.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Osimertinib.Approved
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Osimertinib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Osimertinib.Approved
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Osimertinib.Approved, Nutraceutical
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Osimertinib.Approved
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Osimertinib.Approved, Investigational
CarbinoxamineThe serum concentration of Carbinoxamine can be increased when it is combined with Osimertinib.Approved
CariprazineThe serum concentration of Cariprazine can be increased when it is combined with Osimertinib.Approved
CarmustineThe serum concentration of Carmustine can be decreased when it is combined with Osimertinib.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Osimertinib.Approved, Investigational
CelecoxibThe serum concentration of Celecoxib can be increased when it is combined with Osimertinib.Approved, Investigational
CeliprololThe serum concentration of Celiprolol can be increased when it is combined with Osimertinib.Approved, Investigational
CephalexinThe serum concentration of Cephalexin can be increased when it is combined with Osimertinib.Approved, Vet Approved
CeritinibThe serum concentration of Osimertinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Osimertinib.Withdrawn
CevimelineThe serum concentration of Cevimeline can be increased when it is combined with Osimertinib.Approved
Chenodeoxycholic acidThe serum concentration of Chenodeoxycholic acid can be increased when it is combined with Osimertinib.Approved
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Osimertinib.Approved, Illicit
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Osimertinib.Approved, Vet Approved
ChlorphenamineThe serum concentration of Chlorphenamine can be increased when it is combined with Osimertinib.Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Osimertinib.Approved, Vet Approved
ChlorzoxazoneThe serum concentration of Chlorzoxazone can be increased when it is combined with Osimertinib.Approved
CholecalciferolThe serum concentration of Cholecalciferol can be increased when it is combined with Osimertinib.Approved, Nutraceutical
CiclesonideThe serum concentration of Ciclesonide can be increased when it is combined with Osimertinib.Approved, Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Osimertinib.Approved
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Osimertinib.Approved
CinnarizineThe serum concentration of Cinnarizine can be decreased when it is combined with Osimertinib.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Osimertinib.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Osimertinib.Approved
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Osimertinib.Approved
ClenbuterolThe serum concentration of Clenbuterol can be decreased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
ClevidipineThe serum concentration of Clevidipine can be decreased when it is combined with Osimertinib.Approved
ClindamycinThe serum concentration of Clindamycin can be increased when it is combined with Osimertinib.Approved, Vet Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Osimertinib.Approved, Illicit
ClofazimineThe serum concentration of Clofazimine can be increased when it is combined with Osimertinib.Approved, Investigational
ClofibrateThe serum concentration of Clofibrate can be increased when it is combined with Osimertinib.Approved, Investigational
clomethiazoleThe serum concentration of clomethiazole can be increased when it is combined with Osimertinib.Investigational
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Osimertinib.Approved, Vet Approved
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Osimertinib.Approved, Illicit
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Osimertinib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Osimertinib.Approved, Nutraceutical
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Osimertinib.Approved, Illicit
ClotiazepamThe serum concentration of Clotiazepam can be increased when it is combined with Osimertinib.Approved, Illicit
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Osimertinib.Approved
CobicistatThe serum concentration of Osimertinib can be increased when it is combined with Cobicistat.Approved
CocaineThe serum concentration of Cocaine can be increased when it is combined with Osimertinib.Approved, Illicit
CodeineThe serum concentration of Codeine can be increased when it is combined with Osimertinib.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Osimertinib.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Osimertinib.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated estrogens can be increased when it is combined with Osimertinib.Approved
CopanlisibThe serum concentration of Copanlisib can be increased when it is combined with Osimertinib.Approved
Cortisone acetateThe serum concentration of Cortisone acetate can be increased when it is combined with Osimertinib.Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Osimertinib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Osimertinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Osimertinib.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Osimertinib.Experimental
CytarabineThe serum concentration of Cytarabine can be increased when it is combined with Osimertinib.Approved, Investigational
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Osimertinib.Approved
DacarbazineThe serum concentration of Dacarbazine can be decreased when it is combined with Osimertinib.Approved, Investigational
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Osimertinib.Approved
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Osimertinib.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Osimertinib.Approved
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Osimertinib.Approved, Investigational
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Osimertinib.Approved, Investigational
DarunavirThe serum concentration of Darunavir can be increased when it is combined with Osimertinib.Approved
DasabuvirThe serum concentration of Dasabuvir can be increased when it is combined with Osimertinib.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Osimertinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Osimertinib.Approved
DeflazacortThe serum concentration of Deflazacort can be increased when it is combined with Osimertinib.Approved
DelavirdineThe serum concentration of Delavirdine can be increased when it is combined with Osimertinib.Approved
DesipramineThe serum concentration of Desipramine can be decreased when it is combined with Osimertinib.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Osimertinib.Approved
DesvenlafaxineThe serum concentration of Desvenlafaxine can be increased when it is combined with Osimertinib.Approved
DeutetrabenazineThe serum concentration of Deutetrabenazine can be increased when it is combined with Osimertinib.Approved, Investigational
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
Dexchlorpheniramine maleateThe serum concentration of Dexchlorpheniramine maleate can be increased when it is combined with Osimertinib.Approved
DexfenfluramineThe serum concentration of Dexfenfluramine can be decreased when it is combined with Osimertinib.Approved, Illicit, Investigational, Withdrawn
DexlansoprazoleThe serum concentration of Dexlansoprazole can be increased when it is combined with Osimertinib.Approved
DextromethorphanThe serum concentration of Dextromethorphan can be increased when it is combined with Osimertinib.Approved
DextropropoxypheneThe serum concentration of Dextropropoxyphene can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational, Withdrawn
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Osimertinib.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Osimertinib.Approved, Vet Approved
DienogestThe serum concentration of Dienogest can be increased when it is combined with Osimertinib.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Osimertinib.Approved, Investigational
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Osimertinib.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Osimertinib.Approved
DihydrocodeineThe serum concentration of Dihydrocodeine can be increased when it is combined with Osimertinib.Approved, Illicit
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Osimertinib.Approved
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Osimertinib.Approved
DinoprostoneThe serum concentration of Dinoprostone can be decreased when it is combined with Osimertinib.Approved
DiphenhydramineThe serum concentration of Diphenhydramine can be decreased when it is combined with Osimertinib.Approved
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Osimertinib.Approved
DisulfiramThe serum concentration of Disulfiram can be increased when it is combined with Osimertinib.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Osimertinib.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Osimertinib.Approved
DolasetronThe serum concentration of Dolasetron can be increased when it is combined with Osimertinib.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
DonepezilThe serum concentration of Donepezil can be increased when it is combined with Osimertinib.Approved
DorzolamideThe serum concentration of Dorzolamide can be increased when it is combined with Osimertinib.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Osimertinib.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Osimertinib.Approved, Investigational
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Osimertinib.Approved, Illicit
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Osimertinib.Approved
DuloxetineThe serum concentration of Duloxetine can be decreased when it is combined with Osimertinib.Approved
DutasterideThe serum concentration of Dutasteride can be increased when it is combined with Osimertinib.Approved, Investigational
EfavirenzThe serum concentration of Efavirenz can be increased when it is combined with Osimertinib.Approved, Investigational
ElbasvirThe serum concentration of Elbasvir can be increased when it is combined with Osimertinib.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Osimertinib.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Osimertinib.Approved
EltrombopagThe serum concentration of Eltrombopag can be decreased when it is combined with Osimertinib.Approved
ElvitegravirThe serum concentration of Elvitegravir can be increased when it is combined with Osimertinib.Approved
EnalaprilThe serum concentration of Enalapril can be increased when it is combined with Osimertinib.Approved, Vet Approved
EnasidenibThe serum concentration of Enasidenib can be increased when it is combined with Osimertinib.Approved
EnzalutamideThe serum concentration of Enzalutamide can be increased when it is combined with Osimertinib.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Osimertinib.Approved, Investigational
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Osimertinib.Approved
ErgocalciferolThe serum concentration of Ergocalciferol can be increased when it is combined with Osimertinib.Approved, Nutraceutical
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Osimertinib.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Osimertinib.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Osimertinib.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Osimertinib.Approved, Investigational
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Osimertinib.Approved, Vet Approved
EscitalopramThe serum concentration of Escitalopram can be increased when it is combined with Osimertinib.Approved, Investigational
EsomeprazoleThe serum concentration of Esomeprazole can be increased when it is combined with Osimertinib.Approved, Investigational
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Osimertinib.Approved, Illicit
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
Estradiol valerate/DienogestThe serum concentration of Estradiol valerate/Dienogest can be increased when it is combined with Osimertinib.Approved, Investigational
EstramustineThe serum concentration of Estramustine can be increased when it is combined with Osimertinib.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be increased when it is combined with Osimertinib.Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Osimertinib.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be increased when it is combined with Osimertinib.Approved
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Osimertinib.Approved
EthanolThe serum concentration of Ethanol can be increased when it is combined with Osimertinib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Osimertinib.Approved
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Osimertinib.Approved
EthylmorphineThe serum concentration of Ethylmorphine can be increased when it is combined with Osimertinib.Approved, Illicit
EtizolamThe serum concentration of Etizolam can be increased when it is combined with Osimertinib.Approved
EtonogestrelThe serum concentration of Etonogestrel can be increased when it is combined with Osimertinib.Approved, Investigational
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Osimertinib.Approved
EtoricoxibThe serum concentration of Etoricoxib can be increased when it is combined with Osimertinib.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be increased when it is combined with Osimertinib.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Osimertinib.Approved
ExemestaneThe serum concentration of Exemestane can be increased when it is combined with Osimertinib.Approved, Investigational
FamciclovirThe serum concentration of Famciclovir can be increased when it is combined with Osimertinib.Approved
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Osimertinib.Approved
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Osimertinib.Approved, Investigational
FenofibrateThe serum concentration of Fenofibrate can be increased when it is combined with Osimertinib.Approved
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Osimertinib.Approved
FinasterideThe serum concentration of Finasteride can be increased when it is combined with Osimertinib.Approved
FingolimodThe serum concentration of Fingolimod can be increased when it is combined with Osimertinib.Approved, Investigational
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Osimertinib.Approved
FlunarizineThe serum concentration of Flunarizine can be decreased when it is combined with Osimertinib.Approved
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Osimertinib.Approved, Investigational
FlunitrazepamThe serum concentration of Flunitrazepam can be increased when it is combined with Osimertinib.Approved, Illicit
FluorometholoneThe serum concentration of Fluorometholone can be increased when it is combined with Osimertinib.Approved
FluorouracilThe serum concentration of Fluorouracil can be decreased when it is combined with Osimertinib.Approved
FluoxetineThe serum concentration of Fluoxetine can be increased when it is combined with Osimertinib.Approved, Vet Approved
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Osimertinib.Approved, Illicit
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Osimertinib.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Osimertinib.Approved
Fluticasone propionateThe serum concentration of Fluticasone propionate can be increased when it is combined with Osimertinib.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Osimertinib.Approved
FluvoxamineThe serum concentration of Fluvoxamine can be decreased when it is combined with Osimertinib.Approved, Investigational
FosamprenavirThe serum concentration of Fosamprenavir can be increased when it is combined with Osimertinib.Approved
FosphenytoinThe serum concentration of Osimertinib can be decreased when it is combined with Fosphenytoin.Approved
FrovatriptanThe serum concentration of Frovatriptan can be decreased when it is combined with Osimertinib.Approved, Investigational
FulvestrantThe serum concentration of Fulvestrant can be increased when it is combined with Osimertinib.Approved, Investigational
GalantamineThe serum concentration of Galantamine can be increased when it is combined with Osimertinib.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Osimertinib.Approved, Investigational
GemfibrozilThe serum concentration of Gemfibrozil can be increased when it is combined with Osimertinib.Approved
GenisteinThe serum concentration of Genistein can be decreased when it is combined with Osimertinib.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Osimertinib.Experimental
GlipizideThe serum concentration of Glipizide can be increased when it is combined with Osimertinib.Approved
GlyburideThe serum concentration of Glyburide can be increased when it is combined with Osimertinib.Approved
GranisetronThe serum concentration of Granisetron can be increased when it is combined with Osimertinib.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Osimertinib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Osimertinib.Investigational, Withdrawn
GuanabenzThe serum concentration of Guanabenz can be decreased when it is combined with Osimertinib.Approved, Investigational
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Osimertinib.Approved, Investigational
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Osimertinib.Approved
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Osimertinib.Approved
HalothaneThe serum concentration of Halothane can be increased when it is combined with Osimertinib.Approved, Vet Approved
HesperetinThe serum concentration of Hesperetin can be decreased when it is combined with Osimertinib.Approved
HexobarbitalThe serum concentration of Hexobarbital can be increased when it is combined with Osimertinib.Approved
HistamineThe serum concentration of Histamine can be increased when it is combined with Osimertinib.Approved, Investigational
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Osimertinib.Approved, Illicit
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Osimertinib.Approved, Vet Approved
HydromorphoneThe serum concentration of Hydromorphone can be increased when it is combined with Osimertinib.Approved, Illicit
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Osimertinib.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Osimertinib.Approved
IcotinibThe serum concentration of Icotinib can be increased when it is combined with Osimertinib.Approved, Investigational
IdelalisibThe serum concentration of Osimertinib can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of Ifosfamide can be increased when it is combined with Osimertinib.Approved
IloperidoneThe serum concentration of Iloperidone can be increased when it is combined with Osimertinib.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Osimertinib.Approved
ImidafenacinThe serum concentration of Imidafenacin can be increased when it is combined with Osimertinib.Approved, Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Osimertinib.Approved
ImiquimodThe serum concentration of Imiquimod can be increased when it is combined with Osimertinib.Approved, Investigational
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Osimertinib.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Osimertinib.Approved
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Osimertinib.Approved
Ipratropium bromideThe serum concentration of Ipratropium bromide can be increased when it is combined with Osimertinib.Approved
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Osimertinib.Approved, Investigational
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Osimertinib.Approved, Investigational
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Osimertinib.Approved
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Osimertinib.Approved
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Osimertinib.Approved
ItraconazoleThe serum concentration of Itraconazole can be increased when it is combined with Osimertinib.Approved, Investigational
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Osimertinib.Approved
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Osimertinib.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Osimertinib.Approved, Vet Approved
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Osimertinib.Approved, Investigational
IxazomibThe serum concentration of Ixazomib can be increased when it is combined with Osimertinib.Approved
KetamineThe serum concentration of Ketamine can be increased when it is combined with Osimertinib.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Osimertinib.Approved
KetobemidoneThe serum concentration of Ketobemidone can be increased when it is combined with Osimertinib.Approved, Investigational
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Osimertinib.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Osimertinib.Experimental
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Osimertinib.Approved, Investigational
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Osimertinib.Approved, Investigational
LaquinimodThe serum concentration of Laquinimod can be increased when it is combined with Osimertinib.Investigational
LeflunomideThe serum concentration of Leflunomide can be decreased when it is combined with Osimertinib.Approved, Investigational
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Osimertinib.Approved
LercanidipineThe serum concentration of Lercanidipine can be increased when it is combined with Osimertinib.Approved, Investigational
LetrozoleThe serum concentration of Letrozole can be increased when it is combined with Osimertinib.Approved, Investigational
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Osimertinib.Approved, Investigational
LevocetirizineThe serum concentration of Levocetirizine can be increased when it is combined with Osimertinib.Approved
Levomethadyl AcetateThe serum concentration of Levomethadyl Acetate can be increased when it is combined with Osimertinib.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Osimertinib.Approved
LevonorgestrelThe serum concentration of Levonorgestrel can be increased when it is combined with Osimertinib.Approved, Investigational
LevothyroxineThe serum concentration of Levothyroxine can be increased when it is combined with Osimertinib.Approved
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Osimertinib.Approved, Vet Approved
LisurideThe serum concentration of Lisuride can be increased when it is combined with Osimertinib.Approved, Investigational
LomefloxacinThe serum concentration of Lomefloxacin can be decreased when it is combined with Osimertinib.Approved, Investigational
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Osimertinib.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Osimertinib.Approved
LopinavirThe serum concentration of Lopinavir can be increased when it is combined with Osimertinib.Approved
LoratadineThe serum concentration of Loratadine can be increased when it is combined with Osimertinib.Approved
LorcaserinThe serum concentration of Lorcaserin can be increased when it is combined with Osimertinib.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Osimertinib.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Osimertinib.Approved, Investigational
LumacaftorThe serum concentration of Osimertinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe serum concentration of Lumefantrine can be increased when it is combined with Osimertinib.Approved
LumiracoxibThe serum concentration of Lumiracoxib can be decreased when it is combined with Osimertinib.Approved, Investigational
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Osimertinib.Approved
MacitentanThe serum concentration of Macitentan can be increased when it is combined with Osimertinib.Approved
MalathionThe serum concentration of Malathion can be decreased when it is combined with Osimertinib.Approved, Investigational
MaprotilineThe serum concentration of Maprotiline can be decreased when it is combined with Osimertinib.Approved
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Osimertinib.Approved, Investigational
MebendazoleThe serum concentration of Mebendazole can be increased when it is combined with Osimertinib.Approved, Vet Approved
Medroxyprogesterone acetateThe serum concentration of Medroxyprogesterone acetate can be increased when it is combined with Osimertinib.Approved, Investigational
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Osimertinib.Approved
MelatoninThe serum concentration of Melatonin can be decreased when it is combined with Osimertinib.Approved, Nutraceutical, Vet Approved
MeloxicamThe serum concentration of Meloxicam can be increased when it is combined with Osimertinib.Approved, Vet Approved
MenadioneThe serum concentration of Menadione can be decreased when it is combined with Osimertinib.Approved, Nutraceutical
MephenytoinThe serum concentration of Mephenytoin can be decreased when it is combined with Osimertinib.Investigational, Withdrawn
MethadoneThe serum concentration of Methadone can be increased when it is combined with Osimertinib.Approved
MethaqualoneThe serum concentration of Methaqualone can be increased when it is combined with Osimertinib.Illicit, Withdrawn
MethoxsalenThe serum concentration of Methoxsalen can be increased when it is combined with Osimertinib.Approved
MethoxyfluraneThe serum concentration of Methoxyflurane can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Osimertinib.Approved, Vet Approved
MethyltestosteroneThe serum concentration of Methyltestosterone can be increased when it is combined with Osimertinib.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Osimertinib.Experimental
MetronidazoleThe serum concentration of Metronidazole can be increased when it is combined with Osimertinib.Approved
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Osimertinib.Approved
MianserinThe serum concentration of Mianserin can be increased when it is combined with Osimertinib.Approved, Investigational
MibefradilThe serum concentration of Mibefradil can be increased when it is combined with Osimertinib.Investigational, Withdrawn
MiconazoleThe serum concentration of Miconazole can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Osimertinib.Approved, Illicit
MidostaurinThe serum concentration of Midostaurin can be increased when it is combined with Osimertinib.Approved
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Osimertinib.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Osimertinib.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Osimertinib.Approved
MitotaneThe serum concentration of Osimertinib can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Osimertinib.Approved, Investigational
MontelukastThe serum concentration of Montelukast can be increased when it is combined with Osimertinib.Approved
MorphineThe serum concentration of Morphine can be increased when it is combined with Osimertinib.Approved, Investigational
muraglitazarThe serum concentration of muraglitazar can be decreased when it is combined with Osimertinib.Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Osimertinib.Approved, Investigational
NabumetoneThe serum concentration of Nabumetone can be decreased when it is combined with Osimertinib.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Osimertinib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Osimertinib.Approved, Vet Approved
NaproxenThe serum concentration of Naproxen can be decreased when it is combined with Osimertinib.Approved, Vet Approved
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Osimertinib.Approved, Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Osimertinib.Approved, Withdrawn
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Osimertinib.Approved
NeratinibThe serum concentration of Neratinib can be increased when it is combined with Osimertinib.Approved, Investigational
NevirapineThe serum concentration of Nevirapine can be increased when it is combined with Osimertinib.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Osimertinib.Approved
NicotineThe serum concentration of Nicotine can be increased when it is combined with Osimertinib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Osimertinib.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Osimertinib.Approved, Investigational
NilvadipineThe serum concentration of Nilvadipine can be increased when it is combined with Osimertinib.Approved, Investigational
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Osimertinib.Approved
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Osimertinib.Approved
NitrazepamThe serum concentration of Nitrazepam can be increased when it is combined with Osimertinib.Approved
NitrendipineThe serum concentration of Nitrendipine can be increased when it is combined with Osimertinib.Approved, Investigational
Nitric OxideThe serum concentration of Nitric Oxide can be decreased when it is combined with Osimertinib.Approved
NorethisteroneThe serum concentration of Norethisterone can be increased when it is combined with Osimertinib.Approved
NorgestrelThe serum concentration of Norgestrel can be increased when it is combined with Osimertinib.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Osimertinib.Approved
OdanacatibThe serum concentration of Odanacatib can be increased when it is combined with Osimertinib.Investigational
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Osimertinib.Approved, Investigational
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Osimertinib.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Osimertinib.Experimental, Investigational
OlopatadineThe serum concentration of Olopatadine can be increased when it is combined with Osimertinib.Approved
OmeprazoleThe serum concentration of Omeprazole can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Osimertinib.Approved
OrphenadrineThe serum concentration of Orphenadrine can be increased when it is combined with Osimertinib.Approved
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Osimertinib.Approved
OxaliplatinThe serum concentration of Oxaliplatin can be decreased when it is combined with Osimertinib.Approved, Investigational
OxazepamThe serum concentration of Oxazepam can be increased when it is combined with Osimertinib.Approved
OxtriphyllineThe serum concentration of Oxtriphylline can be decreased when it is combined with Osimertinib.Approved
OxybutyninThe serum concentration of Oxybutynin can be increased when it is combined with Osimertinib.Approved, Investigational
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational
OxymorphoneThe serum concentration of Oxymorphone can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Osimertinib.Approved, Vet Approved
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Osimertinib.Approved
PalonosetronThe serum concentration of Palonosetron can be increased when it is combined with Osimertinib.Approved, Investigational
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Osimertinib.Approved, Investigational
PantoprazoleThe serum concentration of Pantoprazole can be increased when it is combined with Osimertinib.Approved
ParamethadioneThe serum concentration of Paramethadione can be increased when it is combined with Osimertinib.Approved
ParamethasoneThe serum concentration of Paramethasone can be increased when it is combined with Osimertinib.Approved
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Osimertinib.Approved
ParicalcitolThe serum concentration of Paricalcitol can be increased when it is combined with Osimertinib.Approved, Investigational
ParitaprevirThe serum concentration of Paritaprevir can be increased when it is combined with Osimertinib.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Osimertinib.Approved
PentamidineThe serum concentration of Pentamidine can be increased when it is combined with Osimertinib.Approved
PentobarbitalThe serum concentration of Osimertinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PentoxifyllineThe serum concentration of Pentoxifylline can be decreased when it is combined with Osimertinib.Approved, Investigational
PerampanelThe serum concentration of Perampanel can be increased when it is combined with Osimertinib.Approved
PergolideThe serum concentration of Pergolide can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved, Withdrawn
PerhexilineThe serum concentration of Perhexiline can be increased when it is combined with Osimertinib.Approved, Investigational
PermethrinThe serum concentration of Permethrin can be increased when it is combined with Osimertinib.Approved, Investigational
PerospironeThe serum concentration of Perospirone can be increased when it is combined with Osimertinib.Approved
PerphenazineThe serum concentration of Perphenazine can be increased when it is combined with Osimertinib.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Osimertinib.Experimental
PethidineThe serum concentration of Pethidine can be increased when it is combined with Osimertinib.Approved
PhenacetinThe serum concentration of Phenacetin can be increased when it is combined with Osimertinib.Withdrawn
PhenobarbitalThe serum concentration of Osimertinib can be decreased when it is combined with Phenobarbital.Approved
PhenoxybenzamineThe serum concentration of Phenoxybenzamine can be increased when it is combined with Osimertinib.Approved
PhenprocoumonThe serum concentration of Phenprocoumon can be increased when it is combined with Osimertinib.Approved, Investigational
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Osimertinib.Approved, Vet Approved
PilocarpineThe serum concentration of Pilocarpine can be increased when it is combined with Osimertinib.Approved
PimecrolimusThe serum concentration of Pimecrolimus can be increased when it is combined with Osimertinib.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Osimertinib.Approved
PinacidilThe serum concentration of Pinacidil can be increased when it is combined with Osimertinib.Withdrawn
PioglitazoneThe serum concentration of Pioglitazone can be increased when it is combined with Osimertinib.Approved, Investigational
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Osimertinib.Approved, Investigational
PodofiloxThe serum concentration of Podofilox can be increased when it is combined with Osimertinib.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Osimertinib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Osimertinib.Approved
PosaconazoleThe serum concentration of Posaconazole can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
PrasteroneThe serum concentration of Prasterone can be increased when it is combined with Osimertinib.Approved, Nutraceutical
PrasugrelThe serum concentration of Prasugrel can be increased when it is combined with Osimertinib.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Osimertinib.Approved
PrazepamThe serum concentration of Prazepam can be increased when it is combined with Osimertinib.Approved, Illicit
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Osimertinib.Approved, Vet Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Osimertinib.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Osimertinib.Approved, Vet Approved
PrimaquineThe serum concentration of Primaquine can be increased when it is combined with Osimertinib.Approved
PrimidoneThe serum concentration of Osimertinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProchlorperazineThe serum concentration of Prochlorperazine can be increased when it is combined with Osimertinib.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Osimertinib.Approved, Vet Approved
ProguanilThe serum concentration of Proguanil can be increased when it is combined with Osimertinib.Approved
PromazineThe serum concentration of Promazine can be increased when it is combined with Osimertinib.Approved, Vet Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Osimertinib.Approved
PropofolThe serum concentration of Propofol can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
Propoxyphene napsylateThe serum concentration of Propoxyphene napsylate can be increased when it is combined with Osimertinib.Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Osimertinib.Approved, Investigational
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Osimertinib.Experimental
PyrazinamideThe serum concentration of Pyrazinamide can be increased when it is combined with Osimertinib.Approved
QuazepamThe serum concentration of Quazepam can be increased when it is combined with Osimertinib.Approved, Illicit
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Osimertinib.Approved
QuinacrineThe serum concentration of Quinacrine can be increased when it is combined with Osimertinib.Approved, Investigational
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Osimertinib.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Osimertinib.Approved
RabeprazoleThe serum concentration of Rabeprazole can be increased when it is combined with Osimertinib.Approved, Investigational
RaloxifeneThe serum concentration of Raloxifene can be increased when it is combined with Osimertinib.Approved, Investigational
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Osimertinib.Approved, Investigational
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Osimertinib.Approved
RanolazineThe serum concentration of Osimertinib can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineThe serum concentration of Rasagiline can be decreased when it is combined with Osimertinib.Approved
ReboxetineThe serum concentration of Reboxetine can be increased when it is combined with Osimertinib.Approved, Investigational
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Osimertinib.Approved
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Osimertinib.Approved, Investigational
ResveratrolThe serum concentration of Resveratrol can be decreased when it is combined with Osimertinib.Approved, Experimental, Investigational
RetapamulinThe serum concentration of Retapamulin can be increased when it is combined with Osimertinib.Approved
RifabutinThe serum concentration of Rifabutin can be increased when it is combined with Osimertinib.Approved
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Osimertinib.Approved
RifapentineThe serum concentration of Osimertinib can be decreased when it is combined with Rifapentine.Approved
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Osimertinib.Approved
RiluzoleThe serum concentration of Riluzole can be decreased when it is combined with Osimertinib.Approved, Investigational
RimonabantThe serum concentration of Rimonabant can be increased when it is combined with Osimertinib.Approved, Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Osimertinib.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Osimertinib.Approved, Investigational
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Osimertinib.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Osimertinib.Approved
RizatriptanThe serum concentration of Rizatriptan can be decreased when it is combined with Osimertinib.Approved
RofecoxibThe serum concentration of Rofecoxib can be increased when it is combined with Osimertinib.Investigational, Withdrawn
RolapitantThe serum concentration of Rolapitant can be increased when it is combined with Osimertinib.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Osimertinib.Approved, Investigational
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Osimertinib.Approved, Investigational
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Osimertinib.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Osimertinib.Approved
RotigotineThe serum concentration of Rotigotine can be increased when it is combined with Osimertinib.Approved
RoxithromycinThe serum concentration of Roxithromycin can be increased when it is combined with Osimertinib.Approved, Investigational, Withdrawn
RucaparibThe serum concentration of Rucaparib can be increased when it is combined with Osimertinib.Approved, Investigational
RupatadineThe serum concentration of Rupatadine can be increased when it is combined with Osimertinib.Approved
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Osimertinib.Approved
SafinamideThe serum concentration of Safinamide can be increased when it is combined with Osimertinib.Approved
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Osimertinib.Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Osimertinib.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Osimertinib.Approved
SelegilineThe serum concentration of Selegiline can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Osimertinib.Approved
SeratrodastThe serum concentration of Seratrodast can be increased when it is combined with Osimertinib.Approved
SertindoleThe serum concentration of Sertindole can be increased when it is combined with Osimertinib.Approved, Investigational, Withdrawn
SertralineThe serum concentration of Sertraline can be increased when it is combined with Osimertinib.Approved
SevofluraneThe serum concentration of Sevoflurane can be increased when it is combined with Osimertinib.Approved, Vet Approved
SibutramineThe serum concentration of Sibutramine can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational, Withdrawn
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Osimertinib.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Osimertinib.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Osimertinib.Approved
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Osimertinib.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Osimertinib.Approved, Investigational
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Osimertinib.Approved
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Osimertinib.Approved, Investigational
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Osimertinib.Approved, Investigational
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Osimertinib.Approved
St. John's WortThe serum concentration of Osimertinib can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Stiripentol can be decreased when it is combined with Osimertinib.Approved
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Osimertinib.Approved, Investigational
SulfadiazineThe serum concentration of Sulfadiazine can be increased when it is combined with Osimertinib.Approved, Vet Approved
SulfamethoxazoleThe serum concentration of Sulfamethoxazole can be increased when it is combined with Osimertinib.Approved
SulfinpyrazoneThe serum concentration of Sulfinpyrazone can be increased when it is combined with Osimertinib.Approved
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Osimertinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be increased when it is combined with Osimertinib.Approved
Synthetic Conjugated Estrogens, BThe serum concentration of Synthetic Conjugated Estrogens, B can be increased when it is combined with Osimertinib.Approved
TacrineThe serum concentration of Tacrine can be decreased when it is combined with Osimertinib.Investigational, Withdrawn
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Osimertinib.Approved, Investigational
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Osimertinib.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Osimertinib.Approved
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Osimertinib.Approved, Investigational
TasosartanThe serum concentration of Tasosartan can be increased when it is combined with Osimertinib.Approved
Taurochenodeoxycholic acidThe serum concentration of Taurochenodeoxycholic acid can be increased when it is combined with Osimertinib.Experimental
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Osimertinib.Approved, Withdrawn
TelithromycinThe serum concentration of Telithromycin can be increased when it is combined with Osimertinib.Approved
TemafloxacinThe serum concentration of Temafloxacin can be decreased when it is combined with Osimertinib.Withdrawn
TemazepamThe serum concentration of Temazepam can be increased when it is combined with Osimertinib.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Osimertinib.Approved
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Osimertinib.Approved
TerbinafineThe serum concentration of Terbinafine can be increased when it is combined with Osimertinib.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Terfenadine can be increased when it is combined with Osimertinib.Withdrawn
TeriflunomideThe serum concentration of Osimertinib can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Tesmilifene can be increased when it is combined with Osimertinib.Investigational
TestosteroneThe serum concentration of Testosterone can be increased when it is combined with Osimertinib.Approved, Investigational
TetracyclineThe serum concentration of Tetracycline can be increased when it is combined with Osimertinib.Approved, Vet Approved
ThalidomideThe serum concentration of Thalidomide can be decreased when it is combined with Osimertinib.Approved, Investigational, Withdrawn
TheobromineThe serum concentration of Theobromine can be decreased when it is combined with Osimertinib.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Osimertinib.Approved
ThiabendazoleThe serum concentration of Thiabendazole can be decreased when it is combined with Osimertinib.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be decreased when it is combined with Osimertinib.Approved, Withdrawn
ThiotepaThe serum concentration of Thiotepa can be increased when it is combined with Osimertinib.Approved
ThiothixeneThe serum concentration of Thiothixene can be decreased when it is combined with Osimertinib.Approved
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Osimertinib.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Osimertinib.Approved
TiclopidineThe serum concentration of Ticlopidine can be increased when it is combined with Osimertinib.Approved
TinidazoleThe serum concentration of Tinidazole can be increased when it is combined with Osimertinib.Approved, Investigational
TiotropiumThe serum concentration of Tiotropium can be increased when it is combined with Osimertinib.Approved
TipranavirThe serum concentration of Tipranavir can be increased when it is combined with Osimertinib.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be decreased when it is combined with Osimertinib.Approved
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Osimertinib.Approved, Investigational
TolperisoneThe serum concentration of AV650 can be decreased when it is combined with Osimertinib.Approved, Investigational
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Osimertinib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Osimertinib.Approved
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Osimertinib.Approved, Investigational
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Osimertinib.Approved, Investigational
TramadolThe serum concentration of Tramadol can be increased when it is combined with Osimertinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Osimertinib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Osimertinib.Approved
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Osimertinib.Approved, Investigational
TretinoinThe serum concentration of Tretinoin can be increased when it is combined with Osimertinib.Approved, Investigational, Nutraceutical
TriamcinoloneThe serum concentration of Triamcinolone can be increased when it is combined with Osimertinib.Approved, Vet Approved
TriamtereneThe serum concentration of Triamterene can be decreased when it is combined with Osimertinib.Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Osimertinib.Approved
TrifluoperazineThe serum concentration of Trifluoperazine can be decreased when it is combined with Osimertinib.Approved
TrimethadioneThe serum concentration of Trimethadione can be increased when it is combined with Osimertinib.Approved
TrimethoprimThe serum concentration of Trimethoprim can be increased when it is combined with Osimertinib.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Osimertinib.Approved
TroglitazoneThe serum concentration of Troglitazone can be increased when it is combined with Osimertinib.Investigational, Withdrawn
TroleandomycinThe serum concentration of Troleandomycin can be increased when it is combined with Osimertinib.Approved
UdenafilThe serum concentration of Udenafil can be increased when it is combined with Osimertinib.Approved, Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Osimertinib.Approved
VadimezanThe serum concentration of Vadimezan can be decreased when it is combined with Osimertinib.Investigational
ValbenazineThe serum concentration of Valbenazine can be increased when it is combined with Osimertinib.Approved, Investigational
ValdecoxibThe serum concentration of Valdecoxib can be increased when it is combined with Osimertinib.Investigational, Withdrawn
VandetanibThe serum concentration of Vandetanib can be increased when it is combined with Osimertinib.Approved
VanoxerineThe serum concentration of Vanoxerine can be increased when it is combined with Osimertinib.Investigational
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Osimertinib.Approved
VelpatasvirThe serum concentration of Velpatasvir can be increased when it is combined with Osimertinib.Approved
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Osimertinib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Osimertinib.Approved
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Osimertinib.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Osimertinib.Approved
VicrivirocThe serum concentration of Vicriviroc can be increased when it is combined with Osimertinib.Investigational
VilanterolThe serum concentration of Vilanterol can be increased when it is combined with Osimertinib.Approved
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Osimertinib.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Osimertinib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Osimertinib.Approved, Investigational
VindesineThe serum concentration of Vindesine can be increased when it is combined with Osimertinib.Approved, Investigational
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Osimertinib.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Osimertinib.Approved
VoriconazoleThe serum concentration of Voriconazole can be increased when it is combined with Osimertinib.Approved, Investigational
VortioxetineThe serum concentration of Vortioxetine can be increased when it is combined with Osimertinib.Approved
VoxilaprevirThe serum concentration of Voxilaprevir can be increased when it is combined with Osimertinib.Approved
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Osimertinib.Approved
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Osimertinib.Approved, Vet Approved
ZafirlukastThe serum concentration of Zafirlukast can be increased when it is combined with Osimertinib.Approved, Investigational
ZalcitabineThe serum concentration of Zalcitabine can be increased when it is combined with Osimertinib.Approved, Investigational
ZaleplonThe serum concentration of Zaleplon can be increased when it is combined with Osimertinib.Approved, Illicit, Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Osimertinib.Approved
ZileutonThe serum concentration of Zileuton can be increased when it is combined with Osimertinib.Approved, Investigational, Withdrawn
ZiprasidoneThe serum concentration of Ziprasidone can be increased when it is combined with Osimertinib.Approved
ZolmitriptanThe serum concentration of Zolmitriptan can be decreased when it is combined with Osimertinib.Approved, Investigational
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Osimertinib.Approved
ZomepiracThe serum concentration of Zomepirac can be increased when it is combined with Osimertinib.Withdrawn
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Osimertinib.Approved, Investigational
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Osimertinib.Approved
Food Interactions
Not Available

References

Synthesis Reference

Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL: Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. Pubmed

General References
  1. Xu M, Xie Y, Ni S, Liu H: The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC). Ann Transl Med. 2015 May;3(7):96. doi: 10.3978/j.issn.2305-5839.2015.03.60. [PubMed:26015938]
  2. Tan CS, Gilligan D, Pacey S: Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer. Lancet Oncol. 2015 Sep;16(9):e447-59. doi: 10.1016/S1470-2045(15)00246-6. [PubMed:26370354]
  3. Ayeni D, Politi K, Goldberg SB: Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer. Clin Cancer Res. 2015 Sep 1;21(17):3818-20. doi: 10.1158/1078-0432.CCR-15-1211. Epub 2015 Jul 13. [PubMed:26169963]
  4. Yosaatmadja Y, Silva S, Dickson JM, Patterson AV, Smaill JB, Flanagan JU, McKeage MJ, Squire CJ: Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed. J Struct Biol. 2015 Dec;192(3):539-44. doi: 10.1016/j.jsb.2015.10.018. Epub 2015 Nov 2. [PubMed:26522274]
  5. Greig SL: Osimertinib: First Global Approval. Drugs. 2016 Feb;76(2):263-73. doi: 10.1007/s40265-015-0533-4. [PubMed:26729184]
  6. Shea M, Costa DB, Rangachari D: Management of advanced non-small cell lung cancers with known mutations or rearrangements: latest evidence and treatment approaches. Ther Adv Respir Dis. 2016 Apr;10(2):113-29. doi: 10.1177/1753465815617871. Epub 2015 Nov 30. [PubMed:26620497]
  7. Liao BC, Lin CC, Yang JC: Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2015 Mar;27(2):94-101. doi: 10.1097/CCO.0000000000000164. [PubMed:25611025]
  8. Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, Brannigan BW, Harris PL, Haserlat SM, Supko JG, Haluska FG, Louis DN, Christiani DC, Settleman J, Haber DA: Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med. 2004 May 20;350(21):2129-39. Epub 2004 Apr 29. [PubMed:15118073]
  9. Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W: AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. [PubMed:24893891]
External Links
PubChem Compound
71496458
PubChem Substance
310265210
ChemSpider
31042598
BindingDB
50029668
ChEBI
90943
ChEMBL
CHEMBL3353410
PharmGKB
PA166131626
HET
YY3
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Osimertinib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
4zau
FDA label
Download (183 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingNot AvailableCarcinoma, Non-Small-Cell Lung With EGFR Mutation Positive1
1Active Not RecruitingOtherAdvanced (Inoperable) Non Small Cell Lung Cancer / Advanced Non Small Cell Lung Cancer2
1Active Not RecruitingTreatmentEGFR Mutation Positive Advanced Non Small Cell Lung Cancer1
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedBasic ScienceHealthy Volunteers2
1CompletedTreatmentOncology1
1Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1RecruitingTreatmentAdvanced Non Small Cell Lung Cancer1
1RecruitingTreatmentEGFR Activating Mutation / EGFR Exon 19 Deletion Mutation / EGFR NP_005219.2:p.G719X / EGFR NP_005219.2:p.L858R / EGFR NP_005219.2:p.L861Q / EGFR T790M Mutation Negative / Recurrent Non-Small Cell Lung Carcinoma / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v71
1RecruitingTreatmentEGFR Activating Mutation / Recurrent Non-Small Cell Lung Carcinoma / Stage III Non-Small Cell Lung Cancer / Stage III Non-Small Cell Lung Cancer AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v7 / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v7 / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v71
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)3
1RecruitingTreatmentRecurrent Non-Small Cell Lung Carcinoma / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v7 / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v7 / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v71
1RecruitingTreatmentTumors, Solid1
1, 2Active Not RecruitingTreatmentAdvanced (Inoperable) Non Small Cell Lung Cancer / Advanced Non Small Cell Lung Cancer1
1, 2RecruitingTreatmentEGFR Gene Mutations / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2RecruitingTreatmentEGFR-mutant Lung Cancers / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2CompletedTreatmentLocally Advanced or Metastatic Non Small Cell Lung Cancer Stage IIIb - IV1
2Not Yet RecruitingTreatmentEGFR Exon 20 Insertion Mutation / Recurrent Non-Small Cell Lung Carcinoma / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v7 / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v71
2Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2Not Yet RecruitingTreatmentLung Cancers1
2RecruitingNot AvailableLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentAdenocarcinoma of the Lung / Neoplasms, Lung1
2RecruitingTreatmentAdenocarcinomas / Lung Cancer Non-Small Cell Cancer (NSCLC) / Squamous Cell Carcinoma (SCC)1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentEGFR Activating Mutation / EGFR NP_005219.2:p.T790M / Metastatic Malignant Neoplasm in the Brain / Non-Small Cell Lung Carcinoma (NSCLC) / Recurrent Non-Small Cell Lung Carcinoma1
2RecruitingTreatmentEGFR Gene Mutations / Neoplasms, Lung1
2RecruitingTreatmentFailed Tyrosine Kinase Inhibitors / Non-Small Cell Lung Cancer With EGFR T790M Mutation / With Brain and/or Leptomeningeal Metastasis1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentLung Cancers1
2RecruitingTreatmentLung Cancers / Targeted Therapy1
2RecruitingTreatmentNon Small Cell Lung Cancer Metastatic1
2, 3RecruitingTreatmentProgression Free Survival1
3Active Not RecruitingTreatmentAnticancer Treatment1
3Active Not RecruitingTreatmentLocally Advanced or Metastatic EGFR T790M+ NSCLC1
3Not Yet RecruitingTreatmentEGFR Mutation Positive Locally Advanced or Metastatic Non-Small Cell Lung Cancer1
3RecruitingTreatmentStage IB-IIIA Non-small Cell Lung Carcinoma1
Not AvailableCompletedNot AvailableT790M Positive NSCLC Patients1
Not AvailableNo Longer AvailableNot AvailableEGFR T790M Mutation Positive NSCLC1
Not AvailableRecruitingNot AvailableLung Cancer Non-Small Cell Cancer (NSCLC)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral40 mg
TabletOral80 mg
Tablet, film coatedOral40 mg
Tablet, film coatedOral40 1/1
Tablet, film coatedOral80 1/1
Tablet, film coatedOral80 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8946235No2012-08-082032-08-08Us
US9732058No2012-07-252032-07-25Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0224 mg/mLALOGPS
logP4.47ALOGPS
logP4.49ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)13.64ChemAxon
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area87.55 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity150.32 m3·mol-1ChemAxon
Polarizability56.84 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-alkylindoles. These are compounds containing an indole moiety that carries an alkyl chain at the 1-position.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Indoles and derivatives
Sub Class
N-alkylindoles
Direct Parent
N-alkylindoles
Alternative Parents
Aminophenyl ethers / Methoxyanilines / Indoles / Phenoxy compounds / Methoxybenzenes / Anisoles / Dialkylarylamines / Alkyl aryl ethers / Aminopyrimidines and derivatives / N-methylpyrroles
show 8 more
Substituents
N-alkylindole / Indole / Methoxyaniline / Aminophenyl ether / Anisole / Phenol ether / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Aniline or substituted anilines / Phenoxy compound
show 27 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Ubiquitin protein ligase binding
Specific Function
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TG...
Gene Name
EGFR
Uniprot ID
P00533
Uniprot Name
Epidermal growth factor receptor
Molecular Weight
134276.185 Da
References
  1. Yosaatmadja Y, Silva S, Dickson JM, Patterson AV, Smaill JB, Flanagan JU, McKeage MJ, Squire CJ: Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed. J Struct Biol. 2015 Dec;192(3):539-44. doi: 10.1016/j.jsb.2015.10.018. Epub 2015 Nov 2. [PubMed:26522274]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inducer
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da

Drug created on November 18, 2015 10:23 / Updated on December 11, 2017 13:02