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Identification
NameTrastuzumab emtansine
Accession NumberDB05773
TypeBiotech
GroupsApproved
DescriptionTrastuzumab emtansine, formerly called Trastuzumab-DM1 (T-DM1) is a first-in-class HER2 antibody drug conjugate (ADC) comprised of Genentech's trastuzumab antibody linked to ImmunoGen's cell-killing agent, DM1. T-DM1 combines two strategies-- anti-HER2 activity and targeted intracellular delivery of the potent anti-microtubule agent, DM1 (a maytansine derivative)--to produce cell cycle arrest and apoptosis. Trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.
Protein structureNo structure small
Related Articles
Protein chemical formulaNot Available
Protein average weightNot Available
SequencesNot Available
Synonyms
Ado-trastuzumab
Ado-trastuzumab emtansine
T-DM1
Trastuzumab emtansine
Trastuzumab-DM1
Trastuzumab-MCC-DM1
External Identifiers
  • PRO-132365
  • PRO132365
  • RG-3502
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KadcylaPowder, for solution20 mgIntravenousHoffmann La Roche Limited2013-10-09Not applicableCanada
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
KadcylaInjection, powder, lyophilized, for solution20 mg/mLIntravenousGenentech, Inc.2013-02-22Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIISE2KH7T06F
CAS number1018448-65-1
Pharmacology
IndicationUsed in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment.
Structured Indications
PharmacodynamicsTrastuzumab emtansine was evaluated in two Herceptin-responsive and one Herceptin-resistant breast tumor models. In the Herceptin-responsive models, Trastuzumab-DM1 caused complete tumor regression in all mice, whereas Herceptin alone slowed tumor growth. In the Herceptin- resistant model, Herceptin alone had no effect on tumor growth. In contrast, Trastuzumab-DM1 caused >90% tumor reduction in all mice. In this Herceptin- resistant model, tumor regrowth was observed after cessation of Trastuzumab- DM1 treatment, yet regression re-occurred when dosing was resumed. The effect was specific for HER2-positive tumors. Thus the physiological effects of trastuzumab emtansine are cell cycle arrest and cell death by apoptosis.
Mechanism of actionTrastuzumab emtansine is a HER2 antibody drug conjugate. The antibody portion is trastuzumab, which is humanized anti-HER2 IgG1, and produced in the mammalian Chinese Hamster Ovary cells. The drug portion is DM1, which is a maytansine derivative that inhibits microtubules. These two portions are covalently connected by 4-[N-maleimidomethyl] cyclohexane-1-carboxylate (MCC), which is a stable thioether linker. Together MCC and DM1 are called emtansine and are produced by chemical synthesis. Trastuzumab emtansine binds to the HER2 receptor’s sub-domain IV and goes into the cell by receptor-mediated endocytosis. Lysosomes degrade trastuzumab emtansine and release DM1. DM1 binds to tubulin in microtubules and inhibits microtubule function producing cell arrest and apoptosis. As well, similar to trastuzumab, in vitro studies have shown that both HER2 receptor signalling inhibition and antibody-dependent cytotoxicity are mediated by trastuzumab emtansine.
TargetKindPharmacological actionActionsOrganismUniProt ID
Receptor tyrosine-protein kinase erbB-2Proteinyes
antibody
HumanP04626 details
Related Articles
AbsorptionThe absorption/ bioavailability should be close to 100% since trastuzumab emtansine is administered IV.
Volume of distribution

The volume of distribution of trastuzumab emtansine is about 3.13 L.

Protein bindingDM1 has a plasma protein binding value of 93%.
Metabolism

Trastuzumab emtansine undergoes lysosomal degradation to MCC-DM1, Lys-MCC-DM1, and DM1. All of these products are detected at low levels in the plasma. DM1 undergoes further degradation by CYP3A4 and CYP3A5, but DM1 does not induce or inhibit any of the CYP450 enzymes.

Route of eliminationThe route of elimination has not yet been fully elucidated.
Half lifeTrastuzumab emtansine has a long half life of about 4 days.
Clearance

After IV infusion, trastuzumab emtansine has a clearance of 0.68 L/day.

ToxicityThe FDA label includes a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetaminophenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
AfatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Alfentanil.Approved, Illicit
ALT-110The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with ALT-110.Investigational
AmantadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Trastuzumab emtansine.Investigational
AprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Aprepitant.Approved, Investigational
AstemizoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Trastuzumab emtansine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Azithromycin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Trastuzumab emtansine.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.Approved
BenzocaineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
BexaroteneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Boceprevir.Approved
BortezomibThe metabolism of Trastuzumab emtansine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Trastuzumab emtansine.Approved
CaffeineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Trastuzumab emtansine can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with CDX-110.Investigational
CeritinibThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ceritinib.Approved
ChloroquineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Clarithromycin.Approved
ClemastineThe metabolism of Trastuzumab emtansine can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Clozapine.Approved
CobicistatThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Cobicistat.Approved
ColchicineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
CyclosporineThe metabolism of Trastuzumab emtansine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dactinomycin.Approved
DarunavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Darunavir.Approved
DasatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Trastuzumab emtansine can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Trastuzumab emtansine.Approved
DesipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
DesloratadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
DihydroergotamineThe metabolism of Trastuzumab emtansine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Trastuzumab emtansine can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Trastuzumab emtansine.Approved, Investigational
DoxazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Trastuzumab emtansine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Trastuzumab emtansine can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Elbasvir.Approved
EnalaprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ergotamine.Approved
ErythromycinThe metabolism of Trastuzumab emtansine can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Estrone.Approved
EtoposideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fidaxomicin.Approved
FingolimodTrastuzumab emtansine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Fluconazole.Approved
FluoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Trastuzumab emtansine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Trastuzumab emtansine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with G17DT.Investigational
GefitinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with GI-5005.Investigational
GlyburideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Indinavir.Approved
IndomethacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with INGN 225.Investigational
IsavuconazoniumThe metabolism of Trastuzumab emtansine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Trastuzumab emtansine can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Leflunomide.Approved, Investigational
LevofloxacinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Lopinavir.Approved
LoratadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Trastuzumab emtansine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Lumacaftor.Approved
MaprotilineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Trastuzumab emtansine.Withdrawn
MethadoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Natalizumab.Approved, Investigational
NefazodoneThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Nelfinavir.Approved
NeostigmineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Trastuzumab emtansine can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Trastuzumab emtansine can be decreased when combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Norethisterone.Approved
OlaparibThe metabolism of Trastuzumab emtansine can be decreased when combined with Olaparib.Approved
OmeprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Trastuzumab emtansine.Approved
P-NitrophenolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Trastuzumab emtansine.Approved, Vet Approved
PalbociclibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Paroxetine.Approved, Investigational
PentobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe metabolism of Trastuzumab emtansine can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Trastuzumab emtansine can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Trastuzumab emtansine.Approved, Investigational
PimozideThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pimozide.Approved
Platelet Activating FactorThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Trastuzumab emtansine can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Trastuzumab emtansine.Approved
RanitidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Reserpine.Approved
RifabutinThe metabolism of Trastuzumab emtansine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Trastuzumab emtansine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Trastuzumab emtansine can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Trastuzumab emtansine.Approved
RolapitantThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rolapitant.Approved
SaquinavirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Trastuzumab emtansine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Simvastatin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Trastuzumab emtansine.Approved
SirolimusThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Trastuzumab emtansine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine.Approved, Investigational
TacrolimusThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telaprevir.Approved
TelithromycinThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Telithromycin.Approved
TelmisartanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Terfenadine.Withdrawn
TesmilifeneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with TG4010.Investigational
TicagrelorThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Trastuzumab emtansine can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tocilizumab.Approved
TofacitinibTrastuzumab emtansine may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Tolvaptan.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Trastuzumab emtansine.Approved, Investigational
TrazodoneThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Troleandomycin.Approved
VenlafaxineThe metabolism of Trastuzumab emtansine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Trastuzumab emtansine can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of the active metabolites of Trastuzumab emtansine can be increased when Trastuzumab emtansine is used in combination with Voriconazole.Approved, Investigational
ZimelidineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Trastuzumab emtansine can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. [PubMed:19010901 ]
External Links
ATC CodesL01XC14
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (428 KB)
MSDSDownload (381 KB)
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous20 mg/mL
Powder, for solutionIntravenous20 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Molecular Weight:
137909.27 Da
References
  1. Barginear MF, John V, Budman DR: Trastuzumab-DM1: a clinical update of the novel antibody-drug conjugate for HER2-overexpressing breast cancer. Mol Med. 2013 Jan 22;18:1473-9. doi: 10.2119/molmed.2012.00302. [PubMed:23196784 ]
  2. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. [PubMed:19010901 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
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
Molecular Weight:
141477.255 Da
Comments
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Drug created on November 18, 2007 11:27 / Updated on August 17, 2016 12:24