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Identification
NameRegorafenib
Accession NumberDB08896
TypeSmall Molecule
GroupsApproved
DescriptionRegorafenib is an orally-administered inhibitor of multiple kinases. It is used for the treatment of metastatic colorectal cancer and advanced gastrointestinal stromal tumours. FDA approved on September 27, 2012.
Structure
Thumb
Synonyms
BAY 73-4506
Regorafenibum
External Identifiers
  • BAY 73-4506
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
StivargaTablet40 mgOralBayer Inc2013-04-02Not applicableCanada
StivargaTablet, film coated40 mgOralBayer Pharma Ag2013-08-26Not applicableEu
StivargaTablet, film coated40 mgOralBayer Pharma Ag2013-08-26Not applicableEu
StivargaTablet, film coated40 mg/1OralBayer Health Care Pharmaceuticals Inc.2012-09-27Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Regorafenib monohydrate
ThumbNot applicableDBSALT001750
Categories
UNII24T2A1DOYB
CAS number755037-03-7
WeightAverage: 482.815
Monoisotopic: 482.076880893
Chemical FormulaC21H15ClF4N4O3
InChI KeyFNHKPVJBJVTLMP-UHFFFAOYSA-N
InChI
InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
IUPAC Name
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
SMILES
CNC(=O)C1=CC(OC2=CC(F)=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=CC=N1
Pharmacology
IndicationRegorafenib is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. Regorafenib is also indicated for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate.
Structured Indications
PharmacodynamicsNot Available
Mechanism of actionRegorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E , SAPK2, PTK5, and Abl at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma.
TargetKindPharmacological actionActionsOrganismUniProt ID
Proto-oncogene tyrosine-protein kinase receptor RetProteinyes
inhibitor
HumanP07949 details
Vascular endothelial growth factor receptor 1Proteinyes
inhibitor
HumanP17948 details
Vascular endothelial growth factor receptor 2Proteinyes
inhibitor
HumanP35968 details
Vascular endothelial growth factor receptor 3Proteinyes
inhibitor
HumanP35916 details
Mast/stem cell growth factor receptor KitProteinyes
inhibitor
HumanP10721 details
Platelet-derived growth factor receptor alphaProteinyes
inhibitor
HumanP16234 details
Platelet-derived growth factor receptor betaProteinyes
inhibitor
HumanP09619 details
Fibroblast growth factor receptor 1Proteinyes
inhibitor
HumanP11362 details
Fibroblast growth factor receptor 2Proteinyes
inhibitor
HumanP21802 details
Angiopoietin-1 receptorProteinyes
inhibitor
HumanQ02763 details
Discoidin domain-containing receptor 2Proteinyes
inhibitor
HumanQ16832 details
High affinity nerve growth factor receptorProteinyes
inhibitor
HumanP04629 details
Ephrin type-A receptor 2Proteinyes
inhibitor
HumanP29317 details
RAF proto-oncogene serine/threonine-protein kinaseProteinyes
inhibitor
HumanP04049 details
Serine/threonine-protein kinase B-rafProteinyes
inhibitor
HumanP15056 details
Mitogen-activated protein kinase 11Proteinyes
inhibitor
HumanQ15759 details
Tyrosine-protein kinase FRKProteinyes
inhibitor
HumanP42685 details
Tyrosine-protein kinase ABL1Proteinyes
inhibitor
HumanP00519 details
Related Articles
AbsorptionCmax = 2.5 μg/mL; Tmax = 4 hours; AUC = 70.4 μg*h/mL; Cmax, steady-state = 3.9 μg/mL; AUC, steady-state = 58.3 μg*h/mL; The mean relative bioavailability of tablets compared to an oral solution is 69% to 83%.
Volume of distribution

Regorafenib undergoes enterohepatic circulation with multiple plasma concentration peaks observed across the 24-hour dosing interval.

Protein bindingRegorafenib is highly bound (99.5%) to human plasma proteins.
Metabolism

Regorafenib is metabolized by CYP3A4 and UGT1A9. The main circulating metabolites of regorafenib measured at steady-state in human plasma are M-2 (N-oxide) and M-5 (N-oxide and N-desmethyl), both of them having similar in vitro pharmacological activity and steady-state concentrations as regorafenib. M-2 and M-5 are highly protein bound (99.8% and 99.95%, respectively).

Route of eliminationApproximately 71% of a radiolabeled dose was excreted in feces (47% as parent compound, 24% as metabolites) and 19% of the dose was excreted in urine (17% as glucuronides) within 12 days after administration of a radiolabeled oral solution at a dose of 120 mg.
Half lifeRegorafenib, 160 mg oral dose = 28 hours (14 - 58 hours); M2 metabolite, 160 mg oral dose = 25 hours (14-32 hours); M5 metabolite, 160 mg oral dose = 51 hours (32-72 hours);
ClearanceNot Available
ToxicityThe most common adverse reactions (≥20%) are asthenia/fatigue, HFSR, diarrhea, decreased appetite/food intake, hypertension, mucositis, dysphonia, and infection, pain (not otherwise specified), decreased weight, gastrointestinal and abdominal pain, rash, fever, and nausea
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololRegorafenib may increase the bradycardic activities of Acebutolol.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Regorafenib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Regorafenib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Regorafenib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Regorafenib.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Regorafenib.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Regorafenib.Approved, Investigational
AlprenololRegorafenib may increase the bradycardic activities of Alprenolol.Approved, Withdrawn
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Regorafenib.Approved, Investigational
AmiodaroneThe serum concentration of Regorafenib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Regorafenib.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Regorafenib.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Regorafenib.Investigational
Aop200704Regorafenib may increase the bradycardic activities of Aop200704.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Regorafenib.Approved
AprepitantThe serum concentration of Regorafenib can be increased when it is combined with Aprepitant.Approved, Investigational
ArotinololRegorafenib may increase the bradycardic activities of Arotinolol.Approved
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Regorafenib.Approved, Investigational
AtazanavirThe serum concentration of Regorafenib can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololRegorafenib may increase the bradycardic activities of Atenolol.Approved
AtomoxetineThe metabolism of Regorafenib can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Regorafenib.Approved, Investigational
BefunololRegorafenib may increase the bradycardic activities of Befunolol.Experimental
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Regorafenib.Approved, Vet Approved
BetaxololRegorafenib may increase the bradycardic activities of Betaxolol.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Regorafenib.Approved, Investigational
BevantololRegorafenib may increase the bradycardic activities of Bevantolol.Approved
BexaroteneThe serum concentration of Regorafenib can be decreased when it is combined with Bexarotene.Approved, Investigational
BisoprololRegorafenib may increase the bradycardic activities of Bisoprolol.Approved
BoceprevirThe serum concentration of Regorafenib can be increased when it is combined with Boceprevir.Approved
BopindololRegorafenib may increase the bradycardic activities of Bopindolol.Approved
BortezomibThe metabolism of Regorafenib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Regorafenib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Regorafenib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Regorafenib.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Regorafenib.Approved, Investigational
BucindololRegorafenib may increase the bradycardic activities of Bucindolol.Investigational
BufuralolRegorafenib may increase the bradycardic activities of Bufuralol.Experimental, Investigational
BupranololRegorafenib may increase the bradycardic activities of Bupranolol.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Regorafenib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Regorafenib.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Regorafenib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Regorafenib.Approved
CarbamazepineThe serum concentration of Regorafenib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Regorafenib.Approved
CarteololRegorafenib may increase the bradycardic activities of Carteolol.Approved
CarvedilolRegorafenib may increase the bradycardic activities of Carvedilol.Approved, Investigational
CeliprololRegorafenib may increase the bradycardic activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Regorafenib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Regorafenib.Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Regorafenib.Approved, Vet Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Regorafenib.Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Regorafenib.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Regorafenib.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Regorafenib.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Regorafenib.Approved
ClarithromycinThe serum concentration of Regorafenib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Regorafenib can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Regorafenib.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Regorafenib.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Regorafenib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Regorafenib.Approved, Nutraceutical
ClotrimazoleThe metabolism of Regorafenib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Regorafenib.Approved
CobicistatThe serum concentration of Regorafenib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Regorafenib.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Regorafenib.Approved
ConivaptanThe serum concentration of Regorafenib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Regorafenib.Approved
CrizotinibThe metabolism of Regorafenib can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Regorafenib.Approved, Investigational
CyclosporineThe metabolism of Regorafenib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Regorafenib.Approved
DabrafenibThe serum concentration of Regorafenib can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Regorafenib.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Regorafenib.Approved
DarunavirThe serum concentration of Regorafenib can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Regorafenib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Regorafenib.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Regorafenib.Approved
DeferasiroxThe serum concentration of Regorafenib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Regorafenib can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Regorafenib.Approved
DexamethasoneThe serum concentration of Regorafenib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Regorafenib.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Regorafenib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Regorafenib.Approved
DigoxinRegorafenib may increase the bradycardic activities of Digoxin.Approved
DihydroergotamineThe metabolism of Regorafenib can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Regorafenib.Illicit
DiltiazemRegorafenib may increase the bradycardic activities of Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Regorafenib.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Regorafenib.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Regorafenib.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Regorafenib.Approved, Investigational
DoxycyclineThe metabolism of Regorafenib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Regorafenib can be decreased when combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Regorafenib.Approved
EfavirenzThe serum concentration of Regorafenib can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Regorafenib.Approved, Investigational
EnzalutamideThe serum concentration of Regorafenib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Regorafenib.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Regorafenib.Approved, Investigational
ErythromycinThe metabolism of Regorafenib can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Regorafenib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmololRegorafenib may increase the bradycardic activities of Esmolol.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Regorafenib.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Regorafenib.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Regorafenib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Regorafenib.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Regorafenib.Approved
EtravirineThe serum concentration of Regorafenib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Regorafenib.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Regorafenib.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Regorafenib.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Regorafenib.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Regorafenib.Approved
FluconazoleThe metabolism of Regorafenib can be decreased when combined with Fluconazole.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Regorafenib.Approved
FluvoxamineThe metabolism of Regorafenib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Regorafenib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Regorafenib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Regorafenib can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Regorafenib can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Regorafenib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Regorafenib.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Regorafenib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Regorafenib.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Regorafenib.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Regorafenib.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Regorafenib.Approved
IdelalisibThe serum concentration of Regorafenib can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Regorafenib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Regorafenib.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Regorafenib.Approved
IndenololRegorafenib may increase the bradycardic activities of Indenolol.Withdrawn
IndinavirThe serum concentration of Regorafenib can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Regorafenib.Approved, Investigational
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Regorafenib.Approved, Investigational
IsavuconazoniumThe metabolism of Regorafenib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Regorafenib can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Regorafenib can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineRegorafenib may increase the bradycardic activities of Ivabradine.Approved
IvacaftorThe serum concentration of Regorafenib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Regorafenib.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Regorafenib.Approved
KetoconazoleThe serum concentration of Regorafenib can be increased when it is combined with Ketoconazole.Approved, Investigational
LabetalolRegorafenib may increase the bradycardic activities of Labetalol.Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Regorafenib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Regorafenib.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Regorafenib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Regorafenib.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Regorafenib.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Regorafenib.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Regorafenib.Approved, Investigational
LevobunololRegorafenib may increase the bradycardic activities of Levobunolol.Approved
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Regorafenib.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Regorafenib.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Regorafenib.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Regorafenib.Approved
LopinavirThe serum concentration of Regorafenib can be increased when it is combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Regorafenib.Approved
LovastatinThe metabolism of Regorafenib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Regorafenib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Regorafenib can be decreased when it is combined with Lumacaftor.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Regorafenib.Approved, Investigational
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Regorafenib.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Regorafenib.Approved, Vet Approved
MetipranololRegorafenib may increase the bradycardic activities of Metipranolol.Approved
MetoprololRegorafenib may increase the bradycardic activities of Metoprolol.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Regorafenib.Approved, Illicit
MifepristoneThe serum concentration of Regorafenib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Regorafenib.Approved
MitotaneThe serum concentration of Regorafenib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Regorafenib.Approved, Investigational
ModafinilThe serum concentration of Regorafenib can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Regorafenib.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Regorafenib.Approved, Investigational
NadololRegorafenib may increase the bradycardic activities of Nadolol.Approved
NafcillinThe serum concentration of Regorafenib can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Regorafenib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Regorafenib.Approved, Vet Approved
NefazodoneThe serum concentration of Regorafenib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Regorafenib can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Regorafenib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Regorafenib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Regorafenib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Regorafenib.Approved
NilotinibThe metabolism of Regorafenib can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Regorafenib.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Regorafenib.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Regorafenib.Approved, Investigational
OlaparibThe metabolism of Regorafenib can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Regorafenib.Approved
OsimertinibThe serum concentration of Regorafenib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Regorafenib.Approved
OxprenololRegorafenib may increase the bradycardic activities of Oxprenolol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Regorafenib.Approved, Vet Approved
PalbociclibThe serum concentration of Regorafenib can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Regorafenib.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Regorafenib.Approved
PenbutololRegorafenib may increase the bradycardic activities of Penbutolol.Approved, Investigational
PentobarbitalThe serum concentration of Regorafenib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe serum concentration of Regorafenib can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Regorafenib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PindololRegorafenib may increase the bradycardic activities of Pindolol.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Regorafenib.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Regorafenib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Regorafenib.Approved
PosaconazoleThe serum concentration of Regorafenib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PractololRegorafenib may increase the bradycardic activities of Practolol.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Regorafenib.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Regorafenib.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Regorafenib.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Regorafenib.Approved, Vet Approved
PrimidoneThe serum concentration of Regorafenib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Regorafenib.Approved, Vet Approved
PropranololRegorafenib may increase the bradycardic activities of Propranolol.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Regorafenib.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Regorafenib.Approved
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Regorafenib.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Regorafenib.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Regorafenib.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Regorafenib.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Regorafenib.Approved
RifabutinThe serum concentration of Regorafenib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Regorafenib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Regorafenib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Regorafenib.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Regorafenib.Approved, Investigational
RitonavirThe serum concentration of Regorafenib can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Regorafenib.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Regorafenib.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Regorafenib.Approved, Vet Approved
SaquinavirThe serum concentration of Regorafenib can be increased when it is combined with Saquinavir.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Regorafenib.Approved
SildenafilThe metabolism of Regorafenib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Regorafenib.Approved
SiltuximabThe serum concentration of Regorafenib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Regorafenib can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Regorafenib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Regorafenib.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Regorafenib.Approved, Investigational
SotalolRegorafenib may increase the bradycardic activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Regorafenib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Regorafenib.Experimental
St. John's WortThe serum concentration of Regorafenib can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Regorafenib can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Regorafenib can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Regorafenib.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Regorafenib.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Regorafenib.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Regorafenib.Approved
TelaprevirThe serum concentration of Regorafenib can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Regorafenib can be increased when it is combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Regorafenib.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Regorafenib.Approved
TiclopidineThe metabolism of Regorafenib can be decreased when combined with Ticlopidine.Approved
TimololRegorafenib may increase the bradycardic activities of Timolol.Approved
TocilizumabThe serum concentration of Regorafenib can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Regorafenib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Regorafenib.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Regorafenib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Regorafenib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Regorafenib.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Regorafenib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Regorafenib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Regorafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Regorafenib.Approved
VenlafaxineThe metabolism of Regorafenib can be decreased when combined with Venlafaxine.Approved
VerapamilRegorafenib may increase the bradycardic activities of Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Regorafenib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Regorafenib.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Regorafenib.Approved
VoriconazoleThe serum concentration of Regorafenib can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Regorafenib.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Regorafenib.Approved
ZiprasidoneThe metabolism of Regorafenib can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • When taken with a high-fat meal, AUC increased by 48% and decreased mean AUC of M2 and M5 metabolites by 20% and 51% respectively.
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL01XE21
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (457 KB)
MSDSDownload (479 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9649
Blood Brain Barrier+0.851
Caco-2 permeable-0.5138
P-glycoprotein substrateNon-substrate0.5086
P-glycoprotein inhibitor INon-inhibitor0.7141
P-glycoprotein inhibitor IINon-inhibitor0.9359
Renal organic cation transporterNon-inhibitor0.8938
CYP450 2C9 substrateNon-substrate0.6569
CYP450 2D6 substrateNon-substrate0.8212
CYP450 3A4 substrateNon-substrate0.5341
CYP450 1A2 substrateInhibitor0.6168
CYP450 2C9 inhibitorNon-inhibitor0.6171
CYP450 2D6 inhibitorNon-inhibitor0.9145
CYP450 2C19 inhibitorInhibitor0.637
CYP450 3A4 inhibitorNon-inhibitor0.7339
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6629
Ames testNon AMES toxic0.8143
CarcinogenicityNon-carcinogens0.8684
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7885 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9488
hERG inhibition (predictor II)Non-inhibitor0.6415
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral40 mg
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral40 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2315715 No2010-06-222018-12-22Canada
CA2526636 No2012-10-022024-05-19Canada
CA2549558 No2010-08-312020-01-12Canada
US7351834 No2000-01-122020-01-12Us
US8637553 No2011-02-162031-02-16Us
US8680124 No2010-06-022030-06-02Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00102 mg/mLALOGPS
logP4.53ALOGPS
logP4.49ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)10.52ChemAxon
pKa (Strongest Basic)2.02ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area92.35 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity114.73 m3·mol-1ChemAxon
Polarizability41.23 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassEthers
Sub ClassDiarylethers
Direct ParentDiarylethers
Alternative Parents
Substituents
  • Diaryl ether
  • N-phenylurea
  • Pyridine carboxylic acid or derivatives
  • Pyridinecarboxamide
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Urea
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation upon binding with glial cell derived neurotrophic factor family ligands. Phosphorylates PTK2/FAK1. Regulates both cell death/survival balance and positional information. Required for the molecular mechanisms orchestration during in...
Gene Name:
RET
Uniprot ID:
P07949
Molecular Weight:
124317.465 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vegf-b-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation ...
Gene Name:
FLT1
Uniprot ID:
P17948
Molecular Weight:
150767.185 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domai...
Gene Name:
KDR
Uniprot ID:
P35968
Molecular Weight:
151525.555 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardiovascular system during embryonic development. Promotes proliferation, survival and migration of endothelial cells, and regulates angiogenic sprouting. Signaling by activated FLT4 leads to enhanced pr...
Gene Name:
FLT4
Uniprot ID:
P35916
Molecular Weight:
152755.94 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1...
Gene Name:
KIT
Uniprot ID:
P10721
Molecular Weight:
109863.655 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for...
Gene Name:
PDGFRA
Uniprot ID:
P16234
Molecular Weight:
122668.46 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vascular endothelial growth factor binding
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of peri...
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular Weight:
123966.895 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (...
Gene Name:
FGFR1
Uniprot ID:
P11362
Molecular Weight:
91866.935 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an...
Gene Name:
FGFR2
Uniprot ID:
P21802
Molecular Weight:
92024.29 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from ...
Gene Name:
TEK
Uniprot ID:
Q02763
Molecular Weight:
125829.005 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine kinase that functions as cell surface receptor for fibrillar collagen and regulates cell differentiation, remodeling of the extracellular matrix, cell migration and cell proliferation. Required for normal bone development. Regulates osteoblast differentiation and chondrocyte maturation via a signaling pathway that involves MAP kinases and leads to the activation of the transcription fa...
Gene Name:
DDR2
Uniprot ID:
Q16832
Molecular Weight:
96735.44 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympathetic and nervous neurons. High affinity receptor for NGF which is its primary ligand, it can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 ...
Gene Name:
NTRK1
Uniprot ID:
P04629
Molecular Weight:
87496.465 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the lig...
Gene Name:
EPHA2
Uniprot ID:
P29317
Molecular Weight:
108265.585 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Serine/threonine-protein kinase that acts as a regulatory link between the membrane-associated Ras GTPases and the MAPK/ERK cascade, and this critical regulatory link functions as a switch determining cell fate decisions including proliferation, differentiation, apoptosis, survival and oncogenic transformation. RAF1 activation initiates a mitogen-activated protein kinase (MAPK) cascade that com...
Gene Name:
RAF1
Uniprot ID:
P04049
Molecular Weight:
73051.025 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, and thereby contributes to the MAP kinase signal transduction pathway.
Gene Name:
BRAF
Uniprot ID:
P15056
Molecular Weight:
84436.135 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK11 is one of the four p38 MAPKs which play an important role in the cascades of cellular responses evoked by extracellular stimuli such as proinflammatory cytokines or physical stress leading to direct activation of transcription factors. Accordingly, p38 MAPKs phosphorylate a broad r...
Gene Name:
MAPK11
Uniprot ID:
Q15759
Molecular Weight:
41356.875 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase that negatively regulates cell proliferation. Positively regulates PTEN protein stability through phosphorylation of PTEN on 'Tyr-336', which in turn prevents its ubiquitination and degradation, possibly by reducing its binding to NEDD4. May function as a tumor suppressor.
Gene Name:
FRK
Uniprot ID:
P42685
Molecular Weight:
58253.61 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Syntaxin binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 ...
Gene Name:
ABL1
Uniprot ID:
P00519
Molecular Weight:
122871.435 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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
substrateinhibitor
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
Comments
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Drug created on June 03, 2013 16:30 / Updated on December 07, 2016 02:39