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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 mg/1oralBayer Health Care Pharmaceuticals Inc.2012-09-27Not applicableUs
StivargaFilm-coated tablet40 mgOral useBayer Pharma Ag2013-08-26Not applicableEu
StivargaFilm-coated tablet40 mgOral useBayer Pharma Ag2013-08-26Not applicableEu
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 KeyInChIKey=FNHKPVJBJVTLMP-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
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
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.
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.
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
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
Film-coated tabletOral use40 mg
Tabletoral40 mg
Tablet, film coatedoral40 mg/1
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
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)
Interactions
Drug Interactions
Drug
AcebutololRegorafenib may increase the bradycardic activities of Acebutolol.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Regorafenib.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Regorafenib.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Regorafenib.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Regorafenib.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Regorafenib.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Regorafenib.
AlprenololRegorafenib may increase the bradycardic activities of Alprenolol.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Regorafenib.
AmiodaroneThe serum concentration of Regorafenib can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Regorafenib.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Regorafenib.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Regorafenib.
AprepitantThe serum concentration of Regorafenib can be increased when it is combined with Aprepitant.
ArotinololRegorafenib may increase the bradycardic activities of Arotinolol.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Regorafenib.
AtazanavirThe serum concentration of Regorafenib can be increased when it is combined with Atazanavir.
AtenololRegorafenib may increase the bradycardic activities of Atenolol.
AtomoxetineThe metabolism of Regorafenib can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Regorafenib.
BefunololRegorafenib may increase the bradycardic activities of Befunolol.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Regorafenib.
BetaxololRegorafenib may increase the bradycardic activities of Betaxolol.
BevacizumabBevacizumab may increase the cardiotoxic activities of Regorafenib.
BevantololRegorafenib may increase the bradycardic activities of Bevantolol.
BexaroteneThe serum concentration of Regorafenib can be decreased when it is combined with Bexarotene.
BisoprololRegorafenib may increase the bradycardic activities of Bisoprolol.
BoceprevirThe serum concentration of Regorafenib can be increased when it is combined with Boceprevir.
BopindololRegorafenib may increase the bradycardic activities of Bopindolol.
BortezomibThe metabolism of Regorafenib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Regorafenib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Regorafenib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Regorafenib.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Regorafenib.
BufuralolRegorafenib may increase the bradycardic activities of Bufuralol.
BupranololRegorafenib may increase the bradycardic activities of Bupranolol.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Regorafenib.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Regorafenib.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Regorafenib.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Regorafenib.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Regorafenib.
CarbamazepineThe serum concentration of Regorafenib can be decreased when it is combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Regorafenib.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Regorafenib.
CarteololRegorafenib may increase the bradycardic activities of Carteolol.
CarvedilolRegorafenib may increase the bradycardic activities of Carvedilol.
CeliprololRegorafenib may increase the bradycardic activities of Celiprolol.
CeritinibThe serum concentration of Regorafenib can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Regorafenib.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Regorafenib.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Regorafenib.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Regorafenib.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Regorafenib.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Regorafenib.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Regorafenib.
ClarithromycinThe serum concentration of Regorafenib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Regorafenib can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Regorafenib.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Regorafenib.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Regorafenib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Regorafenib.
ClotrimazoleThe metabolism of Regorafenib can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Regorafenib.
CobicistatThe serum concentration of Regorafenib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Regorafenib.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Regorafenib.
ConivaptanThe serum concentration of Regorafenib can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Regorafenib.
CrizotinibThe metabolism of Regorafenib can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Regorafenib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Regorafenib.
CyclosporineThe metabolism of Regorafenib can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Regorafenib.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Regorafenib.
DabrafenibThe serum concentration of Regorafenib can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Regorafenib.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Regorafenib.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Regorafenib.
DarunavirThe serum concentration of Regorafenib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Regorafenib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Regorafenib.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Regorafenib.
DeferasiroxThe serum concentration of Regorafenib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Regorafenib can be decreased when combined with Delavirdine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Regorafenib.
DexamethasoneThe serum concentration of Regorafenib can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Regorafenib.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Regorafenib.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Regorafenib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Regorafenib.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Regorafenib.
DigoxinRegorafenib may increase the bradycardic activities of Digoxin.
DigoxinDigoxin may decrease the cardiotoxic activities of Regorafenib.
DihydroergotamineThe metabolism of Regorafenib can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Regorafenib.
DiltiazemThe metabolism of Regorafenib can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Regorafenib.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Regorafenib.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Regorafenib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Regorafenib.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Regorafenib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Regorafenib.
DoxycyclineThe metabolism of Regorafenib can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Regorafenib can be decreased when combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Regorafenib.
EfavirenzThe serum concentration of Regorafenib can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Regorafenib.
EnzalutamideThe serum concentration of Regorafenib can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Regorafenib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Regorafenib.
ErythromycinThe metabolism of Regorafenib can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Regorafenib.
Eslicarbazepine acetateThe serum concentration of Regorafenib can be decreased when it is combined with Eslicarbazepine acetate.
EsmololRegorafenib may increase the bradycardic activities of Esmolol.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Regorafenib.
EstriolThe serum concentration of Estriol can be increased when it is combined with Regorafenib.
EstroneThe serum concentration of Estrone can be increased when it is combined with Regorafenib.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Regorafenib.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Regorafenib.
EtravirineThe serum concentration of Regorafenib can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Regorafenib.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Regorafenib.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Regorafenib.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Regorafenib.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Regorafenib.
FluconazoleThe metabolism of Regorafenib can be decreased when combined with Fluconazole.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Regorafenib.
FluvoxamineThe metabolism of Regorafenib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Regorafenib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Regorafenib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Regorafenib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Regorafenib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Regorafenib.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Regorafenib.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Regorafenib.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Regorafenib.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Regorafenib.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Regorafenib.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Regorafenib.
IdelalisibThe serum concentration of Regorafenib can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Regorafenib can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Regorafenib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Regorafenib.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Regorafenib.
IndenololRegorafenib may increase the bradycardic activities of Indenolol.
IndinavirThe serum concentration of Regorafenib can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Regorafenib.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Regorafenib.
IsavuconazoniumThe metabolism of Regorafenib can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Regorafenib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Regorafenib can be increased when it is combined with Itraconazole.
IvabradineRegorafenib may increase the bradycardic activities of Ivabradine.
IvacaftorThe serum concentration of Regorafenib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Regorafenib.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Regorafenib.
KetoconazoleThe serum concentration of Regorafenib can be increased when it is combined with Ketoconazole.
LabetalolRegorafenib may increase the bradycardic activities of Labetalol.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Regorafenib.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Regorafenib.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Regorafenib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Regorafenib.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Regorafenib.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Regorafenib.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Regorafenib.
LevobunololRegorafenib may increase the bradycardic activities of Levobunolol.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Regorafenib.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Regorafenib.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Regorafenib.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Regorafenib.
LopinavirThe serum concentration of Regorafenib can be increased when it is combined with Lopinavir.
LosartanThe serum concentration of Losartan can be increased when it is combined with Regorafenib.
LovastatinThe metabolism of Regorafenib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Regorafenib can be increased when it is combined with Luliconazole.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Regorafenib.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Regorafenib.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Regorafenib.
MetipranololRegorafenib may increase the bradycardic activities of Metipranolol.
MetoprololRegorafenib may increase the bradycardic activities of Metoprolol.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Regorafenib.
MifepristoneThe metabolism of Regorafenib can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Regorafenib.
MitotaneThe serum concentration of Regorafenib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Regorafenib.
ModafinilThe serum concentration of Regorafenib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Regorafenib.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Regorafenib.
NadololRegorafenib may increase the bradycardic activities of Nadolol.
NafcillinThe serum concentration of Regorafenib can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Regorafenib.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Regorafenib.
NefazodoneThe serum concentration of Regorafenib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Regorafenib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Regorafenib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Regorafenib can be decreased when it is combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Regorafenib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Regorafenib.
NilotinibThe metabolism of Regorafenib can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Regorafenib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Regorafenib.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Regorafenib.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Regorafenib.
OlaparibThe metabolism of Regorafenib can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Regorafenib.
OsimertinibThe serum concentration of Regorafenib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Regorafenib.
OxprenololRegorafenib may increase the bradycardic activities of Oxprenolol.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Regorafenib.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Regorafenib.
PalbociclibThe serum concentration of Regorafenib can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Regorafenib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Regorafenib.
PenbutololRegorafenib may increase the bradycardic activities of Penbutolol.
PentobarbitalThe serum concentration of Regorafenib can be decreased when it is combined with Pentobarbital.
PhenobarbitalThe serum concentration of Regorafenib can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Regorafenib.
PhenytoinThe serum concentration of Regorafenib can be decreased when it is combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Regorafenib.
PindololRegorafenib may increase the bradycardic activities of Pindolol.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Regorafenib.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Regorafenib.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Regorafenib.
PosaconazoleThe serum concentration of Regorafenib can be increased when it is combined with Posaconazole.
PractololRegorafenib may increase the bradycardic activities of Practolol.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Regorafenib.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Regorafenib.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Regorafenib.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Regorafenib.
PrimidoneThe serum concentration of Regorafenib can be decreased when it is combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Regorafenib.
PropranololRegorafenib may increase the bradycardic activities of Propranolol.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Regorafenib.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Regorafenib.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Regorafenib.
QuinineThe serum concentration of Quinine can be increased when it is combined with Regorafenib.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Regorafenib.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Regorafenib.
RanolazineThe metabolism of Regorafenib can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Regorafenib.
RifabutinThe serum concentration of Regorafenib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Regorafenib can be decreased when it is combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Regorafenib.
RifapentineThe serum concentration of Regorafenib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Regorafenib.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Regorafenib.
RitonavirThe serum concentration of Regorafenib can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Regorafenib.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Regorafenib.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Regorafenib.
SaquinavirThe serum concentration of Regorafenib can be increased when it is combined with Saquinavir.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Regorafenib.
SildenafilThe metabolism of Regorafenib can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Regorafenib.
SiltuximabThe serum concentration of Regorafenib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Regorafenib can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Regorafenib.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Regorafenib.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Regorafenib.
SotalolRegorafenib may increase the bradycardic activities of Sotalol.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Regorafenib.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Regorafenib.
St. John's WortThe serum concentration of Regorafenib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Regorafenib can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Regorafenib can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Regorafenib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Regorafenib.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Regorafenib.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Regorafenib.
TelaprevirThe serum concentration of Regorafenib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Regorafenib can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Regorafenib.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Regorafenib.
TiclopidineThe metabolism of Regorafenib can be decreased when combined with Ticlopidine.
TimololRegorafenib may increase the bradycardic activities of Timolol.
TocilizumabThe serum concentration of Regorafenib can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Regorafenib.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Regorafenib.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Regorafenib.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Regorafenib.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Regorafenib.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Regorafenib.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Regorafenib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Regorafenib.
VenlafaxineThe metabolism of Regorafenib can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Regorafenib.
VerapamilThe metabolism of Regorafenib can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Regorafenib.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Regorafenib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Regorafenib.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Regorafenib.
VoriconazoleThe serum concentration of Regorafenib can be increased when it is combined with Voriconazole.
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Regorafenib.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Regorafenib.
ZiprasidoneThe metabolism of Regorafenib can be decreased when combined with Ziprasidone.
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.

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 September 28, 2016 02:27