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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Sunitinib
- Accession Number
- DB01268 (DB07417)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.
- Structure
Structure for DB01268 (Sunitinib)
- Synonyms
- Sunitinibum
- External IDs
- SU-011248 / SU-11248 / SU011248 / SU11248
- Product Ingredients
Ingredient UNII CAS InChI Key Sunitinib malate LVX8N1UT73 341031-54-7 LBWFXVZLPYTWQI-IPOVEDGCSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Sutent Capsule 25 mg Oral Pfizer 2006-07-19 Not applicable EU 
Sutent Capsule 25 mg/1 Oral Pfizer Laboratories Div Pfizer Inc. 2006-01-26 Not applicable US 
Sutent Capsule 12.5 mg Oral Pfizer 2006-06-22 Not applicable Canada 
Sutent Capsule 25 mg Oral Pfizer 2006-07-19 Not applicable EU Sutent Capsule 50 mg Oral Pfizer 2006-06-22 Not applicable Canada Sutent Capsule 37.5 mg Oral Pfizer 2006-07-19 Not applicable EU Sutent Capsule 50 mg/1 Oral Pfizer Laboratories Div Pfizer Inc. 2006-01-26 Not applicable US Sutent Capsule 12.5 mg Oral Pfizer 2006-07-19 Not applicable EU Sutent Capsule 12.5 mg Oral Pfizer 2006-07-19 Not applicable EU Sutent Capsule 12.5 mg/1 Oral Pfizer Laboratories Div Pfizer Inc. 2006-01-26 Not applicable US - Categories
- Angiogenesis Inhibitors
- Angiogenesis Modulating Agents
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- Blood Glucose Lowering Agents
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Growth Inhibitors
- Growth Substances
- Hypoglycemia-Associated Agents
- Immunosuppressive Agents
- Kinase Inhibitor
- P-glycoprotein/ABCB1 Inhibitors
- P-glycoprotein/ABCB1 Substrates
- Potential QTc-Prolonging Agents
- Protein Kinase Inhibitors
- QTc Prolonging Agents
- Tyrosine Kinase Inhibitors
- UNII
- V99T50803M
- CAS number
- 557795-19-4
- Weight
- Average: 398.4738
Monoisotopic: 398.211804333 - Chemical Formula
- C22H27FN4O2
- InChI Key
- WINHZLLDWRZWRT-ATVHPVEESA-N
- InChI
- InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
- IUPAC Name
- N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide
- SMILES
- CCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C
Pharmacology
- Indication
For the treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
- Associated Conditions
- Pharmacodynamics
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA on January 26, 2006.
- Mechanism of action
Sunitinib is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.
Target Actions Organism APlatelet-derived growth factor receptor beta inhibitorHuman AVascular endothelial growth factor receptor 1 inhibitorHuman AMast/stem cell growth factor receptor Kit inhibitorHuman AVascular endothelial growth factor receptor 2 inhibitorHuman AVascular endothelial growth factor receptor 3 inhibitorHuman AReceptor-type tyrosine-protein kinase FLT3 inhibitorHuman AMacrophage colony-stimulating factor 1 receptor inhibitorHuman APlatelet-derived growth factor receptor alpha inhibitorHuman - Absorption
Maximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Sunitinib may be taken with or without food. The pharmacokinetics were similar in healthy volunteers and in the solid tumor patient populations tested, including patients with GIST and RCC.
- Volume of distribution
- 2230 L (apparent volume of distribution, Vd/F)
- Protein binding
Binding of sunitinib and its primary metabolite to human plasma protein in vitro was 95% and 90%, respectively.
- Metabolism
Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4.
- Route of elimination
Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose.
- Half life
Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
- Clearance
- 34 - 62 L/h [Total oral clearance]
- Toxicity
The maximally tolerated dose for rat, mouse, and dog when given orally is greater than 500 mg/kg. The maximally tolerated dose of a non-human primate is greater 1200 mg/kg.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 3A4 --- (A;A) / (A;G) G > A ADR Directly Studied Patients with metastatic renal cell carcinoma who carry this polymorphism in CYP3A4 are at a higher risk of experiencing drug-induced hypertension when treated with sunitinib. Details
Interactions
- Drug Interactions
Drug Interaction Drug group (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE may increase the hypoglycemic activities of Sunitinib. Experimental 2-mercaptobenzothiazole The metabolism of Sunitinib can be decreased when combined with 2-mercaptobenzothiazole. Vet Approved 2,4-thiazolidinedione 2,4-thiazolidinedione may increase the hypoglycemic activities of Sunitinib. Investigational 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Sunitinib. Experimental Acarbose Acarbose may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Acetaminophen The serum concentration of Sunitinib can be increased when it is combined with Acetaminophen. Approved Acetohexamide Acetohexamide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Withdrawn Acetyl sulfisoxazole The metabolism of Sunitinib can be decreased when combined with Acetyl sulfisoxazole. Approved, Vet Approved Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Sunitinib. Approved Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Sunitinib. Experimental Acetylsalicylic acid Acetylsalicylic acid may increase the hypoglycemic activities of Sunitinib. Approved, Vet Approved Afatinib The serum concentration of Afatinib can be increased when it is combined with Sunitinib. Approved AICA ribonucleotide AICA ribonucleotide may increase the hypoglycemic activities of Sunitinib. Experimental, Investigational Alaproclate Alaproclate may increase the hypoglycemic activities of Sunitinib. Experimental Allicin Allicin may increase the hypoglycemic activities of Sunitinib. Investigational Alogliptin Alogliptin may increase the hypoglycemic activities of Sunitinib. Approved Aloxiprin Aloxiprin may increase the hypoglycemic activities of Sunitinib. Experimental Aminosalicylic Acid Aminosalicylic Acid may increase the hypoglycemic activities of Sunitinib. Approved Amiodarone The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Amiodarone. Approved, Investigational Amlodipine The serum concentration of Sunitinib can be increased when it is combined with Amlodipine. Approved Amorolfine The metabolism of Sunitinib can be decreased when combined with Amorolfine. Approved, Investigational Amphetamine Amphetamine may increase the hypoglycemic activities of Sunitinib. Approved, Illicit, Investigational Amphotericin B The metabolism of Sunitinib can be decreased when combined with Amphotericin B. Approved, Investigational Anagrelide Sunitinib may increase the QTc-prolonging activities of Anagrelide. Approved Ancestim The risk or severity of cytotoxicity can be increased when Ancestim is combined with Sunitinib. Approved, Investigational, Withdrawn Anidulafungin The metabolism of Sunitinib can be decreased when combined with Anidulafungin. Approved, Investigational Anthrax immune globulin human The risk or severity of adverse effects can be increased when Sunitinib is combined with Anthrax immune globulin human. Approved Apalutamide The serum concentration of Sunitinib can be decreased when it is combined with Apalutamide. Approved, Investigational Aprepitant The serum concentration of Sunitinib can be increased when it is combined with Aprepitant. Approved, Investigational Arsenic trioxide Sunitinib may increase the QTc-prolonging activities of Arsenic trioxide. Approved, Investigational Artemether The metabolism of Sunitinib can be decreased when combined with Artemether. Approved Asenapine Sunitinib may increase the QTc-prolonging activities of Asenapine. Approved Atazanavir The metabolism of Sunitinib can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Sunitinib can be decreased when combined with Atomoxetine. Approved Azithromycin Sunitinib may increase the QTc-prolonging activities of Azithromycin. Approved Bacillus calmette-guerin substrain connaught live antigen The risk or severity of adverse effects can be increased when Sunitinib is combined with Bacillus calmette-guerin substrain connaught live antigen. Approved, Investigational Bacillus calmette-guerin substrain tice live antigen The risk or severity of adverse effects can be increased when Sunitinib is combined with Bacillus calmette-guerin substrain tice live antigen. Approved Bafilomycin A1 The metabolism of Sunitinib can be decreased when combined with Bafilomycin A1. Experimental Balaglitazone Balaglitazone may increase the hypoglycemic activities of Sunitinib. Investigational Balsalazide Balsalazide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Sunitinib. Investigational Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Sunitinib is combined with Beclomethasone dipropionate. Approved, Investigational Bedaquiline Sunitinib may increase the QTc-prolonging activities of Bedaquiline. Approved Bempedoic acid Bempedoic acid may increase the hypoglycemic activities of Sunitinib. Investigational Benmoxin Benmoxin may increase the hypoglycemic activities of Sunitinib. Withdrawn Benzatropine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Benzatropine. Approved Benzoic Acid The metabolism of Sunitinib can be decreased when combined with Benzoic Acid. Approved, Investigational Benzyl alcohol The serum concentration of Sunitinib can be increased when it is combined with Benzyl alcohol. Approved Bepridil The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Bepridil. Approved, Withdrawn Bevacizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Bevacizumab. Approved, Investigational Bifonazole The metabolism of Sunitinib can be decreased when combined with Bifonazole. Approved, Investigational Boceprevir The metabolism of Sunitinib can be decreased when combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Sunitinib can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Sunitinib can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Sunitinib. Approved Brefeldin A The metabolism of Sunitinib can be decreased when combined with Brefeldin A. Experimental Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Sunitinib. Approved, Investigational Brofaromine Brofaromine may increase the hypoglycemic activities of Sunitinib. Experimental Brompheniramine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Brompheniramine. Approved Budesonide The risk or severity of adverse effects can be increased when Budesonide is combined with Sunitinib. Approved Buformin Buformin may increase the hypoglycemic activities of Sunitinib. Investigational, Withdrawn Butenafine The metabolism of Sunitinib can be decreased when combined with Butenafine. Approved Butoconazole The metabolism of Sunitinib can be decreased when combined with Butoconazole. Approved Cabazitaxel The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Sunitinib. Approved Caffeine The serum concentration of Sunitinib can be increased when it is combined with Caffeine. Approved Canagliflozin Canagliflozin may increase the hypoglycemic activities of Sunitinib. Approved Candicidin The metabolism of Sunitinib can be decreased when combined with Candicidin. Withdrawn Capric acid The metabolism of Sunitinib can be decreased when combined with Capric acid. Experimental Carbamazepine The serum concentration of Sunitinib can be decreased when it is combined with Carbamazepine. Approved, Investigational Carbaspirin calcium Carbaspirin calcium may increase the hypoglycemic activities of Sunitinib. Experimental, Investigational Carbutamide Carbutamide may increase the hypoglycemic activities of Sunitinib. Experimental Caroxazone Caroxazone may increase the hypoglycemic activities of Sunitinib. Withdrawn Carvedilol The serum concentration of Sunitinib can be increased when it is combined with Carvedilol. Approved, Investigational Caspofungin The metabolism of Sunitinib can be decreased when combined with Caspofungin. Approved Castanospermine Castanospermine may increase the hypoglycemic activities of Sunitinib. Experimental Ceritinib The serum concentration of Sunitinib can be increased when it is combined with Ceritinib. Approved Cerulenin The metabolism of Sunitinib can be decreased when combined with Cerulenin. Approved Cetirizine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Cetirizine. Approved Chloroquine Sunitinib may increase the QTc-prolonging activities of Chloroquine. Approved, Investigational, Vet Approved Chloroxine The metabolism of Sunitinib can be decreased when combined with Chloroxine. Approved Chlorphenamine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Chlorphenamine. Approved Chlorpromazine Sunitinib may increase the QTc-prolonging activities of Chlorpromazine. Approved, Investigational, Vet Approved Chlorpropamide Chlorpropamide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Ciclopirox The metabolism of Sunitinib can be decreased when combined with Ciclopirox. Approved, Investigational Ciglitazone Ciglitazone may increase the hypoglycemic activities of Sunitinib. Experimental Cimetidine The serum concentration of Cimetidine can be increased when it is combined with Sunitinib. Approved, Investigational Cinnarizine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Cinnarizine. Approved, Investigational Cinoxacin Cinoxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Withdrawn Ciprofloxacin The therapeutic efficacy of Sunitinib can be increased when used in combination with Ciprofloxacin. Approved, Investigational Cisapride Sunitinib may increase the QTc-prolonging activities of Cisapride. Approved, Investigational, Withdrawn Citalopram Sunitinib may increase the QTc-prolonging activities of Citalopram. Approved Clarithromycin The metabolism of Sunitinib can be decreased when combined with Clarithromycin. Approved Clemastine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Clemastine. Approved, Investigational Clostridium tetani toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Sunitinib is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated). Approved Clotrimazole The metabolism of Sunitinib can be decreased when combined with Clotrimazole. Approved, Vet Approved Clozapine Sunitinib may increase the QTc-prolonging activities of Clozapine. Approved Cobicistat The metabolism of Sunitinib can be decreased when combined with Cobicistat. Approved Colchicine The serum concentration of Colchicine can be increased when it is combined with Sunitinib. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Sunitinib. Approved, Investigational Cordycepin The metabolism of Sunitinib can be decreased when combined with Cordycepin. Investigational Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Sunitinib is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated). Approved Crizotinib The metabolism of Sunitinib can be decreased when combined with Crizotinib. Approved Curcumin The metabolism of Sunitinib can be decreased when combined with Curcumin. Approved, Investigational Cyclobenzaprine Cyclobenzaprine may decrease the hypoglycemic activities of Sunitinib. Approved Cyclophosphamide Cyclophosphamide may increase the cardiotoxic activities of Sunitinib. Approved, Investigational Cyclosporine The risk or severity of adverse effects can be increased when Cyclosporine is combined with Sunitinib. Approved, Investigational, Vet Approved Cymarin Cymarin may decrease the cardiotoxic activities of Sunitinib. Experimental Dabigatran etexilate The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Sunitinib. Approved Dabrafenib The serum concentration of Sunitinib can be decreased when it is combined with Dabrafenib. Approved, Investigational Dapagliflozin The serum concentration of Dapagliflozin can be increased when it is combined with Sunitinib. Approved Dapoxetine Dapoxetine may increase the hypoglycemic activities of Sunitinib. Investigational Darunavir The metabolism of Sunitinib can be decreased when combined with Darunavir. Approved Dasatinib The serum concentration of Sunitinib can be increased when it is combined with Dasatinib. Approved, Investigational Deferasirox The serum concentration of Sunitinib can be decreased when it is combined with Deferasirox. Approved, Investigational Delavirdine The metabolism of Sunitinib can be decreased when combined with Delavirdine. Approved Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Sunitinib. Approved Deoxyspergualin Deoxyspergualin may increase the hypoglycemic activities of Sunitinib. Investigational Dersalazine Dersalazine may increase the hypoglycemic activities of Sunitinib. Investigational Deslanoside Deslanoside may decrease the cardiotoxic activities of Sunitinib. Approved Desvenlafaxine Desvenlafaxine may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Dexamethasone The serum concentration of Sunitinib can be decreased when it is combined with Dexamethasone. Approved, Investigational, Vet Approved Dexbrompheniramine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Dexbrompheniramine. Approved Dexniguldipine The serum concentration of Sunitinib can be increased when it is combined with Dexniguldipine. Experimental Dexverapamil The serum concentration of Sunitinib can be increased when it is combined with Dexverapamil. Experimental Dichlorophene The metabolism of Sunitinib can be decreased when combined with Dichlorophene. Vet Approved Diflunisal Diflunisal may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Digitoxin Digitoxin may decrease the cardiotoxic activities of Sunitinib. Approved, Investigational Digoxin Digoxin may decrease the cardiotoxic activities of Sunitinib. Approved Digoxin Immune Fab (Ovine) Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Sunitinib. Approved Dihydroergotamine The metabolism of Sunitinib can be decreased when combined with Dihydroergotamine. Approved, Investigational Diltiazem The metabolism of Sunitinib can be decreased when combined with Diltiazem. Approved, Investigational Dimenhydrinate The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Dimenhydrinate. Approved Diphenhydramine The risk or severity of QTc prolongation can be increased when Diphenhydramine is combined with Sunitinib. Approved, Investigational Disopyramide Sunitinib may increase the QTc-prolonging activities of Disopyramide. Approved Docetaxel The risk or severity of adverse effects can be increased when Docetaxel is combined with Sunitinib. Approved, Investigational Dofetilide Sunitinib may increase the QTc-prolonging activities of Dofetilide. Approved, Investigational Dolasetron Sunitinib may increase the QTc-prolonging activities of Dolasetron. Approved, Investigational Domperidone Sunitinib may increase the QTc-prolonging activities of Domperidone. Approved, Investigational, Vet Approved Doxazosin The serum concentration of Sunitinib can be increased when it is combined with Doxazosin. Approved Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Sunitinib. Approved, Investigational Doxycycline The metabolism of Sunitinib can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Doxylamine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Doxylamine. Approved, Vet Approved Dronedarone Sunitinib may increase the QTc-prolonging activities of Dronedarone. Approved Droperidol Sunitinib may increase the QTc-prolonging activities of Droperidol. Approved, Vet Approved Dulaglutide Dulaglutide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Duloxetine Duloxetine may increase the hypoglycemic activities of Sunitinib. Approved Econazole The metabolism of Sunitinib can be decreased when combined with Econazole. Approved Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Sunitinib. Approved Efinaconazole The metabolism of Sunitinib can be decreased when combined with Efinaconazole. Approved Eliglustat Sunitinib may increase the QTc-prolonging activities of Eliglustat. Approved Emopamil The serum concentration of Sunitinib can be increased when it is combined with Emopamil. Experimental Empagliflozin Empagliflozin may increase the hypoglycemic activities of Sunitinib. Approved Englitazone Englitazone may increase the hypoglycemic activities of Sunitinib. Experimental Enoxacin Enoxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Enzalutamide The serum concentration of Sunitinib can be decreased when it is combined with Enzalutamide. Approved Erythromycin The metabolism of Sunitinib can be decreased when combined with Erythromycin. Approved, Investigational, Vet Approved Escitalopram Sunitinib may increase the QTc-prolonging activities of Escitalopram. Approved, Investigational Estradiol The serum concentration of Estradiol can be increased when it is combined with Sunitinib. Approved, Investigational, Vet Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be increased when it is combined with Sunitinib. Approved Etoperidone Etoperidone may increase the hypoglycemic activities of Sunitinib. Withdrawn Everolimus The serum concentration of Everolimus can be increased when it is combined with Sunitinib. Approved Exenatide Exenatide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Famotidine The risk or severity of QTc prolongation can be increased when Famotidine is combined with Sunitinib. Approved Felodipine The serum concentration of Sunitinib can be increased when it is combined with Felodipine. Approved, Investigational Fentanyl The serum concentration of Sunitinib can be increased when it is combined with Fentanyl. Approved, Illicit, Investigational, Vet Approved Fenticonazole The metabolism of Sunitinib can be decreased when combined with Fenticonazole. Experimental Fingolimod Sunitinib may increase the immunosuppressive activities of Fingolimod. Approved, Investigational Flecainide Sunitinib may increase the QTc-prolonging activities of Flecainide. Approved, Withdrawn Fleroxacin Fleroxacin may increase the hypoglycemic activities of Sunitinib. Approved Fluconazole The metabolism of Sunitinib can be decreased when combined with Fluconazole. Approved, Investigational Flucytosine The metabolism of Sunitinib can be decreased when combined with Flucytosine. Approved, Investigational Flumequine Flumequine may increase the hypoglycemic activities of Sunitinib. Withdrawn Fluoxetine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Fluoxetine. Approved, Vet Approved Fluoxymesterone Fluoxymesterone may increase the hypoglycemic activities of Sunitinib. Approved, Illicit Flupentixol Sunitinib may increase the QTc-prolonging activities of Flupentixol. Approved, Investigational, Withdrawn Fluticasone propionate The risk or severity of adverse effects can be increased when Sunitinib is combined with Fluticasone propionate. Approved Flutrimazole The metabolism of Sunitinib can be decreased when combined with Flutrimazole. Experimental Fluvoxamine The serum concentration of Sunitinib can be increased when it is combined with Fluvoxamine. Approved, Investigational Fosamprenavir The metabolism of Sunitinib can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Sunitinib can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The serum concentration of Sunitinib can be decreased when it is combined with Fosphenytoin. Approved, Investigational Furazolidone Furazolidone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved Furosemide The therapeutic efficacy of Sunitinib can be increased when used in combination with Furosemide. Approved, Vet Approved Fusidic Acid The serum concentration of Sunitinib can be increased when it is combined with Fusidic Acid. Approved, Investigational G17DT The risk or severity of adverse effects can be increased when Sunitinib is combined with G17DT. Investigational Gadobenic acid Sunitinib may increase the QTc-prolonging activities of Gadobenic acid. Approved, Investigational Gallopamil The serum concentration of Sunitinib can be increased when it is combined with Gallopamil. Investigational Garenoxacin Garenoxacin may increase the hypoglycemic activities of Sunitinib. Investigational Gatifloxacin Gatifloxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Sunitinib. Approved Gemifloxacin Sunitinib may increase the QTc-prolonging activities of Gemifloxacin. Approved, Investigational GI-5005 The risk or severity of adverse effects can be increased when Sunitinib is combined with GI-5005. Investigational Gitoformate Gitoformate may decrease the cardiotoxic activities of Sunitinib. Experimental Glibornuride Glibornuride may increase the hypoglycemic activities of Sunitinib. Investigational, Withdrawn Gliclazide Gliclazide may increase the hypoglycemic activities of Sunitinib. Approved Glimepiride Glimepiride may increase the hypoglycemic activities of Sunitinib. Approved Glipizide Glipizide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Gliquidone Gliquidone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational GLPG-0492 GLPG-0492 may increase the hypoglycemic activities of Sunitinib. Investigational Glyburide The serum concentration of Glyburide can be increased when it is combined with Sunitinib. Approved Glycerin The serum concentration of Sunitinib can be increased when it is combined with Glycerin. Approved, Investigational Glyphosate The metabolism of Sunitinib can be decreased when combined with Glyphosate. Experimental Goserelin Sunitinib may increase the QTc-prolonging activities of Goserelin. Approved Granisetron Sunitinib may increase the QTc-prolonging activities of Granisetron. Approved, Investigational Grepafloxacin Grepafloxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Withdrawn Griseofulvin The metabolism of Sunitinib can be decreased when combined with Griseofulvin. Approved, Investigational, Vet Approved Guacetisal Guacetisal may increase the hypoglycemic activities of Sunitinib. Experimental Gusperimus Gusperimus may increase the hypoglycemic activities of Sunitinib. Investigational Hachimycin The metabolism of Sunitinib can be decreased when combined with Hachimycin. Experimental Haloperidol Sunitinib may increase the QTc-prolonging activities of Haloperidol. Approved Haloprogin The metabolism of Sunitinib can be decreased when combined with Haloprogin. Approved, Withdrawn Harmaline Harmaline may increase the hypoglycemic activities of Sunitinib. Experimental Hemoglobin crosfumaril Hemoglobin crosfumaril may increase the hypoglycemic activities of Sunitinib. Experimental Hepatitis A Vaccine The risk or severity of adverse effects can be increased when Sunitinib is combined with Hepatitis A Vaccine. Approved Hepatitis B Vaccine (Recombinant) The risk or severity of adverse effects can be increased when Sunitinib is combined with Hepatitis B Vaccine (Recombinant). Approved, Withdrawn Hexetidine The metabolism of Sunitinib can be decreased when combined with Hexetidine. Approved, Investigational Human rabies virus immune globulin The risk or severity of adverse effects can be increased when Sunitinib is combined with Human rabies virus immune globulin. Approved Hydracarbazine Hydracarbazine may increase the hypoglycemic activities of Sunitinib. Experimental Hydrochlorothiazide The therapeutic efficacy of Sunitinib can be decreased when used in combination with Hydrochlorothiazide. Approved, Vet Approved Hydrocortisone The risk or severity of adverse effects can be increased when Hydrocortisone is combined with Sunitinib. Approved, Vet Approved Hydrocortisone acetate The risk or severity of adverse effects can be increased when Sunitinib is combined with Hydrocortisone acetate. Approved, Vet Approved Hydrocortisone butyrate The risk or severity of adverse effects can be increased when Sunitinib is combined with Hydrocortisone butyrate. Approved, Vet Approved Hydroxyzine The risk or severity of QTc prolongation can be increased when Hydroxyzine is combined with Sunitinib. Approved Ibandronate The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Sunitinib is combined with Ibandronate. Approved, Investigational Ibuprofen The serum concentration of Sunitinib can be increased when it is combined with Ibuprofen. Approved Ibutilide Sunitinib may increase the QTc-prolonging activities of Ibutilide. Approved Idelalisib The metabolism of Sunitinib can be decreased when combined with Idelalisib. Approved Iloperidone Sunitinib may increase the QTc-prolonging activities of Iloperidone. Approved Imatinib The metabolism of Sunitinib can be decreased when combined with Imatinib. Approved Indalpine Indalpine may increase the hypoglycemic activities of Sunitinib. Investigational, Withdrawn Indinavir The metabolism of Sunitinib can be decreased when combined with Indinavir. Approved INGN 201 The risk or severity of adverse effects can be increased when Sunitinib is combined with INGN 201. Investigational INGN 225 The risk or severity of adverse effects can be increased when Sunitinib is combined with INGN 225. Investigational Insulin Aspart Sunitinib may increase the hypoglycemic activities of Insulin Aspart. Approved Insulin Detemir Sunitinib may increase the hypoglycemic activities of Insulin Detemir. Approved Insulin Glargine Insulin Glargine may increase the hypoglycemic activities of Sunitinib. Approved Insulin Glulisine Sunitinib may increase the hypoglycemic activities of Insulin Glulisine. Approved Insulin Human Insulin Human may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Insulin Lispro Insulin Lispro may increase the hypoglycemic activities of Sunitinib. Approved Insulin Pork Insulin Pork may increase the hypoglycemic activities of Sunitinib. Approved Iproclozide Iproclozide may increase the hypoglycemic activities of Sunitinib. Withdrawn Iproniazid Iproniazid may increase the hypoglycemic activities of Sunitinib. Withdrawn Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Sunitinib. Approved, Investigational Isavuconazole The serum concentration of Sunitinib can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Sunitinib can be decreased when combined with Isavuconazonium. Approved, Investigational Isocarboxazid Isocarboxazid may increase the hypoglycemic activities of Sunitinib. Approved Isoconazole The metabolism of Sunitinib can be decreased when combined with Isoconazole. Approved Isradipine The serum concentration of Sunitinib can be increased when it is combined with Isradipine. Approved, Investigational Itraconazole The metabolism of Sunitinib can be decreased when combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Sunitinib can be increased when it is combined with Ivacaftor. Approved Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Sunitinib is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated). Approved Ketoconazole The metabolism of Sunitinib can be decreased when combined with Ketoconazole. Approved, Investigational Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Sunitinib. Approved, Investigational Lamotrigine The serum concentration of Lamotrigine can be increased when it is combined with Sunitinib. Approved, Investigational Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Sunitinib. Experimental Lanreotide Sunitinib may increase the hypoglycemic activities of Lanreotide. Approved Lawsone The metabolism of Sunitinib can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE. Experimental Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Sunitinib. Approved Leflunomide The risk or severity of adverse effects can be increased when Sunitinib is combined with Leflunomide. Approved, Investigational Lenvatinib Sunitinib may increase the QTc-prolonging activities of Lenvatinib. Approved, Investigational Leuprolide Sunitinib may increase the QTc-prolonging activities of Leuprolide. Approved, Investigational Levetiracetam The serum concentration of Levetiracetam can be increased when it is combined with Sunitinib. Approved, Investigational Levofloxacin Sunitinib may increase the QTc-prolonging activities of Levofloxacin. Approved, Investigational Levomilnacipran Levomilnacipran may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Levonorgestrel The therapeutic efficacy of Sunitinib can be decreased when used in combination with Levonorgestrel. Approved, Investigational Lidocaine The serum concentration of Sunitinib can be increased when it is combined with Lidocaine. Approved, Vet Approved Linagliptin Linagliptin may increase the hypoglycemic activities of Sunitinib. Approved Liraglutide Liraglutide may increase the hypoglycemic activities of Sunitinib. Approved Lomefloxacin Lomefloxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Lomerizine The serum concentration of Sunitinib can be increased when it is combined with Lomerizine. Experimental Loperamide The serum concentration of Loperamide can be increased when it is combined with Sunitinib. Approved Lopinavir The metabolism of Sunitinib can be decreased when combined with Lopinavir. Approved Loratadine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Loratadine. Approved, Investigational Lorpiprazole The serum concentration of Sunitinib can be increased when it is combined with Lorpiprazole. Approved Losartan The serum concentration of Sunitinib can be increased when it is combined with Losartan. Approved Lovastatin The metabolism of Sunitinib can be decreased when combined with Lovastatin. Approved, Investigational Luliconazole The serum concentration of Sunitinib can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Sunitinib can be decreased when it is combined with Lumacaftor. Approved Lumefantrine Sunitinib may increase the QTc-prolonging activities of Lumefantrine. Approved Mebanazine Mebanazine may increase the hypoglycemic activities of Sunitinib. Withdrawn Mecasermin Sunitinib may increase the hypoglycemic activities of Mecasermin. Approved, Investigational Mepartricin The metabolism of Sunitinib can be decreased when combined with Mepartricin. Experimental Mepyramine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Mepyramine. Approved, Vet Approved Mesalazine Mesalazine may increase the hypoglycemic activities of Sunitinib. Approved Mesterolone Mesterolone may increase the hypoglycemic activities of Sunitinib. Experimental Metformin Metformin may increase the hypoglycemic activities of Sunitinib. Approved Methadone Sunitinib may increase the QTc-prolonging activities of Methadone. Approved Methimazole The risk or severity of adverse effects can be increased when Sunitinib is combined with Methimazole. Approved Methyl salicylate Methyl salicylate may increase the hypoglycemic activities of Sunitinib. Approved, Vet Approved Methylene blue Methylene blue may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Sunitinib. Approved, Vet Approved Methyltestosterone Methyltestosterone may increase the hypoglycemic activities of Sunitinib. Approved Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Sunitinib. Experimental Metoclopramide The risk or severity of QTc prolongation can be increased when Metoclopramide is combined with Sunitinib. Approved, Investigational Mevastatin The metabolism of Sunitinib can be decreased when combined with Mevastatin. Experimental Mibefradil The metabolism of Sunitinib can be decreased when combined with Mibefradil. Investigational, Withdrawn Micafungin The metabolism of Sunitinib can be decreased when combined with Micafungin. Approved, Investigational Miconazole The serum concentration of Sunitinib can be increased when it is combined with Miconazole. Approved, Investigational, Vet Approved Mifepristone The serum concentration of Sunitinib can be increased when it is combined with Mifepristone. Approved, Investigational Miglitol Miglitol may increase the hypoglycemic activities of Sunitinib. Approved Miglustat Miglustat may increase the hypoglycemic activities of Sunitinib. Approved Milnacipran Milnacipran may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Miltefosine The metabolism of Sunitinib can be decreased when combined with Miltefosine. Approved, Investigational Minaprine Minaprine may increase the hypoglycemic activities of Sunitinib. Approved Mitiglinide Mitiglinide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Mitotane The serum concentration of Sunitinib can be decreased when it is combined with Mitotane. Approved Moclobemide Moclobemide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Monensin The metabolism of Sunitinib can be decreased when combined with Monensin. Vet Approved Moxifloxacin The therapeutic efficacy of Sunitinib can be increased when used in combination with Moxifloxacin. Approved, Investigational Myxothiazol The metabolism of Sunitinib can be decreased when combined with Myxothiazol. Experimental Naftifine The metabolism of Sunitinib can be decreased when combined with Naftifine. Approved Nalidixic Acid Nalidixic Acid may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Sunitinib. Approved Nandrolone Nandrolone may increase the hypoglycemic activities of Sunitinib. Experimental, Investigational Nandrolone decanoate Nandrolone decanoate may increase the hypoglycemic activities of Sunitinib. Approved, Illicit Natalizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Natalizumab. Approved, Investigational Natamycin The metabolism of Sunitinib can be decreased when combined with Natamycin. Approved Nateglinide Nateglinide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Nefazodone The metabolism of Sunitinib can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The metabolism of Sunitinib can be decreased when combined with Nelfinavir. Approved Nemonoxacin Nemonoxacin may increase the hypoglycemic activities of Sunitinib. Investigational Netupitant The serum concentration of Sunitinib can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The serum concentration of Sunitinib can be decreased when it is combined with Nevirapine. Approved Nialamide Nialamide may increase the hypoglycemic activities of Sunitinib. Withdrawn Nicardipine The serum concentration of Sunitinib can be increased when it is combined with Nicardipine. Approved, Investigational Nifedipine The serum concentration of Nifedipine can be increased when it is combined with Sunitinib. Approved Nifuratel The metabolism of Sunitinib can be decreased when combined with Nifuratel. Experimental Niguldipine The serum concentration of Sunitinib can be increased when it is combined with Niguldipine. Experimental Nikkomycin Z The metabolism of Sunitinib can be decreased when combined with Nikkomycin Z. Investigational Nilotinib Sunitinib may increase the QTc-prolonging activities of Nilotinib. Approved, Investigational Nimodipine The serum concentration of Sunitinib can be increased when it is combined with Nimodipine. Approved, Investigational Nisoldipine The serum concentration of Sunitinib can be increased when it is combined with Nisoldipine. Approved Nitrendipine The serum concentration of Sunitinib can be increased when it is combined with Nitrendipine. Approved, Investigational Nitroaspirin Nitroaspirin may increase the hypoglycemic activities of Sunitinib. Investigational Nitroxoline The metabolism of Sunitinib can be decreased when combined with Nitroxoline. Approved Norfloxacin Norfloxacin may increase the hypoglycemic activities of Sunitinib. Approved Ocrelizumab Ocrelizumab may increase the immunosuppressive activities of Sunitinib. Approved, Investigational Octamoxin Octamoxin may increase the hypoglycemic activities of Sunitinib. Withdrawn Octreotide Octreotide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Ofloxacin Sunitinib may increase the QTc-prolonging activities of Ofloxacin. Approved Olaparib The metabolism of Sunitinib can be decreased when combined with Olaparib. Approved Oleandrin Oleandrin may decrease the cardiotoxic activities of Sunitinib. Experimental, Investigational Olsalazine Olsalazine may increase the hypoglycemic activities of Sunitinib. Approved Omeprazole The serum concentration of Sunitinib can be increased when it is combined with Omeprazole. Approved, Investigational, Vet Approved Omoconazole The metabolism of Sunitinib can be decreased when combined with Omoconazole. Experimental Ondansetron The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Ondansetron. Approved Osimertinib The serum concentration of Sunitinib can be increased when it is combined with Osimertinib. Approved Ouabain Ouabain may decrease the cardiotoxic activities of Sunitinib. Approved Oxandrolone Oxandrolone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Oxiconazole The metabolism of Sunitinib can be decreased when combined with Oxiconazole. Approved Oxolinic acid Oxolinic acid may increase the hypoglycemic activities of Sunitinib. Experimental Oxymetholone Oxymetholone may increase the hypoglycemic activities of Sunitinib. Approved, Illicit Paclitaxel The risk or severity of adverse effects can be increased when Paclitaxel is combined with Sunitinib. Approved, Vet Approved Pafuramidine The metabolism of Sunitinib can be decreased when combined with Pafuramidine. Investigational Palbociclib The serum concentration of Sunitinib can be increased when it is combined with Palbociclib. Approved, Investigational Paliperidone Sunitinib may increase the QTc-prolonging activities of Paliperidone. Approved Panobinostat Sunitinib may increase the QTc-prolonging activities of Panobinostat. Approved, Investigational Pargyline Pargyline may increase the hypoglycemic activities of Sunitinib. Approved Paroxetine The serum concentration of Sunitinib can be increased when it is combined with Paroxetine. Approved, Investigational Pasireotide Sunitinib may increase the hypoglycemic activities of Pasireotide. Approved Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Sunitinib. Approved Pazufloxacin Pazufloxacin may increase the hypoglycemic activities of Sunitinib. Investigational Pefloxacin Pefloxacin may increase the hypoglycemic activities of Sunitinib. Approved Pegvisomant Pegvisomant may increase the hypoglycemic activities of Sunitinib. Approved Pentamidine The metabolism of Sunitinib can be decreased when combined with Pentamidine. Approved, Investigational Pentobarbital The serum concentration of Sunitinib can be decreased when it is combined with Pentobarbital. Approved, Investigational, Vet Approved Perflutren Sunitinib may increase the QTc-prolonging activities of Perflutren. Approved Peruvoside Peruvoside may decrease the cardiotoxic activities of Sunitinib. Experimental Phenelzine Phenelzine may increase the hypoglycemic activities of Sunitinib. Approved Phenformin Phenformin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Withdrawn Pheniprazine Pheniprazine may increase the hypoglycemic activities of Sunitinib. Withdrawn Pheniramine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Pheniramine. Approved Phenobarbital The serum concentration of Sunitinib can be decreased when it is combined with Phenobarbital. Approved, Investigational Phenoxypropazine Phenoxypropazine may increase the hypoglycemic activities of Sunitinib. Withdrawn Phenyl aminosalicylate Phenyl aminosalicylate may increase the hypoglycemic activities of Sunitinib. Approved Phenytoin The serum concentration of Sunitinib can be decreased when it is combined with Phenytoin. Approved, Vet Approved Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sunitinib. Approved, Investigational Pimozide Sunitinib may increase the QTc-prolonging activities of Pimozide. Approved Pioglitazone Pioglitazone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Pipemidic acid Pipemidic acid may increase the hypoglycemic activities of Sunitinib. Experimental Pirlindole Pirlindole may increase the hypoglycemic activities of Sunitinib. Approved Piromidic acid Piromidic acid may increase the hypoglycemic activities of Sunitinib. Experimental Pitolisant The serum concentration of Sunitinib can be decreased when it is combined with Pitolisant. Approved, Investigational Pivhydrazine Pivhydrazine may increase the hypoglycemic activities of Sunitinib. Withdrawn Posaconazole The metabolism of Sunitinib can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Pramlintide Pramlintide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Sunitinib. Approved, Vet Approved Pregabalin The risk or severity of heart failure can be increased when Pregabalin is combined with Sunitinib. Approved, Illicit, Investigational Primaquine Sunitinib may increase the QTc-prolonging activities of Primaquine. Approved Primidone The serum concentration of Sunitinib can be decreased when it is combined with Primidone. Approved, Vet Approved Procainamide Sunitinib may increase the QTc-prolonging activities of Procainamide. Approved Procaine Procaine may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved Procarbazine Procarbazine may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Promazine Sunitinib may increase the QTc-prolonging activities of Promazine. Approved, Vet Approved Promethazine The serum concentration of Sunitinib can be increased when it is combined with Promethazine. Approved, Investigational Propafenone The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Propafenone. Approved Propranolol The serum concentration of Propranolol can be increased when it is combined with Sunitinib. Approved, Investigational Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Sunitinib. Experimental Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Sunitinib. Approved Prulifloxacin Prulifloxacin may increase the hypoglycemic activities of Sunitinib. Investigational Pyrrolnitrin The metabolism of Sunitinib can be decreased when combined with Pyrrolnitrin. Experimental Quetiapine The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Quetiapine. Approved Quinidine Sunitinib may increase the QTc-prolonging activities of Quinidine. Approved, Investigational Quinine Sunitinib may increase the QTc-prolonging activities of Quinine. Approved Rabies virus inactivated antigen, A The risk or severity of adverse effects can be increased when Sunitinib is combined with Rabies virus inactivated antigen, A. Approved, Investigational Rabies virus inactivated antigen, A The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Sunitinib. Approved, Investigational Radicicol The metabolism of Sunitinib can be decreased when combined with Radicicol. Experimental Ranitidine The serum concentration of Sunitinib can be increased when it is combined with Ranitidine. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Sunitinib. Approved, Investigational Rasagiline Rasagiline may increase the hypoglycemic activities of Sunitinib. Approved Repaglinide Repaglinide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Rifabutin The serum concentration of Sunitinib can be decreased when it is combined with Rifabutin. Approved, Investigational Rifampicin The serum concentration of Sunitinib can be decreased when it is combined with Rifampicin. Approved Rifapentine The serum concentration of Sunitinib can be decreased when it is combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Sunitinib. Approved, Investigational Rindopepimut The risk or severity of adverse effects can be increased when Sunitinib is combined with Rindopepimut. Investigational Roflumilast Roflumilast may increase the immunosuppressive activities of Sunitinib. Approved Rosiglitazone Rosiglitazone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Rosoxacin Rosoxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Sunitinib. Approved Rotavirus Vaccine The risk or severity of adverse effects can be increased when Sunitinib is combined with Rotavirus Vaccine. Approved Rubella virus vaccine The risk or severity of adverse effects can be increased when Sunitinib is combined with Rubella virus vaccine. Approved, Investigational Rucaparib The metabolism of Sunitinib can be decreased when combined with Rucaparib. Approved, Investigational Rufloxacin Rufloxacin may increase the hypoglycemic activities of Sunitinib. Experimental Safrazine Safrazine may increase the hypoglycemic activities of Sunitinib. Withdrawn Salbutamol The risk or severity of QTc prolongation can be increased when Salbutamol is combined with Sunitinib. Approved, Vet Approved Salicylhydroxamic Acid The metabolism of Sunitinib can be decreased when combined with Salicylhydroxamic Acid. Experimental Salicylic acid Salicylic acid may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved Salmeterol The risk or severity of QTc prolongation can be increased when Salmeterol is combined with Sunitinib. Approved Salmonella typhi ty2 vi polysaccharide antigen The risk or severity of adverse effects can be increased when Sunitinib is combined with Salmonella typhi ty2 vi polysaccharide antigen. Approved Salmonella typhi Ty21a live antigen The risk or severity of adverse effects can be increased when Sunitinib is combined with Salmonella typhi ty21a live antigen. Approved Saquinavir The metabolism of Sunitinib can be decreased when combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Sunitinib can be decreased when used in combination with Sarilumab. Approved, Investigational Saxagliptin Saxagliptin may increase the hypoglycemic activities of Sunitinib. Approved Selegiline Selegiline may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved Sertaconazole The metabolism of Sunitinib can be decreased when combined with Sertaconazole. Approved, Investigational Sertraline Sertraline may increase the hypoglycemic activities of Sunitinib. Approved Sildenafil The metabolism of Sunitinib can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Sunitinib. Approved Siltuximab The serum concentration of Sunitinib can be decreased when it is combined with Siltuximab. Approved, Investigational Silver sulfadiazine The therapeutic efficacy of Sunitinib can be increased when used in combination with Silver sulfadiazine. Approved, Vet Approved Simeprevir The serum concentration of Sunitinib can be increased when it is combined with Simeprevir. Approved Sinefungin The metabolism of Sunitinib can be decreased when combined with Sinefungin. Experimental Sirolimus The metabolism of Sunitinib can be decreased when combined with Sirolimus. Approved, Investigational Sitafloxacin Sitafloxacin may increase the hypoglycemic activities of Sunitinib. Experimental, Investigational Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Sunitinib. Approved, Investigational Sotagliflozin Sotagliflozin may increase the hypoglycemic activities of Sunitinib. Investigational Sotalol Sunitinib may increase the QTc-prolonging activities of Sotalol. Approved Sparfloxacin Sparfloxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational SRP 299 The risk or severity of adverse effects can be increased when Sunitinib is combined with SRP 299. Investigational St. John's Wort The serum concentration of Sunitinib can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stanolone Stanolone may increase the hypoglycemic activities of Sunitinib. Illicit, Investigational Stanozolol Stanozolol may increase the hypoglycemic activities of Sunitinib. Approved, Vet Approved Stiripentol The serum concentration of Sunitinib can be increased when it is combined with Stiripentol. Approved Sulconazole The metabolism of Sunitinib can be decreased when combined with Sulconazole. Approved Sulfadiazine Sulfadiazine may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved Sulfamethoxazole Sulfamethoxazole may increase the hypoglycemic activities of Sunitinib. Approved Sulfasalazine The risk or severity of adverse effects can be increased when Sunitinib is combined with Sulfasalazine. Approved Sulfisoxazole The metabolism of Sunitinib can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Sulodexide Sulodexide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Sunitinib. Approved, Investigational Tacrolimus Tacrolimus may increase the immunosuppressive activities of Sunitinib. Approved, Investigational Tavaborole The metabolism of Sunitinib can be decreased when combined with Tavaborole. Approved, Investigational Tecemotide The risk or severity of adverse effects can be increased when Sunitinib is combined with Tecemotide. Investigational Telaprevir The metabolism of Sunitinib can be decreased when combined with Telaprevir. Approved, Withdrawn Telavancin Sunitinib may increase the QTc-prolonging activities of Telavancin. Approved Telithromycin The metabolism of Sunitinib can be decreased when combined with Telithromycin. Approved Temafloxacin Temafloxacin may increase the hypoglycemic activities of Sunitinib. Withdrawn Temsirolimus The risk or severity of adverse effects can be increased when Temsirolimus is combined with Sunitinib. Approved Terodiline The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Terodiline. Experimental Testosterone Testosterone may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Testosterone cypionate Testosterone cypionate may increase the hypoglycemic activities of Sunitinib. Approved Testosterone enanthate Testosterone enanthate may increase the hypoglycemic activities of Sunitinib. Approved Testosterone propionate Testosterone propionate may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Vet Approved, Withdrawn Testosterone undecanoate Testosterone undecanoate may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Tetrabenazine Sunitinib may increase the QTc-prolonging activities of Tetrabenazine. Approved, Investigational Tetracycline The serum concentration of Tetracycline can be increased when it is combined with Sunitinib. Approved, Vet Approved Tetrandrine The risk or severity of adverse effects can be increased when Sunitinib is combined with Tetrandrine. Experimental TG4010 The risk or severity of adverse effects can be increased when Sunitinib is combined with TG4010. Investigational Thioridazine Sunitinib may increase the QTc-prolonging activities of Thioridazine. Approved, Withdrawn Thymol The metabolism of Sunitinib can be decreased when combined with Thymol. Approved Ticlopidine The metabolism of Sunitinib can be decreased when combined with Ticlopidine. Approved Tocilizumab The serum concentration of Sunitinib can be decreased when it is combined with Tocilizumab. Approved Tofacitinib Sunitinib may increase the immunosuppressive activities of Tofacitinib. Approved, Investigational Tolazamide Tolazamide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Tolbutamide Tolbutamide may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Tolciclate The metabolism of Sunitinib can be decreased when combined with Tolciclate. Experimental Toloxatone Toloxatone may increase the hypoglycemic activities of Sunitinib. Approved Topiramate The serum concentration of Topiramate can be increased when it is combined with Sunitinib. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Sunitinib. Approved, Investigational Toremifene Sunitinib may increase the QTc-prolonging activities of Toremifene. Approved, Investigational Tranylcypromine Tranylcypromine may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Trastuzumab Trastuzumab may increase the cardiotoxic activities of Sunitinib. Approved, Investigational Trimetrexate The metabolism of Sunitinib can be decreased when combined with Trimetrexate. Approved, Investigational Troglitazone Troglitazone may increase the hypoglycemic activities of Sunitinib. Investigational, Withdrawn Trolamine salicylate Trolamine salicylate may increase the hypoglycemic activities of Sunitinib. Approved Trovafloxacin Trovafloxacin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational, Withdrawn Typhoid Vaccine The risk or severity of adverse effects can be increased when Sunitinib is combined with Typhoid Vaccine. Approved Valproic Acid The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Valproic Acid. Approved, Investigational Vandetanib Sunitinib may increase the QTc-prolonging activities of Vandetanib. Approved Varicella Zoster Vaccine (Live/Attenuated) The risk or severity of adverse effects can be increased when Sunitinib is combined with Varicella Zoster Vaccine (Live/Attenuated). Approved Vecuronium The serum concentration of Vecuronium can be increased when it is combined with Sunitinib. Approved Vemurafenib The serum concentration of Sunitinib can be decreased when it is combined with Vemurafenib. Approved Venlafaxine The serum concentration of Venlafaxine can be increased when it is combined with Sunitinib. Approved Verapamil The serum concentration of Sunitinib can be increased when it is combined with Verapamil. Approved Vildagliptin Vildagliptin may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Vincristine The excretion of Vincristine can be decreased when combined with Sunitinib. Approved, Investigational Voglibose Voglibose may increase the hypoglycemic activities of Sunitinib. Approved, Investigational Voriconazole The metabolism of Sunitinib can be decreased when combined with Voriconazole. Approved, Investigational Wortmannin The metabolism of Sunitinib can be decreased when combined with Wortmannin. Experimental Yellow Fever Vaccine The risk or severity of adverse effects can be increased when Sunitinib is combined with Yellow Fever Vaccine. Approved, Investigational Zidovudine The risk or severity of adverse effects can be increased when Sunitinib is combined with Zidovudine. Approved Zimelidine Zimelidine may increase the hypoglycemic activities of Sunitinib. Withdrawn Ziprasidone Sunitinib may increase the QTc-prolonging activities of Ziprasidone. Approved Zoledronic acid The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Sunitinib is combined with Zoledronic acid. Approved Zuclopenthixol Sunitinib may increase the QTc-prolonging activities of Zuclopenthixol. Approved, Investigational - Food Interactions
- Not Available
References
- Synthesis Reference
Ettore BIGATTI, Augusto CANAVESI, Peter Lindsay MACDONALD, Francesca Scarpitta, "PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF." U.S. Patent US20090247767, issued October 01, 2009.
US20090247767- General References
- Motzer RJ, Hutson TE, Tomczak P, Michaelson MD, Bukowski RM, Rixe O, Oudard S, Negrier S, Szczylik C, Kim ST, Chen I, Bycott PW, Baum CM, Figlin RA: Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007 Jan 11;356(2):115-24. [PubMed:17215529]
- Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, McArthur G, Judson IR, Heinrich MC, Morgan JA, Desai J, Fletcher CD, George S, Bello CL, Huang X, Baum CM, Casali PG: Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006 Oct 14;368(9544):1329-38. [PubMed:17046465]
- External Links
- Human Metabolome Database
- HMDB0015397
- KEGG Drug
- D06402
- PubChem Compound
- 5329102
- PubChem Substance
- 46507140
- ChemSpider
- 4486264
- BindingDB
- 4814
- ChEBI
- 38940
- ChEMBL
- CHEMBL535
- Therapeutic Targets Database
- DCL000646
- PharmGKB
- PA162372840
- HET
- B49
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Sunitinib
- ATC Codes
- L01XE04 — Sunitinib
- AHFS Codes
- 10:00.00 — Antineoplastic Agents
- PDB Entries
- 2y7j / 3g0e / 3g0f / 3miy / 3ti1 / 4agd / 4ks8 / 4qmz
- FDA label
- Download (159 KB)
- MSDS
- Download (98.3 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Pfizer Inc.
- Dosage forms
Form Route Strength Capsule Oral 12.5 mg Capsule Oral 12.5 mg/1 Capsule Oral 25 mg/1 Capsule Oral 25 mg Capsule Oral 37.5 mg Capsule Oral 37.5 mg/1 Capsule Oral 50 mg/1 Capsule Oral 50 mg - Prices
Unit description Cost Unit Sutent 50 mg capsule 333.39USD capsule Sutent 25 mg capsule 187.28USD capsule Sutent 12.5 mg capsule 93.64USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) CA2395461 No 2010-05-25 2020-12-22 Canada CA2399358 No 2006-03-21 2021-02-15 Canada US6573293 No 2001-02-15 2021-02-15 US US7211600 No 2000-12-22 2020-12-22 US US7125905 No 2001-02-15 2021-02-15 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility >25 mg/mL over pH of 1.2 to 6.8 FDA label logP 5.2 FDA label pKa 8.95 FDA label - Predicted Properties
Property Value Source Water Solubility 0.0308 mg/mL ALOGPS logP 3.24 ALOGPS logP 2.93 ChemAxon logS -4.1 ALOGPS pKa (Strongest Acidic) 11.46 ChemAxon pKa (Strongest Basic) 9.04 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 77.23 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 116.27 m3·mol-1 ChemAxon Polarizability 44.32 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9938 Blood Brain Barrier + 0.7993 Caco-2 permeable - 0.5948 P-glycoprotein substrate Substrate 0.8648 P-glycoprotein inhibitor I Inhibitor 0.6809 P-glycoprotein inhibitor II Non-inhibitor 0.5466 Renal organic cation transporter Non-inhibitor 0.7385 CYP450 2C9 substrate Non-substrate 0.8727 CYP450 2D6 substrate Non-substrate 0.7716 CYP450 3A4 substrate Substrate 0.641 CYP450 1A2 substrate Non-inhibitor 0.5626 CYP450 2C9 inhibitor Non-inhibitor 0.6437 CYP450 2D6 inhibitor Non-inhibitor 0.6846 CYP450 2C19 inhibitor Non-inhibitor 0.6261 CYP450 3A4 inhibitor Non-inhibitor 0.5991 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7032 Ames test Non AMES toxic 0.5699 Carcinogenicity Non-carcinogens 0.784 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6794 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8597 hERG inhibition (predictor II) Inhibitor 0.8398
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as indolines. These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Indolines
- Direct Parent
- Indolines
- Alternative Parents
- Pyrrole carboxamides / Substituted pyrroles / Aryl fluorides / Benzenoids / Vinylogous amides / Heteroaromatic compounds / Trialkylamines / Secondary carboxylic acid amides / Amino acids and derivatives / Lactams show 6 more
- Substituents
- Dihydroindole / Pyrrole-3-carboxamide / Pyrrole-3-carboxylic acid or derivatives / Aryl fluoride / Aryl halide / Substituted pyrrole / Benzenoid / Pyrrole / Heteroaromatic compound / Vinylogous amide show 20 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- monocarboxylic acid amide, pyrroles (CHEBI:38940)
Targets
- 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...
- Gene Name
- PDGFRB
- Uniprot ID
- P09619
- Uniprot Name
- Platelet-derived growth factor receptor beta
- Molecular Weight
- 123966.895 Da
References
- Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485]
- Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309]
- Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710]
- Pietras K, Hanahan D: A multitargeted, metronomic, and maximum-tolerated dose "chemo-switch" regimen is antiangiogenic, producing objective responses and survival benefit in a mouse model of cancer. J Clin Oncol. 2005 Feb 10;23(5):939-52. Epub 2004 Nov 22. [PubMed:15557593]
- Gollob JA: Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):167-74. [PubMed:16425993]
- 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 ...
- Gene Name
- FLT1
- Uniprot ID
- P17948
- Uniprot Name
- Vascular endothelial growth factor receptor 1
- Molecular Weight
- 150767.185 Da
References
- O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525]
- Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763]
- 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 main...
- Gene Name
- KIT
- Uniprot ID
- P10721
- Uniprot Name
- Mast/stem cell growth factor receptor Kit
- Molecular Weight
- 109863.655 Da
References
- Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309]
- Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999]
- Joensuu H: Second line therapies for the treatment of gastrointestinal stromal tumor. Curr Opin Oncol. 2007 Jul;19(4):353-8. [PubMed:17545799]
- Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710]
- Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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 ...
- Gene Name
- KDR
- Uniprot ID
- P35968
- Uniprot Name
- Vascular endothelial growth factor receptor 2
- Molecular Weight
- 151525.555 Da
References
- Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485]
- Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999]
- Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710]
- Schoffski P, Dumez H, Clement P, Hoeben A, Prenen H, Wolter P, Joniau S, Roskams T, Van Poppel H: Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review. Ann Oncol. 2006 Aug;17(8):1185-96. Epub 2006 Jan 17. [PubMed:16418310]
- Amino N, Ideyama Y, Yamano M, Kuromitsu S, Tajinda K, Samizu K, Hisamichi H, Matsuhisa A, Shirasuna K, Kudoh M, Shibasaki M: YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. [PubMed:16533791]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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 cardi...
- Gene Name
- FLT4
- Uniprot ID
- P35916
- Uniprot Name
- Vascular endothelial growth factor receptor 3
- Molecular Weight
- 152755.94 Da
References
- Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763]
- Deprimo SE, Bello CL, Smeraglia J, Baum CM, Spinella D, Rini BI, Michaelson MD, Motzer RJ: Circulating protein biomarkers of pharmacodynamic activity of sunitinib in patients with metastatic renal cell carcinoma: modulation of VEGF and VEGF-related proteins. J Transl Med. 2007 Jul 2;5:32. [PubMed:17605814]
- Katoh Y, Katoh M: Comparative integromics on VEGF family members. Int J Oncol. 2006 Jun;28(6):1585-9. [PubMed:16685460]
- Gridelli C, Maione P, Del Gaizo F, Colantuoni G, Guerriero C, Ferrara C, Nicolella D, Comunale D, De Vita A, Rossi A: Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer. Oncologist. 2007 Feb;12(2):191-200. [PubMed:17296815]
- Ahmed SI, Thomas AL, Steward WP: Vascular endothelial growth factor (VEGF) inhibition by small molecules. J Chemother. 2004 Nov;16 Suppl 4:59-63. [PubMed:15688612]
- 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 cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells...
- Gene Name
- FLT3
- Uniprot ID
- P36888
- Uniprot Name
- Receptor-type tyrosine-protein kinase FLT3
- Molecular Weight
- 112902.51 Da
References
- O'Farrell AM, Abrams TJ, Yuen HA, Ngai TJ, Louie SG, Yee KW, Wong LM, Hong W, Lee LB, Town A, Smolich BD, Manning WC, Murray LJ, Heinrich MC, Cherrington JM: SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16. [PubMed:12531805]
- O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525]
- Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710]
- Schmidt-Arras D, Schwable J, Bohmer FD, Serve H: Flt3 receptor tyrosine kinase as a drug target in leukemia. Curr Pharm Des. 2004;10(16):1867-83. [PubMed:15180525]
- Yee KW, Schittenhelm M, O'Farrell AM, Town AR, McGreevey L, Bainbridge T, Cherrington JM, Heinrich MC: Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells. Blood. 2004 Dec 15;104(13):4202-9. Epub 2004 Aug 10. [PubMed:15304385]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Protein homodimerization activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor ...
- Gene Name
- CSF1R
- Uniprot ID
- P07333
- Uniprot Name
- Macrophage colony-stimulating factor 1 receptor
- Molecular Weight
- 107982.955 Da
References
- Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB: Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006 Apr;5(4):1007-13. [PubMed:16648572]
- Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763]
- 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 chem...
- Gene Name
- PDGFRA
- Uniprot ID
- P16234
- Uniprot Name
- Platelet-derived growth factor receptor alpha
- Molecular Weight
- 122668.46 Da
References
- Prenen H, Cools J, Mentens N, Folens C, Sciot R, Schoffski P, Van Oosterom A, Marynen P, Debiec-Rychter M: Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Clin Cancer Res. 2006 Apr 15;12(8):2622-7. [PubMed:16638875]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein group
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- Filppula AM, Neuvonen PJ, Backman JT: In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9. doi: 10.1124/dmd.114.057695. Epub 2014 Apr 8. [PubMed:24713129]
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Atpase activity, coupled to transmembrane movement of substances
- Specific Function
- May be an organic anion pump relevant to cellular detoxification.
- Gene Name
- ABCC4
- Uniprot ID
- O15439
- Uniprot Name
- Multidrug resistance-associated protein 4
- Molecular Weight
- 149525.33 Da
References
- Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380]
- 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
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380]
- Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380]
- 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 fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380]
- Dai CL, Liang YJ, Wang YS, Tiwari AK, Yan YY, Wang F, Chen ZS, Tong XZ, Fu LW: Sensitization of ABCG2-overexpressing cells to conventional chemotherapeutic agent by sunitinib was associated with inhibiting the function of ABCG2. Cancer Lett. 2009 Jun 28;279(1):74-83. doi: 10.1016/j.canlet.2009.01.027. Epub 2009 Feb 18. [PubMed:19232821]
- Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320]
Drug created on May 16, 2007 14:11 / Updated on August 14, 2018 04:31