Identification

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
Thumb
Synonyms
  • sunitinib
  • Sunitinibum
External IDs
SU-011248 / SU-11248 / SU011248 / SU11248
Product Ingredients
IngredientUNIICASInChI Key
Sunitinib malateLVX8N1UT73341031-54-7LBWFXVZLPYTWQI-IPOVEDGCSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SutentCapsule12.5 mg/1OralPfizer Laboratories Div Pfizer Inc.2006-01-26Not applicableUs
SutentCapsule12.5 mgOralPfizer2006-06-22Not applicableCanada
SutentCapsule50 mgOralPfizer2006-07-19Not applicableEu
SutentCapsule50 mgOralPfizer2006-06-22Not applicableCanada
SutentCapsule25 mgOralPfizer2006-07-19Not applicableEu
SutentCapsule50 mg/1OralPfizer Laboratories Div Pfizer Inc.2006-01-26Not applicableUs
SutentCapsule12.5 mgOralPfizer2006-07-19Not applicableEu
SutentCapsule37.5 mgOralPfizer2006-07-19Not applicableEu
SutentCapsule25 mg/1OralPfizer Laboratories Div Pfizer Inc.2006-01-26Not applicableUs
SutentCapsule25 mgOralPfizer2006-06-22Not applicableCanada
Categories
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.

TargetActionsOrganism
APlatelet-derived growth factor receptor beta
inhibitor
Human
AVascular endothelial growth factor receptor 1
inhibitor
Human
AMast/stem cell growth factor receptor Kit
inhibitor
Human
AVascular endothelial growth factor receptor 2
inhibitor
Human
AVascular endothelial growth factor receptor 3
inhibitor
Human
AReceptor-type tyrosine-protein kinase FLT3
inhibitor
Human
AMacrophage colony-stimulating factor 1 receptor
inhibitor
Human
APlatelet-derived growth factor receptor alpha
inhibitor
Human
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/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 3A4---(A;A) / (A;G)G > AADR Directly StudiedPatients 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
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Sunitinib.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Sunitinib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Sunitinib is combined with 2-Methoxyethanol.
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Sunitinib is combined with 2,4-thiazolidinedione.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Sunitinib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Sunitinib.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Sunitinib can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Sunitinib.
5-FluorouridineThe risk or severity of QTc prolongation can be increased when 5-Fluorouridine is combined with Sunitinib.
6-Deoxyerythronolide BThe metabolism of Sunitinib can be decreased when combined with 6-Deoxyerythronolide B.
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
  1. 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]
  2. 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
PhaseStatusPurposeConditionsCount
0CompletedTreatmentGlioblastomas / Neoplasms, Brain1
0CompletedTreatmentTumors, Solid1
1Active Not RecruitingTreatmentAdult Solid Neoplasm1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentClear-cell Metastatic Renal Cell Carcinoma / Renal Cell Adenocarcinoma1
1Active Not RecruitingTreatmentGastrointestinal Stromal Tumors1
1Active Not RecruitingTreatmentMetastatic Brain Tumors1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceBlood Pressures1
1CompletedDiagnosticRenal Cell Adenocarcinoma1
1CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome / Acute Undifferentiated Leukemia (AUL) / Adult Acute Lymphoblastic Leukemia in Remission / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Grade III Lymphomatoid Granulomatosis / Adult Langerhans Cell Histiocytosis / Adult Nasal Type Extranodal NK/T-Cell Lymphoma / Aggressive NK-cell Leukemia / AIDS-Related Diffuse Large Cell Lymphoma / AIDS-Related Diffuse Mixed Cell Lymphoma / AIDS-Related Diffuse Small Cleaved Cell Lymphoma / AIDS-related Immunoblastic Large Cell Lymphoma / AIDS-Related Lymphoblastic Lymphoma / Aids-related Malignancies / AIDS-related Small Noncleaved Cell Lymphoma / Anaplastic Large Cell Lymphoma / Angioimmunoblastic T-Cell Lymphoma / Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative / Chronic Eosinophilic Leukemia (CEL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic Myelomonocytic Leukemia / Chronic Neutrophilic Leukemia / Chronic Phase Chronic Myelogenous Leukemia / Clear Cell Renal Cell Carcinoma / Cutaneous B-Cell Non-Hodgkin Lymphoma / De Novo Myelodysplastic Syndromes / Essential Thrombocythemia (ET) / Extramedullary Plasmacytoma / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Hepatosplenic T-Cell Lymphoma / HIV-associated Hodgkin Lymphoma / Human Immunodeficiency Virus (HIV) Infections / Intraocular Lymphoma / Isolated Plasmacytoma of Bone / Leukemia, Prolymphocytic / Light Chain Deposition Disease / Malignant mast cell neoplasm / Myelodysplastic Syndrome With Isolated Del(5q) / Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable / Myeloid/NK-cell Acute Leukemia / Nodal marginal zone B-cell lymphomas / Noncutaneous Extranodal Lymphoma / Osteolytic Lesions of Multiple Myeloma / Peripheral T-Cell Lymphoma (PTCL) / Plasma Cell Neoplasms / Polycythemia Vera (PV) / Post Transplant Lymphoproliferative Disorder / Previously Treated Myelodysplastic Syndromes / Primary Myelofibrosis / Primary Systemic Amyloidosis / Progressive Hairy Cell Leukemia, Initial Treatment / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Adult Diffuse Small Cleaved Cell Lymphoma / Recurrent Adult Grade III Lymphomatoid Granulomatosis / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult Immunoblastic Large Cell Lymphoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Adult T-Cell Leukemia/Lymphoma / Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Mycosis Fungoides/Sezary Syndrome / Recurrent Small Lymphocytic Lymphoma / Refractory Hairy Cell Leukemia / Refractory Multiple Myeloma / Relapsing Chronic Myelogenous Leukemia / Renal Cell Cancer, Recurrent / Stage IV Renal Cell Cancer / T-Cell Large Granular Lymphocyte Leukemia / Testicular Lymphoma / Unspecified Adult Solid Tumor, Protocol Specific / Waldenström's Macroglobulinemia (WM)1
1CompletedTreatmentAdenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage III Pancreatic Cancer / Stage IV Pancreatic Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentAdult Solid Neoplasm / Clear Cell Renal Cell Carcinoma / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentAdvanced Solid Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentCancer, Breast1
1CompletedTreatmentCancer, Breast / Neoplasms / Tumors, Solid1
1CompletedTreatmentCentral Nervous System Metastases / Childhood Central Nervous System Choriocarcinoma / Childhood Central Nervous System Embryonal Tumor / Childhood Central Nervous System Germ Cell Tumor / Childhood Central Nervous System Germinoma / Childhood Central Nervous System Mixed Germ Cell Tumor / Childhood Central Nervous System Teratoma / Childhood Central Nervous System Yolk Sac Tumor / Recurrent Childhood Central Nervous System Embryonal Tumor / Unspecified Childhood Solid Tumor, Protocol Specific1
1CompletedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Cancer, Recurrent / Stage I Renal Cell Cancer / Stage II Renal Cell Cancer / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentClear Cell Sarcoma of the Kidney / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
1CompletedTreatmentGIST / Renal Cancers1
1CompletedTreatmentGlioblastomas1
1CompletedTreatmentHead and Neck Carcinoma / Malignancies / Nervous System Neoplasms / Pelvic Cancer / Thoracic Neoplasms1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
1CompletedTreatmentMalignancies2
1CompletedTreatmentMetastatic Melanoma1
1CompletedTreatmentMetastatic Renal Cell Cancer1
1CompletedTreatmentMetastatic Renal Cell Carcinoma / Renal Cancers1
1CompletedTreatmentNeoplasms2
1CompletedTreatmentNeoplasms, Breast2
1CompletedTreatmentNeoplasms, Colorectal1
1CompletedTreatmentNeoplasms, Malignant1
1CompletedTreatmentNeoplasms / Neoplasms, Colorectal1
1CompletedTreatmentNon GIST Sarcomas1
1CompletedTreatmentProstate Cancer2
1CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma2
1CompletedTreatmentRenal Cell Adenocarcinoma2
1CompletedTreatmentSoft Tissue Sarcoma (STS)1
1CompletedTreatmentStomach Neoplasms3
1CompletedTreatmentTumors, Solid3
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia Acute Myeloid Leukemia (AML) / Untreated Adult Acute Myeloid Leukemia1
1RecruitingTreatmentProstatic Neoplasms1
1RecruitingTreatmentTumors, Solid1
1TerminatedTreatmentAdvanced Solid Tumors / Cancer, Advanced1
1TerminatedTreatmentCancer, Breast1
1TerminatedTreatmentClear-cell Metastatic Renal Cell Carcinoma / Genitourinary tract neoplasm / Kidney Diseases / Neoplasms / Neoplasms by Histologic Type / Neoplasms, Kidney / Renal Cell Adenocarcinoma / Urologic Diseases / Urologic Neoplasms1
1TerminatedTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
1TerminatedTreatmentGastrointestinal Stromal Tumors1
1TerminatedTreatmentMetastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Stage III Salivary Gland Cancer / Stage III Squamous Cell Carcinoma of the Hypopharynx / Stage III Squamous Cell Carcinoma of the Larynx / Stage III Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage III Squamous Cell Carcinoma of the Nasopharynx / Stage III Squamous Cell Carcinoma of the Oropharynx / Stage III Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage III Verrucous Carcinoma of the Larynx / Stage III Verrucous Carcinoma of the Oral Cavity / Stage IV Salivary Gland Cancer / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IV Verrucous Carcinoma of the Larynx / Stage IV Verrucous Carcinoma of the Oral Cavity / Tongue Cancer / Untreated Metastatic Squamous Neck Cancer With Occult Primary1
1TerminatedTreatmentRenal Cancers1
1TerminatedTreatmentTumors1
1Unknown StatusTreatmentMalignant Solid Tumours1
1WithdrawnTreatmentAnaplastic Gliomas / Gliosarcoma / Recurrent Glioblastoma1
1, 2Active Not RecruitingTreatmentExtensive Stage Small Cell Lung Cancer / Extensive Stage Small Cell Lung Carcinoma / Recurrent Small Cell Lung Carcinoma / Refractory Small cell lung cancer1
1, 2Active Not RecruitingTreatmentGastrointestinal Stromal Tumors1
1, 2Active Not RecruitingTreatmentMalignancies1
1, 2CompletedTreatmentCancer, Breast3
1, 2CompletedTreatmentGastrointestinal Stromal Tumors1
1, 2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2CompletedTreatmentMalignancies1
1, 2CompletedTreatmentProstatic Neoplasms1
1, 2CompletedTreatmentRenal Cell Adenocarcinoma1
1, 2Not Yet RecruitingTreatmentEbola Virus Disease1
1, 2RecruitingTreatmentAdvanced Renal Cell Carcinoma / Renal Cancers / Renal Cell Adenocarcinoma1
1, 2RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
1, 2RecruitingTreatmentRenal Cell Adenocarcinoma1
1, 2RecruitingTreatmentSarcoma, Bone / Soft Tissue Sarcoma (STS)1
1, 2TerminatedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer / Recurrent Prostate Cancer / Stage I Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
1, 2TerminatedTreatmentCarcinoma, Colorectal1
1, 2TerminatedTreatmentMelanoma1
1, 2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
1, 2TerminatedTreatmentMetastatic Malignant Melanoma1
1, 2TerminatedTreatmentNeoplasms, Breast1
1, 2TerminatedTreatmentRenal Cell Adenocarcinoma3
1, 2TerminatedTreatmentVon Hippel-Lindau Syndrome1
1, 2Unknown StatusTreatmentCancer, Breast1
1, 2Unknown StatusTreatmentSoft Tissue Sarcoma (STS)1
1, 2Unknown StatusTreatmentUrinary Bladder Neoplasms1
2Active Not RecruitingTreatmentAdvanced Rare Tumours1
2Active Not RecruitingTreatmentAdvanced Renal Cell Carcinoma1
2Active Not RecruitingTreatmentCarcinoid Tumors1
2Active Not RecruitingTreatmentClear Cell Renal Cell Carcinoma / Clear-cell Kidney Carcinoma / RCC / Renal Cancers1
2Active Not RecruitingTreatmentClear Cell Renal Cell Carcinoma / Metastatic Renal Cell Cancer / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v7 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V71
2Active Not RecruitingTreatmentEndometrial Adenocarcinomas / Endometrial Endometrioid Adenocarcinoma / Endometrial Serous Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage IVA Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer AJCC v7 / Stage IVB Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer AJCC v7 / Uterine Carcinosarcoma / Uterine Corpus Carcinosarcoma1
2Active Not RecruitingTreatmentEsophageal Cancers1
2Active Not RecruitingTreatmentGenitourinary Cancers / Renal Cancers1
2Active Not RecruitingTreatmentInflammatory carcinoma of the breast / Male Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentMetastatic Clear Cell Renal Cell Carcinoma1
2Active Not RecruitingTreatmentMetastatic Renal Cell Carcinoma3
2Active Not RecruitingTreatmentMetastatic Uveal Melanoma1
2Active Not RecruitingTreatmentNeoplasms, Pancreatic / Neuroendocrine Tumors1
2Active Not RecruitingTreatmentOvarian Clear Cell Adenocarcinoma / Recurrent Ovarian Carcinoma1
2Active Not RecruitingTreatmentProstate Cancer2
2Active Not RecruitingTreatmentRecurrent Thyroid Gland Carcinoma / Stage III Thyroid Gland Follicular Carcinoma / Stage III Thyroid Gland Follicular Carcinoma AJCC v7 / Stage III Thyroid Gland Medullary Carcinoma / Stage III Thyroid Gland Medullary Carcinoma AJCC v7 / Stage IV Thyroid Gland Follicular Carcinoma / Stage IV Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IV Thyroid Gland Medullary Carcinoma / Stage IV Thyroid Gland Medullary Carcinoma AJCC v7 / Stage IV Thyroid Gland Papillary Carcinoma / Stage IV Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVA Thyroid Gland Follicular Carcinoma / Stage IVA Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVA Thyroid Gland Medullary Carcinoma / Stage IVA Thyroid Gland Medullary Carcinoma AJCC v7 / Stage IVA Thyroid Gland Papillary Carcinoma / Stage IVA Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVB Thyroid Gland Follicular Carcinoma / Stage IVB Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVB Thyroid Gland Medullary Carcinoma / Stage IVB Thyroid Gland Medullary Carcinoma AJCC v7 / Stage IVB Thyroid Gland Papillary Carcinoma / Stage IVB Thyroid Gland Papillary Carcinoma AJCC v7 / Stage IVC Thyroid Gland Follicular Carcinoma / Stage IVC Thyroid Gland Follicular Carcinoma AJCC v7 / Stage IVC Thyroid Gland Medullary Carcinoma / Stage IVC Thyroid Gland Medullary Carcinoma AJCC v7 / Stage IVC Thyroid Gland Papillary Carcinoma / Stage IVC Thyroid Gland Papillary Carcinoma AJCC v7 / Thyroid Gland Oncocytic Follicular Carcinoma / Unresectable Thyroid Gland Carcinoma1
2Active Not RecruitingTreatmentRenal Cancers2
2Active Not RecruitingTreatmentRenal Cell Adenocarcinoma4
2Active Not RecruitingTreatmentRenal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v7 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V71
2Active Not RecruitingTreatmentRenal Cell Carcinoma, Metastatic1
2Active Not RecruitingTreatmentThymic Carcinoma1
2Active Not RecruitingTreatmentAdvanced thymic carcinoma / Thymus Neoplasms1
2Active Not RecruitingTreatmentUrinary Tract Urothelial Carcinoma1
2CompletedTreatmentAcinar Cell Adenocarcinoma of the Pancreas / Duct Cell Adenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage IV Pancreatic Cancer1
2CompletedTreatmentAcral Lentiginous Malignant Melanoma / Mucosal Lentiginous Melanoma1
2CompletedTreatmentAdenocarcinoma of the Cervix / Cervical Adenosquamous Cell Carcinoma / Cervical Squamous Cell Carcinoma / Recurrent Cervical Cancer / Stage IVB Cervical Cancer1
2CompletedTreatmentAdenocarcinomas1
2CompletedTreatmentAdenocarcinomas of the Gastroesophageal Junction / Esophageal Cancers1
2CompletedTreatmentAdenocarcinomas / Lung Cancers1
2CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Diffuse Astrocytoma / Adult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Adult Mixed Glioma / Adult Oligodendroglioma / Adult Pineal Gland Astrocytoma1
2CompletedTreatmentAdult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Stage IV Adult Diffuse Large Cell Lymphoma1
2CompletedTreatmentAdult Malignant Fibrous Histiocytoma of Bone / Cancer of the Ovary / Desmoid Tumors / Endometrial Cancers / Sarcomas / Small Intestine Cancer1
2CompletedTreatmentAdults / Bladder Cancers / Urothelial Cancer1
2CompletedTreatmentAdvanced Biliary Tract Adenocarcinoma1
2CompletedTreatmentAdvanced Gastric Cancer1
2CompletedTreatmentAdvanced Malignant Mesothelioma / Recurrent Malignant Mesothelioma1
2CompletedTreatmentAdvanced Non-clear Cell Renal Cell Carcinoma1
2CompletedTreatmentAdvanced/Metastatic Breast Cancer1
2CompletedTreatmentAdverse Effects / Cancer of the Ovary1
2CompletedTreatmentAnaplastic Astrocytoma (AA) / Glioblastomas1
2CompletedTreatmentB-Cell Chronic Lymphocytic Leukemia / Chronic Lymphocytic Leukemia (CLL) - Refractory / Recurrent Small Lymphocytic Lymphoma1
2CompletedTreatmentBladder Cancers1
2CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter1
2CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter / Urethral Cancer2
2CompletedTreatmentBladder Cancers / Urinary Bladder1
2CompletedTreatmentCancer of the Fallopian Tube / Platinum Refractory Epithelial Ovarian Cancer / Primary Cancer of the Peritoneum1
2CompletedTreatmentCancer of the Ovary / Extragonadal Germ Cell Tumor / Teratoma / Testicular germ cell tumour1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentCarcinoma Renal Cells1
2CompletedTreatmentCarcinoma, Adenoid Cystic / Salivary Gland Cancers1
2CompletedTreatmentCarcinoma, Renal Cell Metastasis1
2CompletedTreatmentChildhood Cerebellar Anaplastic Astrocytoma / Childhood Cerebral Anaplastic Astrocytoma / Childhood Cerebral Astrocytoma / Childhood Infratentorial Ependymoma / Childhood Mixed Glioma / Childhood Oligodendroglioma / Childhood Supratentorial Ependymoma / Recurrent Childhood Cerebellar Astrocytoma / Recurrent Childhood Cerebral Astrocytoma / Recurrent Childhood Ependymoma / Recurrent Childhood Subependymal Giant Cell Astrocytoma1
2CompletedTreatmentChronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndromes / Myelodysplastic Syndromes / Secondary Myelodysplastic Syndromes1
2CompletedTreatmentClear Cell Renal Cell Carcinoma / Stage IV Renal Cell Cancer1
2CompletedTreatmentClear Cell, Metastatic Renal Cell Carcinoma1
2CompletedTreatmentCns Cancer / Hemangioblastomas / Intracranial Hemangiopericytoma / Meningiomas / Neurofibromatosis1
2CompletedTreatmentDifferentiated Thyroid Cancer (DTC) / Follicular Thyroid Cancer / Thyroid Papillary Carcinoma1
2CompletedTreatmentDisease-Free Survival / Neoplasms, Hormone-Dependent / Prostatic Neoplasms / Survival Rate / Tumor Markers, Biological1
2CompletedTreatmentEsophageal Cancers2
2CompletedTreatmentExtensive-Stage Small Cell Lung Cancer1
2CompletedTreatmentFibrosarcomas malignant / Leiomyosarcomas / Liposarcoma / Malignant Fibrous Histiocytoma1
2CompletedTreatmentGastro Intestinal Stromal Tumor1
2CompletedTreatmentGastrointestinal Stromal Tumors2
2CompletedTreatmentGlioblastomas1
2CompletedTreatmentHepatic Metastases / Metastatic Colorectal Cancers1
2CompletedTreatmentHepatocellular,Carcinoma / Liver Cancer1
2CompletedTreatmentIslet Cell Tumor / Neuroendocrine Tumors1
2CompletedTreatmentLiver Cancer1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)5
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2CompletedTreatmentLung Cancers2
2CompletedTreatmentMalignancies / Renal Cell Adenocarcinoma1
2CompletedTreatmentMalignancies / Thyroid Carcinoma1
2CompletedTreatmentMalignant Neoplasm of Pancreas2
2CompletedTreatmentMelanoma (Skin) / Metastatic Cancers / Renal Cancers1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentMetastatic Cancers / Renal Cancers1
2CompletedTreatmentMetastatic Hormone Refractory Prostate Cancer1
2CompletedTreatmentMetastatic Melanoma1
2CompletedTreatmentMetastatic Renal Cell Cancer / Renal Cell Adenocarcinoma1
2CompletedTreatmentMetastatic Renal Cell Carcinoma3
2CompletedTreatmentMetastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity1
2CompletedTreatmentNeoplasm Metastases / Renal Cell Adenocarcinoma1
2CompletedTreatmentNeoplasms, Breast4
2CompletedTreatmentNeoplasms, Colorectal1
2CompletedTreatmentNeoplasms, Hepatic / Unresectable Hepatocellular Carcinoma1
2CompletedTreatmentNeuroendocrine Tumors1
2CompletedTreatmentNon-Small Cell Lung Cancer Recurrent / Recurrent Non-Small Cell Lung Carcinoma / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v7 / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v71
2CompletedTreatmentNon-clear Cell Renal Cell Cancer1
2CompletedTreatmentParaganglioma / Pheochromocytomas1
2CompletedTreatmentPatients With Advanced Urothelial Carcinoma / Transitional Cell Carcinoma1
2CompletedTreatmentProgressive Neuroendocrine Tumors of pancreatic origin1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentProstate Cancer / Prostatectomy1
2CompletedTreatmentRecurrent Bladder Cancer / Transitional Cell Carcinoma of the Bladder1
2CompletedTreatmentRecurrent Fallopian Tube Cancer / Recurrent Ovarian Epithelial Cancer / Recurrent Primary Peritoneal Cavity Cancer / Stage IIIA Fallopian Tube Cancer / Stage IIIA Ovarian Epithelial Cancer / Stage IIIA Primary Peritoneal Cavity Cancer / Stage IIIB Fallopian Tube Cancer / Stage IIIB Ovarian Epithelial Cancer / Stage IIIB Primary Peritoneal Cavity Cancer / Stage IIIC Fallopian Tube Cancer / Stage IIIC Ovarian Epithelial Cancer / Stage IIIC Primary Peritoneal Cavity Cancer / Stage IV Fallopian Tube Cancer / Stage IV Ovarian Epithelial Cancer / Stage IV Primary Peritoneal Cavity Cancer1
2CompletedTreatmentRecurrent Thyroid Cancer / Stage IVA Follicular Thyroid Cancer / Stage IVA Papillary Thyroid Cancer / Stage IVB Follicular Thyroid Cancer / Stage IVB Papillary Thyroid Cancer / Stage IVC Follicular Thyroid Cancer / Stage IVC Papillary Thyroid Cancer / Thyroid Gland Medullary Carcinoma1
2CompletedTreatmentRecurrent Uterine Sarcoma / Uterine Leiomyosarcoma1
2CompletedTreatmentRefractory Multiple Myeloma / Stage I Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
2CompletedTreatmentRelapsed or Cisplatin-Refractory Germ Cell Cancer1
2CompletedTreatmentRenal Cancers4
2CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
2CompletedTreatmentRenal Cell Adenocarcinoma7
2CompletedTreatmentStomach Neoplasms1
2CompletedTreatmentUnresectable and Advanced Cholangiocarcinoma1
2CompletedTreatmentUnresectable or Metastatic Colorectal Cancer1
2CompletedTreatmentUrothelial Cancer1
2CompletedTreatmentVon Hippel-Lindau Disease1
2Not Yet RecruitingTreatmentCentral Nervous System Sarcoma / Gliosarcoma1
2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Acute Myelogenous Leukaemia (AML) / Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Chronic Myelomonocytic Leukemia / Myelodysplastic Syndrome / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Refractory Adult Acute Lymphoblastic Leukemia1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentAlveolar Soft Part Sarcoma (ASPS)1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentCancer, Breast / Lung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Neoplasm of Stomach / Prostate Cancer / Tumors, Solid1
2RecruitingTreatmentCiliary Body and Choroid Melanoma, Medium/Large Size / Ciliary Body and Choroid Melanoma, Small Size / Iris Melanoma / Stage I Intraocular Melanoma / Stage IIA Intraocular Melanoma / Stage IIB Intraocular Melanoma / Stage IIIA Intraocular Melanoma / Stage IIIB Intraocular Melanoma / Stage IIIC Intraocular Melanoma1
2RecruitingTreatmentClear Cell Metastatic Renal Cell Carcinoma1
2RecruitingTreatmentClear Cell Renal Cell Carcinoma2
2RecruitingTreatmentGlioblastoma Multiforme (GBM)1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Small Cell Lung Carcinoma / Thymic Carcinoma1
2RecruitingTreatmentMalignant Neoplasms of Urinary Tract / Renal Cell Adenocarcinoma1
2RecruitingTreatmentMalignant Progressive Pheochromocytoma and Paraganglioma (PPGL)1
2RecruitingTreatmentMetastatic Renal Cell Cancer / Neoplasms, Kidney1
2RecruitingTreatmentMetastatic Renal Cell Carcinoma2
2RecruitingTreatmentNeuroendocrine Carcinomas / Neuroendocrine Neoplasms / Neuroendocrine Tumors / Neuroendocrine Tumors of the Gastrointestinal Tract and Pancreas1
2RecruitingTreatmentPancreatic Neuroendocrine Carcinoma1
2RecruitingTreatmentPancreatic Neuroendocrine Tumour Metastatic1
2RecruitingTreatmentRenal Cell Adenocarcinoma1
2RecruitingTreatmentThymic Carcinoma / Type B3 Thymoma1
2SuspendedTreatmentRenal Cell Adenocarcinoma1
2SuspendedTreatmentRenal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v7 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V7 / Type 1 Papillary Renal Cell Carcinoma / Type 2 Papillary Renal Cell Carcinoma / Unresectable Renal Cell Carcinoma1
2SuspendedTreatmentThymic Carcinoma1
2TerminatedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Acute Undifferentiated Leukemia (AUL) / Adult Acute Lymphoblastic Leukemia in Remission / Adult Acute Myeloid Leukemia in Remission / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative / Blastic Phase Chronic Myelogenous Leukemia / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic Myelomonocytic Leukemia / Chronic Phase Chronic Myelogenous Leukemia / Leukemia, Prolymphocytic / Malignant mast cell neoplasm / Meningeal Chronic Myelogenous Leukemia / Primary Myelofibrosis / Progressive Hairy Cell Leukemia, Initial Treatment / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Refractory Hairy Cell Leukemia / Relapsing Chronic Myelogenous Leukemia / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Stage I Chronic Lymphocytic Leukemia / Stage II Chronic Lymphocytic Leukemia / Stage III Chronic Lymphocytic Leukemia / Stage IV Chronic Lymphocytic Leukemia / T-Cell Large Granular Lymphocyte Leukemia / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Adult Acute Myeloid Leukemia / Untreated Hairy Cell Leukemia1
2TerminatedTreatmentAdult Primary Hepatocellular Carcinoma / Advanced Adult Primary Liver Cancer / Localized Unresectable Adult Primary Liver Cancer / Recurrent Adult Primary Liver Cancer1
2TerminatedTreatmentAdvanced Disease / Neoplasms, Pancreatic / Neuroendocrine Tumors / Sunitinib1
2TerminatedTreatmentAnaplastic Gliomas / Glioblastoma Multiforme (GBM) / Malignant Gliomas1
2TerminatedTreatmentAscites1
2TerminatedTreatmentBladder Cancers1
2TerminatedTreatmentBladder Cancers / Transitional Cell Carcinoma1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentChemo-refractory Melanoma1
2TerminatedTreatmentCognitive/Functional Effects / Metastatic Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
2TerminatedTreatmentFibrolamellar Hepatocellular Carcinoma / Hepatocellular,Carcinoma1
2TerminatedTreatmentGenitourinary Disease1
2TerminatedTreatmentHemangioblastomas / Renal Cell Adenocarcinoma / Von Hippel-Lindau Syndrome1
2TerminatedTreatmentIntraocular Melanoma / Malignant Conjunctival Neoplasm1
2TerminatedTreatmentLiver Cancer2
2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2TerminatedTreatmentLung Cancers1
2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
2TerminatedTreatmentMetastatic Colorectal Cancers1
2TerminatedTreatmentMetastatic Renal Cell Carcinoma2
2TerminatedTreatmentNeurofibromatosis / NF1 / Plexiform Neurofibromas1
2TerminatedTreatmentNeoplasms, Colorectal1
2TerminatedTreatmentPalliative Treatment / Recurrent Disease / Squamous Cell Head and Neck Carcinoma1
2TerminatedTreatmentProstate Cancer1
2TerminatedTreatmentRenal Cancers1
2TerminatedTreatmentRenal Cell Adenocarcinoma4
2TerminatedTreatmentTransitional Cell Carcinoma of the Bladder1
2TerminatedTreatmentTumors, Solid1
2Unknown StatusBasic ScienceHormone Refractory Prostate Cancer1
2Unknown StatusTreatmentAdrenocortical Carcinoma1
2Unknown StatusTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter / Urethral Cancer1
2Unknown StatusTreatmentClear Cell Renal Cell Carcinoma / Metastasis1
2Unknown StatusTreatmentGlioblastoma Multiforme (GBM)1
2Unknown StatusTreatmentHormone Refractory / Prostate Cancer1
2Unknown StatusTreatmentIntraocular Melanoma1
2Unknown StatusTreatmentLung Cancer Metastatic / Renal Cell Adenocarcinoma1
2Unknown StatusTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2Unknown StatusTreatmentLung Cancers / Malignancies1
2Unknown StatusTreatmentMetastatic Renal Cell Carcinoma1
2Unknown StatusTreatmentRenal Cancers3
2Unknown StatusTreatmentSoft Tissue Sarcoma (STS)1
2WithdrawnTreatmentClassic Kaposi Sarcoma / Kaposi's Sarcoma AIDS Related1
2WithdrawnTreatmentColorectal Cancers / Metastatic Cancers1
2WithdrawnTreatmentLocally Metastatic Malignant Neoplasm1
2WithdrawnTreatmentLung Cancers1
2WithdrawnTreatmentMelanoma1
2WithdrawnTreatmentRenal Cell Adenocarcinoma2
2, 3CompletedTreatmentLiver Cancer1
2, 3RecruitingTreatmentGBM / Glioblastoma Multiforme (GBM) / Glioblastoma, Adult / Glioblastomas / Recurrent Brain Tumors1
3Active Not RecruitingTreatmentAdvanced Renal Cell Carcinoma / Metastatic Renal Cell Carcinoma1
3Active Not RecruitingTreatmentLocally Advanced or Metastatic Renal Cell Carcinoma / Renal Cell Adenocarcinoma1
3Active Not RecruitingTreatmentRenal Cell Adenocarcinoma4
3CompletedTreatmentClear Cell Renal Cell Carcinoma / Stage I Renal Cell Cancer / Stage II Renal Cell Cancer / Stage III Renal Cell Cancer1
3CompletedTreatmentGastrointestinal Stromal Tumors1
3CompletedTreatmentMetastatic Colorectal Cancers1
3CompletedTreatmentMetastatic Renal Cell Carcinoma1
3CompletedTreatmentNeoplasms, Breast3
3CompletedTreatmentNeoplasms, Kidney1
3CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
3CompletedTreatmentRenal Cell Adenocarcinoma3
3CompletedTreatmentStage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
3Not Yet RecruitingTreatmentGastrointestinal Stromal Tumors1
3Not Yet RecruitingTreatmentMetastatic Renal Cell Carcinoma / Renal Cell Adenocarcinoma1
3RecruitingTreatmentCarcinoma NOS / Enzyme Inhibitors / Kidney Diseases / Neoplasms by Site / Neoplasms, Kidney / Protein Kinase Inhibitors / Renal Cell Adenocarcinoma / Urologic Neoplasms1
3RecruitingTreatmentRenal Cell Adenocarcinoma2
3TerminatedTreatmentAdvanced Renal Cell Carcinoma / Metastatic Renal Cell Carcinoma / Renal Cell Adenocarcinoma1
3TerminatedTreatmentCarcinoma, Islet Cell / Carcinoma, Pancreatic1
3TerminatedTreatmentGastrointestinal Stromal Tumors1
3TerminatedTreatmentHepatocellular,Carcinoma1
3TerminatedTreatmentNeoplasms, Breast1
3TerminatedTreatmentProstatic Neoplasms1
4CompletedOtherWell-differentiated Pancreatic Neuroendocrine Tumor1
4CompletedTreatmentGastrointestinal Neoplasms, Gastrointestinal Stromal Tumors1
4CompletedTreatmentGastrointestinal Stroma Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC) / Renal-cell Cancer1
4CompletedTreatmentRenal Cell Adenocarcinoma1
4RecruitingOtherMetastatic Renal Cell Cancer1
4RecruitingTreatmentRefractory Solid Tumors1
4TerminatedNot AvailableMetastatic Renal Cell Carcinoma2
4TerminatedTreatmentMetastatic Renal Cell Carcinoma1
Not AvailableActive Not RecruitingNot AvailableMetastatic Renal Cell Carcinoma1
Not AvailableActive Not RecruitingDiagnosticAdvanced Solid Tumors / Malignancies1
Not AvailableActive Not RecruitingDiagnosticRenal Cell Adenocarcinoma / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
Not AvailableApproved for MarketingNot AvailableNeoplasms, Gastrointestinal1
Not AvailableApproved for MarketingNot AvailableRenal Cell Adenocarcinoma1
Not AvailableCompletedNot AvailableAdvanced or Metastatic Renal Cell Carcinoma / Renal Cancers1
Not AvailableCompletedNot AvailableGastrointestinal Stromal Tumors2
Not AvailableCompletedNot AvailableMetastatic Clear Cell Renal Cell Carcinoma1
Not AvailableCompletedNot AvailableMetastatic Renal Cell Carcinoma1
Not AvailableCompletedNot AvailableNeoplasms / Renal Cell Adenocarcinoma1
Not AvailableCompletedNot AvailableRenal Cell Adenocarcinoma3
Not AvailableCompletedDiagnosticKidney (Renal Cell) Cancer / Neoplasms, Kidney / Renal Cell Adenocarcinoma1
Not AvailableCompletedTreatmentAdvanced Breast Cancer / Advanced Gastric Cancer / Advanced/Metastatic Non-Small Cell Lung Cancer / Gastrointestinal Stromal Tumors / Hepatocellular,Carcinoma / Lung Cancer Non-Small Cell Cancer (NSCLC) / Malignant neoplasm of islets of Langerhans / Metastatic Breast Cancer [F] / Metastatic Castration Resistant Prostate Cancer / Metastatic Renal Cell Cancer / Progressive Neuroendocrine Tumors of pancreatic origin / Thyroid Cancers1
Not AvailableCompletedTreatmentMetastatic Renal Cell Carcinoma1
Not AvailableCompletedTreatmentNeoplasms1
Not AvailableCompletedTreatmentRenal Cancers2
Not AvailableCompletedTreatmentTumors, Solid1
Not AvailableNot Yet RecruitingNot AvailableRenal Neoplasms / Targeted Molecular Therapy1
Not AvailableRecruitingNot AvailableCarcinoma, Renal Cell, Advanced / Gastrointestinal Stroma Tumors / Mantle Cell Lymphoma (MCL)1
Not AvailableRecruitingNot AvailableComplete Remission in Renal Cell Carcinoma1
Not AvailableRecruitingNot AvailableGIST1
Not AvailableRecruitingNot AvailableMetastatic Renal Cell Carcinoma1
Not AvailableRecruitingNot AvailablePancreatic Neuroendocrine Tumor, Well Differentiated and Progressive1
Not AvailableRecruitingNot AvailableProgressive Neuroendocrine Tumors of pancreatic origin1
Not AvailableRecruitingDiagnosticHigh-Grade Gliomas / Malignancies1
Not AvailableRecruitingTreatmentRefractory Solid Tumors1
Not AvailableRecruitingTreatmentRenal Cancers1
Not AvailableTerminatedNot AvailableColorectal Cancers / Hepatocellular Cancer / Lung Cancer Non-Small Cell Cancer (NSCLC) / Renal Cell Adenocarcinoma1
Not AvailableTerminatedSupportive CareRenal Cell Cancer, Recurrent / Stage IV Renal Cell Cancer / Tiredness1
Not AvailableTerminatedTreatmentRenal Cell Adenocarcinoma1
Not AvailableTerminatedTreatmentTumors1
Not AvailableUnknown StatusDiagnosticRenal Cancers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Pfizer Inc.
Dosage forms
FormRouteStrength
CapsuleOral12.5 mg
CapsuleOral12.5 mg/1
CapsuleOral25 mg/1
CapsuleOral25 mg
CapsuleOral37.5 mg/1
CapsuleOral37.5 mg
CapsuleOral50 mg/1
CapsuleOral50 mg
Prices
Unit descriptionCostUnit
Sutent 50 mg capsule333.39USD capsule
Sutent 25 mg capsule187.28USD capsule
Sutent 12.5 mg capsule93.64USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2395461No2010-05-252020-12-22Canada
CA2399358No2006-03-212021-02-15Canada
US6573293No2003-06-032021-02-15Us
US7211600No2007-05-012020-12-22Us
US7125905No2006-10-242021-02-15Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility>25 mg/mL over pH of 1.2 to 6.8FDA label
logP5.2 FDA label
pKa8.95 FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.0308 mg/mLALOGPS
logP3.24ALOGPS
logP2.93ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)11.46ChemAxon
pKa (Strongest Basic)9.04ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area77.23 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity116.27 m3·mol-1ChemAxon
Polarizability44.32 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9938
Blood Brain Barrier+0.7993
Caco-2 permeable-0.5948
P-glycoprotein substrateSubstrate0.8648
P-glycoprotein inhibitor IInhibitor0.6809
P-glycoprotein inhibitor IINon-inhibitor0.5466
Renal organic cation transporterNon-inhibitor0.7385
CYP450 2C9 substrateNon-substrate0.8727
CYP450 2D6 substrateNon-substrate0.7716
CYP450 3A4 substrateSubstrate0.641
CYP450 1A2 substrateNon-inhibitor0.5626
CYP450 2C9 inhibitorNon-inhibitor0.6437
CYP450 2D6 inhibitorNon-inhibitor0.6846
CYP450 2C19 inhibitorNon-inhibitor0.6261
CYP450 3A4 inhibitorNon-inhibitor0.5991
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7032
Ames testNon AMES toxic0.5699
CarcinogenicityNon-carcinogens0.784
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6794 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8597
hERG inhibition (predictor II)Inhibitor0.8398
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as 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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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
  1. 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]
  2. 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
  1. 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]
  2. 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]
  3. Joensuu H: Second line therapies for the treatment of gastrointestinal stromal tumor. Curr Opin Oncol. 2007 Jul;19(4):353-8. [PubMed:17545799]
  4. 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]
  5. 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]
  6. 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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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
  1. 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]
  2. 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]
  3. Katoh Y, Katoh M: Comparative integromics on VEGF family members. Int J Oncol. 2006 Jun;28(6):1585-9. [PubMed:16685460]
  4. 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]
  5. 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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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
  1. 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]
  2. 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
  1. 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
  1. 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
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
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...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

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
  1. 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
  1. 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]
  2. 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
  1. 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
  1. 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]
  2. 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]
  3. 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 December 10, 2018 13:38