AV9

TIVOZANIB

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is present as a standalone ligand in 2 entries

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Chemical Component Summary
Name	TIVOZANIB
Synonyms	1-{2-chloro-4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-3-[(3E)-5-methylisoxazol-3(2H)-ylidene]urea
Identifiers	(3E)-1-[2-chloranyl-4-(6,7-dimethoxyquinolin-4-yl)oxy-phenyl]-3-(5-methyl-1,2-oxazol-3-ylidene)urea
Formula	C₂₂ H₁₉ Cl N₄ O₅
Molecular Weight	454.863
Type	NON-POLYMER
Isomeric SMILES	CC1=C/C(=N\C(=O)Nc2ccc(cc2Cl)Oc3ccnc4c3cc(c(c4)OC)OC)/NO1
InChI	InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
InChIKey	SPMVMDHWKHCIDT-UHFFFAOYSA-N

Chemical Details
Formal Charge	0
Atom Count	51
Chiral Atom Count	0
Bond Count	54
Aromatic Bond Count	17

Drug Info: DrugBank

DrugBank ID	DB11800
Name	Tivozanib
Groups	approved investigational
Description	Renal cell carcinoma (RCC) is responsible for 3% of cancer cases[A231314] and is one of the 10 most common cancers in adults. The average age of diagnosis is between age 65 to 74.[L32529] Tivozanib, also known as FOTIVDA, is a kinase inhibitor developed to treat adult patients with relapsed or refractory advanced renal cell carcinoma (RCC) after prior failed systemic therapies. It was approved on March 10, 2021 by the FDA. Marketed by Aveo Oncology, tivozanib is a promising therapy for individuals with RCC who have not been treated successfully with other therapies.[L32524]
Synonyms	Tivozanib Tivozanib hydrochloride
Brand Names	Fotivda
Indication	Tivozanib is approved in the USA for the treatment of relapsed or refractory renal cell carcinoma in adult patients who have undergone two or more systemic therapies.[L32524] In the UK and other countries, is indicated as first line therapy of adults with advanced renal cell carcinoma (RCC) and VEGFR and mTOR pathway inhibitor-naïve patients after disease progression following one previous treatment with cytokine therapy for advanced disease.[L17180]
Categories	Amides Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Inhibitors Benzene Derivatives Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Enzyme Inhibitors Heterocyclic Compounds, Fused-Ring Kinase Inhibitor P-glycoprotein substrates Protein Kinase Inhibitors Receptors, Vascular Endothelial Growth Factor, antagonists & inhibitors Tyrosine Kinase Inhibitors Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
ATC-Code	L01EK03
CAS number	475108-18-0

Drug Targets

Name	Target Sequence	Pharmacological Action	Actions
Vascular endothelial growth factor receptor 1	MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLH...	unknown	inhibitor
Vascular endothelial growth factor receptor 2	MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQ...	unknown	inhibitor
Vascular endothelial growth factor receptor 3	MQRGAALCLRLWLCLGLLDGLVSGYSMTPPTLNITEESHVIDTGDSLSIS...	unknown	inhibitor
Mast/stem cell growth factor receptor Kit	MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRV...	unknown	inhibitor
Platelet-derived growth factor receptor beta	MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTF...	unknown	inhibitor
Receptor-type tyrosine-protein kinase FLT3	MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKS...	unknown	inhibitor
Platelet-derived growth factor receptor alpha	MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCF...	unknown	inhibitor
Protein-tyrosine kinase 6	MVSRDQAHLGPKYVGLWDFKSRTDEELSFRAGDVFHVARKEEQWWWATLL...	unknown
Angiopoietin-1 receptor	MDSLASLVLCGVSLLLSGTVEGAMDLILINSLPLVSDAETSLTCIASGWR...	unknown
Fibroblast growth factor receptor 1	MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDL...	unknown	inhibitor
Hepatocyte growth factor receptor	MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAET...	unknown	inhibitor
Cytochrome P450 3A4	MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNI...	unknown	substrate
Serum albumin	MKWVTFISLLFLFSSAYSRGVFRRDAHKSEVAHRFKDLGEENFKALVLIA...	unknown	binder
P-glycoprotein 1	MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLY...	unknown	substrate
ATP-binding cassette sub-family G member 2	MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKS...	unknown	inhibitor
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Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS. Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682