Cabozantinib Malate

한글명:Cabozantinib Malate

카스 번호1140909-48-3

상품명:Cabozantinib Malate

CBNumberCB22554284

분자식C32H30FN3O10

포뮬러 무게635.6

MOL 파일1140909-48-3.mol

화학적 성질

녹는점	166-169°C
저장 조건	Sealed in dry,Room Temperature
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨, 가열), 피리딘(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 황백색까지
InChIKey	HFCFMRYTXDINDK-NJXVLOPVNA-N
SMILES	[C@@H](O)(C(=O)O)CC(=O)O.C(C1(CC1)C(=O)NC1C=CC(F)=CC=1)(=O)NC1C=CC(OC2=CC=NC3C=C(OC)C(OC)=CC2=3)=CC=1 \|&1:0,r\|

그림문자(GHS)

Cabozantinib Malate 화학적 특성, 용도, 생산

개요
Cabozantinib S-MALATE，formerly known as XL184, trade name Cabometyx, is developed by Exelixis biopharmaceutical company in the United States. The drug is mainly targeted at MET and VEGFR2 tyrosine kinases that associated with the growth and proliferation of prostate cancer, inhibiting tumor metastasis and angiogenesis. Cabozantinib S-MALATE , the malate of Cabozantinib, is an effective VEGFR2 inhibitor, and IC50 is 0.035 nM. It also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2 and AXL, and IC50 is 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM respectively.
Cabozantinib(Cometriq) was granted orphan drug status by the U.S. Food and Drug Administration (FDA) in January 2011. Cabozantinib(Cometriq) is approved by the U.S. FDA for medullary thyroid cancer. and advanced renal cell carcinoma in people who have received prior anti-angiogenic therapy. It is currently undergoing clinical trials for the treatment of prostate, bladder, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, and hepatocellular cancers.
화학적 성질
Cabozantinib (S)-malate salt is a white to off-white solid that is practically insoluble in aqueous media.
용도
Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
정의
ChEBI: Cabozantinib malate is a malate salt that is the mono-(S)-malate salt of cabozantinib. A multi-tyrosine kinase inhibitor, used for the treatment of progressive, metastatic, medullary thyroid cancer. It has a role as a tyrosine kinase inhibitor, an antineoplastic agent and a prodrug. It contains a cabozantinib.
Clinical Use
Cabozantinib (S)-malate (Cometriq®), which was discovered and developed by Exelixis, gained approval by the U.S. FDA in November 2012. The drug’s indication is for the treatment of medullary thyroid cancer (MTC), and is the second drug for this disease after AstraZeneca’s vandetanib (Caprelsa®). The drug was successfully launched on January 24, 2013. Cabozantinib inhibits multiple receptor tyrosine kinases including RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, and TIE-2. It is currently also undergoing clinical trials for the treatment of prostate, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers.
주의 사항
Cometriq has a boxed warning that increases the incidence of gastrointestinal perforation and fistula
Formation and severe bleeding. If you have severe stomach pain, or if you feel that you are suffocating and vomiting while eating or drinking, call your doctor. Warnings and precautions include thrombosis events, Wound complications, hypertension, jaw osteonecrosis, palm-toe erythema paresthesia Syndrome (PPES), proteinuria and reversible posterior leukoencephalopathy syndrome (RPLS).
참고 문헌
[1] yakes f m, chen j, tan j, et al. cabozantinib (xl184), a novel met and vegfr2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. molecular cancer therapeutics, 2011, 10(12): 2298-2308. DOI:10.1158/1535-7163.MCT-11-0264
[2] zhang y, guessous f, kofman a, et al. xl-184, a met, vegfr-2 and ret kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and nsclc. idrugs, 2010, 13(2): 112. PMCID:PMC3268517

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