카보잔티닙

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H315：피부에 자극을 일으킴

  H318：눈에 심한 손상을 일으킴

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

  P310：즉시 의료기관(의사)의 진찰을 받으시오. 삼켰다면 즉시 의료기관(의사)의 도움을 받으시오.

  P321：(…) 처치를 하시오.

  P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

  P362：오염된 의복을 벗고 세척 후에 재사용하기

카보잔티닙 화학적 특성, 용도, 생산

• 개요

  Cabozantinib was approved inNovember 2012 for the treatment of patients with progressive, unresectable, locally advanced, or metastatic medullary thyroid cancer (MTC). Cabozantinib was granted orphan drug status by the FDA to facilitate development of newtreatment options for patients with MTC. It is a member of a class of tyrosine kinase inhibitors (TKIs) with nanomolar pan-inhibitory activity against VEGFR2, MET, and RET among others. Inhibition of the VEGF pathway has been shown preclinically to initially slow tumor growth, but rapid revascularization is followed by aggressive tumor growth. The MET pathway has been implicated in the development of VEGF resistance, so dual VEGF/MET activity is viewed as desirable. In addition, mutations in RET play a particular role in MTC, with 25% of the tumors inheriting a germlinemutation in the proto-oncogene, so multiple tyrosine kinase inhibition may be viewed as particularly beneficial for the treatment of MTC.

• 용도

  Cabozantinib (XL184, BMS-907351) is 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: A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-t rosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.

• 일반 설명

  Class:receptor tyrosine kinase; Treatment: MTC; RCC; HCC; Other name: XL-184, BMS-907351; Elimination half-life = 110 h; Protein binding > 99.7%

• Clinical Use

  Cabozantinib (PF-06463922; brand name Cabometyx; Exelixis, Alameda, CA) is an oral multikinase inhibitor with CNS penetration. It is FDA approved for use in medullary thyroid cancer and as a second-line agent in advanced renal cell carcinoma. In vitro studies found it to exhibit excellent activity against both the wild-type ROS1 fusion and the G2032R and G2026M mutations at concentrations less than 30?nmol/L—a dose much lower than what is clinically achievable [71, 91]. It has been found to inhibit CD74-ROS1-transformed Ba/F3 cells with more potency than entrectinib, brigatinib, lorlatinib [92], or foretinib [71].

• target

  RET/VEGFR

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