엑시티닙

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H400：수생생물에 매우 유독함

• 예방조치문구

  P273：환경으로 배출하지 마시오.

엑시티닙 화학적 특성, 용도, 생산

• 물성

  용해도 DMSO에 용해되고 물과 에탄올에 약간 용해되며 메탄올과 DMF에는 거의 용해되지 않음 준수.

• 개요

  Axitinib (AG-013736)는 VEGFR 1 ~ 3의 강력하고 선택적 인 억제제이다. 트랜 스펙 션 된 또는 내생적인 RTK- 발현 세포에서 Axitinib는 VEGFR-2 및 VEGFR-3의 성장 인자 자극 된 인산화를 강하게 차단하여 평균 IC50 값은 0.2 및 0.1 내지 0.3 nM이다.

• 용도

  Axitinib은 혈관 신생 및 종양 성장에 관여하는 혈관 내피 수용체 (VEGFR-1, VEGFR-2 및 VEGFR-3)를 억제하여 암 진행을 유도하는 것으로 밝혀진 키나아제 억제제이다.

• 개요

  In January 2012, the US FDA approved axitinib (also referred to as AG-013736) for the treatment of advanced renal cell carcinoma (RCC) for patients who have not responded to prior therapy. Axitinib is a pan VEGF inhibitor and functions by binding to the intracellular tyrosine kinase catalytic domain of VEGF leading to blockade of signaling through this angiogenic pathway. Axitinib is50–400 times more potent for VEGF (enzyme Ki and cellular IC_50s for VEGF 1, 2, and 3 are ～0.1 nM) than first-generation inhibitors like sorafenib and sunitinib. Axitinib also inhibits c-Kit and PDGFR(α/β) with enzyme Ki's of ～2 nM and was selective when tested against a broad panel of other protein kinases. Axitinib was discovered by a structure-based drug design approach and binds to the kinase domain of VEGF in a DFG-out conformation. Axitinib blocks VEGF-2 phosphorylation up to 7 h postdose in vivo and inhibits endothelial cell proliferation in xenograft tumors implanted in mice. Synthetic routes to axitinib employing a Migita coupling to form the diaryl sulfide and a Heck reaction to install the 2-styrylpyridine moiety have been reported.

• 화학적 성질

  Off-White Solid

• Characteristics

  Class: receptor tyrosine kinase
  Treatment: RCC
  Oral bioavailability = 58%
  Elimination half-life = 2.5–6.1 h
  Protein binding = 99%

• 용도

  Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.

• 정의

  ChEBI: An indazole substituted at position 3 by a 2-(pyridin-2-yl)vinyl group and at position 6 by a 2-(N-methylaminocarboxy)phenylsulfanyl group. Used for the treatment of advanced renal cell carcinoma after failure of a first line systemic tr atment.

• Clinical Use

  Sold under the brand name Inlyta® by Pfizer, Inc., axitinib was approved by the FDA in January 2012 for the treatment of advanced renal cell carcinoma (RCC), specifically after the failure of other systemic treatments. Axitinib slows cancer cell proliferation by inhibition of the vascular endothelial growth factor (VEGF)/VEGF receptor tyrosine (RTK) signaling pathway. In particular, axitinib is a potent inhibitor of VEGF/RTK 1-3, which selectively slows angiogenesis, vascular permeability, and blood flow in solid tumors.

• 부작용

  The side effects that you should report to your doctor include:
  allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue;
  high blood pressure;
  seizures;
  signs and symptoms of bleeding such as bloody or black, tarry stools; red or dark-brown urine; spitting up blood or brown material that looks like coffee grounds; red spots on the skin; unusual bruising or bleeding from the eye, gums, or nose;
  signs and symptoms of a blood clot such as breathing problems; changes in vision; chest pain; severe, sudden headache; pain, swelling, warmth in the leg; trouble speaking; sudden numbness or weakness of the face, arm, or leg;
  stomach pain.
  The side effects that usually do not require medical attention include constipation cough, diarrhea, loss of appetite, nausea, and vomiting.
  

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