Icotinib

한글명:Icotinib

카스 번호610798-31-7

상품명:Icotinib

CBNumberCB82616025

분자식C22H21N3O4

포뮬러 무게391.42

MOL 파일610798-31-7.mol

화학적 성질

끓는 점	581℃
밀도	1.31
인화점	305℃
저장 조건	Store at -20°C
용해도	insoluble in H2O; ≥129.6 mg/mL in DMSO; ≥14.13 mg/mL in EtOH with ultrasonic
물리적 상태	가루
산도 계수 (pKa)	5.32±0.20(Predicted)
색상	White to off-white

위험 및 안전 성명

HS 번호

29339900

NFPA 704:

	0
2		0

그림문자(GHS)

Icotinib 화학적 특성, 용도, 생산

개요
Icotinib is also known as ConMana. It is a highly selective, first-generation inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TKI), whose mutation and overexpression is involved in many kinds of cancer. Icotinib is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, being capable of blocking the signal transduction cascade. It is currently under investigation for its treatment efficacy on the EGFR+ Non-small cell lung cancer.
용도
Icotinib is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with IC50 of 5 nM.
Indications
Icotinib (Conmana?, BetaPharma), an EGFR inhibitor, was approved by the China State FDA in 2011 for the treatment of NSCLC. Icotinib resembles erlotinib in possessing the N-(3-ethylnylphenyl) quinazolin-4-amine core scaffold of erlotinib that binds to the EGFR ATP pocket. An adjacent hydrophobic group was also retained while the solvent exposed two 2-methoxyethyoxysubstituents at the 6- and 7-positions of the quinazoline core were cyclized to afford the tetraoxacyclododecene moiety of icotinib. Efficacy and safety of icotinib as first-line therapy in patients has been evaluated for advanced NSCLC in recent clinical studies.
일반 설명
Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 52%
Elimination half-life = 5.5 h
참고 문헌
Tan, F., et al. "Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. " Lung Cancer76.2(2012):177-82.
Shi, Y., et al. "Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial." Lancet Oncology 14.10(2013):953-61.
Sun, Y., Y. Shi, and L. Zhang. "A randomized, double-blind phase III study of icotinib versus gefitinib in patients with advanced non-small cell lung cancer (NSCLC) previously treated with chemotherapy (ICOGEN)."Journal of Thoracic Oncology 29.15(2011):-.
https://en.wikipedia.org/wiki/Icotinib

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