이바카프토

이바카프토 속성

이바카프토 C화학적 특성, 용도, 생산

개요

In January 2012, the US FDA approved ivacaftor for the treatment of cystic fibrosis (CF) in patients who have the G551D mutation of the CF transmembrane regulator (CFTR) and are at least 6 years old. Ivacaftor (also known as VX-770) is a CFTR potentiator that increases the open probability of CFTR, thus increasing chloride secretion particularly in the 5% of CF patients with the G551D/F508 gating/ processing mutation. Ivacaftor was discovered by medicinal chemistry optimization of a lead scaffold identified through high-throughput screening of a 228,000 compound collection. In cultured bronchial epithelial cells from a CF patient with F508del, ivacaftor increased chloride secretion (EC₅₀=81 nM). Preparation of ivacaftor is accomplished via a multistep synthesis oftwointermediates, 4-oxo-1,4-dihydroquinoline-3-carboxylic acid and 5-amino-di-tert-butylphenyl methyl carbonate, which are coupled using propane phosphonic acid anhydride (T3P) to afford the amide; deprotection of the phenol then provides ivacaftor.

용도

Ivacaftor (VX-770, Kalydeco) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively

정의

ChEBI: An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.

Pharmacokinetics

Administered as an oral dose, ivacaftor absorbs readily from the gut but has low solubility in water (< 0.05 ug/mL). Taking a 150 mg dose of ivacaftor with a high-fat meal improves absorption, increases AUC by 2.5 times, and delays Tmax from 3 to 5 hours. Dose/time pharmacokinetics follows a linear profile to a dose of 250 mg, though Cmax plateaus for doses 375 mg and higher. Ivacaftor is transported in the plasma highly bound (99%), preferentially to alpha-1-acid glycoprotein and albumin, to its site of action, the apical membrane of epithelial cells. However, no drug-drug interactions related to protein binding competition are expected.

Clinical Use

Vertex’s ivacaftor was granted breakthrough therapy designation by the FDA in January 2012 for cystic fibrosis (CF) patients who bear the G551D mutation in the Cycstic Fibrosis Transmembrane Regulator (CFTR) gene. This CFTR mutation occurs in roughly 4% of the 30,000 people living with CF in the United States. While the compound has been identified as a potentiator in cell-based assays, its mechanism of action is as yet unknown.

이바카프토 준비 용품 및 원자재

원자재

준비 용품

이바카프토 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shijiazhuang Dingmin Pharmaceutical Sciences Co., Ltd.	+86-0311-67591193 +8613931880626	sales02@dingminpharma.com	China	252	58
Zhejiang Brunova Technology Co., Ltd.	8617857108485 17857108485	info@zjbrunova.com	China	46	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	462	58
Capot Chemical Co.,Ltd.	+86-（0）57185586718 +86-13336195806	sales@capot.com	China	29791	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1803	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21634	55
Hangzhou FandaChem Co.,Ltd.	+8615858145714	FandaChem@Gmail.com	China	9083	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32956	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29880	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	965	58

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