Ibrutinib

Ibrutinib C화학적 특성, 용도, 생산

개요

In November 2013, the US FDA approved ibrutinib (also referred to as PCI-32765), for the treatment of patients with mantle cell lymphoma (MCL) who had received at least one prior therapy. Ibrutinib is the second oral agent approved for the treatment of MCL. It works by irreversibly inhibiting Bruton’s tyrosine kinase (Btk) leading to the inhibition of B-cell receptor signaling and resulting in the reduction of malignant B-cell proliferation and induction of cell death. Btk plays an important role in the differentiation, development, proliferation, and survival of B cells via activation of cell-cycle regulators and regulating the expression of pro- and antiapoptotic proteins. Aberrant Btk activity results in a variety of B-cell malignancies including MCL. Ibrutinib inhibits Btk by irreversibly binding to cysteine-481 in the active site thereby inhibiting phosphorylation of tyrosine-223 and affecting downstream B-cell signaling pathways. Ibrutinib is a potent inhibitor of Btk (IC₅₀=0.5 nM) and is efficacious in canine models of B-cell lymphoma. At dose ranges of 2.5–20 mg/kg, there was full occupancy of Btk in peripheral blood and tumor tissue for 24 h. A synthetic route to ibrutinib that employs Suzuki coupling of 3-iodo-1Hpyrazolo[3,4-d]pyrimidin-4-amine with (4-phenoxyphenyl)boronic acid followed by Mitsunobu reaction with N-Boc-3-hydroxypiperidine as key steps has been reported.

용도

Ibrutinib is a highly selective Bruton’s tyrosine kinase (Btk) irreversible inhibitor.

Indications

The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.

정의

ChEBI: A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of he enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.

Ibrutinib 준비 용품 및 원자재

원자재

준비 용품

Ibrutinib 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1815	55
Hebei Jimi Trading Co., Ltd.	+86 319 5273535	bestoneforyou@sina.com	CHINA	292	58
Shenzhen Excellent Biotech Co., Ltd.	13480692018	ramyan@ex-biotech.com	CHINA	955	58
Shenzhen Shengda Pharma Limited	755-85269922 +8613424394241	sales@shengdapharm.com	CHINA	310	58
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15558	58
Hangzhou Huarong Pharm Co., Ltd.	571-86758373 +8613588754946	sales@huarongpharm.com	CHINA	3149	58
Handan Tongyi New Material Technology Co., Ltd	+8617330042575	ty003@handantongyi.com	China	378	58
Jiangsu Monade Biological Technology Co., Ltd.	+8613857751219	gao@mndbio.com	CHINA	240	58
SyncoZymes (Shanghai) Co., Ltd.,	+8613681683526	lchen@syncozymes.com	China	137	58
Qiuxian Baitai New Material Co., LTD	+8619932103556	larissa@qxbttech.com	China	1691	58

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