Lapatinib ditosylate

Lapatinib ditosylate 속성

Lapatinib ditosylate C화학적 특성, 용도, 생산

용도

Lapatinib ditosylate monohydrate is a form of Lapatinib I, an orally active drug for breast cancer as a dual EGFR and erbB-?2 inhibitor.

일반 설명

Lapatinib is available in 250-mg tablets for oral administrationand is used in combination with cabecitabine in thetreatment of breast cancer for those patients that over expressthe type 2 EGF-R and who have previously receivedtaxane, anthracycline, and trastuzumab therapy. The type 2EGF-R is one subtype of this receptor and is also known asHER2 or ErbB-2. The agent is a receptor TK inhibitor targetingthe ErbB-1 and ErbB-2 subtypes. Binding occurs atthe ATP-binding site and thereby prevents phosphorylationand the subsequent activation of other kinase enzymes.ErbB-1 overexpression occurs in approximately27% to 30% of breast cancers, while ErbB-2 is over expressedin 20% to 25% of cases.The agent has demonstratedIC50 values of ＜0.2μM against ErbB-1 and 2 fromseveral different cancer cell lines and dissociates slowly(t_1/2＝300 min) from these receptor TKs.The drug isboth a substrate and an inhibitor of the efflux transportersPgp and BCRP. It is also an inhibitor of the hepatic uptaketransporter OATP1B1, which is an organic anion transporter.The absorption of lapatinib is incomplete andvariable after oral administration. The agent is extensivelymetabolized by CYP3A4 and CYP3A5, with minor contributionsfrom CYP2C19 and CYP2C8. Lapatinib inhibitsCYP3A and CYP2C8 at clinically relevant concentrations.The agent is highly (99%) protein bound and eliminatedprimarily in the feces. The half-life of the agent increaseupon repeated dosing, taking 6 days to reach steady statethat gives an effective half-life of 24 hours. The most commonlyseen adverse effects of lapatinib therapy are skinrash and diarrhea. Skin rash is commonly seen with manyof the other TK inhibitors and agents that target ErbB-1.Lapatinib-induced diarrhea is usually mild to moderate.There have been reports of decreases in left ventricularejection fraction associated with the agent, although thisappears to occur only rarely and is reversible upon discontinuationof therapy.

Lapatinib ditosylate 준비 용품 및 원자재

원자재

준비 용품

Lapatinib ditosylate 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12470	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	6011	58
Hebei Duling International Trade Co. LTD	+8618712993135	sales01@hbduling.cn	China	15734	58
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD.	+86-0531-69954981 +8615666777973	dwyane.wang@boyuanpharm.com	China	211	58
hebei hongtan Biotechnology Co., Ltd	+86-86-1913198-3935 +8617331935328	sales03@chemcn.cn	China	952	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21689	55
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32686	60

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