Gefitinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Gefitinib was introduced in Japan as a daily oral monotherapy for the treatment of inoperable or recurrent non-small cell lung cancers (NSCLC). This inhibits autophosphorylation of EGRF and blocks the cascade of intracellular events which have been implicated in the proliferation, survival and metastasis of cancer cells.

Chemische Eigenschaften

Light-Yellow Crystalline Powder

Indications

The EGFR or ErbB1 inhibitor gefitinib (Iressa(R), AstraZeneca) was originally approved by the US FDA in 2003 under accelerated regulations for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) after progression on docetaxel- and platinum-based chemotherapy.

Allgemeine Beschreibung

Geftinib is available as 250-mg tablets for oral administrationin the treatment of NSCLC for those patients who have failedto respond to platinum-based therapies and docetaxel and hasalso been used against squamous cell cancers of the head andneck. The agent is an inhibitor of the TK of EGF-R and possiblyother TKs as well. Gefitinib is both a substrate and inhibitorof Pgp and BCRP. The agent is absorbed slowly afterbeing administered orally with 60% bioavailability.Metabolism occurs in the liver and is mediated primarily byCYP3A4 to give eight identified metabolites resulting fromdefluorination of the phenyl ring, oxidative-O-demethylation,and multiple products arising as a result of oxidation of themorpholine ring. The O-demethylated product represents thepredominate metabolite and is 14-fold less active comparedwith the parent. The parent and metabolites are eliminated inthe feces with a terminal elimination half-life of 48 hours.The drug appears to be well tolerated with the most commonlyreported side effects being rash and diarrhea. It mayalso cause elevations in blood pressure especially in those patientswith preexisting hypertension, elevation of transaminaselevels, and mild nausea and mucositits.

Allgemeine Beschreibung

Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 60%
Elimination half-life = 48 h
Protein binding = 97%

Biologische Aktivit?t

Orally active, selective inhibitor of EGFR tyrosine kinase (IC 50 = 23-79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts.

Gefitinib Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Gefitinib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15221	58
Yangzhou Qinyuan Pharmatech Co.,ltd	+86-18752526868 +86-18752526868	jennysun@yzqyyykj.com	China	83	58
Hebei Chuanghai Biotechnology Co., Ltd	+8617732866630	abby@chuanghaibio.com	China	8773	58
Hebei Dangtong Import and export Co LTD	+86-86-4001020630 +8619831957301	admin@hbdangtong.com	China	1000	58
Firsky International Trade (Wuhan) Co., Ltd	+8615387054039	admin@firsky-cn.com	China	427	58
shandong perfect biotechnology co.ltd	+86-53169958659 +86-13153181156	sales@sdperfect.com	China	294	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	20202	58
Wuhan Ruichi Technology Co., Ltd	+8613545065237	admin@whrchem.com	China	153	58
Hangzhou Hyper Chemicals Limited	+86-0086-57187702781 +8613675893055	info@hyper-chem.com	China	295	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+86-17396673057	linda@tnjone.com	China	1143	58

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