IXABEPILONE

IXABEPILONE 속성

IXABEPILONE C화학적 특성, 용도, 생산

개요

Ixabepilone, a semisynthetic analog of epothilone B, was launched for the treatment of metastatic or locally advanced breast cancer. It is indicated for use in combination with capecitabine in patients who have previously failed treatment with an anthracycline such as doxorubicin and a taxane such as paclitaxel. It is also approved as monotherapy for the treatment of metastatic or locally advanced breast cancer in patients whose tumors are resistant or refractory to anthracyclines, taxanes, and capecitabine. Ixabepilone is the first member of the epothilone family of anticancer agents to be approved. Epothilones are novel cytotoxic macrolides derived from bacterial fermentation.
Like the taxanes, their mechanism of action involves binding to and stabilizing microtubules, which results in mitotic arrest and apoptosis.
The most common adverse reactions (X20%) associated with ixabelipone as monotherapy or in combination with capecitabine were peripheral sensory neuropathy, fatigue/asthenia, myalgia/arthralgia, alopecia, nausea, vomiting, stomatitis/ mucositis, diarrhea, and musculoskeletal pain. The most common hematologic abnormalities (W 40%) include neutropenia, leukopenia, anemia, and thrombocytopenia. Ixabelipone in combination with capecitabine is contraindicated in patients with AST or ALT W2.5 ULN (upper limit of normal) or bilirubin W1 ULN due to increased risk of toxicity and neutropenia-related death.

용도

Ixabepilone is an anti-tumor agent used in the treatment of patients suffering from solid tumors, such as metastatic breast cancer.

정의

ChEBI: A macrocycle that is a lactam analogue of epothilone B. Binds directly to beta-tubulin subunits on microtubules, leading to suppression of microtubule dynamics.

일반 설명

The epothilones are macrocyclic lactones that have a mechanismof action similar to that of the taxanes but offer severaladvantages.Ixabepilone is the semisyntheticamide analog of epothilone B that is isolated from themyxobacterium Sorangium cellulosum. The epothilonesshowed potent in vitro activity but greatly decreased activityin vivo caused by metabolic instability via hydrolysis ofthe macrocyclic lactone. Conversion to the lactam increasedstability and maintained in vivo activity. Ixabepilone hasbeen recently (2007) approved for the treatment of metastaticbreast cancer that is resistant to the taxanes. The agent isbelieved to bind to the same site occupied by the taxanes.Molecular modeling studies have been utilized to identifya common pharmacophore between the taxanes andepothilones.Like the taxanes, ixabepilone binds to β-tubulin and stabilizesmicrotubules resulting in cell death.The agent is usefulin cancers that have become resistant to the taxanes, becauseit is not removed by Pgp and is still capable of binding to altered beta tubulin to which the taxanes no longer bind.Increased water solubility also allows the agent to be administeredwithout the need for Cremophor EL, reducing thechance of hypersensitivity reactions. The current indicationsfor the agent are in metastatic breast cancer in combinationwith capecitabine after the failure of an anthracycline and ataxane and as monotherapy in metastatic breast cancer afterfailure of an anthracycline, a taxane, and capecitabine. Theagent is extensively metabolized in the liver primarily byCYP3A4 to give over 30 different metabolites. Eliminationoccurs primarily in the feces (65%) with a smaller amount(21%) occurring in the urine. The terminal elimination halflifeis 52 hours. Major toxicities associated with the useof ixabepilone have included peripheral neuropathy andmyelosuppression occurring as neutropenia. Occurring lessfrequently are alopecia, nausea, vomiting, mucositis, diarrhea,and muscle pain.

IXABEPILONE 준비 용품 및 원자재

원자재

준비 용품

IXABEPILONE 공급 업체

공급자	전화	이메일	국가	제품 수	이점
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Hangzhou ICH Biofarm Co., Ltd	+undefined8613073685410	sales@ichemie.com	China	985	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	1000	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
NanJing Spring & Autumn Biological Engineering CO., LTD.	+8613815430202	sale02@cqherb.com	CHINA	376	58
HubeiwidelychemicaltechnologyCo.,Ltd	18627774460	faith@widelychemical.com	CHINA	742	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58

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