Ixabepilone is an epothilone B analog developed by Bristol-Myers Squibb as a cancer drug. On October 16, 2007, the U.S. Food and Drug Administration approved ixabepilone for the treatment of aggressive metastatic or locally advanced breast cancer no longer responding to currently available chemotherapies. Ixabepilone is administered through injection, and will be marketed under the trade name Ixempra. [Wikipedia] Ixabepilone is a semisynthetic analogue of epothilone B. It has a lactone–lactam modification that
minimizes susceptibility to esterase degradation. |
Brands | Ixempra
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Categories | Antineoplastic Agents
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Manufacturers | Bristol myers squibb co
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Synonyms | Aza-epothilone B Azaepothilone B BMS-247550
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indication
Investigated for use/treatment in breast cancer, head and neck cancer, melanoma, lung cancer, lymphoma (non-hodgkin's), prostate cancer, renal cell carcinoma, and cancer/tumors (unspecified).
mechanism of action
Binding of Ixabepilone to beta-tubulins (e.g. beta-III tubulin) stabilizes microtubules. Microtubules are essential to cell division, and epothilones therefore stop cells from properly dividing. Like taxol, Ixabepilone binds to the αβ-tubulin heterodimer subunit. Once bound, the rate of αβ-tubulin dissociation decreases, thus stabilizing the microtubules.
half life
52 hours
route of elimination
Mostly fecal and some renal.
drug interactions
Conivaptan: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ixabepilone. The dose of ixabepilone must be reduced when used with strong inhibitors of CYP3A.1 In one published abstract, ixabepilone 20mg/m2 was the maximum tolerated dose in patients who were also receiving the CYP3A-inhibitor ketoconazole (400mg).
Telithromycin: Telithromycin may reduce clearance of Ixabepilone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ixabepilone if Telithromycin is initiated, discontinued or dose changed.
Voriconazole: Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ixabepilone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of ixabepilone if voriconazole is initiated, discontinued or dose changed.