Melanoma paclitaxel

It has been found that the C-11,12 double bond in paclitaxel was resistant to many reaction conditions, including catalytic hydrogenation and ozonolysis. Harriman et al. reasoned that C-10 acetate may hamper the epoxidation from the p-face and the cupshaped core structure prevents the epoxidation from the ot-face. By removal of 10-acetate in paclitaxel, the 11,12-p-epoxide was formed quantitatively. The 11,12-epoxidized taxoid 27 was only one third as cytotoxic as paclitaxel against B16 melanoma cells. The 11,12 double bond in baccatin was reducible by zinc in acidic conditions. Since treatment of 11,12-dihydro baccatin 28b with base only yielded 13-acetyl-4-... 

Paclitaxel (Taxol ) and its semisynthetic analogue docetaxel (see Figure 5.1) are two of the most important chemotherapeutic drugs, currently used for the treatment of advanced ovarian cancer, metastatic breast cancer, melanoma, non-small-cell lung cancer, and Kar-posi s sarcoma [8,9], More recently, these drugs have been used for the treatment of neck, prostate, and cervical cancers [8, 9],... 

Kunstfeld R, Wickenhauser G, Michaehs U, Teifel M, Umek W, Naujoks K, Wolff K, Petzelbauer P. Paclitaxel encapsulated in cationic liposomes diminishes tumor angiogenesis and melanoma growth in a humanized SCID mouse model. J Invest Dermatol. 2003 120 476-82. 

To determine the biodistribution and pharmacokinetics of CT-2103 and to compare them with paclitaxel administered in Cremophor EL/ethanol, female mice (C57BL/6) with approximately 100 mm subcutaneous B16 melanomas were allocated to two groups, 75 animals per group. One group... 

Gonz lez-Cao M, Viteri S, Diaz-Lagares A, Gonzdlez A, Redondo P, Nieto Y, Espinds J, Chopitea A, Ponz M, Martin-Algarra S. Preliminary results of the combination of bevacizumab and weekly paclitaxel in advanced melanoma. Oncology 2008 74(1-2) 12-6. 

Paclitaxel has also been investigated in the treatment of other carcinomas, including melanomas, head and neck cancers, and leukemia. 

Sagopilone is a fully synthetic epothilone B analogue that has efficacy in ovarian cancer, melanoma, and prostate cancer [160 ]. In in vitro studies sagopilone induces tubulin polymerization more rapidly than paclitaxel or patupilone [161 ]. In animals sagopilone crosses the blood-brain barrier and has activity against glioblastomas and nervous system metastases [162 ]. 

Bedikian AY, Deconti RC, Conry R, Agarwala S, Papadopoulos N, Kim KB, Ernstoff M. Phase 3 study of docosahexaenoic acid-paclitaxel versus dacarbazine in patients with metastatic malignant melanoma. Ann Oncol 2011 22(4) 787-93. 

Homsi J, Bedikian AY, Kim KB, Papadopoulos NE, Hwu WJ, Mahoney SL, Hwu P. Phase 2 open-label study of weekly docosahexaenoic acid-paclitaxel in cutaneous and mucosal metastatic melanoma patients. Melanoma Res 2009 19(4) 238 2. 

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