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Tissue distribution and tumor uptake of folate receptor–targeted epothilone folate conjugate,BMS-753493,in CD2F1 mice after systemic administration

引用

Acta Pharmaceutica Sinica B 2016年第5期6卷 460-467页

作者： Hong Shen Lifei Wang Weiqi Chen krista menard Yang Hong Yuan Tian Samuel J.Bonacorsi W.Griffith Humphreys Francis Y.Lee Jinping Gan Pharmaceutical Candidate Optimization Bristol-Myers Squibb Research & Development Discovery Oncology Bristol-Myers Squibb Research & Development Chemistry Bristol-Myers Squibb Research & Development

To assess targeting of an epothilone folate conjugate(BMS-753493) to the folate receptor(FR)-overexpressed tumor in mice bearing both FRt and FR– tumors,a series of experiments were conducted by quantitative whole-body autoradiography(QWBA) and LC–MS/MS following *** of BMS-753493 or its active moiety,BMS-748285 in mice bearing FRt(98M109) and FR–(M109) *** showed [3H]BMS-753493–derived radioactivity was extensively distributed to various *** FR over-expressing 98M109 tumors showed consistently higher level of radioactivity than FR-negative tumors(i.e.,M109 tumors) up to 48 h post dose of [3H]BMS-753493,despite the magnitude of difference between the tumors is relatively small(generally 3 5-fold).The radioactivity level in 98M109 tumors was 2 12-fold of normal tissues except intestine/content at 48 h post *** selective radioactivity uptake into 98M109 tumors over M109 or normal tissues was observed after *** of the active epothilone,[3H]***–MS/MS measurements demonstrated that the concentrations of BMS-748285,presumably from hydrolysis of the folate conjugate,in 98M109 tumors were greater than those in M109 tumors after *** of BMS-753493(2–3-fold) whereas no differential uptake in the tumors following BMS-748285 *** data were consistent with radioactivity *** results demonstrated that the folate conjugation in BMS-753493 enabled moderately preferential distribution of the active epothilone to FR overexpressing 98M109 tumors,thereby supporting targeted delivery of cytotoxics through the folate receptor.

关键词： Folate receptor Tumor selective targeting Folate receptor–expressing tumor Epothilone folate conjugate Tissue distribution Tumor uptake

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