PT - JOURNAL ARTICLE AU - PAUL A. FOSTER AU - SIMON P. NEWMAN AU - MATHEW P. LEESE AU - SONIA BERNETIERE AU - CHRISTIAN DIOLEZ AU - JOSE CAMARA AU - BEATRICE HACHER AU - MARIE-MADELEINE BARONNET AU - TAUHID ALI AU - BARRY V.L. POTTER AU - MICHAEL J. REED AU - ATUL PUROHIT TI - A New Micronized Formulation of 2-Methoxyestradiol-<em>bis</em>-sulfamate (STX140) is Therapeutically Potent against Breast Cancer DP - 2008 Mar 01 TA - Anticancer Research PG - 577--581 VI - 28 IP - 2A 4099 - http://ar.iiarjournals.org/content/28/2A/577.short 4100 - http://ar.iiarjournals.org/content/28/2A/577.full SO - Anticancer Res2008 Mar 01; 28 AB - There is a continued need for orally bioavailable anticancer compounds that exhibit good efficacy against breast cancer. STX140, a derivative of 2-methoxyestradiol (2-MeOE2), has been shown to have excellent oral bioavailability and significantly reduces tumor growth. A new micronized formulation of STX140 has now been developed and its pharmacokinetics (PK) in rats and effect on MDA-MB-231 breast cancer growth in nude mice was investigated. Materials and Methods: For the PK studies, female Wistar rats were treated orally with STX140 in two separate vehicles (10% tetrahydrofuran (THF) in propylene glycol (PG) or 0.5% methyl cellulose (MC) in saline) and plasma samples taken for high performance liquid chromatography analysis over 48 h. For the tumor efficacy studies, female nude mice were inoculated with MDA-MB-231 breast cancer cells and then treated orally with a range of doses of STX140. Results: The PK studies demonstrated that the THF/PG vehicle resulted in a greater oral bioavailability of STX140 compared to the 0.5% MC vehicle. However, this was not translated to the tumor efficacy studies where STX140 at 20 mg/kg in either vehicle caused a significant reduction in tumor volume. Conclusion: The new micronized formulation of STX140 is orally bioavailable and efficacious at inhibiting MDA-MB-231 breast tumor growth.