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| Routes of administration | By mouth |
| Drug class | Nonsteroidal antiandrogen |
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| Formula | C20H20F3N3O5S |
| Molar mass | 471.45 g·mol−1 |
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BMS-641988 is anonsteroidal antiandrogen which was developed byBristol-Myers Squibb for the treatment ofprostate cancer but was never marketed.[1][2][3] It acts as apotentcompetitive antagonist of theandrogen receptor (AR) (Ki = 10 nM;IC50Tooltip half-maximal inhibitory concentration = 56 nM).[3] The drug was found to have 20-fold higheraffinity for the AR thanbicalutamide inMDA-MB-453cells, and showed 3- to 7-fold theantiandrogenic activity of bicalutamidein vitro.[4] It may have some weakpartial agonist activity at the androgen receptor.[4] BMS-641988 istransformed byCYP3A4 intoBMS-570511, and thismetabolite is thenreduced toBMS-501949 bycytosolicreductases.[5][4] All three compounds show similarantiandrogenic activity.[5] In addition to its antiandrogenic activity, BMS-641988 shows activity as anegative allosteric modulator of theGABAA receptor, and can produceseizures in animals at sufficiently high doses.[6] It also shows somedrug-induced QT prolongation.[6] BMS-641988 reachedphase Iclinical trials prior to the discontinuation of its development.[1] The clinical development of BMS-641988 was terminated due to the occurrence of a seizure in a patient during a phase I study.[5]
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