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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 a nonsteroidal antiandrogen which was developed by Bristol-Myers Squibb for the treatment of prostate cancer but was never marketed.[1][2][3] It acts as a potent competitive antagonist of the androgen receptor (AR) (Ki = 10 nM; IC50Tooltip half-maximal inhibitory concentration = 56 nM).[3] The drug was found to have 20-fold higher affinity for the AR than bicalutamideinMDA-MB-453 cells, and showed 3- to 7-fold the antiandrogenic activity of bicalutamide in vitro.[4] It may have some weak partial agonist activity at the androgen receptor.[4] BMS-641988 is transformedbyCYP3A4 into BMS-570511, and this metabolite is then reducedtoBMS-501949bycytosolic reductases.[5][4] All three compounds show similar antiandrogenic activity.[5] In addition to its antiandrogenic activity, BMS-641988 shows activity as a negative allosteric modulator of the GABAA receptor, and can produce seizures in animals at sufficiently high doses.[6] It also shows some drug-induced QT prolongation.[6] BMS-641988 reached phase I clinical 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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