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molecules of the year

BAY 1214784

oral hGnRH-R hormone receptor antagonist

to treat of uterine fibroids, Ph. I completed

from cell-based 2.5M cmpd HTS + opt.

J. Med. Chem., Oct. 22, 2020 issue

Bayer AG, Berlin, DE

BAY-1214784
1 min read

October’s molecule, the Bayer hGnRH-R antagonist BAY 1214784, is intended as an oral, once-daily treatment for uterine fibroids, a highly common problem in adult women that can lead to infertility. Existing treatments include hGnRH-R blockers which have undesirable side effects such as induction of menopausal symptoms due to their influence on both LH and FSH hormone levels. The chemically distinct Bayer molecule differentiates from prior molecules by having a PK/PD profile that allows only partial lowering of LH levels only. The bar for safety in a large indication with otherwise healthy individuals is very high, but BAY 1214784 successful advanced to clinical testing and completed a Ph. I study with good tolerability at doses up to 450 mg QD.


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