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Drug intelligence / Profile preview
R-β-mefenetame
- Development stage
- Preclinical
- Lead developer
- National Institute of Cardiology Ignacio Chávez
- Modality
- Small Molecules
01
Overview
R-β-mefenetame is a novel synthetic aminoestrogen enantiomer developed as a lead candidate for safer estrogen-based therapies, such as hormone replacement therapy (HRT) and gender-affirming hormone therapy (GAHT). It exhibits significant antithrombotic, anticoagulant, and antiplatelet activities. In preclinical murine models, R-β-mefenetame markedly prolongs whole-blood clotting time and reduces collagen-induced platelet aggregation. Mechanistically, it shows preferential conformational selectivity toward the G protein-coupled estrogen receptor (GPER1) and interacts with estrogen receptors alpha (ER-α) and beta (ER-β).
- Other names
- R-beta-MefenetameR-β-Mefenetame
02
Targets
ESR1 (ERα)ESR2 (ERβ)GPER1 (G protein-coupled estrogen receptor 1)
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