Follicle-stimulating hormone (FSH), acting on its receptor (FSHR), plays a pivotal role in the stimulation of follicular development and maturation. Multiple injections of FSH are used in clinics for ovulation induction and for in-vitro fertilization. An orally bioavailable FSH mimetics would increase patient convenience and compliance. Our effort leading to orally active positive allosteric modulators (PAM) targeting FSHR will be described. We will present SAR, selectivity, DMPK, efficacy, safety and tox from selected examples and preclinical candidates.

Discovery of oral FSHR (follicle stimulating hormone receptor) allosteric modulators

249th National Meeting (2015)

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