Drug intelligence / Profile preview

ADX68692

Development stage
Preclinical
Lead developer
Addex Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

ADX68692 is an orally active, nonsteroidal small‑molecule **negative allosteric modulator** of the follicle‑stimulating hormone receptor (FSHR), originally developed by Addex Therapeutics as a potential contraceptive agent. Identified through high‑throughput screening of an Addex corporate library against human FSHR, ADX68692 binds an allosteric site on the receptor and inhibits FSH‑stimulated Gs/cAMP signaling, leading to reduced progesterone and estradiol production in rat granulosa cells and impaired ovulation in vivo, without blocking FSH binding or receptor internalization.[1][3][5] It also exhibits cross‑reactive negative allosteric activity on the luteinizing hormone/choriogonadotropin receptor (LHCGR), modulating hCG‑induced steroidogenesis in Leydig cell models, and has been studied preclinically for biased antagonism of gonadotropin receptor pathways relevant to fertility control.[2][3][4]

02

Targets

FSHR (Follicle-stimulating hormone receptor)LHCGR (Luteinizing hormone/choriogonadotropin receptor)

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