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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]
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