Selective Progesterone Receptor Modulator Asoprisnil (J867) Inhibits Proliferation and Induces Apoptosis in Cultured Uterine Leiomyoma Cells But Not in Cultured Normal Myometrial Cells

Translational research in women's health: From bedside to bench and from bench to bedside

“…The decreased synthesis of collagens may reduce collagen deposition in the extracellular spaces, thereby impairing the tissue integrity and inhibiting the expansion of uterine myomas. Similar effects were obtained by treatment with another PRM, J867 asoprisnil [15][16][17][18][19].…”

Role of nonhuman primate models in the discovery and clinical development of selective progesterone receptor modulators (SPRMs)

“…The results of an in vitro study with leiomyoma and myometrial primary cell cultures showed that asoprisnil inhibits proliferation and induces apoptosis of leiomyoma cells without having any effects on the normal myometrial cells [40]. In this study, the proliferation marker PCNA was used to quantify the effects on proliferation, whereas TUNEL assay was used to determine the effects on apoptosis.…”

Novel actions of progesterone: what we know today and what will be the scenario in the future?

“…Asoprisnil, binds with high affinity to progesterone receptors, moderate affinity to glucocorticoid receptors, low affinity to androgen receptors and has no affinity for oestrogen or mineralocorticoid receptors [39] . Observations demonstrate that SPRM not only inhibit proliferation and stimulate apoptosis of cultured leiomyoma cells but also suppress collagen synthesis in a cell‐type specific manner, which points to a mechanism beneficial in leiomyoma, [36,40–42] apoptosis is by activation of TRAIL‐mediated apoptotic pathway in leiomyoma cultures [43] . These drugs may prove a boon for leiomyoma and endometriosis, with a well‐tolerated adverse drug reaction profile [33] …”