Selective progesterone receptor modulators-mechanisms and therapeutic utility.

Selective progesterone receptor modulators-mechanisms and therapeutic utility. Endocr Rev. 2020 May 04;: Authors: Islam S, Afrin S, Jones SI, Segars J Abstract Selective progesterone receptor modulators (SPRMs) are new class of compounds developed to target the progesterone receptor with a mix of agonist and antagonist properties. These compounds have been introduced for treatment of several gynecological conditions based on the critical role of progesterone in reproduction and reproductive tissues. In patients with uterine fibroids, mifepristone and ulipristal acetate have consistently demonstrated efficacy, and vilaprisan is currently under investigation, while studies of asoprisnil and telapristone were halted for safety concerns. Mifepristone demonstrated utility for management of endometriosis, while data are limited regarding the efficacy of asoprisnil, ulipristal acetate, telapristone, and vilaprisan for this condition. Currently, none of the SPRMs have shown therapeutic success in treating endometrial cancer. Multiple SPRMs have been assessed for efficacy in treating PR-positive recurrent breast cancer, with in vivo studies suggesting a benefit of mifepristone, and multiple in vitro models suggesting the efficacy of ulipristal acetate and telapristone. Mifepristone, ulipristal acetate, vilaprisan, and asoprisnil effectively treated heavy menstrual bleeding (HBM) in patients with uterine fibroids, but limited data exist regard...
Source: Endocrine Reviews - Category: Endocrinology Tags: Endocr Rev Source Type: research