estradiol + drospirenone (Bayer)

estradiol + drospirenone (BAY 86-4891) is a combined oral contraceptive (COC) formulation developed by Bayer. It consists of the natural estrogen estradiol (E2) and the fourth-generation progestin drospirenone (DRSP). Drospirenone is a spironolactone analogue that possesses unique antimineralocorticoid and antiandrogenic properties, distinguishing it from earlier progestins. The combination works primarily by suppressing ovulation through the activation of progesterone receptors, which inhibits the secretion of luteinizing hormone (LH), while the estrogenic component provides cycle control and further suppresses follicle-stimulating hormone (FSH). This specific formulation was evaluated in Phase 2 clinical trials to assess bleeding patterns and safety using various continuous regimens (without a pill-free interval) in healthy women. While Bayer markets other drospirenone-containing products like Yasmin and Yaz, those utilize the synthetic estrogen ethinyl estradiol, making BAY 86-4891 a distinct developmental candidate focused on the use of natural estradiol for contraception.

Other names

E2/DRSPestradiol/drospirenone