Tissue-selective ERα partial agonist

Name: Tissue-selective ERα partial agonist
Creator: Jason Cafer, MD

Tissue-selective estrogen receptor alpha (ERα) partial agonist

Tissue-selective ("SERM") behavior — agonist in some tissues (bone, endometrium, lipids), antagonist in others (breast)
Net effect set by tissue coactivator/corepressor context

Drugs with this mechanism (6)

Bazedoxifene — SERM paired with conjugated estrogens to protect the endometrium without a progestin; thromboembolism risk remains.
Clomiphene — Estrogen-receptor modulator that induces ovulation.
Ospemifene — Oral SERM for dyspareunia from vulvovaginal atrophy.
Raloxifene — SERM that protects bone and lowers breast-cancer risk without stimulating the uterus.
Tamoxifen — The classic breast-cancer SERM; a prodrug activated by CYP2D6.
Toremifene — SERM for metastatic breast cancer in postmenopausal patients; QT prolongation, thromboembolism, and endometrial cancer risks.