Estetrol is used in hormonal therapy, particularly in menopausal hormone treatment and contraception. It acts as a selective estrogen receptor modulator, providing estrogenic effects in certain tissues while minimizing stimulation in others, which may reduce risks associated with traditional estrogen therapies. In oral contraceptives, estetrol is combined with progestins to suppress ovulation while maintaining a favorable safety profile for venous thromboembolism and liver metabolism. Its tissue-selective activity supports bone health and alleviates menopausal symptoms such as hot flashes and vaginal atrophy, with potentially lower impact on breast and endometrial tissue compared to other estrogens.