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megestrol acetate + conjugated estrogens
- Development stage
- Discontinued
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Megestrol acetate + Premarin is a combination therapy consisting of megestrol acetate (a synthetic progestin) and conjugated estrogens (marketed as Premarin). Megestrol acetate acts primarily as an agonist of the progesterone receptor, exerting antigonadotropic effects and weak glucocorticoid activity. Conjugated estrogens are a mixture of estrogenic compounds that act as agonists at the estrogen receptor. This combination has been studied in hormone-responsive advanced breast cancer to assess whether sequential administration improves outcomes compared to progestin alone. The mechanism involves modulation of hormone receptors in target tissues; however, clinical trials have not shown superiority over single-agent progestin therapy for this indication[1][3].
- Other names
- megestrol acetate + PremarinPRE/MEGmegestrol acetate + conjugated equine estrogens
02
Targets
ESR2 (ERβ)PR (Progesterone receptor)ESR1 (ERα)
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