Drug intelligence / Profile preview

medroxyprogesterone acetate

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

Medroxyprogesterone acetate is a synthetic progestin (a derivative of progesterone) used as a contraceptive and in the treatment of secondary amenorrhea (absence of menstrual periods), abnormal uterine bleeding due to hormonal imbalance, endometrial hyperplasia prevention in postmenopausal women on estrogen therapy, endometriosis-associated pain, and as palliative therapy for certain cancers such as endometrial and renal carcinoma. It is also used for hormone-responsive cancers like breast cancer in postmenopausal women and can be prescribed to manage appetite loss or hot flushes related to other hormone therapies. Medroxyprogesterone acetate works primarily by acting as an agonist at the progesterone receptor; it transforms proliferative into secretory endometrium when administered with adequate estrogen levels and inhibits gonadotropin production when given parenterally at higher doses. This inhibition prevents follicular maturation and ovulation[1][4][5][8]. The drug was first approved by the FDA in 1959[4]. The developers and manufacturers for major brands are: Pfizer.

Brand names
ProveraDepo-ProveraDepo-subQ ProveraCurretabAmenPremphasePrempro
Other names
medroxyprogesterone
02

Targets

PR (Progesterone receptor)GR (Glucocorticoid receptor)AR (Adrenergic receptors)

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