Promestriene Active Pharmaceutical Ingredient

Promestriene, a synthetic estrogen, is commonly used in topical formulations for treating various conditions associated with estrogen deficiency, particularly in the urogenital tract. Below is a detailed description of Promestriene's Active Pharmaceutical Ingredient (API) characteristics:

Chemical and Physical Properties
IUPAC Name: (17β)-3-methoxy-17-methylestra-1,3,5(10)-triene-17-ol
Molecular Formula: C20H28O2
Molecular Weight: 300.44 g/mol
Chemical Class: Steroidal estrogen
Structure: Promestriene is an estrogen ester derived from estradiol, featuring a methoxy group on the aromatic A-ring and a methyl substitution at the 17-position.
Pharmacological Profile
Mechanism of Action:

Promestriene acts as a local estrogen agonist.
It binds to estrogen receptors (ERα and ERβ) in the target tissues, enhancing the expression of estrogen-responsive genes.
The action is localized, minimizing systemic absorption and associated systemic estrogenic effects.
Therapeutic Effects:

Restores the trophic condition of estrogen-deficient tissues.
Increases collagen, elastin, and glycoproteins in the vaginal and urogenital mucosa.
Enhances hydration, elasticity, and epithelial proliferation of tissues.
Promotes healing and reduces inflammation in atrophic and damaged tissues.
Indications
Promestriene is primarily indicated for:

Vaginal Atrophy: Often postmenopausal or associated with hormonal imbalance.
Dystrophic Vaginitis: Includes inflammation, dryness, or atrophy.
Vulvovaginal Conditions: Such as pruritus, dyspareunia, or irritation.
Healing Adjunct: Following gynecological procedures or for vulvar dystrophy.
Dosage Forms and Administration
Topical Creams and Suppositories: