17α-Hydroxyprogesterone

17α-Hydroxyprogesterone (17-OHP) is an endogenous progestogen and a key intermediate in the biosynthesis of steroid hormones.

It plays a critical role in cortisol and sex hormone production, particularly in the adrenal cortex and gonads. Clinically, serum 17-OHP levels serve as a primary biomarker for congenital adrenal hyperplasia (CAH), especially 21-hydroxylase deficiency. Its structural specificity-featuring a hydroxyl group at the C17α position-enables selective receptor binding and enzymatic conversion. As a research-grade compound, it supports mechanistic studies in endocrinology, enzyme kinetics, and diagnostic assay development.

Biological Functions and Mechanism of Action

• Endogenous Progestogen:

Secreted by the adrenal glands and gonads, it participates in the regulation of the menstrual cycle and the development of the female reproductive system.

• Hormone Precursor:

It is an important intermediate in the synthesis of cortisol, androstenedione, testosterone, and estrogens.

• Receptor Activity:

Acts as a progesterone receptor (PR) agonist, with effects similar to progesterone.

Functions as a mineralocorticoid receptor (MR) antagonist.

Acts as a weak partial agonist of the glucocorticoid receptor (GR), with potency far lower than cortisol.

Clinical Applications

Previously used for the prevention of preterm birth, especially in high-risk women with a history of preterm delivery; however, its use has become restricted due to potential teratogenic risks.

Used in the treatment of recurrent miscarriage, dysfunctional uterine bleeding, and endometriosis.

Not recommended for routine contraception, as it lacks estrogenic activity and is associated with relatively frequent side effects.

Safety and Precautions

Contraindications:

Patients with acute or chronic hepatitis or nephritis

Individuals with a history of thrombotic disorders

Breastfeeding women or those with breast masses

Use with caution in patients with uterine fibroids or hypertension

Common Adverse Reactions:

Menstrual irregularities (prolonged menstruation, irregular bleeding, etc.)

Nausea, dizziness, fatigue, breast tenderness

Discontinue immediately in cases of severe allergic reactions or development of breast lumps

Drug Interactions:

Enzyme inducers (such as carbamazepine and phenytoin) may accelerate its metabolism and reduce therapeutic efficacy

May inhibit the metabolism of cyclosporine, increasing its plasma concentration and the risk of toxicity

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