High Standard EP Cyproterone Acetate CAS 427-51-0 with ready stock and fast delivery

Cyproterone Acetate More Info

Cyproterone acetate (CPA) is a synthetic steroidal medication with multiple hormonal activities, primarily used as an antiandrogen and progestin. It is employed in various clinical settings, including treatment of androgen-dependent conditions, hormonal birth control, and prostate cancer.

Mechanism of Action

Antiandrogenic activity: CPA acts as a competitive antagonist at androgen receptors (AR), blocking the effects of androgens such as testosterone and dihydrotestosterone on target tissues. This reduces androgen-dependent cellular activities, including growth stimulation in prostate cancer cells and androgen-related skin conditions.
Progestogenic activity: CPA is a highly potent progestogen, activating progesterone receptors (PR) to exert progestational effects, which contribute to its use in hormonal contraception and suppression of gonadotropin secretion.
Additional activities: CPA has weak partial agonist activity at glucocorticoid receptors (GR), weak steroidogenesis inhibition, and agonist activity at the pregnane X receptor. It has no estrogenic or antimineralocorticoid activity.

Application

Prostate cancer: CPA lowers testosterone production by the testes and blocks androgen receptors, slowing or stopping growth of androgen-dependent prostate cancer cells. It is used especially in advanced or metastatic prostate cancer, often in combination with other hormonal therapies. CPA can also prevent tumor flare when starting LHRH agonists.
Androgen-dependent skin and hair conditions: Used to treat acne, seborrhea, hirsutism (excessive body hair), and scalp hair loss.
Hormonal contraception: CPA is combined with estrogens in some birth control pills for its progestogenic and antiandrogenic effects.
Other uses: Treatment of early puberty, transgender hormone therapy, reduction of sex drive in hypersexuality or paraphilias.

Routes of Administration

Oral: CPA is commonly administered orally as tablets, with near-complete (100%) bioavailability. The usual oral dose ranges from 2 mg (for mild conditions) up to 300 mg daily (for prostate cancer), divided into 2-3 doses with meals.
Intramuscular injection: CPA is also available as an oily solution for intramuscular injection, typically 300 mg weekly for prostate cancer treatment. Injection and oral forms can be interchanged during long-term therapy.

Safety and Side Effects

Very common (≥10%): General disorders, psychiatric disorders, reproductive system and breast disorders, elevated liver enzymes.
Common (1-10%): Weight changes (gain or loss, possibly fluid retention), psychiatric disorders, respiratory symptoms like shortness of breath.
Uncommon (0.1-1%): Decreased libido in women, rash.
Rare (0.01-0.1%): Hypersensitivity reactions including rash, itching, shortness of breath; increased libido in women.
Very rare (<0.01%): Benign and malignant liver tumors, osteoporosis, galactorrhea, sleep disturbances.
Warnings: High doses of CPA have been linked to an increased risk of meningioma (a type of brain tumor), leading regulatory agencies like the European Medicines Agency to recommend using the lowest effective dose or alternative treatments when possible.

Pharmacokinetics

Absorption: CPA is absorbed slowly but completely from the gastrointestinal tract, reaching peak plasma concentrations 3 to 4 hours after oral dosing.
Distribution: CPA is highly and exclusively bound to albumin in plasma, with extensive tissue distribution.
Metabolism: Metabolized in the liver primarily by hydroxylation and conjugation. The major active metabolite is 15β-hydroxycyproterone acetate (15β-OH-CPA).
Elimination: CPA has a long elimination half-life of about 38 ± 5 hours (approximately 2 to 4 days). Excretion occurs mainly via feces (~60%) and to a lesser extent urine (~33%).
Special populations: No detailed pharmacokinetic studies in renal impairment, but caution is advised since one-third of CPA is renally excreted.

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