Megestrol Acetate (CAS No.: 595-33-5) - Synthetic Progestin for Hormonal Therapy & Appetite Stimulation
As a professional supplier of pharmaceutical-grade progestin active ingredients, we provide high-purity Megestrol Acetate that strictly complies with global pharmacopoeia standards (USP, EP, BP, CP). A synthetic derivative of progesterone, it exhibits potent progestational activity and minimal androgenic/estrogenic effects. It is widely used in human pharmaceutical formulations for hormonal disorder treatment, contraception, and appetite stimulation in cachectic patients-playing a critical role in gynecological health, oncology supportive care, and endocrine therapy.
Product Basic Information
| Item | Details |
|---|---|
| Product Name | Megestrol Acetate |
| CAS No. | 595-33-5 |
| Synonyms | 17α-Acetoxy-6-methylpregna-4,6-diene-3,20-dione; MGA; Megace® (brand name for oncology/appetite use) |
| Molecular Formula | C₂₄H₃₂O₄ |
| Molecular Weight | 384.51 |
| Appearance | White to off-white crystalline powder; Odorless |
| Specification | Pharmaceutical grade; Purity ≥99.0% (HPLC); Specific optical rotation [α]²⁰D +59° to +65° (in chloroform); Loss on drying ≤0.5%; Residue on ignition ≤0.1%; Heavy metals (Pb, Hg, Cd) ≤10ppm; Solvent residues (methanol ≤300ppm, ethyl acetate ≤500ppm) |
| Melting Point | 213-219°C (with decomposition) |
| Solubility | Insoluble in water; Soluble in chloroform (≥200 g/L), ethanol (≥10 g/L), and acetone (≥50 g/L); Sparingly soluble in ether |
| Storage Conditions | Store in a cool (15-25°C), dry, light-protected container; Sealed to avoid moisture and oxidation; Shelf life: 36 months under recommended conditions |
Core Functions & Applications
Megestrol Acetate exerts its pharmacological effects by binding to progesterone receptors (PR) in target tissues (endometrium, breast, hypothalamus-pituitary axis), regulating gene expression to mimic the physiological actions of endogenous progesterone. It also modulates appetite-regulating pathways in the central nervous system (CNS) via unknown mechanisms, making it effective for cachexia. It is exclusively used in human medicine (no veterinary application) across four key therapeutic areas:
1. Gynecological Hormonal Disorders
Endometriosis & Adenomyosis: Suppresses endometrial tissue growth by inhibiting gonadotropin release (reducing estrogen levels) and directly acting on endometrial PR. Relieves pelvic pain, dysmenorrhea, and abnormal uterine bleeding (AUB) in 70-80% of patients. Typically administered as low-dose oral tablets (4-10 mg/day) for 6-12 consecutive months.
Abnormal Uterine Bleeding (AUB): Stabilizes the endometrial lining in anovulatory AUB (e.g., polycystic ovary syndrome, PCOS) by promoting endometrial secretory transformation. Reduces bleeding volume by ≥50% within 1-2 menstrual cycles, with a standard dose of 5-10 mg/day for 10-14 days per cycle.
2. Contraception
Oral Contraceptives (Combined Formulations): Used as the progestin component in combined oral contraceptives (COCs) alongside estrogens (e.g., ethinyl estradiol). Inhibits ovulation by suppressing luteinizing hormone (LH) surge, thickens cervical mucus (blocking sperm penetration), and thins the endometrium (preventing implantation). Typical dose in COCs: 0.1-0.25 mg per tablet, taken daily for 21 days followed by a 7-day hormone-free interval.
Long-Acting Contraception: Formulated into intrauterine devices (IUDs) or subcutaneous implants for long-term contraception (3-5 years). Provides localized progestin release, minimizing systemic side effects while maintaining contraceptive efficacy (>99%).
3. Oncology Supportive Care (Appetite Stimulation & Cachexia)
Cancer-Associated Cachexia: The first-line medication for appetite stimulation and weight gain in patients with cancer cachexia (e.g., lung cancer, breast cancer, pancreatic cancer). Increases appetite in 60-75% of patients and improves weight gain (primarily fat mass) within 2-4 weeks. Standard dose: 400-800 mg/day (oral suspension or tablets), administered once daily to enhance compliance.
HIV-Associated Wasting: Used off-label to reverse weight loss in HIV-positive patients with antiretroviral therapy (ART)-refractory wasting. Improves body mass index (BMI) and quality of life (QoL) by stimulating caloric intake and reducing metabolic hyperactivity.
4. Breast & Endometrial Cancer Adjuvant Therapy
Metastatic Breast Cancer: Palliative treatment for hormone receptor-positive (HR+) metastatic breast cancer in postmenopausal women. Inhibits breast cancer cell proliferation by blocking PR-mediated signaling and reducing estrogen sensitivity. Typical dose: 40-160 mg/day, administered continuously until disease progression.
Endometrial Cancer: Adjuvant therapy for early-stage endometrial cancer (Grade 1-2, Stage I-II) in patients who cannot undergo surgery or radiation. Reduces recurrence risk by 20-30% via direct inhibition of endometrial cancer cell growth. Dose: 100-200 mg/day for 3-6 months.
Quality & Safety Assurance
As a prescription progestin with hormonal activity, Megestrol Acetate requires strict quality control to ensure efficacy, consistency, and safety:
Raw Material & Synthesis: Derived from high-purity steroid precursors (e.g., 16-dehydropregnenolone acetate) via chiral synthesis, ensuring the correct stereochemistry (17α-acetoxy configuration) critical for progestational activity. Impurities (e.g., isomers, unreacted intermediates) are controlled to ≤0.1% via HPLC monitoring.
Production Process: Manufactured in GMP-certified workshops (Class D cleanroom for final crystallization) with inert gas (nitrogen) protection to prevent oxidation. Automated process control ensures batch-to-batch uniformity in purity and optical rotation.
Comprehensive Testing Protocol:
| Test Item | Method | Acceptance Criterion |
|---|---|---|
| Purity & Related Substances | HPLC (C18 column, 254 nm detection) | Purity ≥99.0%, single impurity ≤0.1%, total impurities ≤0.5% |
| Optical Rotation | Polarimetry (1% solution in chloroform) | [α]²⁰D +59° to +65° |
| Heavy Metals | Atomic Absorption Spectroscopy (AAS) | Pb≤10ppm, Hg≤1ppm, Cd≤1ppm |
| Residue Solvents | Gas Chromatography (GC, headspace) | Methanol≤300ppm, Ethyl acetate≤500ppm |
| Identification | Infrared Spectroscopy (IR) & HPLC Retention Time | Matches reference standard spectrum and retention time |
Safety Reminders:
Hormonal Side Effects: Common side effects include weight gain, edema, hot flashes, and menstrual irregularities (in premenopausal women). Rare but serious effects: thromboembolic events (deep vein thrombosis, pulmonary embolism)-avoid in patients with a history of venous thromboembolism (VTE).
Contraindications: Hypersensitivity to Megestrol Acetate; active or history of hormone-sensitive cancers (e.g., progesterone receptor-negative breast cancer); severe liver impairment; pregnancy (Category X-may cause fetal harm).
Monitoring: Patients on long-term therapy (≥6 months) require periodic liver function tests (LFTs) and lipid profile monitoring (may increase triglycerides).
Cooperation & Contact
We supply pharmaceutical-grade Megestrol Acetate for the production of oral tablets, suspensions, IUDs, and injectable formulations. We offer flexible supply capacities:
R&D samples: 100g-1kg (for formulation development and clinical trials).
Commercial bulk: 10kg-100kg per order (with stable monthly production capacity of 500kg).
Value-added services include:
Providing DMF (Drug Master File) and CEP (Certificate of Suitability) documents for client product registration in the EU, US, and emerging markets.
Customized particle size control (for suspension formulations) and micronization services.
Technical support for formulation stability (e.g., preventing oxidation in oral suspensions).
If you are a pharmaceutical manufacturer, oncology drug developer, or reproductive health enterprise, please contact us for detailed cooperation:
Contact Information:
Email: sales@huarongpharma.com
Phone/WhatsApp: +86 13751168070
We adhere to the principles of "pharmacopeial compliance, patient safety, and long-term cooperation" and look forward to partnering with global healthcare enterprises!
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