Abiraterone Acetate (CAS No.: 154229-18-2) - Targeted Androgen Synthesis Inhibitor for Advanced Prostate Cancer
As a professional supplier of pharmaceutical-grade oncology active ingredients, we provide high-purity Abiraterone Acetate that strictly complies with global pharmacopoeia standards (USP, EP, BP). A first-in-class oral androgen synthesis inhibitor, it is a cornerstone in the treatment of metastatic castration-resistant prostate cancer (mCRPC) and metastatic castration-sensitive prostate cancer (mCSPC)-two advanced stages of prostate cancer driven by androgen signaling. Its mechanism of targeting androgen production outside the testes (e.g., in the adrenal glands, prostate tumor tissue) addresses a critical unmet need in patients with progressive disease despite standard hormonal therapy.
Product Basic Information
| Item | Details |
|---|---|
| Product Name | Abiraterone Acetate |
| CAS No. | 154229-18-2 |
| Synonyms | (3β)-17-(3-Pyridinyl)androsta-5,16-dien-3-yl acetate; Zytiga® (brand name for commercial formulations) |
| Molecular Formula | C₂₆H₃₃NO₂ |
| Molecular Weight | 391.54 |
| Appearance | White to off-white crystalline powder; Odorless |
| Specification | - Pharmaceutical Grade: Purity ≥99.0% (HPLC); Assay (as abiraterone acetate) 98.0%–102.0%; Specific optical rotation [α]²⁰D +14° to +18° (in chloroform); Loss on drying ≤0.5%; Heavy metals (Pb≤5ppm, Hg≤1ppm, Cd≤1ppm); Residual solvents (ethanol ≤500ppm, acetone ≤500ppm) |
| Melting Point | 110–114°C (with decomposition) |
| Solubility | Practically insoluble in water (≈0.1 mg/L at 25°C); Soluble in ethanol (≈2 mg/mL), methanol (≈3 mg/mL), and chloroform (≈50 mg/mL); Sparingly soluble in ethyl acetate |
| Storage Conditions | Store in a cool (2–8°C), dry, light-protected container; Sealed to prevent moisture absorption, oxidation, and photodegradation; Shelf life: 36 months for pharmaceutical grade (when stored per conditions) |
Core Functions & Mechanism of Action
Prostate cancer growth is highly dependent on androgens (male sex hormones, e.g., testosterone, dihydrotestosterone/DHT). Standard hormonal therapy (androgen deprivation therapy/ADT) reduces testicular androgen production but does not block androgen synthesis in other tissues (adrenal glands, prostate tumor cells) or from adrenal precursors (e.g., dehydroepiandrosterone/DHEA).
Abiraterone Acetate is a prodrug-it is converted in the body to its active form, abiraterone, which irreversibly inhibits cytochrome P450 17A1 (CYP17A1). CYP17A1 is a key enzyme in androgen synthesis that catalyzes two critical steps:
17α-hydroxylation: Converts pregnenolone/progesterone to 17α-hydroxypregnenolone/17α-hydroxyprogesterone.
C17,20-lyase activity: Converts these 17α-hydroxy metabolites to DHEA (a precursor of testosterone and DHT).
By blocking CYP17A1, abiraterone eliminates nearly all sources of androgens (testicular, adrenal, and tumor-derived), suppressing prostate cancer cell growth and survival.
Clinical Applications (Human Oncology)
Abiraterone Acetate is approved globally for the treatment of advanced prostate cancer, always used in combination with prednisone/prednisolone (a corticosteroid) to mitigate side effects (e.g., mineralocorticoid excess). Its key indications include:
1. Metastatic Castration-Resistant Prostate Cancer (mCRPC)
mCRPC is prostate cancer that progresses despite ADT (castrate levels of testosterone). Abiraterone Acetate is used in two settings:
Post-chemotherapy mCRPC: For patients who have received prior docetaxel (a chemotherapy drug). Oral dose: 1000 mg once daily (on an empty stomach) + prednisone 5 mg twice daily. Clinical trials (e.g., COU-AA-301) showed extended overall survival (OS: 15.8 months vs. 11.2 months with placebo) and delayed disease progression.
Pre-chemotherapy mCRPC: For patients who have not received prior chemotherapy. Oral dose: 1000 mg once daily + prednisone 5 mg twice daily. Trials (e.g., COU-AA-302) demonstrated improved OS (34.7 months vs. 30.3 months with placebo) and reduced pain progression.
2. Metastatic Castration-Sensitive Prostate Cancer (mCSPC)
mCSPC is prostate cancer that has spread to distant sites (e.g., bones, lymph nodes) but still responds to ADT. Abiraterone Acetate is approved for use in combination with ADT and prednisone:
Oral dose: 1000 mg once daily + prednisone 5 mg twice daily + ADT (e.g., luteinizing hormone-releasing hormone agonists/antagonists). Trials (e.g., LATITUDE, STAMPEDE) showed significant OS benefit (median OS not reached vs. 34.7 months with ADT alone) and reduced risk of disease progression or death by ~50%.
3. Other Investigational Uses
Research is ongoing to expand its use to:
Non-metastatic castration-resistant prostate cancer (nmCRPC).
Prostate cancer in patients with BRCA mutations (targeting DNA repair-deficient tumors).
Quality & Safety Assurance
As a specialized oncology drug with strict clinical requirements, Abiraterone Acetate requires rigorous quality control to ensure efficacy, purity, and safety:
1. Manufacturing & Purity Control
Synthesis: Produced via multi-step chiral chemical synthesis (involving steroid nucleus construction and pyridine ring attachment), with strict control over stereochemistry (to ensure the active 3β-isomer). Purification via column chromatography and recrystallization removes impurities (e.g., diastereomers, synthetic byproducts) to ≤0.1%.
GMP Compliance: Manufactured in Grade A/B cleanrooms (per ICH Q7 guidelines) to prevent microbial contamination and cross-contamination with other drugs.
2. Critical Quality Attributes (CQAs)
| Test Item | Method | Acceptance Criterion |
|---|---|---|
| Purity & Assay | HPLC (C18 column, 254 nm detection) | ≥99.0% purity; 98.0%–102.0% assay |
| Chiral Purity (3β-isomer) | Chiral HPLC (cellulose-based column) | ≥99.5% (active isomer); ≤0.5% (inactive 3α-isomer) |
| Related Substances | HPLC (gradient elution) | Single impurity ≤0.2%; total impurities ≤0.5% |
| Heavy Metals | ICP-MS (Inductively Coupled Plasma-Mass Spectrometry) | Pb≤5ppm, Hg≤1ppm, Cd≤1ppm, As≤1ppm |
| Residual Solvents | GC (headspace sampling) | Class 2 solvents (ethanol, acetone) ≤500ppm; Class 1 solvents (benzene, methanol) not detected |
| Dissolution Rate (Tablets) | USP Apparatus II (paddle method, 0.05M HCl + 0.5% sodium lauryl sulfate) | ≥80% dissolved in 60 minutes |
3. Safety Considerations
Side Effects: Most common side effects are related to mineralocorticoid excess (due to CYP17A1 inhibition affecting cortisol synthesis) and include hypertension, hypokalemia (low potassium), fluid retention, and edema. These are managed with concurrent prednisone. Rare but serious side effects include hepatotoxicity (monitor liver function tests/LFTs monthly), cardiac arrhythmias, and adrenal insufficiency.
Contraindications: Hypersensitivity to abiraterone acetate or any excipients; severe hepatic impairment (Child-Pugh Class C); pregnancy (teratogenic risk-women of childbearing age should avoid exposure).
Drug Interactions: Avoid concurrent use with strong CYP3A4 inducers (e.g., rifampin, phenytoin)-they reduce abiraterone levels. Use caution with warfarin (increases bleeding risk) and digoxin (increases hypokalemia-related arrhythmia risk).
Cooperation & Contact
We supply pharmaceutical-grade Abiraterone Acetate in specialized packaging (amber glass vials with desiccants) to maintain stability:
Packaging: 1g, 10g, 100g, or custom quantities (for R&D or commercial manufacturing), sealed under nitrogen to prevent oxidation.
Technical Support: Provide detailed COA (Certificate of Analysis), stability data, and regulatory documentation (DMF, CEP) to support drug registration in global markets (US, EU, APAC).
If you are a pharmaceutical manufacturer, oncology R&D company, or contract manufacturing organization (CMO) focused on cancer therapies, please contact us for detailed cooperation:
Contact Information:
Email: sales@huarongpharma.com
Phone/WhatsApp: +86 13751168070
We adhere to the principles of "oncology-grade quality, regulatory compliance, and patient safety" and look forward to supporting the development and supply of life-saving prostate cancer treatments!
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