Abiraterone (CAS No.: 154229-19-3) - Active Androgen Synthesis Inhibitor for Advanced Prostate Cancer Therapy
As a professional supplier of pharmaceutical-grade oncology active pharmaceutical ingredients (APIs), we provide high-purity Abiraterone that strictly adheres to global pharmacopoeia standards (USP, EP, BP). As the active metabolite of Abiraterone Acetate (a widely used prodrug), this compound serves as a core component in targeted therapy for advanced prostate cancer. It specifically blocks androgen production outside the testes (e.g., in adrenal glands and prostate tumor tissues), addressing unmet needs in patients with progressive disease despite standard androgen deprivation therapy (ADT) and serving as a critical raw material for oncology drug manufacturers worldwide.
Product Basic Information
| Item | Details |
|---|---|
| Product Name | Abiraterone |
| CAS No. | 154229-19-3 |
| Synonyms | (3β)-17-(3-Pyridinyl)androsta-5,16-dien-3-ol; Active metabolite of Abiraterone Acetate |
| Molecular Formula | C₂₄H₃₁NO |
| Molecular Weight | 349.51 |
| Appearance | White to off-white crystalline powder; Odorless |
| Specification | - Pharmaceutical Grade: Purity ≥99.0% (HPLC); Assay (as Abiraterone) 98.0%–102.0%; Specific optical rotation [α]²⁰D +15° to +19° (in chloroform, c=1); Loss on drying ≤0.5%; Residue on ignition ≤0.1%; Heavy metals (Pb≤5ppm, Hg≤1ppm, Cd≤1ppm, As≤1ppm); Residual solvents (ethanol ≤500ppm, acetone ≤500ppm, chloroform ≤60ppm) |
| Melting Point | 227–229°C (with slight decomposition) |
| Boiling Point | 500.2°C at 760 mmHg (theoretical) |
| Solubility | Practically insoluble in water (≈0.05 mg/L at 25°C); Soluble in chloroform (≈60 mg/mL), methanol (≈5 mg/mL), ethanol (≈3 mg/mL); Sparingly soluble in ethyl acetate |
| Storage Conditions | Store in a cool (2–8°C), dry, light-protected amber glass container; Sealed under nitrogen to prevent moisture absorption, oxidation, and photodegradation; Avoid contact with oxidizing agents, strong acids, and strong bases; Shelf life: 36 months for pharmaceutical grade (when stored per conditions) |
Core Mechanism & Therapeutic Value
Prostate cancer growth is highly dependent on androgens (e.g., testosterone, dihydrotestosterone/DHT). While standard ADT reduces testicular androgen production, it fails to block androgen synthesis in adrenal glands and prostate tumor cells-these "extra-testicular" androgens drive disease progression in advanced stages.
Abiraterone (the active form of Abiraterone Acetate) exerts its targeted anti-cancer effect by irreversibly inhibiting cytochrome P450 17A1 (CYP17A1)-a key enzyme in the androgen synthesis pathway. CYP17A1 catalyzes two critical reactions:
- 17α-hydroxylation: Converts pregnenolone/progesterone (adrenal precursors) to 17α-hydroxypregnenolone/17α-hydroxyprogesterone.
- C17,20-lyase activity: Converts these 17α-hydroxy metabolites to dehydroepiandrosterone (DHEA)-the primary precursor of testosterone and DHT.
By blocking CYP17A1, the drug eliminates nearly all sources of androgens (testicular, adrenal, and tumor-derived), drastically reducing androgen levels in the body and suppressing prostate cancer cell proliferation and survival.
Application Scenarios
It is primarily used as a pharmaceutical API for manufacturing oral oncology formulations (tablets/capsules) to treat advanced prostate cancer. Its clinical applications (via formulated products) include:
1. Metastatic Castration-Resistant Prostate Cancer (mCRPC)
For patients with mCRPC (prostate cancer that progresses despite castrate testosterone levels), the formulated product (administered as Abiraterone Acetate) is combined with prednisone (a corticosteroid) to mitigate side effects. Clinical data show it extends overall survival (OS) by 4–6 months and delays disease progression compared to placebo.
2. Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)
In high-risk mHSPC (cancer that has spread to distant sites but still responds to ADT), treatment with prednisone plus ADT reduces the risk of disease progression or death by ~50% and significantly extends OS (median OS not reached in trials vs. 34.7 months with ADT alone).
3.R&D & Formulation Development
The compound is also used in preclinical and clinical R&D for:
- Optimizing drug delivery systems (e.g., improving solubility to enhance oral bioavailability).
- Developing combination therapies (e.g., with PARP inhibitors for BRCA-mutated prostate cancer).
- Investigating potential applications in other androgen-driven diseases (e.g., certain types of breast cancer).
Quality & Safety Assurance
As a specialized oncology API, Abiraterone requires strict quality control to ensure efficacy, purity, and compliance with global regulatory standards:
1. Manufacturing & Purity Control
Synthesis Process: Produced via multi-step chiral chemical synthesis (including steroid nucleus construction, pyridine ring attachment, and hydroxyl group protection/deprotection). Strict control over stereochemistry ensures the active 3β-isomer accounts for ≥99.5% of the final product.
Purification: Purified via column chromatography and recrystallization to remove impurities (e.g., diastereomers, synthetic byproducts) - single impurity ≤0.2%, total impurities ≤0.5%.
GMP Compliance: Manufactured in Grade A/B cleanrooms (per ICH Q7 guidelines) with full traceability of raw materials and production processes; regular audits by third-party regulatory authorities (e.g., FDA, EMA).
2. Comprehensive Testing Protocol
| Test Item | Method | Acceptance Criterion |
|---|---|---|
| Purity & Assay | HPLC (C18 column, 254 nm detection) | Purity ≥99.0%; Assay 98.0%–102.0% |
| Chiral Purity | Chiral HPLC (cellulose tris(3,5-dimethylphenylcarbamate) column) | Active 3β-isomer ≥99.5%; Inactive 3α-isomer ≤0.5% |
| 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, FID detector) | Class 2 solvents ≤500ppm; Class 1 solvents not detected |
| Loss on Drying | Gravimetric method (105°C for 2 hours) | ≤0.5% |
| Identification | IR Spectroscopy & HPLC Retention Time | Matches reference standard spectrum; Retention time consistent with standard |
3. Safety Reminders (for Formulated Products)
Side Effects: When used in clinical practice (as part of formulated drugs), common side effects include hypertension, hypokalemia (low potassium), fluid retention, and edema (managed with concurrent prednisone). Rare but serious risks include hepatotoxicity (monitor liver function monthly) and cardiac arrhythmias.
Contraindications: Hypersensitivity to Abiraterone or excipients; severe hepatic impairment (Child-Pugh Class C); pregnancy (teratogenic risk-women of childbearing age should avoid exposure to the API).
Drug Interactions: Avoid concurrent use with strong CYP3A4 inducers (e.g., rifampin, phenytoin) as they reduce Abiraterone levels; use caution with warfarin (increased bleeding risk) and digoxin (increased arrhythmia risk).
Cooperation & Technical Support
We supply pharmaceutical-grade Abiraterone in customized packaging to meet the needs of drug manufacturers and R&D institutions:
Packaging Options: 1g, 10g, 100g, or 1kg amber glass vials (sealed with Teflon-lined caps and desiccants) for small-batch R&D; 5kg, 25kg fiber drums (with aluminum foil liners) for commercial production-all under nitrogen protection.
Regulatory Documentation: Provide comprehensive technical files, including Certificate of Analysis (COA), Drug Master File (DMF), Certificate of Suitability (CEP), and stability data (accelerated, long-term) to support drug registration in the EU, US, China, and other global markets.
Value-Added Services: Offer customized impurity profiling, solubility enhancement consulting, and preclinical formulation support (e.g., for lipid-based delivery systems) to optimize product development.
Contact Us
If you are a pharmaceutical manufacturer, oncology R&D company, or contract manufacturing organization (CMO) focused on prostate cancer therapies, we welcome you to cooperate with us:
Contact Information:
Email: sales@huarongpharma.com
Phone/WhatsApp: +86 13751168070
Address: [Your Company Address, e.g., No. XX, High-Tech Zone, Chengdu, Sichuan, China]
We adhere to the principles of "oncology-grade quality, regulatory compliance, and customer-centricity" and are committed to providing reliable APIs for life-saving cancer treatments worldwide!
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