API Posaconazole

Posaconazole More Info

Posaconazole is a broad-spectrum triazole antifungal agent designed for the prevention and treatment of invasive fungal infections (IFIs). As a second-generation triazole, it offers enhanced activity against a wide range of pathogenic fungi, including azole-resistant strains, making it a critical therapeutic option in immunocompromised patient populations. Approved by the FDA, EMA, NMPA, and other global regulatory authorities, it is available in multiple dosage forms (oral suspension, delayed-release tablets, intravenous injection) to address diverse clinical needs.

Mechanism of Action

Posaconazole exerts its antifungal effect by inhibiting fungal ergosterol biosynthesis—a key component of fungal cell membranes. It selectively binds to cytochrome P450 14α-demethylase (CYP51), an enzyme critical for converting lanosterol to ergosterol. This inhibition disrupts cell membrane integrity, leading to increased permeability, cell leakage, and ultimately fungal cell death. Unlike first-generation triazoles, posaconazole exhibits higher affinity for fungal CYP51, providing broader spectrum coverage and improved efficacy against resistant pathogens (e.g., Aspergillus fumigatus, Candida glabrata).

Pharmaceutical Specifications (API Grade)

Chemical Name: (3R,5R)-5-(4-(4-(4-fluorophenyl)-1,3-dioxolan-2-yl)phenyl)-3-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1-(1H-1,2,4-triazol-1-yl)pentan-2-one

Molecular Formula: C₂₂H₂posaconazole₄FN₅O₄

Molecular Weight: 413.43 g/mol

Physical Traits: White to off-white crystalline powder; slightly soluble in water, soluble in methanol, ethanol, and dimethyl sulfoxide (DMSO); melting point: 170–174°C

Quality Standards: ≥99.0% purity (HPLC); individual impurity ≤0.1%, total impurities ≤0.5% (ICH Q9 compliant); meets USP-NF, EP, JP pharmacopoeial requirements

Compliance: ICH Q7 (GMP for APIs), ICH Q10, ISO 9001, and ISO 14001 certified; free of heavy metals (Pb ≤10 ppm, As ≤2 ppm) and residual solvents (ICH Q3C compliant)

Approved Therapeutic Indications

Posaconazole is indicated for:

Prevention of IFIs: In immunocompromised adults (e.g., hematopoietic stem cell transplant recipients with graft-versus-host disease, patients with hematologic malignancies undergoing chemotherapy) against Aspergillus and Candida infections.

Treatment of IFIs: For patients with invasive aspergillosis (IA) refractory to amphotericin B or itraconazole; invasive candidiasis (IC) in patients intolerant to other antifungals; and oropharyngeal candidiasis (OPC), including refractory cases in HIV-positive patients.

Pediatric Use: Approved for children ≥3 years (oral suspension) and ≥13 years (tablets/injection) for prevention and treatment of IFIs, based on weight-based dosing.

Regulatory & Quality Assurance

Regulatory Support: Type II Drug Master File (DMF) registered with FDA, EMA, and NMPA; comprehensive clinical (Phase I–IV), toxicological, and pharmacokinetic data packages available to support finished product registration.

Certifications: GMP (Good Manufacturing Practices) certified; compliance with global pharmaceutical quality standards (ICH Q7, Q9, Q10) and environmental management (ISO 14001).

Safety Profile: Well-tolerated with a favorable adverse event profile; key safety data includes minimal hepatotoxicity (compared to other triazoles) and low drug-drug interaction potential (via CYP3A4 inhibition, manageable with dosage adjustments).

Packaging, Storage & Shelf Life

Packaging: 1kg, 5kg, or 25kg sealed fiber drums with double polyethylene inner liners—moisture-proof, light-resistant, and tamper-evident. Custom packaging (100g, 500g) available for research or clinical trials.

Storage Conditions: Store at 2–8°C in a cool, dry, well-ventilated area; protect from direct sunlight, high humidity (≤60%), and oxidizing agents. Avoid freezing.

Shelf Life: 24 months from the manufacturing date when stored per specifications; full stability data (accelerated and long-term) provided upon request.

Commercial Supply Details

Minimum Order Quantity (MOQ): 100g (laboratory/research samples); bulk orders (≥1kg) with volume-based pricing.

Lead Time: 4–6 weeks for standard API orders; customized specifications (e.g., particle size, impurity limits) require 6–8 weeks.

Supply Chain: Traceable raw material sourcing (ISO 13485-certified suppliers); full batch documentation included with each shipment (Certificate of Analysis, CoA; Batch Record Summary; stability reports).

Trade & Market Insights

HS Code: 2933.99 (Other heterocyclic compounds)—complies with global import/export regulations for pharmaceuticals.

Market Demand: Driven by the rising incidence of IFIs in immunocompromised populations (e.g., cancer patients, transplant recipients, HIV/AIDS patients) and the growing threat of azole-resistant fungi. Key markets include North America, Europe, and Asia-Pacific.

Key Selling Points: Broad-spectrum antifungal activity, efficacy against resistant strains, multiple dosage form compatibility, robust regulatory support (DMF), GMP certification, and consistent batch quality for pharmaceutical formulation.