Product Identification
|
Property |
Details |
|
International Nonproprietary Name (INN) |
Olaparib |
|
Chemical Name |
2-[4-(3-cyclopropanecarbonyl-4-piperazinecarbonyl)benzyl]-1-phthalazinone |
|
CAS Registry Number |
763113-22-0 |
|
Molecular Formula |
C24H23FN4O3 |
|
Molecular Weight |
434.46 g/mol |
|
Physical Description |
White to off-white crystalline powder |
Physical and Chemical Properties
Solubility
Practically insoluble in water; sparingly soluble in dimethyl sulfoxide and methanol
Melting Point Range
105 degrees Celsius to 110 degrees Celsius (Polymorphic form dependent)
Storage Conditions
Store in tightly closed containers under controlled room temperature between 20 degrees Celsius and 25 degrees Celsius, protected from light and moisture
Quality Specifications and Analytical Methods
Assay (Purity on Dry Basis): 98.0 percent to 102.0 percent via High-Performance Liquid Chromatography
Chiral Purity: Greater than or equal to 99.5 percent via Chiral High-Performance Liquid Chromatography
Individual Known Impurity: Less than or equal to 0.10 percent via Gradient High-Performance Liquid Chromatography
Total Impurities: Less than or equal to 0.5 percent via Gradient High-Performance Liquid Chromatography
Residual Solvents: Complies with International Council for Harmonisation limits, including Ethanol less than or equal to 5000 parts per million via Headspace Gas Chromatography
Water Content: Less than or equal to 0.5 percent via Karl Fischer Volumetric Titration
Sulfated Ash: Less than or equal to 0.1 percent via Gravimetric Analysis
Heavy Metals: Less than or equal to 20 parts per million via Inductively Coupled Plasma Mass Spectrometry
Particle Size Distribution: D90 between 10 micrometers and 50 micrometers, customizable
Manufacturing Standards
Production Scale: Multi-kilogram to metric ton annual capacity via dedicated oncology synthesis lines
Reaction Control: Cryogenic and high-pressure reaction monitoring for intermediate steps
Purification Process: Multi-stage crystallization and filtration under controlled cleanroom environments
Containment Measures: Isolator technology and closed-system material transfer ensuring operator safety and zero cross-contamination
Batch Traceability: Complete raw material genealogy tracking from starting material vendor to finished batch
Regulatory Documentation Package
Drug Master File: Available in open and closed part format for regulatory submission support
Certificate of Analysis: Provided with every commercial and pilot batch detailing all release parameters
Stability Data: Long-term studies at 25 degrees Celsius and 60 percent relative humidity, alongside accelerated studies at 40 degrees Celsius and 75 percent relative humidity
Regulatory Compliance: Issued per International Council for Harmonisation Q7 guidelines confirming adherence to current good manufacturing practices
Toxicological Evaluation: Comprehensive genotoxic impurity risk assessment and analytical screening data
Material Certification: Animal-origin-free manufacturing processes and reagents confirmed
Packaging and Logistics
Primary Packaging: Pharmaceutical-grade low-density polyethylene bags, double-tied and heat-sealed
Secondary Packaging: Light-protective black polyethylene liner inserted inside the primary bag
Tertiary Packaging: Rigid fiber drum or certified stainless steel container
Moisture Control: Food-grade silica gel packets placed between primary and secondary liners
Standard Batch Unit: 1 kilogram, 5 kilograms, or 25 kilograms net weight per drum
Labeling Standard: Product name, CAS number, batch number, net weight, manufacturing date, retest date, and storage instructions
Pharmaceutical Applications
Ovarian Cancer Maintenance Therapy: Formulated into oral tablets for maintenance treatment in adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer responding to platinum-based chemotherapy. Precise particle size distribution ensures consistent dissolution rates in finished dosage forms.
Metastatic Breast Cancer Treatment: Integrated into targeted therapies for germline breast cancer susceptibility gene-mutated, human epidermal growth factor receptor 2-negative metastatic breast cancer previously treated with chemotherapy. High enantiomeric purity prevents structural interference during binding to target enzyme catalytic sites.
Pancreatic Cancer Maintenance: Applied in second-line maintenance regimens for patients with deleterious germline breast cancer susceptibility gene-mutated metastatic pancreatic adenocarcinoma. Low impurity profiles minimize potential side effects stemming from synthesis byproducts during long-term administration.
Castration-Resistant Prostate Cancer: Processed into solid oral dosage formulations for homologous recombination repair gene-mutated metastatic castration-resistant prostate cancer. Rigorously controlled residual solvent levels ensure compliance with strict patient safety thresholds in oncology drugs.
FAQ
Q: What is the standard batch size available for commercial orders?
A: Commercial batches are produced at standard scale, with individual batch sizes and multi-delivery schedules tailored to customer manufacturing forecasts and regulatory filing requirements.
Q: Is a Drug Master File accessible for regulatory filings?
A: Yes, a comprehensive Drug Master File is maintained and can be referenced for regulatory submissions in major global jurisdictions upon execution of a letter of access.
Q: How is polymorphic form controlled during synthesis?
A: Crystallization parameters, solvent selection, and drying temperatures are strictly validated to maintain consistent crystal habit and polymorphic stability across production batches.
Q: What level of genotoxic impurity testing is performed?
A: All batches undergo routine screening using validated chromatographic methods to ensure potential process-related genotoxic impurities remain well below acceptable threshold limits defined by regulatory standards.
Q: Can particle size distribution be adjusted for specific formulation needs?
A: Yes, milling and micronization parameters can be adjusted to meet specific particle size distribution requirements for dry powder blending or direct compression processes.
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