Imatinib Mesylate is a targeted small-molecule active pharmaceutical ingredient belonging to the tyrosine kinase inhibitor class. It selectively inhibits Bcr-Abl tyrosine kinase, platelet-derived growth factor receptor, and c-Kit signaling pathways. Engineered for oral solid dosage formulations, it is primarily utilized in therapies addressing Philadelphia chromosome-positive chronic myeloid leukemia and gastrointestinal stromal tumors. Production adheres strictly to current Good Manufacturing Practice guidelines, utilizing validated synthetic routes to maintain stringent impurity profiles and crystalline form consistency. Analytical testing protocols verify structural identity, polymorphic purity, and residual solvent limits to satisfy global pharmacopeial standards.
Product Specifications
|
Parameter |
Specification |
|
Product Name |
Imatinib Mesylate |
|
CAS Number |
220127-57-1 |
|
Molecular Formula |
C29H31N7O . CH4O3S |
|
Molecular Weight |
589.71 g/mol |
|
Chemical Category |
Phenylaminopyrimidine derivative / Tyrosine kinase inhibitor |
|
Appearance |
White to off-white crystalline powder |
|
Solubility |
Very slightly soluble in water, sparingly soluble in methanol, practically insoluble in acetone |
|
Storage Condition |
Store in tight, light-resistant containers at controlled room temperature |
Quality & Analytical Standards
|
Test Parameter |
Acceptance Criteria |
Analytical Method |
|
Identification |
Spectrum matches reference standard; retention time corresponds |
FTIR / HPLC |
|
Assay |
98.5% to 101.5% (anhydrous, solvent-free) |
High-Performance Liquid Chromatography |
|
Polymorphic Form |
Form Alpha / Form Beta as specified |
X-Ray Powder Diffraction |
|
Water Content |
Maximum 0.5% |
Volumetric Karl Fischer titration |
|
Residue on Ignition |
Maximum 0.1% |
Gravimetric analysis |
|
Heavy Metals |
Maximum 10 ppm |
Inductively Coupled Plasma Mass Spectrometry |
|
Individual Impurity |
Maximum 0.10% |
Gradient HPLC |
|
Total Impurities |
Maximum 0.50% |
Gradient HPLC |
|
Residual Solvents |
Compliant with international regulatory limits |
Headspace Gas Chromatography |
|
Particle Size (D90) |
Controlled per milling specification (D90 < 50 µm available) |
Laser Diffraction |
Manufacturing Capabilities
Commercial Scale
Standard batch manufacturing capacity ranges from 100 kg to 500 kg, supporting multi-metric ton annual production.
Synthetic Route
Multi-step organic synthesis featuring validated intermediate isolation and crystallization control.
Facility Standards
Dedicated reactors, closed filtration units, vacuum tray dryers, and advanced micronization systems.
Process Control
Real-time temperature monitoring, reaction endpoint verification via HPLC, and comprehensive intermediate purity checks.
Cleaning Validation
Multi-product analytical residue verification utilizing validated swab and rinse testing protocols.
Regulatory Documentation
Drug Master File: Active regulatory filing available for submission support.
Certificate of Analysis: Provided with every commercial and sample batch.
Safety Data Sheet: Compliant with GHS hazard communication requirements.
Stability Data: Long-term (25°C / 60% RH) and accelerated (40°C / 75% RH) study summaries available.
Genotoxic Impurity Evaluation: Risk assessment and analytical testing reports aligned with current international safety guidelines.
Compliance Statements: Certified free from animal-derived raw materials with full residual solvent declaration.
Packaging & Storage
Double-layer food-grade low-density polyethylene bags, hermetically heat-sealed.
Moisture-barrier aluminum foil bag or tamper-evident polyethylene liner.
Rigid fiber drum or certified corrugated cardboard box equipped with desiccant placement.
25 kg per drum, marked with complete traceability labeling including batch numbers, manufacturing dates, and retest parameters.
Pharmaceutical Applications
Chronic Myeloid Leukemia: Active pharmaceutical ingredient for oral tablets and capsules targeting Philadelphia chromosome-positive chronic myeloid leukemia across chronic, accelerated, and blast crises.
Gastrointestinal Stromal Tumors: Utilized in solid oral dosage preparation for unresectable or metastatic malignant gastrointestinal stromal tumors via targeted receptor kinase blockade.
Acute Lymphoblastic Leukemia: Incorporated into combination chemotherapy regimens to suppress lymphoid blast cell proliferation effectively.
Dermatofibrosarcoma Protuberans: Applied in clinical manufacturing pipelines for adult patients with recurrent or progressive localized tumor growth.
FAQ
Q: What polymorphic forms of Imatinib Mesylate are commercially available?
A: Both Form Alpha and Form Beta crystalline modifications can be synthesized and supplied according to specific formulation requirements and crystal habit preferences.
Q: Is a Drug Master File accessible for regulatory filing?
A: Yes, an active regulatory DMF is maintained and available for reference authorization upon the execution of a confidentiality agreement.
Q: What is the standard retest period for commercial batches?
A: The standard retest period is 36 months when stored under recommended conditions in unopened original containers, supported by real-time stability data.
Q: Can particle size distribution be customized for direct compression or wet granulation?
A: Yes, micronization processes can be adjusted to meet target particle size parameters such as D90 < 20 µm or customized distribution ranges.
Q: How are potential genotoxic and process-related impurities controlled?
A: Impurities are monitored and controlled below strict qualification thresholds using validated gradient HPLC methods aligned with global regulatory guidelines.
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