Imatinib Mesylate is the mesylate salt of imatinib, a small-molecule targeted anticancer agent belonging to the tyrosine kinase inhibitor (TKI) class. It inhibits specific protein tyrosine kinases involved in abnormal cellular signaling and is an important pharmaceutical ingredient in targeted cancer therapy.
Imatinib Mesylate is primarily used in the treatment of Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) and several other cancers and hematological disorders driven by susceptible tyrosine kinase abnormalities.
Imatinib Mesylate is a specialized pharmaceutical API requiring controlled synthesis, purification and comprehensive analytical characterization. Manufacturing quality control generally focuses on identity, assay, related substances, residual solvents, water content, elemental impurities and polymorphic characteristics.
Consistent control of process-related and degradation impurities is important for producing high-quality Imatinib Mesylate suitable for pharmaceutical formulation.
CAS Number: 220127-57-1
Molecular Formula: C29H31N7O·CH4SO3
Molecular Weight: 589.71 g/mol
Chemical Name: Imatinib Mesylate
Drug Class: Antineoplastic Agent
Pharmacological Class: Tyrosine Kinase Inhibitor
Therapeutic Class: Targeted Anticancer Agent
Therapeutic Area: Oncology / Hematology
Imatinib selectively inhibits several clinically important tyrosine kinases, particularly:
In Philadelphia chromosome-positive CML, the BCR-ABL fusion protein produces constitutive tyrosine kinase activity that promotes abnormal proliferation of leukemic cells.
Imatinib binds to the ATP-binding site of susceptible tyrosine kinases and inhibits their signaling activity, thereby reducing proliferation and promoting control of kinase-driven malignant cells.
Imatinib Mesylate is used in approved pharmaceutical formulations for selected conditions including:
Specific indications depend on regulatory approval, disease characteristics and product labeling.
Imatinib is a landmark example of molecularly targeted cancer therapy. Rather than acting broadly on rapidly dividing cells, it targets specific signaling proteins that drive particular malignancies.
Its clinical importance is particularly associated with BCR-ABL-positive leukemia and KIT-driven gastrointestinal stromal tumors.
The BCR-ABL fusion protein results from the characteristic genetic abnormality associated with the Philadelphia chromosome. Its persistent kinase activity contributes to uncontrolled proliferation of leukemic cells.
Imatinib inhibits BCR-ABL kinase activity and thereby suppresses downstream signaling involved in malignant cell growth.
Imatinib Mesylate is a synthetic, nitrogen-containing heterocyclic compound supplied as a pharmaceutical salt. It is generally handled as a white to off-white crystalline powder.
The API exhibits limited aqueous solubility, and its physicochemical properties are important considerations during formulation and solid-state characterization.
Imatinib Mesylate API quality evaluation may include:
Imatinib Mesylate should be stored in a tightly closed container under controlled pharmaceutical conditions and protected from excessive moisture, heat and direct light. Final storage conditions should follow validated stability data and the applicable product specification.
Imatinib Mesylate remains highly relevant to pharmaceutical research involving BCR-ABL inhibition, tyrosine kinase signaling, targeted oncology, KIT inhibition, PDGF receptor pathways and precision cancer medicine.
Imatinib Mesylate is a targeted tyrosine kinase inhibitor with CAS Number 220127-57-1, molecular formula C29H31N7O·CH4SO3, and molecular weight 589.71 g/mol. It inhibits BCR-ABL, KIT and PDGF receptor tyrosine kinases and is used in approved treatments for selected leukemias, gastrointestinal stromal tumors and other kinase-driven malignancies.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 3.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 3.0% |