Lapatinib Ditosylate is the ditosylate salt form of lapatinib, an orally active small-molecule tyrosine kinase inhibitor (TKI). Lapatinib selectively inhibits the intracellular kinase domains of HER2/ErbB2 and EGFR/ErbB1, interfering with receptor signaling involved in cancer-cell proliferation and survival.
Lapatinib Ditosylate is primarily associated with the pharmaceutical treatment of HER2-positive breast cancer in approved clinical settings.
Lapatinib Ditosylate is a specialized oncology pharmaceutical API manufactured through controlled chemical synthesis, purification and salt formation.
Important quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, salt composition, polymorphic form and stability.
CAS Number: 388082-78-8
Molecular Formula: C29H26ClFN4O4S · 2C7H8O3S
Molecular Weight: 925.45 g/mol
Drug Class: Antineoplastic Agent
Pharmacological Class: Tyrosine Kinase Inhibitor
Therapeutic Class: Anticancer / Targeted Therapy
Therapeutic Area: Oncology
Lapatinib Ditosylate provides lapatinib, which reversibly inhibits the intracellular tyrosine kinase domains of:
Blocking these receptors interferes with downstream signaling pathways involved in tumor-cell growth and survival.
Lapatinib Ditosylate is used in approved settings for:
The specific indication and combination depend on the applicable regulatory labeling.
Lapatinib Ditosylate is formed by combining lapatinib with two molecules of p-toluenesulfonic acid (tosylate). The salt form is used as the pharmaceutical active ingredient in marketed lapatinib formulations.
Typical API manufacturing may involve:
Lapatinib Ditosylate API quality evaluation may include:
Lapatinib Ditosylate should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light. Final storage conditions should be established through validated stability studies.
Lapatinib Ditosylate is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 2.0% |