Lapatinib is an orally active tyrosine kinase inhibitor (TKI) that selectively inhibits the intracellular kinase domains of human epidermal growth factor receptor 2 (HER2/ErbB2) and epidermal growth factor receptor (EGFR/ErbB1).
By blocking HER2 and EGFR signaling, lapatinib interferes with pathways involved in tumor-cell proliferation and survival. It is primarily used in the treatment of selected HER2-positive breast cancers.
Lapatinib is a specialized oncology pharmaceutical API manufactured through controlled chemical synthesis, purification and crystallization.
Important quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, polymorphic form and stability.
CAS Number: 231277-92-2
Molecular Formula: C29H26ClFN4O4S
Molecular Weight: 581.06 g/mol
Drug Class: Antineoplastic Agent
Pharmacological Class: Tyrosine Kinase Inhibitor
Therapeutic Class: Anticancer / Targeted Therapy
Therapeutic Area: Oncology
Lapatinib reversibly inhibits the intracellular tyrosine kinase domains of HER2 and EGFR.
This inhibits receptor-mediated signaling pathways that contribute to:
Lapatinib can also inhibit signaling from receptors that form active heterodimers with HER2.
Lapatinib is used in approved settings for:
The specific indication and combination regimen depend on the applicable regulatory labeling.
Lapatinib differs from monoclonal antibodies targeting HER2 because it is a small-molecule intracellular kinase inhibitor. Its oral administration allows systemic exposure and intracellular inhibition of receptor tyrosine kinase signaling.
Typical API manufacturing may involve:
Lapatinib API quality evaluation may include:
Lapatinib 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 is relevant to research involving:
Lapatinib is an oral HER2 and EGFR tyrosine kinase inhibitor with CAS Number 231277-92-2, molecular formula C29H26ClFN4O4S, and molecular weight 581.06 g/mol. It inhibits intracellular receptor tyrosine kinase signaling and is used in selected HER2-positive breast cancer treatment settings.
| 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 | NMT 1.0% |
| Water Content | NMT 2.0% |