Erlotinib Hydrochloride (Erlotinib HCl) is a synthetic small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used as an anticancer pharmaceutical ingredient. It is the hydrochloride salt of erlotinib and is primarily associated with targeted treatment of specific cancers driven by EGFR signaling.
Erlotinib HCl is the hydrochloride salt form of erlotinib, an orally active quinazoline-based EGFR tyrosine kinase inhibitor.
Erlotinib hydrochloride has the molecular formula C₂₂H₂₃N₃O₄·HCl and a molecular weight of 429.90 g/mol. Its CAS Registry Number is 183319-69-9.
Erlotinib reversibly inhibits the kinase activity of the epidermal growth factor receptor (EGFR). It prevents EGFR autophosphorylation and inhibits downstream signaling involved in tumor-cell survival and proliferation.
Erlotinib has higher binding affinity for certain activating EGFR mutations, including exon 19 deletions and exon 21 L858R substitutions, than for wild-type EGFR.
Erlotinib HCl is primarily associated with:
U.S. labeling includes erlotinib for specified patients with metastatic NSCLC containing EGFR exon 19 deletions or exon 21 L858R mutations, and for first-line treatment of locally advanced, unresectable or metastatic pancreatic cancer in combination with gemcitabine.
Erlotinib HCl is a small-molecule oncology API. Pharmaceutical-grade material is characterized through identity, assay, related substances, residual solvents, water content and other applicable quality-control tests.
The hydrochloride salt has pH-dependent aqueous solubility and is reported as practically insoluble in water in current U.S. product labeling.
Erlotinib HCl intended for pharmaceutical manufacturing should comply with the applicable approved specification and relevant pharmacopoeial/regulatory requirements.
Typical quality attributes include:
A qualified supplier should provide Certificate of Analysis (CoA), specification sheet, SDS/MSDS, batch traceability and applicable regulatory documentation.
Store Erlotinib HCl in a tightly closed container, protected from moisture, excessive heat and direct light, according to the approved storage and stability requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 168°C – 172°C |