Pyrotinib API is a targeted oncology pharmaceutical ingredient belonging to the irreversible tyrosine kinase inhibitor class. Pyrotinib primarily inhibits the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), making it an important active pharmaceutical ingredient for research and pharmaceutical development involving HER2-positive malignancies.
The pharmaceutical form associated with marketed pyrotinib products is pyrotinib maleate, specifically the dimaleate salt in a 1:2 ratio. Published product documentation identifies the pyrotinib maleate molecular formula as C₃₂H₃₁ClN₆O₃·2C₄H₄O₄ and molecular weight as 815.22 g/mol.
Pyrotinib is a small-molecule, orally active irreversible dual receptor tyrosine kinase inhibitor. Its chemical structure contains a quinoline core, substituted anilino group, pyridine-containing ether moiety, nitrile group and chiral pyrrolidine-containing acrylamide structure.
The active moiety has CAS 1269662-73-8, molecular formula C₃₂H₃₁ClN₆O₃, and molecular weight 582.21 g/mol. The FDA Substance Registration System identifies this substance under UNII CJN36EQM0H.
For pharmaceutical applications, pyrotinib is used in the form of its maleate salt. The pyrotinib maleate form is identified as CAS 1397922-61-0 with molecular weight 815.22 g/mol.
| Parameter | Details |
|---|---|
| Product Name | Pyrotinib |
| Pharmaceutical Form | Pyrotinib Maleate / Dimaleate |
| Active Moiety CAS | 1269662-73-8 |
| API Salt CAS | 1397922-61-0 |
| Active Moiety Formula | C₃₂H₃₁ClN₆O₃ |
| Maleate Formula | C₃₂H₃₁ClN₆O₃·2C₄H₄O₄ |
| Active Moiety Molecular Weight | 582.21 g/mol |
| Maleate Molecular Weight | 815.22 g/mol |
| FDA UNII – Active Moiety | CJN36EQM0H |
| Drug Class | Irreversible receptor tyrosine kinase inhibitor |
| Main Targets | EGFR and HER2 |
| Physical Form | Solid |
| Stereochemistry | Defined R configuration |
| Therapeutic Area | Oncology |
The FDA substance record confirms the active moiety identity and CAS number, while published pyrotinib maleate documentation confirms the dimaleate composition.
Pyrotinib is primarily associated with oncology applications involving HER2-positive breast cancer. It is an irreversible dual inhibitor targeting EGFR/HER2 signaling pathways. Published clinical documentation describes pyrotinib maleate tablets as being used in combination with capecitabine for HER2-positive recurrent or metastatic breast cancer in the relevant treatment setting.
Its pharmaceutical development applications include:
Analytical literature has also demonstrated HPLC and LC-MS/MS methods for quantitative determination of pyrotinib and its metabolites.
Pyrotinib API requires comprehensive analytical characterization because it is a structurally complex chiral small molecule. Identity and purity can be evaluated using HPLC, LC-MS, NMR, IR and related chromatographic techniques. Commercial research-grade materials currently report HPLC purities above 98%, with individual batches reported at higher purity levels. These commercial values should be treated as reference-material specifications rather than universal pharmacopoeial API limits.
Typical analytical control includes:
Pyrotinib API manufacturing requires controlled synthesis, purification and analytical characterization of both the active moiety and the maleate salt. Particular attention is required for stereochemical integrity, chemical purity, residual solvents, related substances and salt-form consistency.
A pharmaceutical-grade Pyrotinib API manufacturing program should be supported by validated analytical methods, controlled raw materials, batch traceability and appropriate quality documentation.
Pyrotinib maleate should be protected from moisture, excessive heat and light and stored under controlled conditions established through stability studies.
Recommended handling includes:
Commercial reference products commonly recommend low-temperature or controlled storage, although the final commercial API storage condition should be established from the manufacturer's validated stability data.
Pyrotinib API documentation can include:
A reliable Pyrotinib API manufacturing program should combine controlled synthesis, consistent salt formation, validated analytical testing and complete batch documentation. Because public sources do not provide a complete universal pharmacopoeial numerical specification for pyrotinib maleate, the finished API specification should be based on a validated pharmaceutical quality specification rather than unsupported generic limits.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 0.5% |