Neratinib is a synthetic irreversible tyrosine kinase inhibitor (TKI) and antineoplastic pharmaceutical active pharmaceutical ingredient (API). It belongs to the quinoline-based kinase inhibitor class and acts primarily against the HER2 (ErbB2), EGFR (ErbB1), and HER4 (ErbB4) receptor tyrosine kinases.
Neratinib is used as an active pharmaceutical ingredient in the development and manufacture of pharmaceutical formulations for HER2-positive breast cancer. It was developed under the code HKI-272 and is marketed as an oral anticancer medicine.
Neratinib is a specialized oncology pharmaceutical API relevant to targeted cancer therapy, kinase inhibitor research, pharmaceutical formulation development and analytical quality control.
The API is particularly relevant to pharmaceutical research involving HER2 signaling, epidermal growth factor receptor pathways, breast cancer and targeted antineoplastic drug development.
CAS Number: 698387-09-6
Molecular Formula: C₃₀H₂₉ClN₆O₃
Molecular Weight: 557.0 g/mol
Chemical Name: (E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
Development Code: HKI-272
Drug Class: Tyrosine Kinase Inhibitor
Therapeutic Class: Antineoplastic Agent
Therapeutic Area: Oncology
Molecule Type: Synthetic Small Molecule
Target: EGFR / HER2 / HER4
PubChem identifies Neratinib with CAS 698387-09-6, molecular formula C₃₀H₂₉ClN₆O₃ and molecular weight 557.0 g/mol.
Neratinib is an irreversible pan-ErbB tyrosine kinase inhibitor.
Its mechanism includes:
Neratinib forms a covalent interaction with cysteine residues in the kinase domains of HER-family receptors, producing prolonged inhibition of receptor signaling.
Neratinib API is relevant to:
Neratinib is particularly associated with HER2-positive breast cancer and has been approved as an extended adjuvant treatment for certain patients with early-stage HER2-positive breast cancer.
Its activity against HER-family receptor tyrosine kinases makes it an important molecule in targeted oncology research.
HER2 is a receptor tyrosine kinase involved in cellular growth and proliferation. Abnormal HER2 signaling can contribute to the development and progression of certain cancers.
Neratinib irreversibly inhibits HER2 kinase activity, thereby reducing downstream signaling involved in tumor-cell proliferation and survival.
Neratinib is a synthetic organic small molecule with molecular formula C₃₀H₂₉ClN₆O₃ and molecular weight 557.0 g/mol. PubChem reports an XLogP3-AA value of approximately 4.9 and topological polar surface area of approximately 112 Ų.
Neratinib is also commercially encountered in the maleate salt form. Neratinib Maleate has CAS 915942-22-2, while Neratinib Maleate Monohydrate has CAS 1144516-12-0. These should not be confused with the free-base Neratinib API.
A controlled Neratinib API manufacturing process may involve:
Typical Neratinib API testing may include:
Because Neratinib contains a defined E-configured acrylamide moiety, appropriate control of chemical identity and related substances is important during API quality assessment.
Store Neratinib API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
Commercial storage conditions should be established according to validated stability data and the applicable API specification.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |