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Afatinib CAS No 439081-18-2 & 850140-72-6 Pharmaceutical Raw Material
02
introduce
introduce
Afatinib is an oral, irreversible tyrosine kinase inhibitor (TKI) and important antineoplastic pharmaceutical API. It selectively targets EGFR, HER2, and other ErbB family receptors, demonstrating significant clinical efficacy in treating non-small cell lung cancer (NSCLC).
Our products comply with strict international quality standards (USP/EP/BP), ensuring reliable performance and stable supply for pharmaceutical formulation and research applications.
02
Physical and chemical properties
Afatinib exhibits key physical and chemical characteristics to support its pharmaceutical and research applications, as follows:
- Density: 1.380 g/cm³
- Melting Point: 102 °C
- Boiling Point: 676.9±55.0 °C
- Refractive index: 1.668
- Solubility:
Soluble in DMSO (≥24.3 mg/mL) and Ethanol with ultrasonic (≥42.1 mg/mL), slightly soluble in water
- Stability: Stable for 1 year as supplied; solutions in DMSO or ethanol can be stored at -20 °C for up to 2 months.
- Density: 1.380 g/cm³
- Melting Point: 102 °C
- Boiling Point: 676.9±55.0 °C
- Refractive index: 1.668
- Solubility:
Soluble in DMSO (≥24.3 mg/mL) and Ethanol with ultrasonic (≥42.1 mg/mL), slightly soluble in water
- Stability: Stable for 1 year as supplied; solutions in DMSO or ethanol can be stored at -20 °C for up to 2 months.
1. More Durable Mechanism of Action:
As the first approved irreversible ErbB family blocker, it forms covalent bonds with the kinase domains of EGFR, HER2, and HER4, permanently shutting down the signal transduction pathways on which cancer cells rely for survival. In contrast, traditional reversible EGFR-TKIs often lead to acquired resistance in patients after approximately 14 months of treatment.
As the first approved irreversible ErbB family blocker, it forms covalent bonds with the kinase domains of EGFR, HER2, and HER4, permanently shutting down the signal transduction pathways on which cancer cells rely for survival. In contrast, traditional reversible EGFR-TKIs often lead to acquired resistance in patients after approximately 14 months of treatment.
2. Broader Target Coverage:
It not only targets common EGFR activating mutations (e.g., Del 19, L858R) but also rare EGFR mutations (e.g., L861Q, G719X). Additionally, it can target HER2 tyrosine kinase, effectively addressing abnormal cancer cell proliferation caused by EGFR mutations or overexpression of HER2, covering a more comprehensive range of applicable mutation types.
3. Applicability for Post-Resistance Scenarios:
For some patients who develop acquired resistance to other EGFR-TKIs (e.g., resistance related to T790M mutation), it can serve as a next-line treatment option, providing additional therapeutic possibilities for resistant patients.
1. Primarily indicated for the treatment of non-small cell lung cancer (NSCLC), with specific applicable scenarios including:
(1) Adult patients with metastatic or locally advanced NSCLC who have not received prior EGFR and tyrosine kinase inhibitor treatment, and whose tumors test positive for EGFR mutations.
(2) Adult NSCLC patients with squamous histologic progression during or after platinum-based chemotherapy.
(3) Patients with metastatic NSCLC harboring specific abnormal EGFR genes (e.g., activating mutations, genetic abnormalities), especially those with cancer cells that have spread to tissues outside the lungs.
(4) Patients with metastatic squamous NSCLC who have shown poor response to prior platinum-based chemotherapy.
(1) Adult patients with metastatic or locally advanced NSCLC who have not received prior EGFR and tyrosine kinase inhibitor treatment, and whose tumors test positive for EGFR mutations.
(2) Adult NSCLC patients with squamous histologic progression during or after platinum-based chemotherapy.
(3) Patients with metastatic NSCLC harboring specific abnormal EGFR genes (e.g., activating mutations, genetic abnormalities), especially those with cancer cells that have spread to tissues outside the lungs.
(4) Patients with metastatic squamous NSCLC who have shown poor response to prior platinum-based chemotherapy.
2. Pharmaceutical R&D: Serves as a key raw material for formulating oral dosage forms (e.g., tablets under brand name Gilotrif) and as a research tool for studying ErbB family signaling pathways and cancer drug resistance mechanisms.
3. Biomedical Research: Applied in preclinical and clinical studies to evaluate combination therapies with other antineoplastic agents or targeted drugs.
We implement strict full-process quality control, with each batch of Afatinib undergoing rigorous testing of key indicators such as purity, stability, solubility, and biological activity to meet pharmaceutical grade standards.
Equipped with a stable raw material supply chain, we ensure continuous large-scale supply. Our professional technical team provides tailored services, including formulation optimization, application guidance, and post-sales technical support.
Equipped with a stable raw material supply chain, we ensure continuous large-scale supply. Our professional technical team provides tailored services, including formulation optimization, application guidance, and post-sales technical support.
As a second-generation irreversible tyrosine kinase inhibitor, Afatinib plays a crucial role in targeted cancer therapy, particularly in improving the prognosis of NSCLC patients. With its precise targeting, proven clinical efficacy, stable product quality, and reliable supply capacity, we are committed to providing high-quality Afatinib API and professional services for global pharmaceutical companies, research institutions, and clinical applications.
Choose our Afatinib to meet your needs in pharmaceutical formulation, oncology research, and clinical treatment. Contact us for more product details and cooperation support.
Choose our Afatinib to meet your needs in pharmaceutical formulation, oncology research, and clinical treatment. Contact us for more product details and cooperation support.