Active Ingredient History
Afatinib is a anilino-quinazoline derivative and irreversible antagonist of the receptor tyrosine kinase epidermal growth factor receptor family, with antineoplastic activity. Afatinib selectively and covalently binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these kinases. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Afatinib is a substrate and an inhibitor of P-gp and of the transporter BCRP. Co-administration of P-gp inhibitors can increase afatinib exposure while co-administration of chronic Pgp inducers can decrease afatinib exposure. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Adenocarcinoma (Phase 3)
Anemia (Phase 1)
Bile Duct Neoplasms (Phase 2)
Brain Neoplasms (Phase 2)
Breast Neoplasms (Phase 3)
Carcinoma, Squamous Cell (Phase 3)
Carcinoma, Transitional Cell (Phase 2)
Chordoma (Phase 2)
Colonic Neoplasms (Phase 2)
Colorectal Neoplasms (Phase 2)
Digestive System Neoplasms (Phase 2)
Drug Therapy (Phase 2)
Endometrial Neoplasms (Phase 2)
Endometriosis (Phase 1/Phase 2)
Epidermal Growth Factor (Phase 2)
ErbB Receptors (Phase 4)
Esophageal Neoplasms (Phase 2)
Esophageal Squamous Cell Carcinoma (Phase 2)
Gallbladder Neoplasms (Phase 2)
Gastrointestinal Neoplasms (Phase 1/Phase 2)
General Surgery (Phase 2)
Genes, erbB-2 (Phase 2)
Glioblastoma (Phase 1)
Glioma (Phase 2)
Head and Neck Neoplasms (Phase 3)
Healthy Volunteers (Phase 1)
Hodgkin Disease (Phase 1)
Intestinal Neoplasms (Phase 2)
Kidney Neoplasms (Phase 2)
Leukemia, Lymphocytic, Chronic, B-Cell (Phase 1)
Leukemia, Myeloid, Acute (Phase 1)
Leukemia, Myeloid, Chronic-Phase (Phase 1)
Leukemia, Myelomonocytic, Chronic (Phase 1)
Liver Diseases (Phase 1)
Liver Neoplasms (Phase 2)
Lung Neoplasms (Phase 4)
Lymphoma (Phase 2)
Lymphoma, Non-Hodgkin (Phase 1)
Melanoma (Phase 2)
Meninges (Phase 1)
Multiple Myeloma (Phase 2)
Mutation (Phase 2)
Myelodysplastic Syndromes (Phase 1)
Myeloproliferative Disorders (Phase 1)
Neoplasm Metastasis (Phase 2)
Neoplasms ()
Neoplasms, Squamous Cell (Phase 1)
Neuroectodermal Tumors (Phase 1)
Ovarian Neoplasms (Phase 2)
Pancreatic Neoplasms (Phase 2)
Penile Neoplasms (Phase 2)
Primary Myelofibrosis (Phase 1)
Progression-Free Survival (Phase 2)
Prostatic Neoplasms (Phase 2)
Renal Insufficiency (Phase 1)
Rhabdomyosarcoma (Phase 1)
Skin Neoplasms (Phase 2)
Small Cell Lung Carcinoma (Phase 2)
Squamous Cell Carcinoma of Head and Neck (Phase 3)
Stomach Neoplasms (Phase 2)
Thyroid Neoplasms (Phase 2)
Triple Negative Breast Neoplasms (Phase 2)
Ureteral Neoplasms (Phase 2)
Urethral Neoplasms (Phase 2)
Urinary Bladder Neoplasms (Phase 2)
Urologic Neoplasms (Phase 2)
Uterine Cervical Neoplasms (Phase 2)
Uterine Neoplasms (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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