Synonyms: BIBW2992 | Gilotrif®
afatinib is an approved drug (EMA & FDA (2013))
Compound class:
Synthetic organic
Comment: Afatinib is a second-generation, irreversible, covalently-bound EGFR tyrosine kinase inhibitor. It potently and selectively inhibits EGFR and Erbb2 [3,5,7]. Although afatinib demonstrates improved activity against the gatekeeper EGFR T790M resistance mutation, it is equally potent against the wild-type receptor, leading to dose-limiting toxicities and a narrow safety window [8]. Third generation, wild-type sparing inhibitors such as nazartinib are in development to circumvent this problem [4].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖![]() View more information in the IUPHAR Pharmacology Education Project: afatinib |
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No information available. |
Summary of Clinical Use ![]() |
Afatinib is an irreversible kinase inhibitor approved for first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have activating mutations in the epidermal growth factor receptor (EGFR). Such mutations must be confirmed by an FDA-approved test. Marketed formulations contain afatinib dimaleate (PubChem CID 15606394). In April 2016, the US FDA expanded approval to include monotherapy treatment of patients with advanced squamous cell carcinoma of the lung whose disease has progressed after treatment with platinum-based chemotherapy. January 2018, saw FDA approval broadened to include use as first-line treatment for metastatic NSCLC in tumors that have non-resistant EGFR mutations as detected by an FDA-approved test. |
External links ![]() |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |