Generic Name(s):
Trade Name(s):
Gilotrif and Tomtovok
NCI Definition [1]:
An orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly 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 RTKs. 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.

Biomarker-Directed Therapies

Afatinib has been investigated in 37 clinical trials, of which 31 are open and 6 are closed. Of the trials investigating afatinib, 7 are phase 1 (5 open), 4 are phase 1/phase 2 (3 open), 24 are phase 2 (21 open), 1 is phase 2/phase 3 (1 open), and 1 is phase 4 (1 open).

EGFR A763_Y764insFQEA, EGFR Exon 19 Deletion, and EGFR Exon 19 Insertion are the most frequent biomarker inclusion criteria for afatinib clinical trials.

Non-small cell lung carcinoma, malignant solid tumor, and adenocarcinoma of the gastroesophageal junction are the most common diseases being investigated in afatinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Afatinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Afatinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating afatinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,931 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
bibw-2992, Gilotrif, Tomtovok, bibw2992, afatinib (product), bibw 2992, afatinib, afatinibum, afatinib, (2e)-n-(4-(3-chloro-4-fluoroanilino)-7-(((3s)-oxolan-3-yl)oxy)quinoxazolin-6-yl)-4-(dimethylamino)but-2-enamide, afatinib (substance)
Drug Categories [2]:
Tyrosine kinase inhibitors
Drug Target(s) [2]:
NCIT ID [1]:


1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.