Drug glossary Targeted therapy

Afatinib Gilotrif

Used in colorectal cancer outside its approved indication. It appears in 6 clinical trials.

Oral EGFR HER2 ErbB4

United States Off-label

European Union EMA approved Since 2013

Spain Hospital use Used off-label in colorectal cancer

What it is

Afatinib is an irreversible tyrosine kinase inhibitor that targets multiple members of the ErbB family of receptors. In colorectal cancer, afatinib is used off-label in select patients with EGFR-mutated tumors or as part of combination therapy with cetuximab in wild-type KRAS metastatic disease. The drug has been explored in tumor-agnostic approaches based on specific genomic alterations rather than tumor origin.

How it works

Afatinib covalently binds to and irreversibly blocks EGFR (ErbB1), HER2 (ErbB2), and ErbB4 tyrosine kinases by forming a covalent bond with cysteine residues in the ATP-binding sites. This irreversible inhibition prevents autophosphorylation and downstream signaling through pathways including PI3K/AKT and RAS/RAF/MEK, ultimately leading to reduced tumor cell proliferation and survival.

Molecular targets

EGFR HER2 ErbB4

Common side effects

DiarrheaRashAcneiform dermatitisStomatitisParonychiaDecreased appetiteNauseaVomitingFatigueDry skinWeight lossConjunctivitisRhinorrheaEpistaxisDyspnea

Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.

Trials with this drug

1 recruiting

Pemigatinib + Afatinib in Advanced Refractory Solid Tumors NCT06302621 Recruiting Phase 1 United States Sotorasib Activity in Subjects With Advanced Solid Tumors With KRAS p.G12C Mutation (CodeBreak 101) NCT04185883 Active, not recruiting Phase 1 United States, Australia, Austria and 7 more Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1 NCT03785249 Active, not recruiting Phase 1 United States, Puerto Rico Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations NCT02795156 Archived Phase 2 United States Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) NCT02465060 Active, not recruiting Phase 2 United States, Guam, Puerto Rico Dual Targeting of EGFR With Cetuximab and Afatinib to Treat Refractory wtKRAS Metastatic Colorectal Cancer NCT01919879 Archived Phase 2 France

At a glance

Brand name: Gilotrif
Type: Targeted therapy
Route: Oral
Approved (FDA): 2013
Trials: 6 (1 recruiting)

Related drugs

CetuximabImmunotherapy372 trials PanitumumabImmunotherapy127 trials RegorafenibTargeted therapy109 trials FruquintinibTargeted therapy62 trials TrastuzumabImmunotherapy42 trials ErlotinibTargeted therapy20 trials

Medical notice

This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.

Guides that may help

Written for patients and families, in plain language.

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