BIBW-2992 (Gilotrif)

Description

BIBW-2992, also known as afatinib, is an irreversible pan-ErbB family tyrosine kinase inhibitor that targets multiple members of the epidermal growth factor receptor (EGFR) family. In colorectal cancer treatment, this oral targeted therapy has been evaluated for patients with metastatic disease, particularly those with specific EGFR and KRAS mutation profiles. The drug covalently binds to its target receptors, providing sustained inhibition of downstream signaling pathways involved in tumor growth and proliferation.

Mechanism of Action

Afatinib irreversibly binds to and blocks the tyrosine kinase activity of EGFR (ErbB1), HER2 (ErbB2), and ErbB4 receptors by forming covalent bonds with cysteine residues in the ATP-binding sites of these kinases. This blockade prevents autophosphorylation and subsequent activation of downstream signaling cascades including PI3K/AKT and RAS/RAF/MEK/ERK pathways that promote cell proliferation, survival, and metastasis in colorectal tumors.

Molecular Targets

Side Effects

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials