Erlotinib is an epidermal growth factor receptor inhibitor. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.
Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR. Erlotinib D6 is a deuterium labeled Erlotinib .