tcsc0467 Desmethyl Erlotinib

Desmethyl Erlotinib (OSI-420) is an active metabolite of erlotinib, which is a potent EGFR tyrosin kinase inhibitor.

In Vivo: Desmethyl Erlotinib exposure (AUC) in plasma is 30% (range 12-59%) of erlotinib, and Desmethyl Erlotinib clearance is more than 5-fold higher than erlotinib. The CSF penetration of erlotinib and Desmethyl Erlotinib is <5% relative to total plasma concentration^[1].