Afatinib^[1][2] (INN; planned trade name Tomtovok, previously Tovok^[3]) is a candidate drug against non-small cell lung carcinoma, developed by Boehringer Ingelheim. , it is undergoing a Phase III clinical trial for this indication, and Phase II trials for breast, prostate, and head and neck cancers, as well as glioma.^[4][5]

In October 2010 a new Boehringer Ingelheim Phase III trial called "Lux-Lung 5" began with this drug.^[6]

Fall 2010 interim results suggest the drug extended progression-free survival threefold compared to placebo, but did not extend overall survival.^[7]

Mechanism of action

Like lapatinib and neratinib, afatinib is a next generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is investigated for breast cancer as well as other EGFR and Her2 driven cancers.^[5]

References