Though the parent quinazoline molecule is rarely mentioned by itself in technical literature, substituted derivatives have been synthesized for medicinal purposes such as antimalarial and anticancer agents.

[6] In 1903, Siegmund Gabriel reported the synthesis of the parent quinazoline from o-nitrobenzylamine, which was reduced with hydrogen iodide and red phosphorus to 2-aminobenzylamine.

It binds to the ATP-binding site of EGFR, thus inactivating the anti-apoptotic Ras signal transduction cascade preventing further growth of cancer cells.

[11][12][13] In March 2007, GlaxoSmithKline's drug lapatinib was approved by the U.S. FDA to treat advanced-stage or metastatic breast cancer in combination with Roche's capecitabine.

[14][15][16][17] In May 2013, erlotinib, a drug manufactured by Astellas, was approved by the U.S. FDA to treat NSCLC patients with tumors caused by mutations of EGFR.

[18][19] In July 2013, the U.S. FDA approved afatinib, a drug developed by Boehringer Ingelheim, as an irreversible, competitive inhibitor of HER2 and EGFR kinases.