AG-1478 (also known as Tyrphostin AG1478; AG-1478; NSC-693255) is a novel, potent and selective EGFR (epidermal growth factor receptor) inhibitor with potential antitumor and antidiabetic activity.

Rociletinib (formerly CO1686; AVL301; CNX419) is an orally bioavailable, covalent / irreversible, and mutant-selective EGFR (e.g. T790M) inhibitor with potential antineoplastic activity.

OSI-420 HCl (also known as CP-473420; OSI420; Desmethyl Erlotinib), the demethylated and active metabolite of erlotinib, is a potent, selective, orally bioavailable and ATP competitive inhibitor of tyrosine kinase EGFR with potential antineoplastic activity.

WZ3146 (WZ-3146) is a covalent / irreversible and mutant-selective inhibitor of EGFR (L858R and E746_A750) with potential anticancer activity.

Lazertinib (formerly known as GNS-1480; YH-25448; GNS1480; YH25448; LECLAZA) is an oral, highly mutant-selective and irreversible 3rd generation EGFR TKI (Tyrosine-kinase inhibitors) approved in 2021 for the treatment of lung cancer (NSCLC).

Osimertinib mesylate (formerly known as AZD9291; AZD-9291; AZD 9291; mereletinib; Tagrisso), the mesylate salt of osimertinib, is a novel, potent, oral bioavailable, irreversible, and mutant-selective, 3rd generation EGFR inhibitor approved by both FDA and the European Commission for cancer treatment.

Chrysophanic acid (also called Chrysophanol), a naturally occuring anthraquinone isolated from Dianella longifolia, is a selective and potent inhibitor of EGFR/mTOR (epidermal growth factor (EGF) receptor/mammalian target of rapamycin) with potential anti-obesity and antitumor activity.

Lapatinib (formerly GW572016, trade names Tykerb & Tyverb), usually used in the Ditosylate form, is a potent, orally bioavailable dual EGFR/ErbB2 inhibitor with potential anticancer activity.

Icotinib (formerly known as BPI-2009; trade name Conmana), a side chain-cyclized form of erlotinib, is an orally available and specific EGFR inhibitor with potent anticancer activity.

Naquotinib (ASP 8273; ASP-8273; ASP8273) is an irreversible/covalent and 3rd-generation inhibitor of epidermal growth factor receptor (EGFR) with potential antitumor activity.