Lapatinib Ditosylate (formerly GW-572016, GW572016; trade names Tykerb and Tyverb) is an orally bioavailable medication acting as an EGFR (epidermal growth factor receptor) and ErbB2 inhibitor with antineoplastic activity.

Neratinib (formerly known as HKI-272 or PB-272; trade name: Nerlynx) is a highly potent, selective, and orally bioavailable HER2 and EGFR inhibitor with potential antitumor activity.

TAK-285 (TAK285), currently being investigated by Takeda company, is a dual HER2/EGFR(HER1) inhibitor with potential antitumor activity.

Tarloxotinib bromide (formerly TH-4000; PR-610) is a novel quarternary amine-based and irreversible EGFR/HER2 inhibitor designed as a prodrug to selectively release a covalent (irreversible (covalent)) EGFR tyrosine kinase inhibitor under severe hypoxia, a feature of many solid tumors.

CP-724714 (CP724714) is an orally bioavailable, potent, selective inhibitor of HER2/ErbB2 with potential anticancer activity.

(E)-AG 99 is a novel and potent EGFR inhibitor.

WZ8040 is a novel, potent, mutant-selective and covalent / irreversible EGFR(T790M) inhibitor with potential anticancer activity, it does not inhibit the phosphorylation of ERBB2 (T798I).

Osimertinib dimesylate (mereletinib; AZD 9291; AZD9291; AZD-9291; trade name Tagrisso), the dimesylate salt of osimertinib, is an oral bioavailable and covalent/irreversible EGFR inhibitor approved as a cancer treatment in 2017 by both the Food and Drug Administration and the European Commission.

Afatinib (formerly BIBW 2992; BIBW-2992; brand name: Gilotrif), is a potent, covalent/irreversible, and orally bioavailable dual (EGFR/ErbB) receptor tyrosine kinase (RTK) inhibitor with anticancer activity.

PD168393 (PD-168393) is covalent / irreversible, cell-permeable and ATP-competitive EGFR inhibitor with potential anticancer activity.