AC480 (also known as BMS-599626) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1/2 (human epidermal growth factor receptors) with potential anticancer activity.

Mobocertinib (TAK-788; AP-32788; Exkivity), a drug used for the treatment of non-small cell lung cancer (NSCLC), is a novel, highly potent, irreversible and orally bioavailable inhibitor of EGFR and HER2 oncogenic mutants (e.g. exon 20 insertions), and exhibits high selectivity over WT EGFR.

Zorifertinib (formerly AZD3759; AZD-3759; zorifertinibum) is a novel, potent, orally bioavailable, CNS (central nervous system)-penetrant EGFR (epidermal growth factor receptor) inhibitor with potential antitumor activity.

Pelitinib (formerly EKB569; WAY-EKB569; WAY-172569), a 3-cyanoquinoline analog, is an irreversible/covalent EGFR inhibitor with potential antineoplastic activity.

Tyrphostin-9 (also named as Malonoben; SF-6847; RG-50872; AG-17; GCP-5126; NSC-242557) is a novel and potent epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity.

Afatinib dimaleate (the maleate salt form of Afatinib, also know as BIBW-2992; BIBW2992) is a potent, covalent/irreversible, and orally bioavailable dual EGFR/HER2 receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.

WZ4002 (WZ-4002) is a covalent/irreversible and mutant-selective EGFR (e.g. L858R/T790M) inhibitor with potential antitumor activity.

Varlitinib (formerly also known as ARRY543; ARRY-334543; ASLAN001) is a novel, potent, orally bioavailable, selective and reversible ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with potential antitumor activity.

Dacomitinib (formerly aslo known as PF299804, PF299; trade name: Vizimpro) is an orally bioavailable, highly selective, irreversible/covalent, 2nd generation pan-ErbB inhibitor, mostly to EGFR, with IC50 values of 6 nM, 45.7 nM and 73.7 nM for inhibiting EGFR, ERBB2, and ERBB4, respectively in cell-free assays.

Nazartinib (formerly known as EGF816, NVS-816) is a novel, covalent/irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.