. 2020 Dec 20;26(3):e454–e472. doi: 10.1002/onco.13590

Table 4.

TKIs approved and under investigation for various genetic driver alterations in non‐small cell lung cancer in 2020

Oncogene driver	Approved agents	Investigational agents
EGFR	Gefitinib, erlotinib ^a , afatinib, dacomitinib ^b , osimertinib ^c	EA1045, JND3229
EGFR exon 20 insertion Uncommon EGFR mutations, e.g., G719X, L861X, S7681V	Afatinib	Mobocertinib, TAS6417, BDTX‐189, DS2087B, CLN081, osimertinib ^d
ALK	Crizotinib ^a , certitinib, alectinib, brigatinib, lorlatinib ^b	Ensartinib ^b
ROS1	Crizotinib ^a , certinib ^b , entrectinib ^c	Repotrectinib, lorlatinib ^d , taletrectinib
RET	Selpercatinib ^b , pralsetinib ^b	Brigatinib ^d , ensartinib ^b
NTRK	Larotrectinib ^b , entrectinib ^b	Taletrectinib
MET	Capmatinib	Crizotinib ^d , tepotinib, savolitinib
BRAF V600E	Dabrafenib plus trametinib	Encorafenib
KRAS G12C	None	AMG 510, MRTX 849
HER2 exon 20 insertions	None	Trastuzumab emtansine ^d trastuzumab deruxtecan ^d mobocertinib, TAS6417, BDTX‐189, DS2087B, DZD9008, osimertinib ^d
NRG1 fusions	None	tarloxotinib, HER3 antibodies

^{^a}

First‐generation TKI with poor CNS penetration.

^{^b}

Second‐generation TKI with good CNS penetration.

^{^c}

Third‐generation TKI with good CNS penetration, leads to resistance mutations like C797s.

^{^d}

Approved for other indications.

^{^e}

Vandetanib, cabozantinib, and lenvatinib are multi‐TKIs approved in other indications.

Abbreviations: CNS, central nervous system; EGFR, epidermal growth factor receptor; HER, human epidermal growth receptor; TKI, tyrosine kinase inhibitor.