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. Author manuscript; available in PMC: 2022 Sep 1.
Published in final edited form as: Cancer Discov. 2022 Mar 1;12(3):625–643. doi: 10.1158/2159-8290.CD-21-0922

Table 1:

Clinical Trials Targeting KEAP1/NRF2 Mutant Tumors

Trial Drug Study Type Inclusion Intervention Primary Outcomes
KEAPSAKE
NCT04265534
CB-839 (Telaglenastat) Phase 2 Randomized placebo controlled Metastatic NSCLC with mutation in KEAP1, NRF2, or LKB1 Pembrolizumab + Carboplatin + Pemetrexed +/− CB-839 Progression Free Survival Safety and Tolerability Dosing
BeGIN
NCT03872427
CB-839 Phase 2 Open label single arm Advanced tumor with mutation in NF1, KEAP1, or LKB1 CB-839 Best Overall Response Rate
NCT04471415 DRP-104 (Sirpiglenastat) Phase 1 and 2a Dose Escalation Dose expansion Advanced NSCLC with mutation in KEAP1, NRF2, or LKB1 and already received 1st line therapy DRP-104 + Atezolizumab Maximum tolerated dose Area under plasma concentration Cmax of DRP-104
NCT02417701 Sapanisertib Phase 2 Randomized open label Stage IV or recurrent SCC with KEAP1 or NRF2 mutation Docetaxel + Sapanisertib Progression Free Survival