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. Author manuscript; available in PMC: 2021 Feb 1.
Published in final edited form as: Nat Rev Drug Discov. 2020 Jun 11;19(8):533–552. doi: 10.1038/s41573-020-0068-6

Table 1 |.

Single-agent inhibitors in clinical development

Drug Biomarker Disease setting Study phase ClinicalTrials.gov registration
KRAS-G12C inhibitors
AMG 510 KRASG12C mutation Advanced solid tumours I/II NCT03600883
MRTX849 KRASG12C mutation Advanced solid tumours I/II NCT03785249
JNJ-74699157 (ARS-3248) KRASG12C mutation Advanced solid tumours I NCT04006301
LY3499446 KRASG12C mutation Advanced solid tumours I/II NCT04165031
SOS inhibitors
BI-1701963 KRAS mutations Advanced or metastatic solid tumours I NCT04111458
SHP2 inhibitors
RMC-4630 Mutations that hyperactivate the MAPK pathway Relapsed or refractory solid tumours I NCT03634982
TNO155 EGFR or KRASG12C mutations Advanced solid tumours I NCT03114319
Farnesyltransferase inhibitors
Tipifarnib HRAS mutations Thyroid cancer, squamous head and neck cancer and squamous cell carcinoma II NCT02383927
RAF inhibitors
Belvarafenib (HM95573) BRAF, KRAS or NRAS mutations Advanced solid tumours I NCT03118817
LXH-254 MAPK pathway mutation Advanced solid tumours I NCT02607813
MEK inhibitors
Binimetinib (MEK162) NRAS mutation Unresectable or metastatic melanoma III NCT01763164
ERK inhibitors
KO-947 BRAF, KRAS, NRAS or HRAS mutation Advanced solid tumours I NCT03051035
LY-3214996 BRAF or NRAS mutations Metastatic melanoma and NSCLC I NCT02857270
Adoptive cell therapies
Anti-RAS-G12D mTCR HLA-A11:01 RASG12D mutation Advanced solid tumours I/II NCT03745326
Anti-RAS-G12V mTCR HLA-A11:01 RASG12V mutation Advanced solid tumours I/II NCT03190941
Cancer vaccines
mRNA-5671 HLA-A11:01 and/or HLA-C08:02; KRASG12C, KRASG12D, KRASG12V or KRASG13D mutation NSCLC, non-MSI-H CRC, PDAC I NCT03948763

CRC, colorectal cancer; HLA, human leukocyte antigen; MSI-H, microsatellite instability-high; mTCR, murine T cell receptor; NSCLC, non-small-cell lung cancer; PDAC, pancreatic ductal adenocarcinoma; SOS, Son of Sevenless.