Table 1.
Clinical trials of drugs targeting KRAS.
| Therapeutic Family | Clinical Trial | Phase | Drug | Indication | Results |
|---|---|---|---|---|---|
| Pan-RASinh | NCT03114319 | 1 | TNO155 (SHP2i) alone or with nazartinib (EGFRi) | EGFR/KRAS NSCLC, esophageal SCC, H/N SCC, Melanoma | N/A |
| NCT03634982 | 1 | RMC-4630 (SHP2i) | All solid tumors | N/A | |
| NCT04045496 | 1 | JAB-3312 (SHP2i) | All solid tumors | N/A | |
| Pan-RASinh +downstream inh | NCT04111458 | 1 | BI 1701963 (SOS1i) + trametinib (MEKi) | KRAS NSCLC | N/A |
| NCT04916236 | 1 | RMC-4630 (SHP2i) + LY3214996 (ERK1/2i) | KRAS tumors | N/A | |
| Pan- RASinh + IT | NCT04000529 | 1b | TNO155 (SHP2i) + ribociclib (CDK4/6i) or spartalizumab (PD1i) | KRAS NSCLC | N/A |
| Downstream inh | NCT03681483 | 1 | RO5126766 (RAF/MEKi) | KRAS NSCLC | N/A |
| Downstream inh combination | NCT02857270 | 1 | LY3214996 (ERK1/2i) alone or + other drugs | All solid tumors | N/A |
| NCT03284502 | 1b | HM95573 (RAFi) + cobimetinib (MEKi)or cetuximab (EGFRi) | All solid tumors | N/A | |
| NCT03170206 | 1/2 | palbociclib (CDK 4/6i) + binimetinib (MEKi) | KRAS NSCLC | N/A | |
| NCT04620330 | 2 | VS-6766 (RAF/MEKi) + defactinib (FAKi) | G12V or other KRAS NSCLC | N/A | |
| NCT02974725 | 1 | LXH254 (RAFi) + LTT462 (ERK1/2i) or trametinib (MEKi) or ribociclib (CDK4/6i) | KRAS and BRAF tumors | N/A | |
| Downstream inh + Upstream inh | NCT01229150 | 2 | selumetinib (MEKi) + erlotinib (EGFRi) vs selumetinib |
NSCLC | ORR 10% vs 0% OS 21.8 vs 10.5 months |
| NCT02230553 | 1/2 | trametinitb (MEKi) + lapatinib (Erbb1-2i) | KRAS NSCLC | N/A | |
| NCT03704688 | 1/2 | trametinib (MEKi) + poniotinib (VEGFi) | KRAS NSCLC | N/A | |
| NCT04967079 | 1 | trametinib (MEKi) + anlotinib (panRTKi) | KRAS NSCLC | N/A | |
| NCT01859026 | 1/2. | MEK162 (MEKi) + erlotinib | KRAS or EGFR tumors | N/A | |
| NCT04965818 | 1b/2 | futibatinib (FGFRi) + binimetinib (MEKi) | KRAS tumors | N/A | |
| Downstream inh + autophagy inh | NCT04735068 | 2 | binimetinib (MEKi) + hydroxychloroquine | KRAS NSCLC | N/A |
| NCT04892017 | 1 | DCC-3116 (ULK 1/2i) + trametinib (MEKi) | RAS-RAF mutant all solid tumors | N/A | |
| Autophagy inh | NCT03095612 | 1/2 | selinezor (XPO1i) + docetaxel | KRAS NSCLC | N/A |
| Downstream inh + IT | NCT02779751 | 1b | pembrolizumab (PD1i) + abemaciclib (CDKi) | KRAS non squamous NSCLC, sq-NSCLC and Luminal-like breast cancer | N/A |
| NCT02779751 | 1b | pembrolizumab (PDL1i) + abemaciclib (CDKi) | KRAS non squamous NSCLC, sq-NSCLC and Luminal-like breast cancer | N/A | |
| NCT03299088 | 1b | pembrolizumab (PD1i) + trametinib (MEKi) | KRAS NSCLC | N/A | |
| Downstream inh + ChT | NCT03990077 | 1 | HL-085 (MEKi) + docetaxel | KRAS NSCLC | N/A |
| mRNA vaccine | NCT03948763 | 1 | V941 (mRNA vaccine) | All solid tumors | N/A |
| Metabolic modifier | NCT03808558 | 2 | TVB-2640 (FASNi) | KRAS NSCLC | N/A |
Inh/i, inhibitors; IT, immunotherapy; ChT, chemotherapy; NSCLC, non-small cell lung cancer; SCC, squamous cell carcinoma; ORR, overall response rate; N/A, non-assessed.