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. 2024 May 20;9:132. doi: 10.1038/s41392-024-01823-2

Table 1.

The FDA-approved and clinically developed RAS inhibitors in cancer therapies

Target Drug Highest Phase Indications Company/Identifier Status
Farnesyltr-ansferase Tipifarnib Approved Head and neck squamous cell carcinoma harboring HRAS mutations who have progressed following platinum-containing chemotherapy Kura Oncology /
Lonafarnib (SCH66336) Approved Hutchinson-Gilford progeria syndrome and progeroid laminopathies Merck & Co /
III Carcinoma, non-small cell lung, metastases, neoplasm NCT00050336 Terminated
III Myelodysplastic syndromes, leukemia, myelomonocytic, chronic, myelodysplasia, myelomonocytic NCT00109538 Terminated
Salirasib II Non-small cell lung cancer NCT00531401 Completed
SOS BI-1701963 II Advanced solid tumors, KRASG12C mutation NCT04185883 Recruiting
MRTX0902 I/II Solid tumor, advanced solid tumor, non-small cell lung cancer, colorectal cancer NCT05578092 Recruiting
SHP2 RMC-4630 II Non-small cell lung cancer NCT05054725 Active, not recruiting
I/II Solid tumor NCT03989115 Completed
I/II Advanced solid tumors, KRASG12C mutation NCT04185883 Recruiting
I/II Metastatic neoplasm NCT04418661 Active, not recruiting
TNO155 I/II KRASG12C mutant solid tumors, non-small cell lung, carcinoma, colorectal, lung cancer, pulmonary cancer NCT04699188 Recruiting
I/II Advanced cancer, metastatic cancer, malignant neoplastic disease NCT04330664 Active, not recruiting
I/II Advanced solid tumors, KRASG12C mutation NCT04185883 Recruiting
RLY-1971 I Advanced solid tumors, metastatic solid tumors NCT05487235 Recruiting
I Solid tumor, unspecified, adult NCT04252339 Completed
I Colorectal cancer, non-small cell lung cancer NCT05954871 Recruiting
KRASG12C Adagrasib (MRTX849) Approved Solid tumors harboring KRASG12C oncogenic driver mutation, including non-small cell lung cancer and colorectal cancer Mirati Therapeutics /
Sotorasib (AMG510) Approved KRASG12C-mutated locally advanced or metastatic non-small cell lung cancer Amgen /
JNJ-74699157 (ARS-3248) I Neoplasms, advanced solid tumors, non-small cell lung cancer, colorectal cancer NCT04006301 Completed
Divarasib (GDC-6036) III Non-small cell lung cancer NCT03178552 Recruiting
D-1553 II Non-small cell lung cancer NCT05383898 Recruiting
II Non-small cell lung cancer NCT05492045 Recruiting
II Solid tumor, non-small cell lung cancer, colorectal cancer NCT04585035 Recruiting
II Solid tumor NCT05379946 Not yet recruiting
JDQ443 III Non-small cell lung cancer NCT05132075 Recruiting
RMC-6291 I Non-small cell lung cancer, colorectal cancer, pancreatic ductal adenocarcinoma, advanced solid tumor NCT05462717 Recruiting
Non-KRASG12C MRTX1133 I/II Solid tumor, advanced solid tumor, non-small cell lung cancer, colorectal cancer, pancreatic adenocarcinoma NCT05737706 Recruiting
RMC-6236 I Non-small cell lung cancer, colorectal cancer, pancreatic ductal adenocarcinoma, advanced solid tumors NCT05379985 Recruiting
siRNA strategies KRASG12D iExosomes I KRASG12D metastatic pancreatic adenocarcinoma, pancreatic ductal adenocarcinoma NCT03608631 Recruiting
Antisense oligonucleotide AZD4785 I Non-small cell lung cancer, advanced solid tumors NCT03101839 Completed
RAS analog Rigosertib III Metastatic pancreatic adenocarcinoma NCT01360853 Completed
III Myelodysplastic syndromes, chronic myelomonocytic leukemia NCT01928537 Completed
III Myelodysplastic syndromes, chronic myelomonocytic leukemia NCT01241500 Completed
Cancer vaccines mRNA-5671 I

Non-small cell lung cancer

pancreatic cancer,

colorectal cancer

NCT03948763 Completed
Antibody NS1 II

Hematologic malignancy,

acute leukemia,

acute myeloid leukemia,

acute lymphoblastic

NCT05735717 Recruiting

Source: All the information is derived from ClinicalTrials.gov (https://www.clinicaltrials.gov) and the United States Food and Drug Administration.gov (https://www.fda.gov/)