Table 1 The FDA-approved and clinically developed RAS inhibitors in cancer therapies

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, KRAS^G12C 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, KRAS^G12C mutation

NCT04185883

Recruiting

I/II

Metastatic neoplasm

NCT04418661

Active, not recruiting

TNO155

I/II

KRAS^G12C 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, KRAS^G12C 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

KRAS^G12C

Adagrasib (MRTX849)

Approved

Solid tumors harboring KRAS^G12C oncogenic driver mutation, including non-small cell lung cancer and colorectal cancer

Mirati Therapeutics

/

Sotorasib (AMG510)

Approved

KRAS^G12C-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-KRAS^G12C

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

KRAS^G12D iExosomes

I

KRAS^G12D 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