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Drugs against the most common cancer gene, considered impossible to target until sotorasib in 2021.
Covalent G12C inhibitors (sotorasib, adagrasib, divarasib, olomorasib) work in NSCLC and, with cetuximab, in colorectal cancer. Non-covalent G12D inhibitors (zoldonrasib, MRTX1133) and pan-RAS(ON) tri-complex inhibitors (daraxonrasib RMC-6236, in phase 3 RASolute 302 in second-line pancreatic cancer) aim at pancreatic cancer, where KRAS is near-universal. Degraders and vaccines (ELI-002) follow.
Inhibitors bind covalently to the mutant cysteine in the switch-II pocket (G12C), or form a cyclophilin-A-mediated tri-complex that blocks effector binding (RAS(ON) inhibitors).
Adagrasib was the second KRAS G12C inhibitor, with a long half-life and brain penetration, and is approved in lung and colorectal cancer.
The first drug that blocks all active RAS variants, approved by the FDA in August 2026 for metastatic pancreatic cancer, where KRAS drives 90% of tumours.
Divarasib is Roche's KRAS G12C pill, the first to beat the two approved KRAS drugs head-to-head (July 2026).
A next-generation KRAS G12C drug that hits the active form of the protein, from the same company as daraxonrasib.
Fulzerasib was the first KRAS G12C-blocking pill approved in China, for lung cancers carrying that mutation after earlier treatment.
Garsorasib is InventisBio's KRAS G12C-blocking pill, approved in China in 2024 for previously treated lung cancer with that mutation.
Glecirasib is Jacobio's KRAS G12C inhibitor, approved in China in 2024 for previously treated non-small cell lung cancer with that mutation, and in a phase 3 trial against docetaxel.
MRTX1133 was the first potent chemical tool against KRAS G12D, and proved the mutation could be drugged even though it lacks the reactive handle G12C has.
Olomorasib is Lilly's KRAS G12C pill, designed to combine safely with immunotherapy in first-line lung cancer.
Sotorasib (Lumakras) was the first drug to hit KRAS, approved in 2021 after four decades of failure.
The first drug aimed specifically at KRAS G12D, the single most common mutation in pancreatic cancer. Early combination data in 2026 showed half of previously treated patients responding.
One of the most cited trial reports Europe PMC returns for Daraxonrasib in Pancreatic ductal adenocarcinoma, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
The mechanism that let one drug address G12D, G12V and G12R together, which is why the RASolute 302 trial could enrol unselected pancreatic cancer and nearly double survival.
Sotorasib is a guideline-listed later-line option for the 1 to 2 percent of pancreatic cancers with KRAS G12C, and the proof that KRAS in pancreatic cancer is druggable; the larger opportunity lies with inhibitors of G12D and pan-RAS drugs.
Patients with KRAS G12C lung cancer that has progressed after chemo-immunotherapy can take an oral KRAS inhibitor instead of docetaxel and gain a somewhat longer time to progression with fewer severe side effects, but should understand that most tumours become resistant within a year and that survival is not improved. KRAS G12C testing is worthwhile, but first-generation inhibitors are a step rather than a cure; combinations and next-generation inhibitors are the active research fronts.
Patients with metastatic colorectal cancer carrying a KRAS G12C mutation (about 3-4% of cases) who have exhausted standard chemotherapy now have a targeted option that works far better than trifluridine-tipiracil or regorafenib. The higher sotorasib dose is clearly superior, and the EGFR antibody is essential because KRAS inhibition alone has little effect in bowel cancer. Responses are still modest and short-lived compared with EGFR or ALK inhibitors in lung cancer.
Adagrasib joins sotorasib as a later-line option for KRAS G12C pancreatic cancer in guidelines; both drugs are the template for the G12D and pan-RAS inhibitors now in pancreatic trials.
Adagrasib plus cetuximab is an approved option for previously treated KRAS G12C colorectal cancer, alongside sotorasib plus panitumumab; monotherapy is not enough because EGFR signalling reactivates the pathway.
It defines the population the G12C inhibitors address and sets the baseline against which CodeBreaK 300 and KRYSTAL-1 are read.
Query for this technology: (TITLE:"KRAS inhibitor" OR ABSTRACT:"KRAS inhibitor" OR TITLE:"KRAS G12C" OR ABSTRACT:"KRAS G12C" OR TITLE:"KRAS G12D" OR ABSTRACT:"KRAS G12D" OR TITLE:"pan-RAS inhibitor" OR ABSTRACT:"pan-RAS inhibitor"). Results are unfiltered search hits about KRAS & RAS inhibitors, not a curated reading list.
Shares KRAS G12C inhibitor + anti-EGFR antibody (colorectal), Quanta Therapeutics, KRAS G12C metastatic colorectal cancer: specific features of a new emerging target population, KRYSTAL-1: adagrasib with or without cetuximab in KRAS G12C-mutated colorectal cancer.
Shares KRAS G12C metastatic colorectal cancer: specific features of a new emerging target population, KRYSTAL-1: adagrasib in advanced solid tumours harbouring a KRAS G12C mutation, including pancreatic cancer, KRYSTAL-1: adagrasib with or without cetuximab in KRAS G12C-mutated colorectal cancer, CodeBreaK 100: sotorasib in KRAS p.G12C-mutated advanced pancreatic cancer.
Shares A Rollover Study Evaluating Sotorasib With or Without Panitumumab in Participants With KRAS p.G12C Mutation, Study of Sotorasib, Panitumumab and FOLFIRI Versus FOLFIRI With or Without Bevacizumab-awwb in Treatment-naïve Participants With Metastatic Colorectal, Pre-operative Targeted Treatments in Molecularly Selected Resectable Colorectal Cancer (UNICORN), CodeBreaK 300.
Shares KRYSTAL-1: adagrasib in advanced solid tumours harbouring a KRAS G12C mutation, including pancreatic cancer, CodeBreaK 100 (pancreatic cancer cohort), KRAS mutation subtypes (G12C, G12D, G12V), Adagrasib.
Shares A Phase II Study Evaluating JAB-21822 Monotherapy in Adult Patients With Pancreatic Cancer and Other Solid Tumors Harboring the KRAS p.G12C Mutation., A Study of JAB-21822 in Adult Patients With Advanced Solid Tumors Harboring KRAS p.G12C Mutation in China, JAB-21822 in Combination With Cetuximab in Patients With Advanced CRC and Other Solid Tumors With KRAS G12C Mutation, A Study of JAB-21822 in Advanced or Metastatic NSCLC With KRAS p.G12C and STK11 Co-mutation and Wild-type KEAP1.
Shares Frank McCormick, Ostrem and Shokat: the hidden pocket that made KRAS G12C druggable, KRAS roadmap: undruggable → G12C → pan-RAS, KRAS mutation subtypes (G12C, G12D, G12V).
Shares IBI351 Plus Cetuximab β in Untreated Advanced Non-small Cell Lung Cancer With KRAS G12C Mutation, JAB-21822 in Combination With Cetuximab in Patients With Advanced CRC and Other Solid Tumors With KRAS G12C Mutation, A Solid Tumor Study for Long Term Treatment of Cancer Patients Who Participated in Adagrasib Studies, A Multicenter Phase 1b/2 Study of Adagrasib, Cetuximab, and Cemiplimab for Metastatic Colorectal Cancer Harboring KRAS G12C Mutations.
Shares Adagrasib, Daraxonrasib, KRAS G12C-mutant pancreatic ductal adenocarcinoma, Sotorasib.