OnCo
drugsProductPhase 1

MRTX1133

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.

Mirati (now BMS) non-covalent G12D inhibitor; striking regressions in pancreatic PDX models (Nature 2023). Poor oral bioavailability required intravenous dosing in the phase 1/2 trial; development pace slowed after the BMS acquisition, while covalent RAS(ON) competitors advanced.

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MRTX1133
PubChem
Modality
Small-molecule non-covalent KRAS G12D inhibitor
Mechanism
Non-covalent binder to the switch-II pocket of KRAS G12D, inhibiting both ON and OFF states.

Trials

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Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
MRTX1133
intervention: MRTX1133
Open on ClinicalTrials.gov →

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Latest papers

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Literature trend63 papers in the last 12 months+37% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this drug: (TITLE:"MRTX1133" OR ABSTRACT:"MRTX1133") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about MRTX1133, not a curated reading list.

Connected

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