MRTX1133

MRTX1133
Clinical data
Drug class	Antineoplastic agents
ATC code	L01XX77 (WHO) ;
Identifiers
	IUPAC name 4-(4-(3,8-Diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-(((2R,7aS)-2-fluorohexahydro-1H-pyrrolizin-7a-yl)methoxy)pyrido[4,3-d]pyrimidin-7-yl)-5-ethynyl-6-fluoronaphthalen-2-ol;
CAS Number	2621928-55-8;
PubChem CID	156124857;
ChemSpider	114876735;
UNII	DU32DM9CHD;
ChEMBL	ChEMBL4858364;
PDB ligand	6IC (PDBe, RCSB PDB);
Chemical and physical data
Formula	C33H31F3N6O2
Molar mass	600.646 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C#CC1=C(C=CC2=CC(=CC(=C21)C3=NC=C4C(=C3F)N=C(N=C4N5CC6CCC(C5)N6)OC[C@@]78CCCN7C[C@@H](C8)F)O)F;
	InChI InChI=InChI=1S/C33H31F3N6O2/c1-2-23-26(35)7-4-18-10-22(43)11-24(27(18)23)29-28(36)30-25(13-37-29)31(41-15-20-5-6-21(16-41)38-20)40-32(39-30)44-17-33-8-3-9-42(33)14-19(34)12-33/h1,4,7,10-11,13,19-21,38,43H,3,5-6,8-9,12,14-17H2/t19-,20?,21?,33+/m1/s1; Key:SCLLZBIBSFTLIN-IFMUVJFISA-N;

MRTX1133 is an investigational drug that targets the G12D mutation in KRAS dependent cancers.^[1]^[2] MRTX1133 was in a phase 1/2 clinical trial for the treatment of solid tumors,^[3] however the study was terminated in Q1 2025.^[4] MRTX1133 is considered to be harmful from direct skin or eye exposure other than transient irritation. It may cause irritation of the respiratory system if inhaled.^[5]

References

^ "MRTX 1133". AdisInsight. Springer Nature Switzerland AG.
^ Zeissig MN, Ashwood LM, Kondrashova O, Sutherland KD (November 2023). "Next batter up! Targeting cancers with KRAS-G12D mutations". Trends in Cancer. 9 (11): 955–967. doi:10.1016/j.trecan.2023.07.010. PMID 37591766.
^ Clinical trial number NCT05737706 for "Study of MRTX1133 in Patients With Advanced Solid Tumors Harboring a KRAS G12D Mutation" at ClinicalTrials.gov
^ "Bristol exits KRAS G12D". ApexOnco. Retrieved 22 June 2025.
^ "MRTX1133 Safety Data Sheet". TargetMol. Retrieved 11 September 2024.

[1] "MRTX 1133". AdisInsight. Springer Nature Switzerland AG.

[Zeissig_2023-2] Zeissig MN, Ashwood LM, Kondrashova O, Sutherland KD (November 2023). "Next batter up! Targeting cancers with KRAS-G12D mutations". Trends in Cancer. 9 (11): 955–967. doi:10.1016/j.trecan.2023.07.010. PMID 37591766.

[3] Clinical trial number NCT05737706 for "Study of MRTX1133 in Patients With Advanced Solid Tumors Harboring a KRAS G12D Mutation" at ClinicalTrials.gov

[4] "Bristol exits KRAS G12D". ApexOnco. Retrieved 22 June 2025.

[5] "MRTX1133 Safety Data Sheet". TargetMol. Retrieved 11 September 2024.

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See also

References