^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

MRTX0902

i
Other names: MRTX0902
Associations
Company:
BMS
Drug class:
SOS1 inhibitor
Associations
25d
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading. (PubMed, Mol Cancer Ther)
MRTX0902 augmented the antitumor activity of the KRAS G12C inhibitor adagrasib when dosed in combination in eight out of twelve KRAS G12C-mutant human non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) xenograft models. Lastly, combined vertical inhibition of RTK/MAPK pathway signaling by MRTX0902 with inhibitors of EGFR or RAF/MEK led to greater downregulation of pathway signaling and improved antitumor responses in KRAS-MAPK pathway-mutant models. These studies demonstrate the potential clinical application of dual inhibition of SOS1 and KRAS G12C and additional SOS1 combination strategies that will aide in the understanding of SOS1 and RTK/MAPK biology in targeted cancer therapy.
Journal
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • PTEN (Phosphatase and tensin homolog) • NF1 (Neurofibromin 1)
|
KRAS mutation
|
Krazati (adagrasib) • MRTX0902
over1year
A Phase 1/2 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (clinicaltrials.gov)
P1/2, N=225, Recruiting, Mirati Therapeutics Inc. | Not yet recruiting --> Recruiting
Enrollment open • Metastases
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
|
KRAS mutation • EGFR mutation • KRAS G12C • NF1 mutation • KRAS G12
|
Krazati (adagrasib) • MRTX0902
over1year
New P1/2 trial • Metastases
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
|
KRAS mutation • EGFR mutation • KRAS G12C • NF1 mutation • KRAS G12
|
Krazati (adagrasib) • MRTX0902