Drug intelligence / Profile preview

NXP900 + daraxonrasib

Development stage
Unknown
Lead developer
Nuvectis Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

NXP900 + daraxonrasib is an investigational combination therapy being evaluated for the treatment of pancreatic cancer, specifically RAS-driven pancreatic ductal adenocarcinoma (PDAC). NXP900, developed by Nuvectis Pharma, is an oral, highly selective small-molecule inhibitor of SRC-family kinases (specifically SRC and YES1) that locks the target kinase in its native closed conformation (Type 1.5 inhibitor), blocking both its catalytic and scaffolding functions. Daraxonrasib (RMC-6236, brand name Rasonque), developed by Revolution Medicines, is an oral, multi-selective RAS(ON) inhibitor that acts as a non-degrading molecular glue, binding active RAS-GTP and suppressing downstream RAF-MEK-ERK and PI3K-AKT signaling. The combination is designed to target both the primary RAS driver and the SRC/YES1-mediated bypass resistance pathways. An investigator-sponsored trial (IST) of the combination is planned at two U.S. medical centers.

Other names
daraxonrasib + NXP900eCF506 + daraxonrasibeCF506 + RMC-6236NXP900 + RMC-6236NXP900 + RasonqueRMC-6236 + NXP900
02

Targets

HRAS (H-Ras protein)KRAS (Kirsten rat sarcoma viral oncogene homolog)NRAS (Neuroblastoma RAS viral oncogene homolog)PPIA (Peptidyl-prolyl cis-trans isomerase A)SRC (Proto-oncogene tyrosine-protein kinase Src)YES1 (YES proto-oncogene 1 tyrosine kinase)

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