Drug intelligence / Profile preview

zoldonrasib

Development stage
Phase 3
Lead developer
REVOLUTION Medicines
Modality
Small Molecules
Administration
Oral
01

Overview

Zoldonrasib is an investigational oral small molecule inhibitor that selectively targets the active (GTP-bound) form of KRAS with the G12D mutation. It is a novel "RAS(ON)" tri-complex inhibitor designed to bind and inhibit KRAS G12D in its active conformation, distinguishing it from currently approved KRAS G12C inhibitors that target the inactive state. This mechanism may help delay or prevent resistance by blocking signaling even when upstream pathways are activated. Zoldonrasib has shown promising early antitumor activity and acceptable tolerability in phase 1 clinical trials for patients with advanced solid tumors harboring KRAS G12D mutations—including non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma—who have received at least one prior line of therapy. The most common adverse events are low-grade gastrointestinal symptoms such as nausea, diarrhea, and vomiting; severe toxicities are rare[1][3][4][7].

Brand names
zoldonrasib
Other names
zoldonrasibRMC-9805RMC9805RMC 9805
02

Targets

KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)

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