Drug intelligence / Profile preview

jdq443 + ribociclib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

JDQ443 + ribociclib is an investigational oral combination therapy targeting *KRAS^G12C^*-mutant solid tumors, primarily non-small cell lung cancer (NSCLC) and colorectal cancer. **JDQ443** (known as opnurasib) is a covalent, irreversible, small molecule inhibitor that selectively binds to and inhibits KRAS G12C in its inactive GDP-bound state, thereby suppressing oncogenic signaling[1][3]. **Ribociclib** is an oral selective CDK4/6 inhibitor that blocks cell cycle progression by inhibiting cyclin-dependent kinases 4 and 6, which are often dysregulated in cancer. The combination aims to leverage synthetic lethal interaction between KRAS and CDK4/6 pathways, improving outcomes beyond single-agent therapy as demonstrated in preclinical patient-derived xenograft models.

Other names
opnurasib + ribociclibLEE011 + JDQ443
02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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