Drug intelligence / Profile preview

sotorasib + platinum doublet

Development stage
Unknown
Lead developer
Amgen
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Sotorasib + platinum doublet is an investigational combination regimen consisting of the KRAS G12C inhibitor sotorasib (LUMAKRAS) and platinum-doublet chemotherapy (typically carboplatin and pemetrexed). Sotorasib is a small molecule that selectively and irreversibly binds to the cysteine residue of the KRAS G12C mutant protein, locking it in an inactive GDP-bound state to block downstream oncogenic signaling. The addition of platinum-doublet chemotherapy aims to enhance anti-tumor efficacy and delay the emergence of resistance. Developed by Amgen (in collaboration with Astellas BioPharma), this combination is being evaluated in the Phase 3 CodeBreaK 202 trial (NCT05920356) as a first-line treatment for patients with Stage IV or advanced Stage IIIB/C nonsquamous non-small cell lung cancer (NSCLC) that is KRAS G12C-mutant and PD-L1-negative. It has also demonstrated high objective response rates in the frontline setting in the Phase 2 SCARLET trial and Phase 1b CodeBreaK 101 trial.

Other names
sotorasib + carboplatin + pemetrexedsotorasib + pemetrexed + carboplatinsotorasib plus carboplatin and pemetrexedsotorasib plus platinum doubletsotorasib plus platinum doublet chemotherapy
02

Targets

TS (Thymidylate synthase)GART (GAR transformylase)DHFR (Dihydrofolate reductase)DNAKRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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