索托拉西布 sotorasib

Drug Class

KRAS G12C inhibitor

Mechanism

Inhibits KRAS G12C by covalently and irreversibly binding to the unique cysteine residue in the inactive GDP-bound state, locking the protein in the inactive state and blocking downstream oncogenic signaling.

Approved Indication

Treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) who have received at least one prior systemic therapy.

What This Means For Patients

Sotorasib (Lumakras/Lumykras) is a first-in-class targeted KRAS G12C inhibitor approved by the FDA and EMA for patients with pretreated advanced non-small cell lung cancer carrying this mutation. It works by locking the mutated protein in an inactive state to halt tumor growth. Under special import rules, eligible patients can access this treatment in the Boao Lecheng pilot zone.

Regulatory Approvals

• FDA — approved (2021) — label
• EMA — approved (2022) — source

Pivotal Clinical Evidence

• CodeBreaK 100 — Skoulidis et al., N Engl J Med 2021 (NCT03600883) — DOI

Sources

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214665s000lbl.pdf
• https://www.ema.europa.eu/en/medicines/human/EPAR/lumykras