INDICATION

LUMAKRAS is indicated for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy.

This indication is approved under accelerated approval based on overall response rate (ORR) and duration of response (DOR). Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

LUMAKRAS • loo-ma-krass
SOTORASIB • soh-toh-rass-ib
About KRAS G12C
Prevalence
KRASG12C inhibition
Efficacy
CodeBreaK 100
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Prevalence

~ 13% of patients with non-squamous NSCLC have an actionable KRAS G12C mutation1

Prevalence of oncogenic drivers in non-squamous NSCLC1,*

Prevalence of oncogenic drivers in non-squamous NSCLC

  • KRAS mutations—including KRAS G12C—do not typically overlap with other driver mutations and are truncal in nature2
  • Nearly 45% of patients with NSCLC have an actionable oncogenic driver with KRAS G12C and the other 9 actionable biomarkers1,3,†

Learn about testing for KRAS G12C

*Molecular alteration prevalence can vary slightly between different datasets and studies. Values in graph based on approximate molecular alteration frequencies from the AACR genie version 12.0 dataset (N=19,777). Participating institutions include academic centers in Western countries. This graph only includes alterations predictive of response to an FDA-approved drug in locally advanced or metastatic NSCLC.1

†As of December 1, 2022.

AACR, American Association for Cancer Research; ALK, anaplastic lymphoma kinase; BRAF, v-Raf murine sarcoma viral oncogene homolog B; EGFR, epidermal growth factor receptor; HER2, human epidermal growth factor receptor 2; KRAS, Kirsten rat sarcoma viral oncogene homolog; MET, mesenchymal epithelial transition; NGS, next-generation sequencing; NSCLC, non-small cell lung cancer; NTRK, neurotrophic-tropomyosin receptor kinase; RET, rearranged during transfection; ROS1, rearrangement of the receptor tyrosine kinase 1.

KRASG12C inhibition

LUMAKRAS is not a chemotherapy, immunotherapy, or TKI. It’s a highly selective‡ oral inhibitor designed specifically for patients with a KRAS G12C mutation4

KRASG12C-GDP
INACTIVE
KRAS G12C mutation KRAS G12C mutation
LUMAKRAS is designed to inactivate the mutant protein without affecting wild-type KRAS4

LUMAKRAS is specifically designed for patients with a KRAS G12C mutation.
Consider testing all eligible patients with NSCLC for KRAS G12C4,5

‡Cysteine proteome analysis of 6,451 peptides showed sotorasib only covalently engages with Cys12 of KRASG12C. Preclinical studies in 22 cell lines and xenograft models demonstrated that sotorasib does not inhibit KRAS wild-type or non–KRAS G12C lines/tumors.5

GDP, guanosine diphosphate; TKI, tyrosine kinase inhibitor.

Are you ready to test for KRAS G12C?

IMPORTANT SAFETY INFORMATION

Hepatotoxicity

  • LUMAKRAS can cause hepatotoxicity, which may lead to drug-induced liver injury and hepatitis.
  • Among 357 patients who received LUMAKRAS in CodeBreaK 100, hepatotoxicity occurred in 1.7% (all grades) and 1.4% (Grade 3). A total of 18% of patients who received LUMAKRAS had increased alanine aminotransferase (ALT)/increased aspartate aminotransferase (AST); 6% were Grade 3 and 0.6% were Grade 4. In addition to dose interruption or reduction, 5% of patients received corticosteroids for the treatment of hepatotoxicity.
  • Monitor liver function tests (ALT, AST, and total bilirubin) prior to the start of LUMAKRAS, every 3 weeks for the first 3 months of treatment, then once a month or as clinically indicated, with more frequent testing in patients who develop transaminase and/or bilirubin elevations.
  • Withhold, dose reduce or permanently discontinue LUMAKRAS based on severity of adverse reaction.

Interstitial Lung Disease (ILD)/Pneumonitis

  • LUMAKRAS can cause ILD/pneumonitis that can be fatal. Among 357 patients who received LUMAKRAS in CodeBreaK 100 ILD/pneumonitis occurred in 0.8% of patients, all cases were Grade 3 or 4 at onset, and 1 case was fatal. LUMAKRAS was discontinued due to ILD/pneumonitis in 0.6% of patients.
  • Monitor patients for new or worsening pulmonary symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough, fever). Immediately withhold LUMAKRAS in patients with suspected ILD/pneumonitis and permanently discontinue LUMAKRAS if no other potential causes of ILD/pneumonitis are identified.

Most common adverse reactions

  • The most common adverse reactions ≥ 20% were diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough.

Drug interactions

  • Advise patients to inform their healthcare provider of all concomitant medications, including prescription medicines, over‑the‑counter drugs, vitamins, dietary and herbal products.
  • Inform patients to avoid proton pump inhibitors and H2 receptor antagonists while taking LUMAKRAS.
  • If coadministration with an acid-reducing agent cannot be avoided, inform patients to take LUMAKRAS 4 hours before or 10 hours after a locally acting antacid.

INDICATION

LUMAKRAS is indicated for the treatment of adult patients with KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC), as determined by an FDA‑approved test, who have received at least one prior systemic therapy.

This indication is approved under accelerated approval based on overall response rate (ORR) and duration of response (DOR). Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).


Please see full Prescribing Information.

Important Safety Information

Hepatotoxicity

  • LUMAKRAS can cause hepatotoxicity, which may lead to drug-induced liver injury and hepatitis.
  • Among 357 patients who received LUMAKRAS in CodeBreaK 100, hepatotoxicity occurred in 1.7% (all grades) and 1.4% (Grade 3). A total of 18% of patients who received LUMAKRAS had increased alanine aminotransferase (ALT)/increased aspartate aminotransferase (AST); 6% were Grade 3 and 0.6% were Grade 4. In addition to dose interruption or reduction, 5% of patients received corticosteroids for the treatment of hepatotoxicity.
  • Monitor liver function tests (ALT, AST, and total bilirubin) prior to the start of LUMAKRAS, every 3 weeks for the first 3 months of treatment, then once a month or as clinically indicated, with more frequent testing in patients who develop transaminase and/or bilirubin elevations.
  • Withhold, dose reduce or permanently discontinue LUMAKRAS based on severity of adverse reaction.