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).

Dosing

LUMAKRAS is a once-daily oral therapy1

LUMAKRAS® suggested dosing recommendation

LUMAKRAS recommended dose: 960 mg orally, once daily1


  • Treat until disease progression or unacceptable toxicity
LUMAKRAS® can be taken with or without food

LUMAKRAS can be taken with or without food1

Take LUMAKRAS® at the same time each day

LUMAKRAS should be taken at the same time each day1

LUMAKRAS® pill bottle LUMAKRAS® pill bottle

LUMAKRAS is supplied in one bottle containing 240 tablets.1

Please see dosing modifications below.

Administration to patients who have difficulty swallowing solids1

  • Disperse tablets in 120 mL (4 ounces) of non-carbonated, room-temperature water without crushing. No other liquids should be used. Stir until tablets are dispersed into small pieces (the tablets will not completely dissolve) and drink immediately or within 2 hours. The appearance of the mixture may range from pale yellow to bright yellow. Swallow the tablet dispersion. Do not chew pieces of the tablet. Rinse the container with an additional 120 mL (4 ounces) of water and drink. If the mixture is not consumed immediately, stir the mixture again to ensure that tablets are dispersed

Missed dose or vomiting1

  • If a dose of LUMAKRAS is missed by more than 6 hours, take the next dose as prescribed the next day. Do not take 2 doses at the same time to make up for the missed dose
  • If vomiting occurs after taking LUMAKRAS, do not take an additional dose. Take the next dose as prescribed the next day

LUMAKRAS and other drugs1

chart highlighting effects of other drugs on LUMAKRAS chart highlighting effects of other drugs on LUMAKRAS

Dose modifications

Dose reductions due to an adverse reaction occurred in 5% of patients who received LUMAKRAS1

  • Dosage interruptions due to an adverse reaction occurred in 34% of patients who received LUMAKRAS1
Titration

Recommended dose reductions1


  • If adverse reactions occur, a maximum of two dose reductions are permitted2
Starting Dose1
(960 mg)
LUMAKRAS® recommended dosing reductions over time with a starting dose of 960mg
First Dose Reduction1
(480 mg)
LUMAKRAS® recommended dosing reductions over time with a starting dose of 960mg
Second Dose Reduction1
(240 mg)
LUMAKRAS® recommended dosing reductions over time with a starting dose of 960mg
LUMAKRAS® adverse reactions LUMAKRAS® adverse reactions
  • LUMAKRAS should be discontinued if patients are unable to tolerate the minimum dose of 240 mg once daily1
  • No clinically meaningful differences in the pharmacokinetics of LUMAKRAS were observed based on age, sex, race, body weight, line of therapy, and ECOG PS1
  • No dose adjustment is required on the basis of age1

ALT, alanine transaminase; AST, aspartate transaminase; ECOG PS, Eastern Cooperative Oncology Group performance status; ILD, interstitial lung disease; ULN, upper limit of normal.

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.