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

Dosing recommendation

LUMAKRAS™ recommended dose: 960 mg orally, once daily1


  • Treat until disease progression or unacceptable toxicity
Dietary recommendation

LUMAKRAS™ can be taken with or without food1

Dosing schedule

LUMAKRAS™ should be taken at the same time each day1

Packaging Packaging

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

Coadministration with acid-reducing agents1

  • Coadministration of LUMAKRAS™ with gastric acid reducing agents decreased sotorasib concentrations which may reduce the efficacy of sotorasib. Avoid coadministration of LUMAKRAS™ with proton pump inhibitors (PPIs), H2 receptor antagonists, and locally acting antacids. If coadministration with an acid-reducing agent cannot be avoided, administer LUMAKRAS™ 4 hours before or 10 hours after administration of a locally acting antacid

Coadministration with strong CYP3A4 inducers1

  • Coadministration of LUMAKRAS™ with a strong CYP3A4 inducer decreased sotorasib concentrations, which may reduce the efficacy of sotorasib. Avoid coadministration of LUMAKRAS™ with strong CYP3A4 inducers

Coadministration with CYP3A4 substrates1

  • Coadministration of LUMAKRAS™ with a CYP3A4 substrate decreased its plasma concentrations, which may reduce the efficacy of the substrate. Avoid coadministration of LUMAKRAS™ with CYP3A4 sensitive substrates, for which minimal concentration changes may lead to therapeutic failures of the substrate. If coadministration cannot be avoided, increase the sensitive CYP3A4 substrate dosage in accordance with its Prescribing Information

Coadministration with P-glycoprotein (P-gp) substrates1

  • Coadministration of LUMAKRAS™ with a P-gp substrate (digoxin) increased digoxin plasma concentrations, which may increase the adverse reactions of digoxin. Avoid coadministration of LUMAKRAS™ with P-gp substrates, for which minimal concentration changes may lead to serious toxicities. If coadministration cannot be avoided, decrease the P-gp substrate dosage in accordance with its Prescribing Information

Dose modifications

Dose reductions due to an adverse reaction occurred in 5% of patients who received LUMAKRAS™1

  • Dosage interruptions due to an adverse reaction occurred in 34% of patients who received LUMAKRAS™1
Titration

Recommended dose reductions1


  • If adverse reactions occur, a maximum of two dose reductions are permitted2
Starting Dose1
(960 mg)
Oral tablets
First Dose Reduction1
(480 mg)
Oral tablets
Second Dose Reduction1
(240 mg)
Oral tablets
Dosing Table Dosing Table
  • 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.

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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.