|All Grades (%)||Grades 3 to 4 (%)|
|Respiratory, thoracic, and mediastinal disorders|
|Musculoskeletal and connective tissue disorders|
|General disorders and administration site conditions|
|Metabolism and nutrition disorders|
|Infections and infestations|
|Skin and subcutaneous tissue disorders|
*Grading defined by NCI CTCAE version 5.0.
†Abdominal pain includes abdominal pain, abdominal pain upper, abdominal pain lower.1
‡Hepatotoxicity includes alanine aminotransferase increased, aspartate aminotransferase increased, blood bilirubin increased, drug-induced liver injury, hepatitis, hepatotoxicity, liver function test increased, transaminases increased.1
§Cough includes cough, productive cough, and upper-airway cough syndrome.1
**Dyspnea includes dyspnea and dyspnea exertional.1
††Musculoskeletal pain includes back pain, bone pain, musculoskeletal chest pain, musculoskeletal discomfort, musculoskeletal pain, myalgia, neck pain, non-cardiac chest pain, and pain in extremity.1
‡‡Fatigue includes fatigue and asthenia.1
§§Edema includes generalized edema, localized edema, edema, edema peripheral, periorbital edema, and testicular edema.1
***Pneumonia includes pneumonia, pneumonia aspiration, pneumonia bacterial, and pneumonia staphylococcal.1
†††Rash includes dermatitis, dermatitis acneiform, rash, rash-maculopapular, rash pustular.1
Use of anti-emetic and anti-diarrheal medications in CodeBreaK 100:2
Grade 5 adverse reactions occurred in 3.4% of patients who received LUMAKRAS due to respiratory failure (0.8%), pneumonitis (0.4%), cardiac arrest (0.4%), cardiac failure (0.4%), gastric ulcer (0.4%), and pneumonia (0.4%)
Adverse reactions resulting in permanent discontinuation of LUMAKRAS in ≥ 2% of patients included hepatotoxicity (4.9%)
5% of patients experienced a dose reduction due to an adverse reaction
34% of patients experienced a dosage interruption due to an adverse reaction
|Warnings and precautions||Monitoring and dose modification||Relevant clinical data|
|Interstitial Lung Disease (ILD)/Pneumonitis||
|No QTc prolongation||
Per the USPI cardiac electrophysiology section in Pharmacodynamics, at the approved recommended dosage, LUMAKRAS does not cause large mean increases in the QTc interval (> 20 msec).
The LUMAKRAS USPI does not contain any requirements to monitor ECGs and electrolytes.
|No gastrointestinal warnings and precautions||
At the approved recommended dosage, LUMAKRAS USPI does not include a warnings and precautions section on severe gastrointestinal adverse reactions.
The most common adverse reactions (≥ 20%) were diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough.
The most common adverse reactions ≥ 20% were diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough1
ALT, alanine transaminase; AR, adverse reaction; AST, aspartate transaminase; ECG, electrocardiogram; KRAS, Kirsten rat sarcoma viral oncogene homolog; NCI CTCAE, National Cancer Institute Common Terminology Criteria for Adverse Events; NSCLC, non-small cell lung cancer; QTc, QT corrected for heart rate; USPI, United States Prescribing Information.
|Grades 1 to 4 (%)||Grades 3 to 4 (%)|
|Increased aspartate aminotransferase||39||9|
|Increased alanine aminotransferase||38||11|
|Increased alkaline phosphatase||33||2.5|
|Increased urine protein||29||3.9|
|Increased activated partial thromboplastin time||23||1.5|
‡‡‡N=number of patients who had at least one on-study assessment for the parameter of interest.1
Interstitial Lung Disease (ILD)/Pneumonitis
Most common adverse reactions
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.