Active Ingredient: Adagrasib
Adagrasib as monotherapy is indicated for the treatment of adult patients with advanced non-small cell lung cancer (NSCLC) with KRAS G12C mutation and disease progression after at least one prior systemic therapy.
For this indication, competent medicine agencies globally authorize below treatments:
For:
Oral, 600 milligrams adagrasib, 2 times daily.
The recommended dose of adagrasib is 600 mg twice daily.
Treatment with adagrasib is recommended until disease progression or unacceptable toxicity.
Patients should be advised that if less than 4 hours have passed since the scheduled time of dosing, the patient should take the dose as normal. If a dose is missed by more than 4 hours, the dose should be skipped, and dosing should resume at the next scheduled dose. If vomiting occurs after taking a dose, patients should be advised not to take an additional dose. The next dose should be taken as prescribed.
The recommended dose reduction levels for the management of adverse reactions are outlined in Table 1.
Table 1. Recommended dose reduction levels for adverse reactions:
| Dose reduction level | Reduced dosage |
|---|---|
| First dose reduction | Two 200 mg tablets (400 mg) twice daily |
| Second dose reduction | Three 200 mg tablets (600 mg) once daily |
The recommended dose modifications for adverse reactions are provided in Table 2. Severe (e.g., Grade 3) or intolerable adverse reactions require interruption of adagrasib until sufficient improvement is observed before dosing is resumed.
Table 2. Recommended dosage modifications for adverse reactions:
| Adverse reaction | Severitya | Treatment modification |
|---|---|---|
| Nausea or vomiting despite appropriate supportive care (including anti-emetic therapy) | Grade 3 or 4 | Withhold adagrasib until recovery to ≤ Grade 1 or return to baseline Resume adagrasib at the next lower dose level |
| Diarrhoea despite appropriate supportive care (including anti-diarrhoeal therapy) | Grade 3 or 4 | Withhold adagrasib until recovery to ≤ Grade 1 or return to baseline Resume adagrasib at the next lower dose level |
| Hepatotoxicity | Grade 2 AST or ALT (3 to 5 times the ULN) | Decrease adagrasib to the next lower level |
| Grade 3 or 4 AST or ALT (>5 times the ULN) | Withhold adagrasib until recovery to ≤ Grade 1 or return to baseline Resume adagrasib at the next lower dose level | |
| AST or ALT >3 × ULN with total bilirubin >2 × ULN in the absence of alternative causes | Permanently discontinue adagrasib | |
| QTc Prolongation | Grade 3 (QTc ≥501 ms or >60 ms change from baseline) | Withhold adagrasib until recovery to ≤ Grade 1 or return to baseline Resume adagrasib at the next lower dose level |
| Grade 4 (ventricular arrhythmia) | Permanently discontinue adagrasib | |
| Other adverse reactions | Grade 3 or 4 | Withhold adagrasib until recovery to ≤ Grade 1 or return to baseline Resume adagrasib at the next lower dose level |
ALT = alanine aminotransferase; AST = aspartate aminotransferase; ULN = upper limit of normal
a Grading defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 5.0
It can be taken with or without food. Administration with food may improve tolerability.
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