Adagrasib is an irreversible inhibitor of KRASG12C mutation, mainly used for the treatment of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) with specific gene mutations.

Dosage and Administration of Adagrasib

Recommended Dosage and Administration Method

Recommended Dosage: For monotherapy of NSCLC or combination therapy with cetuximab for CRC, the recommended dosage is 600mg orally twice daily.

Treatment Course: Continue medication until disease progression or the occurrence of intolerable toxic reactions.

Administration Method: Take at fixed times every day, either with food or on an empty stomach. Swallow the tablets whole; do not chew, crush, or split them.

Special Management

Vomiting After Medication: If vomiting occurs after taking the medicine, do not take an additional dose. Take the next dose as scheduled.

Missed Dose: If the missed dose is more than 4 hours late, skip the missed dose and take the next dose as planned.

Important Pre-Medication Preparation

Confirmation of Gene Detection: The presence of KRASG12C mutation must be confirmed using a detection method approved by the FDA.

Non-Small Cell Lung Cancer: Detection can be performed based on plasma or tumor specimens.

Colorectal Cancer: Detection must be performed based on tumor specimens.

Dosage Adjustment of Adagrasib

Dosage Adjustment Plan

Implement stepwise dosage adjustment according to the severity of adverse reactions.

First Dose Reduction: Adjust to 400mg twice daily.

Second Dose Reduction: Adjust to 600mg once daily.

If the patient cannot tolerate the dose of 600mg once daily, permanent discontinuation of the drug is required.

QTc Interval Prolongation

If the absolute value of QTc > 500ms or increases by > 60ms compared with the baseline: Suspend medication.

If torsades de pointes (Tdp) occurs: Discontinue the drug permanently.

Hepatotoxicity

Grade 2 elevation of AST or ALT: Reduce the dose directly.

Grade 3 or 4 elevation of AST or ALT: Suspend medication until recovery, then resume at a reduced dose.

AST or ALT > 3×ULN (upper limit of normal) and total bilirubin > 2×ULN: Discontinue the drug permanently.

Interstitial Lung Disease (ILD)/Pneumonitis: Immediately suspend medication for suspected cases of any grade; discontinue the drug permanently after confirmation.

Medication for Special Populations of Adagrasib

Pregnant Women

Currently, there is no data on the use of adagrasib in pregnant women.

Animal studies have shown that no adverse developmental effects or embryo-fetal lethality were observed when the exposure was lower than the clinically recommended dose.

Lactating Women

There is no data indicating whether adagrasib or its metabolites are excreted into human milk.

It is recommended to discontinue breastfeeding during treatment and within 1 week after the last dose.