Medication Guide for Tepotinib

The use of tepotinib must strictly adhere to the principle of individualized treatment. The administration and dosage should be determined by a qualified physician based on the patient's condition, genetic test results, and tolerability.

Standard Dosage for Adult Non-Small Cell Lung Cancer

Dose: Oral administration, once daily, 450 mg per dose.

Treatment Duration: Continue until disease progression or unacceptable toxicity occurs.

Indication: For the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping mutations.

Dosage Adjustments for Renal Impairment

Mild to Moderate Renal Impairment (Creatinine Clearance [CrCl] 30-89 mL/min): Dosage adjustment is not recommended.

Severe Renal Impairment (CrCl <30 mL/min): Insufficient data are available to support dosage adjustment.

Note: The recommended dosage for patients with severe renal impairment has not been established.

Dosage Adjustments for Hepatic Impairment

(I) Dosage Adjustment for Pre-existing Hepatic Impairment (by Child-Pugh Classification)

Mild to Moderate Hepatic Impairment (Child-Pugh Class A or B): Dosage adjustment is not recommended.

Severe Hepatic Impairment (Child-Pugh Class C): Insufficient data are available to support dosage adjustment.

Note: Pharmacokinetic and safety studies have not been conducted in patients with severe hepatic impairment.

(II) Dosage Adjustment for Hepatic Function Abnormalities During Treatment

Adjust the dosage according to the following criteria based on abnormalities in liver function parameters (ALT, AST, total bilirubin):

Elevated ALT and/or AST without concurrent elevation in total bilirubin

Grade 3 abnormality: Withhold treatment until ALT/AST return to baseline levels. If recovery to baseline occurs within 7 days, resume at the original dose. If recovery takes longer than 7 days, resume at a reduced dose (oral administration, once daily, 225 mg per dose).

Grade 4 abnormality: Permanently discontinue treatment.

Elevated ALT and/or AST with concurrent elevation in total bilirubin (in the absence of cholestasis or hemolysis)

If ALT and/or AST >3 × upper limit of normal (ULN) and total bilirubin >2 × ULN: Permanently discontinue treatment.

Elevated total bilirubin without concurrent elevation in ALT and/or AST

Grade 3 abnormality: Withhold treatment until total bilirubin returns to baseline levels. If recovery occurs within 7 days, resume at a reduced dose (oral administration, once daily, 225 mg per dose). If recovery takes longer than 7 days, permanently discontinue treatment.

Grade 4 abnormality: Permanently discontinue treatment.

Dosage Adjustments for Adverse Reactions

(I) Recommended Reduced Dose

The recommended reduced dose for managing adverse reactions is oral administration, once daily, 225 mg per dose. If a patient cannot tolerate the 225 mg daily dose, treatment should be permanently discontinued.

(II) Management of Interstitial Lung Disease (ILD)/Pneumonitis

Regardless of grade: If ILD is suspected, withhold treatment immediately. If ILD is confirmed, permanently discontinue treatment.

(III) Management of Other Adverse Reactions

Grade 2 adverse reaction: Maintain the current dose. If intolerable, consider withholding treatment until the adverse reaction resolves, then resume at the reduced dose.

Grade 3 adverse reaction: Withhold treatment until the adverse reaction resolves, then resume at the reduced dose.

Grade 4 adverse reaction: Permanently discontinue treatment.