zongertinib

　　【Indications】

　　HERNEXEOS(zongertinib)is a kinase inhibitor indicated for adult patients with unresectable or metastatic non-squamous non-small cell lung cancer whose tumors have HER2(ERBB2)tyrosine kinase domain activating mutations confirmed by an authorized assay and who have previously received systemic therapy.Treatment selection should be based on documented HER2 TKD activating mutation status rather than histology alone.

　　【Recommended Dosage】

　　•Confirm the presence of HER2(ERBB2)tyrosine kinase domain activating mutations before starting HERNEXEOS.

　　•Body-weight–based oral dosage:

　　。Less than 90 kg:120 mg

　　。90 kg or more:180 mg

　　•Take HERNEXEOS once daily with or without food until disease progression or unacceptable toxicity.Swallow tablets whole with water;do not split,crush,or chew.

　　【Adverse Reactions】

　　-Most common adverse reactions(>20%):diarrhea,hepatotoxicity,rash,fatigue,nausea.

　　-Most common Grade 3 or 4 laboratory abnormalities(>2%):lymphopenia,increased alanine aminotransferase,increased aspartate aminotransferase,decreased potassium,increased gamma-glutamyl transferase.

　　Hepatic tests,cardiac function,and other toxicity signals should be monitored,with dose interruption,reduction,or discontinuation based on severity.

　　【Pharmacology】

　　Zongertinib is a HER2 kinase inhibitor.In vitro,it inhibits HER2 phosphorylation,reduces downstream signaling such as ERK phosphorylation,and suppresses proliferation of lung cancer cells carrying HER2 tyrosine kinase domain activating mutations.In vivo,it shows antitumor activity in HER2 TKD-mutant non-small cell lung cancer mouse xenograft models,primarily by blocking HER2-driven signaling.

　　【Storage】

　　Store at 20°C to 25°C;short-term excursions may occur between 15°C and 30°C.Keep in the original bottle to protect from moisture,keep the cap tightly closed,and do not remove the desiccant.Use within 3 months after first opening;discard any remaining tablets 3 months after the bottle is opened.