Haiyitan Glumetinib Tablets

1. Indications and Usage
Glumetinib tablets are indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with MET exon 14 skipping mutation as detected by an adequately validated test.
2. Dosage and Administration
Recommended Dosage: The recommended dosage is 300 mg taken orally once daily, taken continuously until disease progression or unacceptable toxicity.
Administration: Must be taken in a fasting state (at least 2 hours before and 1 hour after a meal). Tablets should be swallowed whole with water; do not crush or chew.
Missed Dose: If a dose is missed or vomiting occurs, do not take an extra dose on the same day. Resume with the next scheduled dose.
Dose Modifications: Dose reductions (to 250 mg, 200 mg, or 150 mg) or interruptions are required based on the severity of adverse reactions.
3. Mechanism of Action
Glumetinib is a potent and highly selective type Ib MET inhibitor. It inhibits the autophosphorylation of MET and its downstream signaling pathways, thereby blocking tumor cell proliferation and inducing apoptosis in MET exon 14 skipping-mutated NSCLC cells.
4. Safety and Warnings
Hepatotoxicity: Elevations in liver enzymes (ALT, AST) and bilirubin can occur. Liver function tests must be monitored regularly.
Interstitial Lung Disease/Pneumonitis: May occur; monitor for new pulmonary symptoms and manage according to severity.
QTc Prolongation: Can cause dose-dependent QTc interval prolongation. Electrocardiogram monitoring is necessary.
Edema: Peripheral edema and fluid retention are common adverse reactions.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The most common adverse reactions include edema, headache, decreased appetite, nausea, fatigue, and increased liver enzymes.
Clinical Research: Efficacy and safety were established in the pivotal Phase II GLORY study, which demonstrated an objective response rate of 66% and a median progression-free survival of 8.5 months.
6. Drug Interactions
CYP3A Inhibitors and Inducers: As CYP3A is involved in metabolism, strong CYP3A inhibitors may increase exposure, while strong inducers may decrease exposure. Caution is advised when co-administering such drugs.
Drugs Prolonging QTc: Concomitant use with drugs known to prolong the QTc interval should be approached with caution.
Food: High-fat meals significantly increase the bioavailability and exposure of glumetinib; strict fasting administration is required.
7. Pharmaceutical Information
Composition: The active ingredient is glumetinib.
Appearance: Film-coated tablets (e.g., 50 mg strength).
Storage: Store at controlled room temperature in the original packaging to protect from moisture.