Tuoruida Capmatinib Hydrochloride Tablets

1. Indications and Usage
Non-Small Cell Lung Cancer (NSCLC): Treatment of adult patients with locally advanced or metastatic NSCLC whose tumors are MET exon 14 (METex14) skipping mutation-positive, as detected by an FDA-approved test.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 400 mg taken twice daily with or without food.
Critical Administration Instructions:
Intake: Tablets must be swallowed whole; do not crush, chew, or break.
Missed Dose: If a dose is missed, do not take it as soon as remembered; simply take the next dose at the regular scheduled time.
Vomiting: If vomiting occurs after taking a dose, do not take an extra dose; take the next dose at the regular scheduled time.
Dose Modifications: Reduce to 300 mg twice daily for adverse reactions. If unable to tolerate 200 mg twice daily, permanently discontinue the drug.
3. Mechanism of Action
MET Inhibition: Capmatinib is a selective, ATP-competitive inhibitor of the MET tyrosine kinase.
Pathway Blockade: It inhibits MET phosphorylation, blocking downstream signaling pathways (e.g., RAS-MAPK, PI3K-AKT).
Antitumor Effect: This prevents tumor cell proliferation, migration, and invasion induced by METex14 skipping mutations or MET amplification, inducing tumor cell apoptosis.
4. Safety and Warnings
Interstitial Lung Disease (ILD)/Pneumonitis: Occurs in approximately 4.5%. Monitor for new or progressive respiratory symptoms (dyspnea, cough, fever). Investigate promptly and manage according to severity (permanent discontinuation for severe cases).
Hepatotoxicity: Elevations in ALT, AST, and alkaline phosphatase occur in 13%. Monitor liver function tests before initiation, every 2 weeks for the first 3 months, and monthly thereafter.
Edema: Peripheral edema (52%) and pleural effusion may occur. Monitor body weight and manage symptomatic patients.
Embryo-Fetal Toxicity: May cause fetal harm. Effective contraception is required for females and males with female partners during treatment and for 1 week after the final dose.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions (≥20%): Peripheral edema, nausea, fatigue, vomiting, increased serum creatinine, dyspnea, and decreased appetite.
Common Grade 3-4 Adverse Reactions: Peripheral edema, fatigue, dyspnea, ALT increased, and lipase increased.
Clinical Research Highlights: The GEOMETRY mono-1 trial demonstrated an objective response rate (ORR) of 68% in treatment-naïve patients, with significant intracranial activity (ORR 50%) in patients with brain metastases.
6. Drug Interactions
CYP3A Modulators: Capmatinib is a substrate of CYP3A. Strong CYP3A inhibitors may increase exposure; strong and moderate CYP3A inducers may decrease exposure and are to be avoided.
CYP1A2/P-gp/BCRP Substrates: Capmatinib is an inhibitor. Concomitant use with sensitive substrates of these enzymes/transporters may increase their exposure.
Concomitant Medications: Clinical management should consider dose adjustments or alternative therapies for drugs with narrow therapeutic indices.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Capmatinib.
Appearance: Yellow, oval, film-coated tablets, imprinted with “LO” on one side and “NVR” on the other.
Packaging: Blister packaging or bottles with desiccant (e.g., 150 mg or 200 mg per tablet).
Storage: Store at 20°C to 25°C in the original container with desiccant to protect from moisture. Discard unused tablets 6 weeks after first opening.