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Capmatinib is an oral small molecule kinase inhibitor that selectively targets the mesenchymal epithelial transition factor (MET), specifically targeting mutations that cause MET exon 14 skipping.
1. Common name: Capmatinib (Capmatinib)
2. Trade name: TABRECTA ™
For the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors contain mutations that cause MET exon 14 skipping, and must be confirmed by an FDA-approved detection method.
1. Specifications: 200mg/tablet.
2. Characteristics: 200mg: Yellow oval film-coated tablets, with beveled edges and no scoring, with "LO" engraved on one side and "NVR" engraved on the other side.
1. Active ingredient: Capmatinib (150mg or 200mg, calculated as capmatinib hydrochloride anhydrous, respectively 176.55mg and 235.40mg).
2. Excipients: Colloidal silicon dioxide, crospovidone, magnesium stearate, mannitol, microcrystalline cellulose, povidone, sodium lauryl sulfate; film coating contains iron oxide, hypromellose, polyethylene glycol 4000, talc, titanium dioxide, etc.
1. Recommended dosage: 400 mg orally, twice a day, with food or on an empty stomach.
2. How to take the medicine: Swallow the tablet whole. Do not break, chew or crush it.
3. Missed dose or vomiting: If you miss a dose or vomit, there is no need to take a replacement dose, and you can take the next dose according to the original plan.
Adjust the dose according to the severity of adverse reactions:
1. The first reduction: 300mg twice a day;
2. The second reduction: 200mg twice a day;
3. Permanent discontinuation if 200mg twice a day cannot be tolerated.
Specific adjustment plans include:
1. Interstitial lung disease/pneumonia: Permanently discontinue medication at any grade;
2. Hepatotoxicity: Suspend or reduce the dose according to the degree of increase in ALT/AST and total bilirubin, and permanently discontinue the drug for grade 4;
3. Other adverse reactions:For grade 2, the dose can be maintained or reduced after suspension, for grade 3, the dose can be reduced after suspension, and for grade 4, the drug can be permanently discontinued.
1. Before and after meals: It can be taken with food or on an empty stomach. High-fat diet may increase exposure, but the clinical impact is not significant.
2. Missed dose: There is no need to take the next dose as originally planned.
3. Vomiting: If you vomit after taking the medicine, there is no need to take a supplement.
4. Others:
Monitor liver function regularly before and during treatment;
Pay attention to sun protection and limit ultraviolet exposure;
Patients of childbearing age need to take effective contraceptive measures.
1. Liver insufficiency: No dose adjustment is required for mild and moderate cases, and severe (Child-PughC) cases have not been studied⁸.
2. Renal insufficiency: No dose adjustment is required for mild to moderate (CLcr30-89mL/min), and severe (CLcr15-29mL/min) is not studied.
3. The elderly: Patients aged ≥65 years account for 57%, and the safety and effectiveness are not significantly different from those of younger patients.
4. Pregnant women and lactation period:
Pregnant women may cause fetal harm and need to be informed of the risks and use effective contraception;
It is contraindicated during lactation, and breastfeeding is not recommended within 1 week after stopping the drug⁸.
1. Common adverse reactions (≥20%): Peripheral edema (52%), nausea (44%), fatigue (32%), vomiting (28%), dyspnea (24%), decreased appetite (21%).
2. Serious adverse reactions:
Interstitial lung disease/pneumonia (4.5%, can be fatal);
Hepatotoxicity (ALT/AST elevation, 13%);
Others: non-cardiac chest pain, back pain, fever, etc.
3. Laboratory abnormalities: Reduced albumin (68%), increased creatinine (62%), increased ALT (37%), and decreased lymphocytes (44%).
There are currently no contraindications.
1. Strong CYP3A inducers (such as rifampicin): Avoid combination, which may reduce the exposure of capmatinib;
2. Strong CYP3A inhibitors (such as itraconazole): < /b>Closely monitor adverse reactions;
3. CYP1A2, P-gp, BCRP substrates:may increase the exposure of these drugs, and the dose needs to be adjusted;
4. Proton pump inhibitors:may reduce the exposure of capmatinib.
Save in original packaging, containing desiccant;
Storage at room temperature (20°C–25°C), short-term storage at 15°C–30°C allowed;
Moisture-proof, please discard if not used within 6 weeks after opening¹⁶.