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Indications and Dosage
Oral
Metastatic non-small cell lung carcinoma Adult: In patients whose tumours have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping: 400 mg bid; continue until disease progression or unacceptable toxicity. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline).
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Administration
May be taken with or without food. Swallow whole, do not break/crush/chew.
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Special Precautions
Pregnancy and lactation.
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Adverse Reactions
Significant: Hepatotoxicity, risk for photosensitivity reactions.
Blood and lymphatic system disorders: Leucopenia, lymphocytopenia. Gastrointestinal disorders: Constipation, diarrhoea, nausea, vomiting, acute pancreatitis. General disorders and administration site conditions: Fatigue, fever, non-cardiac chest pain, peripheral oedema. Investigations: Decreased Hb, serum albumin, serum glucose, serum phosphate or serum Na; increased gamma-glutamyl transferase, serum K, serum amylase, serum lipase, serum ALT/AST, serum alkaline phosphatase or serum creatinine. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Back pain. Renal and urinary disorders: Acute renal failure. Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea, pleural effusion, pneumonia. Skin and subcutaneous tissue disorders: Cellulitis, pruritus, urticaria. Potentially Fatal: Interstitial lung disease or pneumonitis. |
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Patient Counseling Information
Limit direct exposure to sunlight or UV light. Use sunscreen or protective clothing.
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Monitoring Parameters
Perform confirmatory test for the presence of a mesenchymal epithelial transition (MET) exon 14 skipping mutation in tumour specimens prior to initiation of therapy. Monitor LFTs (e.g. ALT, AST, total bilirubin) before initiation of therapy, every 2 weeks during the 1st 3 months of therapy, then monthly or if needed. Evaluate pregnancy status prior to use in females of childbearing potential. Monitor for symptoms of interstitial lung disease or pneumonitis, hepatotoxicity, and photosensitivity reactions.
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Drug Interactions
May increase plasma concentration with strong CYP3A inhibitors (e.g. itraconazole). May decrease plasma concentration with moderate or strong CYP3A inducers (e.g. efavirenz, rifampicin), PPIs (e.g. rabeprazole). May increase plasma concentrations of CYP1A2 substrates (e.g. caffeine), P-glycoprotein (P-gp) substrates (e.g. digoxin), Breast Cancer Resistance Protein (BCRP) substrates (e.g. rosuvastatin), MATE1 or MATE2K substrates.
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Action
Description:
Mechanism of Action: Capmatinib is a potent and highly-selective inhibitor of mesenchymal-epithelial transition (MET) receptor tyrosine kinase, including the mutant variant produced by exon 14 skipping. The MET exon 14 skipping leads to a protein with a missing regulatory domain which decreases its negative regulation, resulting in increased downstream MET signalling. It decreases cancer cell growth through MET inhibition. Furthermore, it inhibits MET phosphorylation triggered by binding of hepatocyte growth factor or by MET amplification, and MET-mediated phosphorylation of downstream signalling proteins. Pharmacokinetics: Absorption: Time to peak plasma concentration: Approx 1-2 hours. Distribution: Crosses the blood-brain barrier. Plasma protein binding: 96%. Metabolism: Primarily metabolised in the liver by CYP3A4 and aldehyde oxidase. Excretion: Via faeces (78%, 42% as unchanged drug); urine (22%, mainly as metabolites). Elimination half-life: 6.5 hours. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 25145656, Capmatinib. https://pubchem.ncbi.nlm.nih.gov/compound/Capmatinib. Accessed Aug. 25, 2021. |
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Storage
Store between 20-25°C. Protect from moisture. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
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MIMS Class
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ATC Classification
L01EX17 - capmatinib ; Belongs to the class of other protein kinase inhibitors. Used in the treatment of cancer.
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References
Anon. Capmatinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/07/2021. Anon. Capmatinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/07/2021. Tabrecta 150 mg, 200 mg Tablets (Novartis Pharmaceuticals [HK] Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 17/08/2021. Tabrecta Tablet, Film Coated (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/07/2021. Tabrecta Tablet, Film Coated (Novartis Pharmaceuticals Corporation). U.S. FDA. https://www.fda.gov. Accessed 08/07/2021.
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