Note: Select patients for treatment based on the presence of a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping in tumor or plasma specimens (if not detected in plasma, test tumor tissue if feasible).
Non-small cell lung cancer, metastatic, with mesenchymal-epithelial transition exon 14 skipping mutation: Oral: 400 mg twice daily (Wolf 2020); continue until disease progression or unacceptable toxicity.
Missed dose: If a dose is missed or vomited, administer the next dose at its scheduled time. Do not make up the missed dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Note: Renal function estimated using the Cockcroft-Gault formula.
CrCl ≥30 mL/minute: No dosage adjustment is necessary.
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Preexisting impairment:
Child-Pugh classes A, B, or C: There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically significant effects on pharmacokinetic parameters were observed.
Hepatotoxicity during treatment:
Adverse reaction |
Severity |
Dose modificationa |
---|---|---|
aSee recommended capmatinib dosage level reductions in "Dosing Adjustment for Toxicity". | ||
Increased ALT and/or AST without increased total bilirubin |
Grade 3 |
Withhold capmatinib until recovery to baseline ALT/AST. If recovered to baseline within 7 days, resume capmatinib at the same dose. If not recovered to baseline within 7 days, resume capmatinib at a lower dose. |
Grade 4 |
Permanently discontinue capmatinib. | |
Increased ALT and/or AST with increased total bilirubin in the absence of cholestasis or hemolysis |
ALT and/or AST >3 times ULN with total bilirubin >2 times ULN |
Permanently discontinue capmatinib. |
Increased total bilirubin without concurrent increased ALT and/or AST |
Grade 2 |
Withhold capmatinib until recovery to baseline bilirubin. If recovered to baseline within 7 days, resume capmatinib at the same dose. If not recovered to baseline within 7 days, resume capmatinib at a lower dose. |
Grade 3 |
Withhold capmatinib until recovery to baseline bilirubin. If recovered to baseline within 7 days, resume capmatinib at a reduced dose. If not recovered to baseline within 7 days, permanently discontinue capmatinib. | |
Grade 4 |
Permanently discontinue capmatinib. |
Refer to adult dosing.
Recommended Capmatinib Dosage Level Reductions for Adverse Reactions | ||
---|---|---|
Initial dose is 400 mg twice daily. | ||
Dose reduction |
Dose and schedule | |
First |
300 mg twice daily | |
Second |
200 mg twice daily | |
If unable to tolerate 200 mg twice daily |
Permanently discontinue capmatinib. | |
Recommended Capmatinib Dosage Modifications for Adverse Reactions | ||
Adverse reaction |
Severity |
Dose modification |
Interstitial lung disease/pneumonitis |
Suspected |
Immediately withhold capmatinib. |
Any grade |
Permanently discontinue capmatinib. | |
Other adverse reactions |
Grade 2 |
Maintain current capmatinib dose. If toxicity is intolerable, consider withholding capmatinib until resolved, then resume at a reduced dose. |
Grade 3 |
Withhold capmatinib until resolved, then resume at a reduced dose. | |
Grade 4 |
Permanently discontinue capmatinib. |
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as hydrochloride:
Tabrecta: 150 mg, 200 mg
No
Oral: Administer with or without food. Swallow tablets whole; do not break, crush, or chew.
This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Capmatinib may cause teratogenicity.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Non-small cell lung cancer, metastatic: Treatment of metastatic non-small cell lung cancer (NSCLC) in adults whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping as detected by an approved test.
Capmatinib may be confused with cabozantinib, capecitabine, Capmist, Caprelsa, ceritinib, cobimetinib, crizotinib, imatinib, tepotinib.
This medication is in a class the Institute for Safe Medication Practices (ISMP) includes among its lists of drug classes that have a heightened risk of causing significant patient harm when used in error.
Hepatoxicity, including increased serum alanine aminotransferase, increased serum alkaline phosphatase, and increased serum aspartate aminotransferase, has commonly been reported. Depending on severity, therapy interruption or dose modification may be warranted, including permanent drug discontinuation.
Onset: Varied; median time to onset of ≥ grade 3 elevated ALT/AST was 1.4 months (range: 0.5 to 4.1 months).
Peripheral edema is commonly observed and may be severe (Ref).
Dyspnea is common with use and may be severe (≥ grade 3) (Ref). Interstitial pulmonary disease (ILD)/pneumonitis, potentially life-threatening, has occurred. Symptoms of ILD/pneumonitis typically present as cough, dyspnea, and fever; permanent discontinuation is warranted if ILD/pneumonitis is confirmed.
Onset: Varied; median time to onset of ≥ grade 3 ILD/pneumonitis was 1.4 months (range: 0.2 months to 1.2 years).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Cardiovascular: Peripheral edema (52%)
Endocrine & metabolic: Decreased serum albumin (68%), decreased serum glucose (21%), decreased serum phosphate (23%), decreased serum sodium (23%), increased gamma-glutamyl transferase (29%), increased serum potassium (23%)
Gastrointestinal: Constipation (18%), decreased appetite (21%), diarrhea (18%), increased serum amylase (31%), increased serum lipase (26%), nausea (44%; severe nausea: 2%), vomiting (28%; severe vomiting: 2%)
Hematologic & oncologic: Decreased hemoglobin (24%, grades 3/4: 3%), leukopenia (23%, grades 3/4: <1%), lymphocytopenia (44%, grades 3/4: 14%)
Hepatic: Increased serum alanine aminotransferase (37%), increased serum alkaline phosphatase (32%), increased serum aspartate aminotransferase (25%)
Nervous system: Fatigue (32%), noncardiac chest pain (15%)
Neuromuscular & skeletal: Back pain (14%)
Renal: Increased serum creatinine (62%)
Respiratory: Cough (16%), dyspnea (24%; grades 3/4: 7% [Dhillon 2020])
Miscellaneous: Fever (14%)
1% to 10%:
Dermatologic: Cellulitis (<10%), pruritus (<10%), urticaria (<10%)
Endocrine & metabolic: Weight loss (10%)
Gastrointestinal: Acute pancreatitis (<10%)
Renal: Acute renal failure (<10%, including renal failure syndrome)
Respiratory: Interstitial pulmonary disease (≤5%), pleural effusion (4%), pneumonia (5%), pneumonitis (≤5%)
Frequency not defined: Hepatic: Hepatotoxicity
There are no contraindications listed in the manufacturer's labeling.
Concerns related to adverse effects:
• Photosensitivity: Capmatinib may cause photosensitivity reactions. In a clinical trial, it was recommended that patients take precautions against ultraviolet exposure through the use of sunscreen or protective clothing during capmatinib therapy. Patients should limit direct ultraviolet exposure during treatment with capmatinib.
Other warnings/precautions:
• Appropriate use: Select patients for treatment based on the presence of a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping in tumor or plasma specimens (if not detected in plasma, test tumor tissue if feasible). Information on approved tests is available at http://www.fda.gov/CompanionDiagnostics.
Substrate of CYP3A4 (major), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP/ABCG2, CYP1A2 (moderate), P-glycoprotein/ABCB1
Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider therapy modification
Agomelatine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine. Risk C: Monitor therapy
Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Aliskiren. Risk C: Monitor therapy
Alosetron: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Alosetron. Management: Avoid concomitant use of alosetron and moderate CYP1A2 inhibitors whenever possible. If combined use is necessary, monitor for increased alosetron effects/toxicities. Risk D: Consider therapy modification
Alpelisib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider therapy modification
Bendamustine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Bendamustine. Management: Consider alternatives to moderate CYP1A2 inhibitors during therapy with bendamustine due to the potential for increased bendamustine plasma concentrations and increased bendamustine toxicity. Risk D: Consider therapy modification
Berotralstat: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Berotralstat. Management: Decrease the berotralstat dose to 110 mg daily when combined with P-glycoprotein (P-gp) inhibitors. Risk D: Consider therapy modification
Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Bilastine. Risk X: Avoid combination
Bromazepam: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Bromazepam. Risk C: Monitor therapy
Caffeine and Caffeine Containing Products: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Caffeine and Caffeine Containing Products. Risk C: Monitor therapy
Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Celiprolol. Risk C: Monitor therapy
Cladribine: BCRP/ABCG2 Inhibitors may increase the serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Risk D: Consider therapy modification
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
ClomiPRAMINE: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ClomiPRAMINE. Risk C: Monitor therapy
CloZAPine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Risk C: Monitor therapy
Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a P-gp inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. See interaction monograph for details. Risk D: Consider therapy modification
CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Capmatinib. Risk X: Avoid combination
CYP3A4 Inducers (Strong): May decrease the serum concentration of Capmatinib. Risk X: Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Capmatinib. Risk C: Monitor therapy
Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Risk C: Monitor therapy
Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Digoxin. Management: Measure digoxin serum concentrations before initiating treatment with these P-glycoprotein (P-gp) inhibitors. Reduce digoxin concentrations by either reducing the digoxin dose by 15% to 30% or by modifying the dosing frequency. Risk D: Consider therapy modification
DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Conventional). Risk X: Avoid combination
DULoxetine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of DULoxetine. Risk C: Monitor therapy
Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Edoxaban. Risk C: Monitor therapy
Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide. Risk C: Monitor therapy
Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide Phosphate. Risk C: Monitor therapy
Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Everolimus. Risk C: Monitor therapy
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor therapy
Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lapatinib. Risk C: Monitor therapy
Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Larotrectinib. Risk C: Monitor therapy
Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects. Risk D: Consider therapy modification
Melatonin: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Melatonin. Risk C: Monitor therapy
Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Morphine (Systemic). Risk C: Monitor therapy
Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Nadolol. Risk C: Monitor therapy
Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naldemedine. Risk C: Monitor therapy
Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naloxegol. Risk C: Monitor therapy
OLANZapine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of OLANZapine. Risk C: Monitor therapy
PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
Pentoxifylline: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pentoxifylline. Risk C: Monitor therapy
Pirfenidone: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pirfenidone. Management: Avoid concomitant use of pirfenidone and moderate CYP1A2 inhibitors whenever possible. If combined, decrease the pirfenidone dose to 1,602 mg per day (534 mg three times daily) and monitor for increased pirfenidone toxicities. Risk D: Consider therapy modification
Pomalidomide: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pomalidomide. Risk C: Monitor therapy
Propranolol: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Propranolol. Risk C: Monitor therapy
Ramelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramelteon. Risk C: Monitor therapy
Ramosetron: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramosetron. Risk C: Monitor therapy
Ranolazine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Ranolazine. Risk C: Monitor therapy
Rasagiline: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Rasagiline. Management: Limit rasagiline dose to 0.5 mg once daily in patients taking moderate CYP1A2 inhibitors. Risk D: Consider therapy modification
Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider therapy modification
Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider therapy modification
RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RifAXIMin. Risk C: Monitor therapy
Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider therapy modification
RisperiDONE: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RisperiDONE. Risk C: Monitor therapy
RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RomiDEPsin. Risk C: Monitor therapy
ROPINIRole: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ROPINIRole. Risk C: Monitor therapy
Ropivacaine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ropivacaine. Risk C: Monitor therapy
Rosuvastatin: Capmatinib may increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy
Saquinavir: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Saquinavir. Risk C: Monitor therapy
Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Silodosin. Risk C: Monitor therapy
Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider therapy modification
Sirolimus (Protein Bound): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Sirolimus (Protein Bound). Risk X: Avoid combination
Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Talazoparib. Risk C: Monitor therapy
Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Risk C: Monitor therapy
Tasimelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Tasimelteon. Risk C: Monitor therapy
Tegaserod: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tegaserod. Risk C: Monitor therapy
Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Teniposide. Risk C: Monitor therapy
Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
Theophylline Derivatives: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Theophylline Derivatives. Management: Consider avoidance of this combination. If coadministration is necessary, monitor for increased theophylline serum concentrations and toxicities when combined. Theophylline dose reductions will likely be required. Risk D: Consider therapy modification
TiZANidine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of TiZANidine. Management: If combined use cannot be avoided, initiate tizanidine in adults at 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Risk D: Consider therapy modification
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Ubrogepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Risk D: Consider therapy modification
Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a P-gp inhibitor. Risk D: Consider therapy modification
Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors. Resume the previous venetoclax dose 2 to 3 days after discontinuation of a P-gp inhibitor. Risk D: Consider therapy modification
VinCRIStine (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of VinCRIStine (Liposomal). Risk X: Avoid combination
Evaluate pregnancy status prior to use in patients who could become pregnant.
Patients who could become pregnant should use effective contraception during therapy and for 1 week after the last capmatinib dose. Patients with partners who could become pregnant should use effective contraception during therapy and for 1 week after the last capmatinib dose.
Based on the mechanism of action and data from animal reproduction studies, in utero exposure to capmatinib may cause fetal harm.
It is not known if capmatinib is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 1 week after the last capmatinib dose.
Mesenchymal-epithelial transition (MET) exon 14 skipping mutation status (in tumor or plasma specimens). Monitor LFTs (including ALT, AST, and total bilirubin) prior to therapy initiation, every 2 weeks during the first 3 months of therapy, then once monthly or as clinically necessary (monitor more frequently in patients who develop elevated LFTs). Evaluate pregnancy status prior to use in patients who could become pregnant. Monitor for new or worsening pulmonary symptoms indicative of interstitial lung disease/pneumonitis (eg, dyspnea, cough, fever); monitor for signs/symptoms of hepatoxicity, and photosensitivity reactions. Monitor adherence.
The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.
Capmatinib is a potent and highly-selective inhibitor of mesenchymal-epithelial transition (MET), including the mutant variant produced by exon 14 skipping. MET exon 14 skipping results in increased downstream MET signaling. Through MET inhibition, capmatinib decreases cancer cell growth. Capmatinib inhibits MET phosphorylation triggered by binding of c-MET (also known as hepatocyte growth factor) or by MET amplification, as well as MET-mediated phosphorylation of downstream signaling proteins.
Absorption: >70%.
Distribution: Vdss: 164 L.
Protein binding: 96%.
Metabolism: Primarily hepatic via CYP3A4 and aldehyde oxidase.
Half-life elimination: 6.5 hours.
Time to peak: ~1 to 2 hours.
Excretion: Feces: 78% (42% as unchanged drug); urine: 22% (primarily as metabolites).
Clearance: 24 L/hour.
Tablets (Tabrecta Oral)
150 mg (per each): $214.06
200 mg (per each): $214.06
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