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Larotrectinib is a highly selective tyrosine kinase inhibitor that blocks the activity of TRKA, TRKB and TRKC proteins produced by neurotrophic tyrosine receptor kinase (NTRK) gene fusion by targeting it. Downstream signaling pathways, thereby inhibiting the proliferation and survival of tumor cells
1. Generic name : Larotrectinib
2. Trade name : VITRAKVI®
3. Dosage form : Capsule (100mg)
4. Main ingredient : larotide Nisulfate (25mg capsule contains 30.7mg sulfate, 100mg capsule contains 123mg sulfate, oral solution contains 24.6mg/mL sulfate), excipients include gelatin, titanium dioxide (capsule), hydroxypropyl beta cyclodextrin, sucrose (oral solution), etc.
NTRK gene fusion solid tumor : It is used to treat adults and children with solid tumors that are NTRK gene fusion positive, metastatic, or where surgery may cause serious complications, and there is no satisfactory alternative treatment option or previous treatment failure. This indication is approved under accelerated approval based on overall response rate and duration of response, and further verification of clinical benefit is required.
100mg (white opaque hard capsule).
1. Adults and children with body surface area ≥1.0m² : 100 mg orally, twice a day (about 12 hours apart).
2. Children with body surface area <1.0m² : 100mg/m² orally, 2 times a day (maximum dose 100mg/time).
3. How to take : Swallow the capsule whole, without food or on an empty stomach; after a missed dose, you can take it again if it is >6 hours before the next dose. There is no need to take it again after vomiting.
1. Adverse reactions : Reduce the dose to 75mg (or 75mg/m²) twice a day for the first time, to 50mg (or 50mg/m²) twice a day for the second time, and to 100mg once a day (or 25mg/m² twice a day) for the third time. If it is not tolerated, discontinue the drug permanently.
2. For hepatic insufficiency: The starting dose is halved for patients with moderate to severe (Child-PughB/C).
3. Drug interaction : Halve the dose when combined with a strong CYP3A4 inhibitor, double the dose when combined with a strong CYP3A4 inducer.
1. Neurotoxicity : 53% of patients experience dizziness, ataxia, etc. and need to avoid driving or operating machinery.
2. Hepatotoxicity :Monitor ALT/AST every 2 weeks in the first month of treatment, and then change to monthly monitoring.
3. Drug interactions : Avoid the combined use of strong CYP3A4 inhibitors (such as ketoconazole), inducers (such as rifampicin) and sensitive CYP3A4 substrates (such as midazolam).
1. Pregnant women: : Disabled (animal experiments show teratogenicity).
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week after the last dose.
3. Children : Safety data for children ≥1 month old are limited, and the dose for children ≥12 years old is the same as for adults.
4. U200c for the elderly: No need to adjust the dosage.
1. Common (≥20%) : Fatigue (37%), nausea (29%), dizziness (28%), vomiting (26%), increased AST/ALT (45% each), constipation (23%), diarrhea (22%).
2. Severe reactions : Neurotoxicity (6% grade 3-4), liver toxicity (3% grade 3-4 ALT/AST elevation).
There are no absolute contraindications, but it is prohibited for those who are allergic to the ingredients.
1. Strong CYP3A4 inhibitor : To increase the plasma concentration of larotrectinib, the dose needs to be reduced by 50%.
2. Strong CYP3A4 inducer : To reduce the plasma concentration of larotrectinib, double the dose is required.
3. Sensitive CYP3A4 substrate : may increase its plasma concentration, so combined use should be avoided.
Capsule : Store at room temperature 20-25℃.
Note : NTRK fusion status, liver function and neurological symptoms need to be monitored regularly during treatment. Avoid use with grapefruit or St. John's wort.