.jpeg)
{{ variable.name }}
Common name: Trifluridine Tipiracil Tablets
Trade name: Lonsurf
Full names: Trifluridine Tipiracil Tablets, Lonsurf, Lonsurf, Trifluridine + Tipiracil, TAS-102, FTD/TPI, trifluridine/tipiracil
Indications:
For the treatment of patients with metastatic colorectal cancer who have received fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, anti-VEGF biological therapy and anti-EGFR therapy (RAS wild type).
For the treatment of adult patients with metastatic gastric cancer (mGC, including metastatic gastroesophageal junction adenocarcinoma [mGEJC]).
Usage and dosage:
Recommended dosage and administration: The recommended starting dose for adults is about 35 mg/m2/time, taken orally within 1 hour after breakfast and dinner, twice a day, on days 1-5 and 8-12 of each course of treatment, 28 days is a course of treatment. Administration should be continued until disease progression or intolerable toxicity occurs.
Adverse reactions:
Anemia, neutropenia, weakness/fatigue, nausea, thrombocytopenia, decreased appetite, diarrhea, vomiting, abdominal pain, fever
Contraindications:
Contraindicated in patients with hypersensitivity to the ingredients of this product.
Precautions:
Myelosuppression: Treatment with this product results in an increased incidence of myelosuppression, including anemia, neutropenia, leukopenia and thrombocytopenia. To monitor for toxic effects, a complete blood count must be obtained before initiating treatment with this product and as needed, and at least before the start of each cycle of treatment. Treatment should not be initiated if the absolute neutrophil count is <1.5 × 109/L, or the platelet count is <75 × 109/L, or if there is grade 3 or 4 non-hematological clinically relevant toxicity that has not resolved with prior treatment. Serious infections have been reported in patients treated with this product. Given that most reports are related to myelosuppression, patients should be closely monitored and appropriate management measures should be taken as clinically indicated, such as administration of antimicrobials or granulocyte colony-stimulating factor (G-CSF). In the RECOURSE study, 9.4% of patients in the acetaminophen arm received G-CSF.
Gastrointestinal toxicity: This product causes an increased incidence of gastrointestinal toxicity such as nausea, vomiting and diarrhea. Patients with nausea, vomiting, diarrhea, and other symptoms of gastrointestinal toxicity should be closely monitored, and antiemetic, antidiarrheal, and other measures (e.g., fluid and electrolyte replacement) should be administered as clinically indicated. Dosage adjustments should be made as necessary, such as dosing delays and/or dose reductions.
Abnormal renal function: Use of this product is not recommended in patients with severe renal dysfunction or end-stage renal disease (creatinine clearance [CLcr] <30 mL/min or requiring dialysis) as there are no data on its use in these patients. The incidence of grade ≥3 adverse events (AEs), serious adverse events, dosing delays, and dose reductions was higher (difference of at least 5%) in patients with moderate renal impairment (CLcr 30-59 mL/min) compared with patients with normal renal function (CLcr ≥90 mL/min) or mild renal impairment (CLcr 6089 mL/min). Additionally, trifluridine and tipiracil hydrochloride exposures were higher in patients with moderate renal impairment compared with patients with normal renal function or mild renal impairment. Patients with moderate renal impairment should be monitored more frequently for hematologic toxicities.
Hepatic Function Abnormality: Although based on very limited data, use of this product is not recommended in patients with baseline moderate or severe hepatic dysfunction (National Cancer Institute [NCI] criteria Groups C and D, total bilirubin > 1.5 × ULN) because of the higher incidence of Grade 3 or 4 hyperbilirubinemia in patients with baseline moderate hepatic dysfunction.
Proteinuria: It is recommended to use dipstick urinalysis to monitor proteinuria before starting treatment with this product and during treatment. Lactose intolerance This product contains lactose. Patients with rare hereditary conditions of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not use this product.
Effects on the ability to drive and operate machinery: This product has minimal effects on the ability to drive and operate machinery.
Fatigue, dizziness or discomfort may occur during treatment with this product.
Storage:
Store at controlled room temperature 20-25°C (68-77°F); excursions allowed at 15-30°C (59-86°F).
If stored outside the original bottle, discard after 30 days.
Mechanism of action:
Lonsford is composed of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil in a molar ratio of 1:0.5 (weight ratio 1:0.471). Tipiracil inhibits the metabolism of trifluridine via thymidine phosphorylase thereby increasing its exposure. After the drug enters tumor cells, trifluridine is incorporated into DNA, interfering with DNA synthesis and inhibiting cell proliferation. Antitumor activity of trifluridine/tipiracil was seen in mouse xenograft models of KRAS wild-type and mutant human colorectal cancer.