Brand Name
Lonsurf
Generic Name
Trifluridine
View Brand Information FDA approval date: May 14, 2001
Classification: Nucleoside Metabolic Inhibitor
Form: Tablet, Solution
What is Lonsurf (Trifluridine)?
LONSURF is a combination of trifluridine, a nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase inhibitor, indicated for the treatment of adult patients with: metastatic colorectal cancer as a single agent or in combination with bevacizumab who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.
Approved To Treat
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Brand Information
LONSURF (trifluridine and tipiracil)
1DOSAGE FORMS AND STRENGTHS
Tablets:
- 15 mg trifluridine/6.14 mg tipiracil: white, biconvex, round, film-coated, imprinted with ‘15’ on one side, and ‘102’ and ‘15 mg’ on the other side, in gray ink.
- 20 mg trifluridine/8.19 mg tipiracil: pale red, biconvex, round, film-coated, imprinted with ‘20’ on one side, and ‘102’ and ‘20 mg’ on the other side, in gray ink.
2CONTRAINDICATIONS
None.
3ADVERSE REACTIONS
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Severe Myelosuppression
3.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The data described in the WARNINGS AND PRECAUTIONS section and below reflect exposure to LONSURF at the recommended dose in 533 patients with metastatic colorectal cancer in RECOURSE, 246 patients with metastatic colorectal cancer treated with LONSURF as monotherapy in SUNLIGHT and 335 patients with metastatic gastric cancer in TAGS. Among the 1114 patients who received LONSURF as a single agent, 12% were exposed for 6 months or longer and 1% were exposed for 12 months or longer. The most common adverse reactions or laboratory abnormalities (≥10%) were neutropenia, anemia, thrombocytopenia, fatigue, nausea, decreased appetite, diarrhea, vomiting, abdominal pain, and pyrexia.
Among the 246 patients with metastatic colorectal cancer treated with LONSURF in combination with bevacizumab in SUNLIGHT, 39% were exposed for 6 months or longer, and 14% were exposed for 12 months or longer. The most common adverse reactions or laboratory abnormalities (≥20%) were neutropenia, anemia, thrombocytopenia, fatigue, nausea, increased AST, increased ALT, increased alkaline phosphatase, decreased sodium, diarrhea, abdominal pain, and decreased appetite.
Metastatic Colorectal Cancer
LONSURF as a single agent
The safety of LONSURF was evaluated in RECOURSE, a randomized (2:1), double-blind, placebo-controlled trial in patients with previously treated metastatic colorectal cancer
The study population characteristics were: median age 63 years; 61% male; 57% White, 35% Asian, and 1% Black.
The most common adverse reactions or laboratory abnormalities (≥10% in incidence) in patients treated with LONSURF at a rate that exceeds the rate in patients receiving placebo were anemia, neutropenia, asthenia/fatigue, nausea, thrombocytopenia, decreased appetite, diarrhea, vomiting, abdominal pain, and pyrexia.
In RECOURSE, 3.6% of patients discontinued LONSURF for an adverse reaction and 14% of patients required a dose reduction. The most common adverse reactions or laboratory abnormalities leading to dose reduction were neutropenia, anemia, febrile neutropenia, fatigue, and diarrhea.
Table 3 and Table 4 list the adverse reactions and laboratory abnormalities (graded using CTCAE v4.03), respectively, observed in RECOURSE.
In RECOURSE, pulmonary emboli occurred more frequently in LONSURF-treated patients (2%) compared to no patients on placebo.
LONSURF in combination with bevacizumab
The safety of LONSURF in combination with bevacizumab was evaluated in SUNLIGHT, an international, randomized, open label study in patients with previously treated metastatic colorectal cancer
The study population characteristics were: median age 63 years (20 to 90 years); 52% male; 88% White, 1.4% Black, 0.2% Asian, 0.2% American Indian or Alaska Native, and 9.6% were unknown; and baseline ECOG performance status 0 (46%), 1 (54%), or 2 (0.2%).
Serious adverse reactions occurred in 25% of patients. The most frequent serious adverse reactions (≥2%) were intestinal obstruction (2.8%), and COVID-19 (2%). Fatal adverse reactions occurred in 1.2% of patients who received LONSURF in combination with bevacizumab, including rectal fistula (0.4%), bowel perforation (0.4%) and atrial fibrillation (0.4%).
Permanent treatment discontinuation due to an adverse reaction occurred in 13% of patients. The adverse reaction which resulted in permanent treatment discontinuation in ≥2% of patients was fatigue.
Dosage reductions due to an adverse reaction or laboratory abnormality occurred in 7% of patients. At least one dose reduction in 3.7% of patients was required for neutropenia.
Dosage interruptions due to an adverse reaction occurred in 11% of patients who received LONSURF in combination with bevacizumab. The adverse reaction that required dosage interruption in ≥2% of patients was nausea.
The most common adverse reactions or laboratory abnormalities (≥20% in incidence) in patients treated with LONSURF in combination with bevacizumab were neutropenia, anemia, thrombocytopenia, fatigue, nausea, increased aspartate aminotransferase, increased alanine aminotransferase, increased alkaline phosphatase, decreased sodium, diarrhea, abdominal pain, and decreased appetite.
Metastatic Gastric Cancer
The safety of LONSURF was evaluated in TAGS, an international, randomized (2:1), double-blind, placebo-controlled trial in patients with metastatic gastric or gastroesophageal junction (GEJ) adenocarcinoma who were previously treated with at least 2 prior chemotherapy regimens for advanced disease
The study population characteristics were: median age 63 years (24 to 89 years); 73% male; 70% White, 16% Asian, and 1% Black.
The most common adverse reactions or laboratory abnormalities (≥10% in incidence) in patients treated with LONSURF at a rate that exceeds the rate in patients receiving placebo were neutropenia, anemia, nausea, decreased appetite, thrombocytopenia, vomiting, and diarrhea.
In TAGS, 13% of patients discontinued LONSURF for an adverse reaction and 11% of patients required a dose reduction. The most common adverse reactions or laboratory abnormalities leading to dose reduction were neutropenia, anemia, febrile neutropenia, and diarrhea.
Table 7 and Table 8 list the adverse reactions and laboratory abnormalities (graded using CTCAE v4.03), respectively, observed in TAGS.
In TAGS, pulmonary emboli occurred more frequently in LONSURF-treated patients (3.1%) compared to 1.8% for patients on placebo.
Additional Clinical Experience
Interstitial lung disease was reported in 15 (0.2%) patients, 3 of which were fatal, among approximately 7,000 patients exposed to LONSURF in clinical studies and clinical practice settings in Asia.
4DESCRIPTION
LONSURF contains trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5.
Trifluridine
Trifluridine, a nucleoside metabolic inhibitor, is described chemically as 2’-deoxy-5-(trifluoromethyl) uridine and has the following structural formula:
Trifluridine has a molecular formula C
Tipiracil hydrochloride
Tipiracil hydrochloride, a thymidine phosphorylase inhibitor, is described chemically as 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4-(1
Tipiracil hydrochloride has a molecular formula C
LONSURF (trifluridine and tipiracil) tablets for oral use contain 15 mg of trifluridine and 6.14 mg of tipiracil equivalent to 7.065 mg of tipiracil hydrochloride or 20 mg of trifluridine and 8.19 mg of tipiracil equivalent to 9.420 mg of tipiracil hydrochloride.
LONSURF tablets contain the following inactive ingredients: lactose monohydrate, pregelatinized starch, stearic acid, hypromellose, polyethylene glycol, titanium dioxide, ferric oxide, and magnesium stearate. The tablets are imprinted with ink containing shellac, ferric oxide red, ferric oxide yellow, titanium dioxide, FD&C Blue No. 2 Aluminum Lake, carnauba wax, and talc.
5REFERENCES
1. “OSHA Hazardous Drugs”. OSHA.
6HOW SUPPLIED/STORAGE AND HANDLING
LONSURF 15 mg/6.14 mg tablets are supplied as white, biconvex, round, film-coated tablet, imprinted with ‘15’ on one side, and ‘102’ and ’15 mg’ on the other side, in gray ink. The tablets are packaged in HDPE bottles with child resistant closures in the following presentations:
- 20 count: NDC 64842-1025-1
- 40 count: NDC 64842-1025-2
- 60 count: NDC 64842-1025-3
LONSURF 20 mg/8.19 mg tablets are supplied as pale red, biconvex, round, film-coated tablet, imprinted with ‘20’ on one side, and ‘102’ and ‘20 mg’ on the other side, in gray ink. The tablets are packaged in HDPE bottles with child resistant closures in the following presentations:
- 20 count: NDC 64842-1020-1
- 40 count: NDC 64842-1020-2
- 60 count: NDC 64842-1020-3
Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature].
LONSURF is a cytotoxic drug. Follow applicable special handling and disposal procedures.
If stored outside of original bottle, discard after 30 days.
7PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (
Severe Myelosuppression
Advise patients to immediately contact their healthcare provider if they experience signs or symptoms of infection and advise patients to keep all appointments for blood tests
Gastrointestinal Toxicity
Advise patients to contact their healthcare provider for severe or persistent nausea, vomiting, diarrhea, or abdominal pain
Administration Instructions
Advise patients that LONSURF is available in two strengths and they may receive both strength tablets to provide the prescribed dosage.
Advise patients to take LONSURF with food
Advise patients not to retake doses of LONSURF that are vomited or missed and to continue with the next scheduled dose.
Advise patients that anyone else who handles their medication should wear gloves
Embryo-Fetal Toxicity
Advise pregnant women and females of reproductive potential of the potential risk to the fetus. Advise females to inform their healthcare provider of a known or suspected pregnancy
Advise female patients of reproductive potential to use effective contraception during treatment with LONSURF and for at least 6 months after the final dose
Advise males with female partners of reproductive potential to use condoms during treatment with LONSURF and for at least 3 months after the final dose
Lactation
Advise women not to breastfeed during treatment with LONSURF and for 1 day following the final dose
Manufactured by: Taiho Pharmaceutical Co., Ltd., Japan
LONSURF is a registered trademark of Taiho Pharmaceutical Co., Ltd. used under license by
8PRINCIPAL DISPLAY PANEL
NDC 64842-1025-1
Lonsurf
15 mg/6.14 mg
20 tablets
Rx only
NDC 64842-1025-1
Lonsurf
15 mg/6.14 mg
For oral administraion
Rx only
NDC 64842-1025-2
Lonsurf
15 mg/6.14 mg
40 tablets
Rx only
NDC 64842-1025-2
Lonsurf
15 mg/6.14 mg
For oral administraion
Rx only
NDC 64842-1025-3
Lonsurf
15 mg/6.14 mg
60 tablets
Rx only
NDC 64842-1025-3
Lonsurf
15 mg/6.14 mg
For oral administraion
Rx only
NDC 64842-1020-1
Lonsurf
20 mg/8.19 mg
20 tablets
Rx only
NDC 64842-1020-1
Lonsurf
20 mg/8.19 mg
For oral administraion
Rx only
NDC 64842-1020-2
Lonsurf
20 mg/8.19 mg
40 tablets
Rx only
NDC 64842-1020-2
Lonsurf
20 mg/8.19 mg
For oral administraion
Rx only
NDC 64842-1020-3
Lonsurf
20 mg/8.19 mg
60 tablets
Rx only
NDC 64842-1020-3
Lonsurf
20 mg/8.19 mg
For oral administraion
Rx only
