Bioequivalence Study of Trifluridine and Tipiracil Hydrochloride Tablets on Fasting and Fed in Humans

NCT07492173 | Completed

• 1 other identifier: NTP-FTDTPI-T-BE01
• Study Type: interventional
• Target: 76
• Locations: 1 country
• Sites: 1

Brief Summary

The test formulation of Trifluridine and Tipiracil Tablets (20 mg) is bioequivalent to the reference formulation (Lonsurf®) in Chinese patients with solid tumors under fed and fasting conditions.

Conditions

Solid Tumor Cancer

Outcome Measures

Primary Outcomes (3)

• Peak Plasma Concentration (Cmax)

  24 hours post-dose in each period

• Area under the plasma concentration versus time curve (AUC) 0-t

  24 hours post-dose in each period

• Area under the plasma concentration versus time curve (AUC)0-∞

  24 hours post-dose in each period]

Secondary Outcomes (4)

• maximum plasma concentration (tmax)

  24 hours post-dose in each period

• elimination rate constant（λz）

  24 hours post-dose in each period

• terminal elimination half-life（t1/2）

  24 hours post-dose in each period

• Percentage of residual area（AUC_%Extrap）

  24 hours post-dose in each period

Study Arms (2)

Fasting

OTHER

Drug: Trifluridine and Tipiracil Tablets; Drug: Lonsurf®

Feed

OTHER

Drug: Trifluridine and Tipiracil Tablets; Drug: Lonsurf®

Interventions

Trifluridine and Tipiracil Tablets DRUG

strength: Trifluridine 20 mg, Tipiracil Hydrochloride 9.420 mg (equivalent to Tipiracil 8.19 mg) (strength abbreviated as 20 mg expressed as Trifluridine), batch number: 304220201, manufacturing date: February 23, 2022, tentative expiry date: January 2024; Manufactured by Shandong New Time Pharmaceutical Co., Ltd. Three tablets each time.

Fasting; Feed

Lonsurf® DRUG

Trifluridine and Tipiracil Tablets, strength: 20 mg (expressed as Trifluridine), batch number: 0K71, manufacturing date: November 2, 2020, expiry date: November 1, 2023; Manufactured by Taiho Pharmaceutical Co., Ltd. Kitajima Plant. Three tablets each time.

Fasting; Feed

Eligibility Criteria

• Age: 18 Years - 70 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Aged 18-70 years (inclusive), male or female;
• Patients with solid tumors confirmed by histopathology or cytology;
• Expected survival \> 3 months;
• Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1;
• Able to take oral medication (i.e., not using a feeding tube);
• Adequate organ function based on the following laboratory values obtained within 7 days prior to the first dose:
• Hemoglobin (HB) ≥ 100 g/L;
• Absolute neutrophil count (ANC) ≥ 1.5 × 10⁹/L;
• Platelets (PLT) ≥ 80 × 10⁹/L;
• Total serum bilirubin (TBIL) ≤ 1.5 × upper limit of normal (ULN);
• Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) ≤ 2.5 × ULN, or ≤ 5 × ULN in the presence of liver metastases;
• Creatinine clearance (Ccr) ≥ 60 mL/min;
• Urine protein \< 2+;
• International normalized ratio (INR) \< 1.5; activated partial thromboplastin time (APTT) and prothrombin time (PT) ≤ 1.5 × ULN;
• Normal electrocardiogram or electrocardiogram abnormalities determined by the investigator to be not clinically significant.

You may not qualify if:

• Presence of severe diseases or serious medical conditions (e.g., ileus, gastrointestinal bleeding, intestinal obstruction, pulmonary fibrosis, uncontrolled diabetes (fasting blood glucose (FBG) \> 10 mmol/L), renal insufficiency, hepatic insufficiency, mental illness, cerebrovascular disease, ulcers requiring blood transfusion, etc.);
• Presence of ascites, pleural effusion, or pericardial effusion requiring drainage within 4 weeks prior to screening;
• Occurrence of myocardial infarction, severe/unstable angina pectoris, or symptomatic congestive heart failure of New York Heart Association (NYHA) class III or IV within 12 months prior to the first dose;
• Any clinically significant abnormality in hepatitis B virus surface antigen, Treponema pallidum specific antibody, human immunodeficiency virus antibody, or hepatitis C virus antibody;
• Patients with autoimmune diseases requiring immunosuppressive therapy or a history of organ transplantation;
• Known brain metastases or clinical symptoms suggestive of brain metastases;
• Presence of active infection (i.e., body temperature ≥ 38°C due to infection);
• Any unresolved toxicity of CTCAE grade 2 or higher from any previous treatment (excluding anemia, alopecia, skin pigmentation, and chemotherapy-induced neurotoxicity);
• Receipt of any of the following treatments within the specified time frame prior to screening:
• Major surgery within 4 weeks (major surgery: laparotomy, thoracotomy, and visceral resection by laparoscopic surgery);
• Any anti-tumor therapy within 2 weeks;
• Any investigational drug within 4 weeks;
• Blood transfusion within 2 weeks.
• Prior history of gastrectomy;
• Pregnant or breastfeeding women;

Sponsors & Collaborators

• Shandong New Time Pharmaceutical Co., LTD: lead

Study Sites (1)

Hunan Cancer Hospital

Changsha, Hunan, China

Location

MeSH Terms

Interventions

Trifluridine; tipiracil; trifluridine tipiracil drug combination

Intervention Hierarchy (Ancestors)

Thymidine; Pyrimidine Nucleosides; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Deoxyribonucleosides; Nucleosides; Nucleic Acids, Nucleotides, and Nucleosides

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 19, 2026
• First Posted: March 25, 2026
• Study Start: November 21, 2022
• Primary Completion: June 25, 2023
• Study Completion: June 25, 2023
• Last Updated: March 25, 2026

Record last verified: 2026-03

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)