Trifluridine-tipiracil (Lonsurf)

Other Medications · Approved since 2015

US FDA Approved Oral 3 Clinical Trials
Thymidine phosphorylase DNA synthesis

Description

Trifluridine-tipiracil is an oral nucleoside antimetabolite chemotherapy combination agent approved for treatment of metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy. The medication combines trifluridine, a thymidine-based nucleoside analog, with tipiracil hydrochloride, a thymidine phosphorylase inhibitor that enhances trifluridine bioavailability. It serves as a later-line treatment option for patients with refractory metastatic colorectal cancer who have exhausted standard chemotherapy regimens.

Mechanism of Action

Trifluridine is incorporated into DNA during replication, causing DNA dysfunction and ultimately cell death through its cytotoxic effects on rapidly dividing cancer cells. Tipiracil hydrochloride inhibits thymidine phosphorylase, the enzyme responsible for trifluridine degradation, thereby increasing and maintaining therapeutic levels of trifluridine in plasma and tumor tissues.

Molecular Targets

Side Effects

Neutropenia Anemia Thrombocytopenia Fatigue Nausea Diarrhea Decreased appetite Vomiting Abdominal pain

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT07527858 Phase 2
Recruiting
Study of Denikitug (GS-1811) Given Alone or With Nivolumab or With Chemotherapy in Adults With Advanced Colorectal Cancer
United States, Australia
NCT06607458 Phase 2
Recruiting
Evaluation of the Safety and Efficacy of Treatment w/High Dose Melphalan Given Directly Into the Liver Followed by Treatment w/Approved Cancer Treatment or Approved Cancer Treatment Alone in Patients w/ Metastatic Colorectal Cancer w/Liver Dominant Diseas
United States, Czechia, Germany, Italy, Netherlands, Serbia, Spain, Turkey (Türk
NCT06887218 Phase 2
Recruiting
5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer
United States