TAS-102 (Lonsurf)

Other Medications · Approved since 2015

US FDA Approved EU EMA Approved ES Funded by SNS approved in CRC Oral 2 Clinical Trials
DNA synthesis thymidine phosphorylase

Description

TAS-102 (trifluridine/tipiracil) is an oral nucleoside antimetabolite chemotherapy agent approved for the treatment of metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF therapy, and anti-EGFR therapy (if RAS wild-type). This combination drug consists of trifluridine, a thymidine-based nucleoside analog, and tipiracil, a thymidine phosphorylase inhibitor that prevents degradation of trifluridine. TAS-102 provides a treatment option for heavily pretreated patients with refractory metastatic colorectal cancer who have exhausted standard therapeutic options.

Mechanism of Action

Trifluridine is incorporated into DNA after phosphorylation to its active triphosphate form, causing DNA dysfunction and ultimately cell death. Tipiracil enhances the antitumor activity by inhibiting thymidine phosphorylase, thereby maintaining higher concentrations of trifluridine in plasma and tumor tissues.

Molecular Targets

Side Effects

Neutropenia Anemia Thrombocytopenia Fatigue Nausea Decreased appetite Diarrhea Vomiting Abdominal pain Pyrexia

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

Clinical Trials

NCT03520946 Phase 3
Archived
RAMucirumab in Combination Wth TAS102 vs. TAS102 Alone in Chemotherapy Refractory Metastatic Colorectal Cancer Patients
Germany
NCT03305913 Phase 1
Archived
Regorafenib in Combination With TAS-102 in Subjects With Metastatic Colorectal Cancer Who Have Progressed After Standard Therapy
Germany