Trifluridine and Tipiracil · Lonsurf, TAS 102

What is Trifluridine and Tipiracil?

Trifluridine/tipiracil is a combination of a nucleoside analog and a thymidine phosphorylase inhibitor. Trifluridine is incorporated into DNA to inhibit synthesis and cell proliferation; tipiracil blocks trifluridine metabolism to increase its exposure and has anti-angiogenic activity.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Lonsurf, TAS 102, Trifluridine/Tipiracil

Drug type

Small molecule

Targets

thymidylate synthase (TYMS), thymidine phosphorylase (TYMP)

Mechanism

Inhibitor of thymidylate synthase (TYMS) and thymidine phosphorylase (TYMP)

Pathways

DNA synthesis, nucleotide metabolism, angiogenesis

Therapy area

Oncology

Developer

Taiho Oncology

In trials of

ABBV, INBX, MRK, ONCY

FDA status

Approved as Lonsurf (September 22, 2015), NDA207981 · FDA label

✅ FDA-approved uses

• Metastatic colorectal cancer
• Metastatic gastric or gastroesophageal junction adenocarcinoma

From the indications section of the FDA label (version of Nov 5, 2025). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Anal Cancer MetastaticBiliary Tract Cancer (BTC)Colorectal AdenocarcinomaColorectal CancerEwing SarcomaGastric or Gastroesophageal Junction AdenocarcinomaPancreatic Cancer MetastaticPancreatic Ductal AdenocarcinomaSquamous Cell Carcinoma of the Anus Stage UnspecifiedUnresectable Pancreatic Carcinoma

Other drugs acting on TYMS / TYMP

Sources

• FDA label (DailyMed)
• FDA label Lonsurf (2025-11-05), indications
• NCI Thesaurus
• ClinicalTrials.gov NCT05482893
• ClinicalTrials.gov NCT07280377

Updated Oct 3, 2026.