Drug intelligence / Profile preview

Lonsurf + gemcitabine + nab-paclitaxel

Development stage
Unknown
Lead developer
Taiho Oncology
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral, Intravenous
01

Overview

Lonsurf + gemcitabine + nab-paclitaxel is an experimental combination chemotherapy regimen being evaluated for the treatment of advanced pancreatic ductal adenocarcinoma (PDAC). The regimen consists of Lonsurf—a fixed-dose oral combination of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil—administered alongside intravenous gemcitabine and nab-paclitaxel (albumin-bound paclitaxel). Trifluridine exerts its cytotoxic effect by incorporating into viral and cellular DNA, while tipiracil increases trifluridine bioavailability by inhibiting its degradation by thymidine phosphorylase. Gemcitabine further inhibits DNA synthesis by targeting ribonucleoside reductase and incorporating into DNA, and nab-paclitaxel arrests the cell cycle by stabilizing microtubules. This triplet combination is currently being investigated in a Phase I dose-escalation trial sponsored by Patrick Joseph Loehrer Sr. at Indiana University to determine the recommended phase 2 dose (RP2D) for patients with advanced PDAC.

Other names
trifluridine + tipiracil + gemcitabine + nab-paclitaxelTAS-102 + gemcitabine + nab-paclitaxel
02

Targets

CDA (Cytidine deaminase)DNA polymerase familyRNR (Ribonucleotide reductase)TYMP (Thymidine phosphorylase)TUBB (Tubulin (alpha and beta subunits))DNA

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