Drug intelligence / Profile preview

tucatinib + trastuzumab + fluorouracil + leucovorin + oxaliplatin

Development stage
Unknown
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral (tucatinib), Intravenous (trastuzumab, Fluorouracil, Leucovorin, Oxaliplatin)
01

Overview

This drug is a combination regimen of five agents: **tucatinib** (a selective, reversible small molecule tyrosine kinase inhibitor of HER2), **trastuzumab** (a recombinant humanized IgG1 monoclonal antibody that binds to the extracellular domain of HER2), **fluorouracil** (a pyrimidine antimetabolite that inhibits thymidylate synthase, blocking DNA synthesis), **leucovorin** (a reduced folate used to enhance the cytotoxic and antitumor effects of fluorouracil), and **oxaliplatin** (a platinum-based alkylating agent that cross-links DNA and inhibits replication and transcription). This multidrug combination targets the **HER2-positive pathway** in cancer, combining direct HER2 inhibition and chemotherapy. It is primarily under investigation for metastatic HER2-positive colorectal cancer and has been studied in the MOUNTAINEER-03 and related trials. Tucatinib is developed by Seagen, trastuzumab by Genentech/Roche, fluorouracil and leucovorin are generics, and oxaliplatin is originally by Sanofi.

Brand names
Tukysa (for tucatinib)Herceptin (for trastuzumab)None (for fluorouracil, generic)None (for leucovorin, generic)Eloxatin (for oxaliplatin)
Other names
TUKYSA + Herceptin + 5-FU + leucovorin + Eloxatin (regimen)HER2-targeted regimen with tucatinibHER-2-targeted regimen with tucatinibHER 2-targeted regimen with tucatinib
02

Targets

TS (Thymidylate synthase)DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)

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