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murlentamab + trifluridine + tipiracil
- Development stage
- Unknown
- Lead developer
- Exelixis
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination regimen consisting of **murlentamab**, a monoclonal antibody targeting Anti-Müllerian Hormone Receptor II (AMHRII), and **trifluridine + tipiracil** (marketed as Lonsurf), an oral fixed-dose combination of a nucleoside analog (trifluridine) and a thymidine phosphorylase inhibitor (tipiracil). Murlentamab is designed to activate immune response in the tumor microenvironment, primarily through macrophage and T cell activation. Trifluridine is incorporated into DNA, disrupting DNA function in rapidly dividing cancer cells, while tipiracil inhibits thymidine phosphorylase to increase trifluridine bioavailability. This combination has been investigated in phase 2 trials for metastatic colorectal cancer, demonstrating prolonged progression-free survival, particularly in tumors with medium/high AMHRII expression.
- Brand names
- Lonsurf
- Other names
- FTD/TPITAS-102TAS102TAS 102
02
Targets
DNATS (Thymidylate synthase)TYMP (Thymidine phosphorylase)AMHR2 (Anti-Müllerian hormone receptor type 2)
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