Drug intelligence / Profile preview

tp-1454

Development stage
Phase 1
Lead developer
Sumitomo Pharma America
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

TP-1454 is an orally administered small molecule that acts as a selective activator of the pyruvate kinase M2 isoform (PKM2), a key enzyme in glycolysis. By activating PKM2, TP-1454 aims to reprogram tumor metabolism and modulate the tumor immune microenvironment, potentially destabilizing regulatory T cells and enhancing anti-tumor immune responses. It is being developed primarily for the treatment of advanced metastatic or progressive solid tumors, both as monotherapy and in combination with immune checkpoint inhibitors such as ipilimumab and nivolumab. The drug was originally developed by Tolero Pharmaceuticals and is currently under development by Sumitomo Pharma America (formerly Sumitomo Dainippon Pharma Oncology)[2][3][7]. TP-1454 represents the first PKM2 activator evaluated in cancer patients[7].

02

Targets

PKM2 (Pyruvate kinase M2 isoform)

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