Drug intelligence / Profile preview

KAT-101

Development stage
Phase 2
Lead developer
New G Lab Pharma
Modality
Small Molecules
Administration
Oral, Intratumoral
01

Overview

KAT-101 is a small molecule derivative of 3-bromopyruvic acid under development for the treatment of various cancers, including metastatic hepatocellular carcinoma (HCC), bladder cancer, melanoma, pancreatic cancer, leukemia, fibrolamellar hepatocellular carcinoma (FLC), non-small-cell lung cancer (NSCLC), acute myeloid leukemia (AML), and uterine cancer[1][3][4][8]. The drug acts by targeting glyceraldehyde 3-phosphate dehydrogenase (GAPDH) to disrupt both glycolysis and mitochondrial oxidative phosphorylation in cancer cells. This dual inhibition leads to depletion of adenosine triphosphate (ATP) levels within tumor cells, thereby limiting their energy supply and inducing apoptosis while preventing proliferation[1][3]. Clinical trials are ongoing to evaluate its safety and efficacy in HCC using oral and intratumoral administration routes[2][4][5].

Other names
bromopyruvate3-bromopyruvic acid3-bromo-2-oxopropanoic acid
02

Targets

LDH (L-lactate dehydrogenase A chain)VDAC (Voltage-dependent anion channel)MCT4 (Monocarboxylate transporter 4)GAPDH (Glyceraldehyde-3-phosphate dehydrogenase)PDK (Pyruvate dehydrogenase kinase isoform 1)PDH (Pyruvate dehydrogenase complex)HK2 (Hexokinase Type II)OXPHOS (Mitochondrial OXPHOS complexes)

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