KAT-101 + KAT-201

KAT-101 + KAT-201 is a combination of two clinical derivatives of 3-bromopyruvate (3BP), an alkylating small molecule anti-metabolite that targets key substrates in cancer metabolism. KAT-101 is formulated for oral administration, while KAT-201 is for intratumoral injection. Both are being developed primarily for the treatment of cancers such as lymphoma and hepatocellular carcinoma. The combination aims to enhance antitumor activity by exploiting the metabolic vulnerabilities of cancer cells, inducing cytotoxicity, and overcoming resistance to standard therapies. Preclinical data indicate synergistic efficacy for the combination in animal models of lymphoma, especially in resistant cases, with enhanced tumor regression and minimal weight loss. The main mechanism involves inhibition of glycolysis and other cancer metabolic pathways, primarily through alkylation and inhibition of hexokinase 2 (HK2) and monocarboxylate transporter 1 (MCT1), leading to energy deprivation and cell death in tumor cells[1][2].

Other names

KAT/3BP combination