LB-100

LB-100 is an investigational small molecule drug that acts as a catalytic inhibitor of serine/threonine protein phosphatases, primarily targeting protein phosphatase 2A (PP2A) and also inhibiting serine/threonine-protein phosphatase 5 (PPP5C). It is being developed for the treatment of various cancers and has demonstrated cytotoxic activity against cancer cells in vitro and antitumor activity in animal models. Mechanistically, by inhibiting PP2A (and PPP5C), LB-100 increases stress signals in tumor cells, stimulates cell proliferation, inhibits DNA repair processes, and enhances the effectiveness of other anticancer therapies such as chemotherapy and immune checkpoint inhibitors. The drug is administered intravenously and has shown a favorable safety profile in phase I clinical trials. It is currently under investigation for several cancer indications including glioblastoma (phase II), myelodysplastic syndromes (phase I/II), ovarian cancer (phase I/II), soft tissue sarcoma (phase I/II), and colorectal cancer (phase I). The developer is Lixte Biotechnology Holdings[1][4][5][6][7].

Other names

protein phosphatase 2A inhibitor LB-100PP2A inhibitor LB-100PP-2A inhibitor LB-100PP 2A inhibitor LB-100