Clin. Established chemical inhibitors, such as okadaic acid and cantharidin, are toxic and have limited clinical utility. A 2016 Phase I clinical trial was completed for LB100 in combination with Docetaxol for the treatment of solid tumors . Targets PP2A : In vitro: LB-100 inhibits the cell growth with IC50 of 2.3 μM (in BxPc-3) or 1.7 μM (in Panc-1 cell). Background: - Primary gliomas are an incurable disease in spite of aggressive multimodality therapy consisting of craniotomy, irradiation, and chemotherapy.Therapeutic options for patients with recurrent glioma are limited, and there is an unmet need to identify more effective agents. Similarly, a new BET inhibitor now in clinical trials, BI 894999, reduces tumor growth in vivo and synergistically induces cell death when combined with CDK9 inhibitors, supporting the use of these epigenetic inhibitors in combination strategies .
You may want to think about taking part in a clinical trial. LB-100 is a novel small molecule inhibitor of PP2A. 3.1. PP2A inhibition in … In pre-clinical studies, LB-100, a novel small molecule inhibitor of PP2A, inhibits the growth of a broad spectrum of leukemic and solid tumor cell lines. Protein phosphatase 2A (PP2A) has been proposed as a target for cancer immunotherapy. The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. 5). In addition, a PP2A specific inhibitor LB-100 (in clinical trial for solid tumors) was employed to pharmacologically inhibit PP2A activity. Low micromolar concentrations of LB-100 induced cell death in patient-derived ALL xenografts in parallel with ROS-accumulation and increased S6 and H2AX phosphorylation. Cantharidin, an inhibitor of PP1, PP2A, PP4 and PP5, has been used as an anticancer agent in traditional medicine but has been largely ignored by Western medicine due to toxicities.
Fostriecin, a potent and selective inhibitor of PP2A, was tested as a cancer therapy in a phase I clinical trial but the trial was suspended due to drug instability.
Upon injection, PP2A inhibitor LB-100 inhibits the removal of phosphate groups from proteins essential for cell cycle progression. Cancer Therapy: Clinical Safety, Tolerability, and Preliminary Activity of LB-100, an Inhibitor of Protein Phosphatase 2A, in Patients with Relapsed Solid Tumors: An Open-Label, Dose Escalation, First-in-Human, Phase I Trial Vincent Chung1, Aaron S. Mansfield2, Fadi Braiteh3,4, Donald Richards4,5, Listing a study does not mean it has been evaluated by the U.S. Federal Government. Know the risks and potential benefits of clinical studies and talk to your health care provider before participating. Indeed, new … LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. In addition, a PP2A specific inhibitor LB-100 (in clinical trial for solid tumors) was employed to pharmacologically inhibit PP2A activity. A water soluble inhibitor of the protein phosphatase 2A (PP2A), with potential chemo- and radiotherapy enhancing activity. Fostriecin, another selective inhibitor of PP2A, was evaluated in several NCI (Bethesda, MD)-sponsored phase I trials over 20 years ago. For patients interested in enrolling in the NCI clinical study, please contact NCI’s toll-free number 1-800-4-Cancer (1-800-422-6237) ... PP2A Inhibitor LB …
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