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Trial completion, Enrollment change: Study to Assess the Safety and Pharmacokinetics of WP1122 in Healthy Volunteers (clinicaltrials.gov) - Jan 20, 2023
P1a, N=53, Completed,
X-ray diffraction analysis has been performed for compound WP1122 that was selected for detailed preclinical and subsequent clinical evaluation as potential anticancer or antiviral agent. Active, not recruiting --> Completed | N=80 --> 53
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Enrollment open, Trial completion date, Trial primary completion date: Study to Assess the Safety and Pharmacokinetics of WP1122 in Healthy Volunteers (clinicaltrials.gov) - May 12, 2022
P1a, N=80, Recruiting,
Recruiting --> Active, not recruiting Trial completion date: Jul 2022 --> Oct 2022 | Trial primary completion date: Jul 2022 --> Oct 2022 | Not yet recruiting --> Recruiting
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Trial initiation date: Study to Assess the Safety and Pharmacokinetics of WP1122 in Healthy Volunteers (clinicaltrials.gov) - Feb 15, 2022
P1a, N=80, Not yet recruiting,
Trial completion date: Jul 2022 --> Oct 2022 | Trial primary completion date: Jul 2022 --> Oct 2022 | Not yet recruiting --> Recruiting Initiation date: Jan 2022 --> Apr 2022
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Journal, Epigenetic controller: Synergistic Anticancer Effect of Glycolysis and Histone Deacetylases Inhibitors in a Glioblastoma Model. (Pubmed Central) - Dec 27, 2021
Over the last decade, we have seen tremendous progress in research on 2-deoxy-D-glucose (2-DG) and its analogs...Novel 2-DG analogs such as WP1122 and others have revived the old concept of glycolysis inhibition as an effective anticancer strategy...We focused our efforts on the development of new combinations of anticancer agents coupled with 2-DG and its derivatives, targeting glioblastoma, which is in desperate need of novel approaches and therapeutic options and is particularly suited to glycolysis inhibition, due to its reliance on aerobic glycolysis. Herein, we present evidence that a combined treatment of 2-DG analogs and modulation of histone deacetylases (HDAC) activity via HDAC inhibitors (sodium butyrate and sodium valproate) exerts synergistic cytotoxic effects in glioblastoma U-87 and U-251 cells and represents a promising therapeutic strategy.
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Preclinical, Journal: Hyperpolarized Pyruvate MR Spectroscopy Depicts Glycolytic Inhibition in a Mouse Model of Glioma. (Pubmed Central) - Mar 12, 2020
Large contrast agent-enhanced tumors were shown in mice with glioma at T2-weighted and T1-weighted postcontrast MRI by postimplantation day 40. After treatment with WP1122, a decrease in lactate was observed in mice with glioma (baseline and treatment mean k, 0.027 and 0.018 sec, respectively, P = .01; baseline and posttreatment mean nLac, 0.28 and 0.22, respectively, P = .01) whereas no significant decrease was observed in healthy control mice (baseline and posttreatment mean k, 0.011 and 0.017 sec, respectively, P = .91; baseline and posttreatment mean nLac, 0.16 and 0.21, respectively, P = .84).ConclusionHyperpolarized carbon 13 measurements of pyruvate metabolism can provide rapid feedback for monitoring treatment response in glioma
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