GenSpera (OTCQB:GNSZ) Media Advisory; "Targeting thapsigargin towards tumors" Published in Steroids
SAN ANTONIO - August 28, 2014 (Investorideas.com Biotech Newswire) GenSpera, Inc. (OTCQB:GNSZ), a leader in developing prodrug therapeutics for the treatment of cancer, announces the recent publication of the article "Targeting thapsigargin towards tumors" in the journal Steroids.
The recent article co-authored by Doan, et al. (see full reference below), reviews the evolution and development of GenSpera's prodrug technology platform that is designed to deliver the potent, cytotoxic activity of thapsigargin (from the plant Thapsia garganica) directly to tumors. These efforts led to the development of mipsagargin (G-202), which is now in Phase II clinical trials in liver cancer and brain cancer.
The article details the discovery and isolation of thapsigargin, the elucidation of its molecular structure, and determination of its biochemical and pharmacological activities. These efforts revealed the potential utility of thapsigargin as a potent, but non-selective anti-cancer agent. It was recognized that in order to harness the profound cytotoxic activity of thapsigargin, one would need to develop a way of delivering it specifically to tumors in order to avoid side effects.
The paper also goes on to describe the medicinal chemistry efforts to develop derivatives of thapsigargin in order to create protease-activated prodrugs that could be activated only within the tumors. The in vitro and in vivo experiments led to a number of potentially useful prodrugs directed to the tumor-selective enzymes PSMA, PSA and hK-2. Mipsagargin is the most developmentally advanced drug candidate and is activated by the enzyme PSMA, which is found in the blood vessels of almost all solid tumors.
The review highlights the drug development success that can be achieved through a multidisciplinary and multinational collaboration between academic laboratories and an industrial partner.
Targeting thapsigargin towards tumors
Steroids, available online 24 July 2014, Nhu Thi Quynh Doan, Eleonora Sandholdt Paulsen, Pankaj Sehgal, Jesper Vuust Møller, Poul Nissen, Samuel R. Denmeade, John T. Isaacs, Craig A. Dionne, Søren Brøgger Christensen
GenSpera's technology platform combines a powerful, plant-derived cytotoxin (thapsigargin) with a pro-drug delivery system that provides for the targeted release of drug candidates within a tumor. Unlike typical chemotherapeutic agents, thapsigargin results in cell death irrespective of the rate of cell division, which may provide an effective approach to kill both fast- and slow-growing cancers. GenSpera's lead drug candidate, G-202, is activated by the enzyme PSMA, which is found at high levels in the vasculature of liver and glioblastoma cancers and in the vasculature of almost all other solid tumors. G-202 is therefore expected to have potential efficacy in a wide variety of tumor types.
G-202 Phase II clinical trials are underway in hepatocellular carcinoma, glioblastoma and prostate cancer patients.
Cautionary Statement Regarding Forward Looking Information
This news release may contain forward-looking statements. Investors are cautioned that statements in this press release regarding potential applications of GenSpera's technologies constitute forward-looking statements that involve risks and uncertainties, including, without limitation, risks inherent in the development and commercialization of potential products, uncertainty of clinical trial results or regulatory approvals or clearances, need for future capital, dependence upon collaborators and maintenance of our intellectual property rights. Actual results may differ materially from the results anticipated in these forward-looking statements. Additional information on potential factors that could affect our results and other risks and uncertainties will be detailed from time to time in GenSpera's periodic reports filed with the Securities and Exchange Commission.
Company: Craig Dionne, PhD, CEO GenSpera, Inc. +1-210-479-8112
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