Data from preclinical research presented in a poster at annual meeting of the American Association for Cancer Research (AACR) being held April 18 – 22, 2015 in, Philadelpphia, PA, demonstrates that BTP-114, a novel, personalized cisplatin prodrug being developed byBlend Therapeutics, Inc. (Watertown, MA 02472), a biopharmaceutical company discovering and developing two distinct classes of targeted anti-cancer medicines to advance the treatment of patients with solid tumors,improved and sustained tumor growth inhibition in preclinical models as compared to the conventional platinum cytotoxic cancer drug, cisplatin.
The novel mechanism of action of BTP-114 […] leverages our growing understanding of disregulated cancer metabolism and the molecular underpinning of cancers, enabling the development of the first personalized platinum marking a major advance in the field of platinum anti-cancer agents…
BTP-114 is Blend Therapeutics? lead product candidate for which the company plans to file an Investigational New Drug (IND) application with the U.S. Food and Drug Administration. Once administered, the trial drug rapidly conjugates to serum albumin in blood with a high degree of specificity, and is preferentially taken up by cancer cells with certain molecular profiles, resulting in enhanced DNA damage and cell death.
Platinum-based therapies
?The novel mechanism of action of BTP-114 […] leverages our growing understanding of disregulated cancer metabolism and the molecular underpinning of cancers, enabling the development of the first personalized platinum marking a major advance in the field of platinum anti-cancer agents,? explained Richard Wooster, PhD, President of Research and Development of Blend. ?Designed to overcome limitations of conventional platinum therapies which are the largest class of oncology drugs today, BTP-114 has the potential to increase the proportion of patients who respond and their duration of response to platinum-based therapies.?
Increasing therapeutic use of platinum
The data presented at AACR describes BTP-114?s novel mechanism as a platinum prodrug of cisplatin that covalently attaches to serum albumin in the blood giving a 15-fold increase in exposure and a predicted human plasma half-life of 10 days. The therapeutic dose of platinum was increased by up to 2-fold, resulting in a 15-fold increase in platinum accumulation in multiple xenograft models. BTP-114 was shown to improve efficacy in models of lung and ovarian cancer compared to cisplatin, while reducing key dose limiting toxicities of cisplatin.
BTP-114 was developed by researchers at Blend Therapeutics and builds on the breakthroughs in platinum chemistry pioneered by the company?s scientific co-founder, Professor Stephen J. Lippard of Massachusetts Institute of Technology (MIT).
Last editorial review: July 3, 2015
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