Pelofen, a novel microtubule stabilizing agent for second-line treatment strategies in multidrug resistant oncology patients

01 November 2017 → 31 May 2020
Regional and community funding: Industrial Research Fund
Research disciplines
  • Natural sciences
    • Inorganic chemistry
    • Organic chemistry
    • Theoretical and computational chemistry
    • Other chemical sciences
Microtubule Stabilizing Agents (MSA) Chemotherapy Anti-mitotic Peloruside
Project description

Over the past 15 years, several studies have generated promising results with Peloruside A as a potential anti-cancer agent against a wide range of cancer cells. The main characteristic of Peloruside is the non-taxoid binding site on tubulin, which makes it possible to maintain potency in PTX-resistant cancer cells. The research group has made a diagnosis of cytotoxic substances with a microtubule inhibitor activity, with the potential of paclitaxel bridged.

During the IOF project applications and further in vitro and in ovo characterization, the chemical synthesis process has been optimized and results in a wide range of Peloruside analogues. Pelofen B is the most powerful of all manufactured analogues so far, it is currently available in quantities of in vivo tests from the feed. For example, we wish to evaluate the therapeutic potential of Pelofen as a second-line monotherapy in patients with multi-drug resistant cancer and / or in combination with paclitaxel therapy. Recently, Pelofen received IP protection in the US as well as protection in Europe.

The goal of this project is to determine the therapeutic value of Pelofen and generate solid data to present a partner with a view to a licensing deal. There are also a number of medical conditions: Strong IP position with a patent, a scalable synthesis process, in vitro evidence of efficacy in PTX-resistant cells, good solubility-sensitivity properties and suitability of compound available for preclinical in vivo evaluation in terms of efficacy and safety . Pelofen has great potential to become clinically relevant MSA therapeutics for treatment of many cancers.