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Jun 12, 2012

Boehringer Ingelheim, Polyphor Partner on Macrocyclic Drug R&D

  • Boehringer Ingelheim and Polyphor inked a research collaboration and license agreement through which the latter will apply its MacroFinder® drug discovery platform to identify and optimize macrocyclic drugs against targets selected by BI. The project will focus on targets such as protein-protein interactions that are intractable to small molecule drug discovery approaches. Under terms of the deal BI will be responsible for the development and commercialization of drug candidates, and will pay Polyphor an up-front fee, research funding, and development milestones, plus sales royalties.

    “The conclusion of this agreement constitutes both a scientific and commercial validation of the MacroFinder platform,” comments Jean-Pierre Obrecht, Polyphor’s CEO. “This first MacroFinder collaboration complements the PEMfinder collaboration established with Novartis two years ago.”

    Polyphor is exploiting its PEMfinder and MacroFinder platforms through drug discovery collaborations and to develop an in-house pipeline of Protein Epitope Mimetic (PEM) drugs. The synthetic MacroFinder molecules are generated from modular subunits that can be assembled to display a combination of functional groups to which substituents can be attached. The PEM molecules are fully synthetic cyclic peptide-like molecules that mimic the ß-hairpin and the α-helix motifs that represent the most common secondary protein structures involved in protein-protein interactions (PPIs).

    Both MacroFinder and PEMfinder molecules are fully synthetic, macrocyclic molecules designed to modulate complex PPI targets. But while PEMfinder is designed to addresses mainly extracellular large surface PPI-targets, MacroFinder molecules are designed to penetrate into cells and target intracellular PPIs.

    Polyphor’s in-house pipeline is headed by POL6326, a CXCR4 antagonist which is in Phase II trials as a stand-alone therapy in multiple myeloma patients undergoing autologous hematopoietic stem cell transplantation. POL6326 is also poised to start in Phase II trials as an anticancer agent, and for applications in tissue repair. The firm’s clinical pipeline also includes the PEM platform derived antibiotic candidate POL7080 which is in Phase I trials against Psuedomonas aeruginosa infections. 

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