Inspired by Nature

At the core of Rapafusyn’s platform are its proprietary diverse libraries of FKBP-binding molecular glue macrocycles (RapaGlues™). These RapaGlue™-FKBP complexes present target-specific “effector domain” of the macrocycles to modulate challenging disease targets.  

About Us

At Rapafusyn, we are developing non-degrading molecular glues to tackle difficult drug targets to improve patient outcomes. Rapafusyn has designed and generated large DNA encoded libraries (DELs) and arrayed libraries of non-degrading molecular glues (RapaGlues™) that are designed on a FKBP-binding macrocyclic peptide platform. These libraries have been successful in generating novel chemical starting points for hard-to-drug targets, often with cell permeability right from screening. Moreover, as our molecules are molecular glues, the target-binding peptidic portion is more tunable than traditional macrocyclic peptides.

Our platform targets intracellular proteins and the intracellular domain of transmembrane proteins, such as SLCs and GPCRs. Our modular architecture, chemical, and biological capabilities enable rapid SAR expansion to optimize potency, selectivity, and physiochemical properties to accelerate drug discovery.

Targeting Undruggable Proteins by creating novel protein-protein interactions.

RapaGlues™ are cell-permeable macrocycles that combine an FKBP recognition domain with a small peptidic fragment.  RapaGlues™ drive the assembly of a protein-sized active complex inside the cell by bringing together the abundant intracellular protein FKBP with a target of interest. This complex disrupts the target from binding to its native interaction partner driving therapeutic benefit.

Broad Potential of the Platform

The Rapafusyn platform allows for drugging a wide range of intracellular and transmembrane targets with our molecular glues.

Inhibiting PPIs and intracellular domains of transmembrane proteins are targets where our modality may have advantages over other approaches.

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