Revotar Biopharmaceuticals AG is focusing on an emerging, but challenging target space involved in diverse levels of inflammation/immunological response: Glycan binding proteins being involved in host pathogen interactions, initiation of innate immunity, modulation of adaptive immunity and playing an important role in autoimmunity.

Lectins represent a major group of glycan binding proteins, including the family of selectins (E-, P-, L-selectin).

Selectins, as many other lectins, are challenging to target by drug discovery, due to many reasons:

• Complex carbohydrate-protein interactions
• Multimerization needed for high avidity
• Often functional redundancy of ligands and receptors
• Multiple spots to address on binding domain
• Binding domain often rather flat – with no favorable cavities
• Ligands and receptors subject of activity relevant posttranslational modification (e.g. glycosylations)
• In-vitro assays and in-vivo models may not correlate well
• Not always easily addressed by ‘classic’ discovery (e.g. HTS)
• In the past: glycomimetic drugs often not drug-like

Revotar‘s R&D platform reproducibly proofed to cope with challenging drug discovery & development of glycan-binding protein antagonists:

Successful drug development of

• worldwide most advanced pan-selectin antagonist Bimosiamose
• Successful preclinical & clinical development including several Phase II studies

Successful de novo drug discovery of

• Innovative anti-inflammatory (pan)-selectin antagonists (New Generation Program)
• Highly competitive in vitro/in vivo profile
• Status: early preclinical development

Further reading:
Kooyk & Rabinovich, Protein-glycan interactions in the control of  innate and adaptive immune responses. NATURE IMMUNOLOGY 9, 2008 [link to pubmed]
Varki A, et al, editors.  Essentials of Glycobiology. 2nd edition. Cold Spring Harbor (NY): Cold Spring Harbor Laboratory Press; 2009.[link to pubmed]