Revotar is continuously developing further innovative chemical structures acting as selectin antagonists (new generation compounds). While designing these molecules, the scientists at Revotar employ a wide spectrum of rational drug design techniques. The discovery platform established at Revotar comprises computational chemistry, organic synthesis and a broad portfolio of bio-assays for compound profiling. Having physicochemical and pharmacological boundaries in mind and taking advantage of virtual screening methods, the employees of Revotar were able to identify promising small molecules (Molecular Weight < 500) acting as selectin antagonists.

The New Generation program revealed compounds which:

• Have drug-like properties (e.g. fulfill Lipinsky rules)
• Are novel SMDs with carbohydrate free backbone
• Are potent (pan-) selectin antagonists (nM IC50s in in vitro binding) [Kranich et al., J Med Chem. 2007]
• Show anti-inflammatory efficacy in several selectin-dependent animal models
• Are available for oral, intravenous and inhalative application
• Are protected by a substantial patent portfolio (composition of matter)

Since selectins are involved in the pathogenesis of most inflammatory diseases there is a broad spectrum of therapeutic areas as options for development of New Generation substances.

Revotar currently focuses on developing its New Generation selectin antagonists for respiratory inflammatory indications like COPD and ALI

ongoing/planned activities:

• Extended in vivo evaluation of promising candidates
• Evaluate different indication tailored formulations (e.g. oral or inhalation for COPD)
• Scale-up synthesis of selected compounds
• Start regulatory preclinical safety package