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Palatin uses a rational drug design approach to discover and develop proprietary peptide, peptide mimetic and small molecule agonist compounds, focusing on melanocortin and natriuretic peptide receptor systems. CADD (computer-assisted drug design) receptor homology models are iteratively optimized based on experimental results with Palatin’s extensive in-house peptide and small molecule libraries, supported by conformational analyses of peptide ligands in solution utilizing NMR (nuclear magnetic resonance) spectroscopy. By integrating both technologies Palatin is developing an advanced understanding of the factors which drive agonism. All of the lead compounds in clinical development were developed by Palatin researchers. Palatin has developed a series of proprietary technologies used in its drug development programs. One technology employs novel amino acid mimetics in place of selected amino acids. These mimetics provide the receptor-binding functions of conventional amino acids, while providing structural, functional and physiochemical advantages. The amino acid mimetic technology was employed in PL-3994, Palatin’s compound for treatment of heart failure and difficult-to-control hypertension. The patent-pending amino acid mimetic technology can potentially be used with a wide range of peptide-based compounds. Some compound series have been derived using a proprietary and patented platform technology, called MIDAS™ (Metal Ion-induced Distinctive Array of Structures). This technology employs metal ions to fix the three-dimensional configuration of peptides, forming conformationally rigid molecules that remain folded specifically in their active state. These MIDAS molecules are simple to synthesize, are chemically and proteolytically stable, and have the potential to be orally bioavailable. In addition, MIDAS molecules are information-rich and provide data on structure-activity relationships that can be used to design small molecule, non-peptide drugs. Palatin maintains expertise in both peptide and small molecule chemistries, and has developed a series of drug selection technologies for selecting compounds with desired pharmacological profiles, particularly in the melanocortin receptor field. The drug selection technologies are used to develop and select melanocortin receptor-specific small molecules and peptides with novel properties, including compounds that are effective in the treatment of obesity in animal models but which do not induce a sexual response. Palatin owns 43 issued United States patents and has over 25 pending United States patent applications, many with issued or pending counterpart patents in selected foreign countries. Palatin aggressively seeks patent protection for its technologies and products in the United States and those foreign countries where protection is commercially important. |



