Nestor, J.J., Jr. (2009) Curr Med Chem 16(33): pp4399-4418.
The shortcomings of native peptides as pharmaceuticals have been long known: short duration of action, lack of receptor selectivity, lack of oral bioavailability. However medicinal chemistry offers solutions to the first two limitations and oral bioavailability issues have been addressed with novel routes of administration (e.g. intranasal, inhalation) and injectable depot formulations. The principal issue for peptide drugs has been a short duration of action, widely assumed to be due to proteolysis. While proteolysis is a problem for native peptide structures, modification of the peptide structure by acylation, PEGylation, unnatural amino acids or restricted conformation can largely remove this issue. However rapid clearance from the blood into the urine remains an issue for even proteolytically stable molecules. Medicinal chemistry approaches here have been peptide modifications to slow release from the injection site (hydrophobic, hydrophilic, selfassociating depots), PEGylation, fatty acid acylation, and the like. Medicinal chemistry approaches used in successful peptide pharmaceuticals using unnatural amino acids to achieve depot formation are highlighted in this review.
Genetic Engineering and Biotechnology News Jan. 15, 2013 GEN News Highlights.
Velocity Pharmaceutical Development (VPD) will use a special-purpose virtual development company to carry out research and development of new peptide drugs.
VPD’s development team will manage the development program, which will use EuMederis Pharmaceuticals' EuPort™ technology for improving the design, synthesis, and delivery of peptides. EuPort uses a chemical modification to increase the duration of action and bioavailability of peptides, generating what the company called optimized new chemical entities. The technology is designed to help develop the drugs quickly as well as counteract the short duration of action and self-injection requirements of typical peptide drugs, which limit their utility.
JANUARY 21, 2013
A licensing deal between two California pharmaceutical companies has resulted in the formation a new San Francisco startup developing an unspecified peptide drug candidate.
With the creation of the virtual company Spitfire Pharma Inc., Velocity Pharmaceutical Development LLC said it’s pursuing a drug development program that uses EuMederis Pharmaceuticals’ EuPort technology to improve the design, synthesis and delivery of peptide drugs. According to a recent SEC filing, it looks like the company is getting off the ground by opening a $9.5 million round of financing, at least half a million of which has already been secured.
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