Biopharmaceuticals are increasingly important in the pipelines of major pharmaceutical companies, but key technical issues exist in bringing certain biopharmaceuticals such as peptides to market. Improving delivery technologies, developing peptides with increased stability and half-life, and synthesizing long-chain peptides are some challenges in advancing commercialization.
Compared with other therapeutic proteins, peptides are a niche area. Roughly 430 proteins are in clinical development compared with130 peptides, and 70 proteins are in Phase III and registration compared with 20 peptides (1).
Lured by potential in clinical efficacy, however, the pharmaceutical majors and emerging drug companies are building their pipelines with peptide-based drugs and with technology to optimize the synthesis and delivery of peptides.Pharma majors target peptides
Pfizer. A case in point is Pfizer, Inc. (New York, NY), which earlier this year agreed to acquire BioRexis Pharmaceutical Corporation (King of Prussia, PA), a biopharmaceutical company with several diabetes drug candidates and a protein-engineering technology based upon human transferrin designed to provide therapeutic agents with longer duration of action than synthetic peptides.
BioRexis's lead candidate is a fusion of the well-known glucagon-like peptide (GLP-1), a 30-amino-acid peptide, to transferrin, for treating Type 2 diabetes. Pfizer also is developing a GLP-1 compound (PF 734200) to treat diabetes.
Sanofi-Aventis and Wyeth. Zealand Pharma (Copenhagen, Denmark) is another company specializing in peptide development and technology. Its stabilization of peptide ("SIP") technology is designed to increase biological half-life and improve product stability. Zealand is partnered with Sanofi-Aventis SA (Paris, France) for developing AVE0010, a GLP-1 for treating Type 2 diabetes, and with Wyeth (Madison, NJ) for developing rotigaptide, a peptide cardiovascular drug.
Eli Lilly. Eli Lilly and Company (Indianapolis, IN) has a global development and commercialization pact with Amylin Pharmaceuticals, Inc. (San Diego, CA) for "Byetta" (exenatide), a 39-amino-acid peptide amide with incretin-mimetic actions to treat Type 2 diabetes. The drug received US regulatory approval in 2005 and European approval in 2006.
Amlyin obtains exenatide, the active ingredient in Byetta from peptide supplier Bachem (Torrance, CA) and Mallinckrodt, Inc. (St. Louis, MO) under long-term supply agreements , according to Amylin's 2006 annual report.
The Eli Lilly–Amylin pact includes the development of a long-acting release (LAR) formulation of exenatide. Amylin is working with Alkermes, Inc. (Cambridge, MA) to develop a once-weekly dosing of exenatide. Amylin expects to complete the commercial-scale manufacturing process for the LAR formulation of exenatide and commission a new manufacturing facility in West Chester, Ohio in the second half of 2008, according to Amylin's annual report.