PARIS and BOSTON, Massachusetts, April 26 /PRNewswire/ --
- Nautilus Biotech Presents Data on Modified Interferon-alpha (BELEROFON(R)) and Human Growth Hormone (VITATROPIN(TM)) with High Resistance to Proteases in Blood, Tissues and Intestine at PEGS 2006: The Protein Engineering Summit 24-28 April 2006, Boston USA
Nautilus Biotech S.A., the privately held French biotech company located on the Genopole(R) Campus and developing next-generation therapeutic proteins, today presented data for the first time on its in vivo studies demonstrating that its lead products, BELEROFON(R) and VITATROPIN(TM), show increased resistance to proteolytic degradation in both the blood and intestine, opening up the potential for orally administered protein therapeutics. BELEROFON(R) is a variant of human interferon alpha (IFN-alpha) and VITATROPIN(TM) is a variant of human growth hormone, that have each been engineered to contain a highly targeted single amino acid point mutation.
These new data were presented by Drs. T.Guyon and G.Borrelly, Program Leaders at Nautilus Biotech, during PEGS 2006: The Protein Engineering Summit 24-28 April 2006, Boston USA. Commenting on the results and their significance, Dr Manuel Vega, Chief Executive Officer of Nautilus Biotech, said: "Protein therapeutics are currently administered by injection. However, the frequency of treatment can lead to toxicity and problems with side effects, and need for injection, in itself, means a very poor compliance for patients. Our technology offers the potential to create protein therapeutics that are resistant to proteolytic degradation in the gastrointestinal tract and might thus be administered orally, offering significant healthcare advantages. Nautilus Biotech's proteins are orally available per se, without the need of specific formulations. Nautilus Biotech's proteins offer the potential for a radical change in the paradigm on how patient compliance is achieved, i.e. by changing injectables into pills rather than by decreasing the frequency of injections required, which most of the industry is focused on today."
Previous studies have demonstrated that the single amino acid point mutations on BELEROFON(R) and VITATROPIN(TM) significantly improve their pharmacokinetics and pharmacodynamics profiles following subcutaneous administration in vivo. These new data now further demonstrate that single mutations introduced by Nautilus Biotech block proteolysis in vivo, in the digestive tract, and render proteins orally available without the need for any oral formulation.
The data presented included in vivo studies analysing the pharmacokinetic profiles of the native proteins (IFN-alpha or hGH) in blood in comparison with that of BELEROFON(R) and VITATROPIN(TM) following oral administration. The results showed that the native proteins could not be detected in blood following the oral delivery of the lyophilised proteins in gastro-resistant capsules, even at high doses; likely due to proteolysis in the intestine. In contrast, BELEROFON(R) and VITATROPIN(TM) not only showed survival in the intestine itself, but also absorption into the bloodstream and survival in blood. Furthermore, the variant proteins showed even longer survival in the circulation than the respective native proteins when injected directly in blood. The profiles obtained following oral delivery of Nautilus Biotech's proteins are expected to support therapeutic efficacy of these drugs by oral delivery.
Regulatory toxicity has been successfully completed for BELEROFON(R) and Nautilus Biotech is expected to file an IND for BELEROFON(R) later in 2006, and commence Phase 1 studies in the US in early 2007, with the aim of confirming the enhanced pharmacokinetics and pharmacodynamics profiles of subcutaneous BELEROFON(R) as well as the systemic bioavailability and extended half-life of oral BELEROFON(R). VITATROPIN(TM) will follow with an IND in Q1 2007.
Nautilus Biotech's technology has wide applicability across many therapeutic proteins and protein families. In addition to its in house R&D programmes, Nautilus Biotech is seeking to enter into commercial partnerships with biotech and pharma to apply its expertise across a wider number of protein drug candidates. The therapeutic proteins market is currently valued at over US$30bn, and growing at a rate of 10-15% per annum. Higher resistance to proteolysis offers improvements in drug stability pharmacological profile and, most importantly, makes oral administration feasible, offering the potential for highly differentiated and highly compliant therapeutic products.
Notes to editors:
About Nautilus Biotech
Nautilus Biotech is an innovative company with a pipeline of next-generation therapeutic proteins with superior pharmacological properties. The Company's proprietary technology decreases the rate of proteolytic degradation, offering improvements in drug stability and administration (both frequency and oral availability) by proteases. The potential for oral availability increases the likelihood of patient compliance.
Many marketed therapeutic proteins have clinical limitations, low patient compliance and/or harmful side effects, such as interferon alpha, human growth hormone, and interferon beta, as examples. In addition, many promising therapeutic proteins under development are stuck in late stage clinical phases due to their high toxicity or low stability, in spite of their potential therapeutic efficacy. Nautilus Biotech develops the next generation of protein therapeutics by creating improved products with better profiles in terms of efficacy, safety and ease to use compared to established alternative treatments.
Nautilus Biotech was founded in 2000 and currently employs 29 staff. The company has raised over EUR17 million in venture capital.
About BELEROFON(R)
BELEROFON(R) is Nautilus Biotech's proprietary variant of human IFN-alpha which involves a single amino-acid change compared to native IFN-alpha. The single point mutation introduced to create BELEROFON(R) has been specifically designed to increase the resistance of the entire molecule to proteolysis in blood, tissues and in the intestine. The increased resistance to proteolysis leads to a significantly improved pharmacokinetics and pharmacodynamics profile. Resistance to intestinal proteases allows BELEROFON(R) to survive in the intestine and to reach the blood stream when administered through the digestive tract.
Whilst long-lasting in serum and orally available, BELEROFON(R) also shows the high biological activity associated with native IFN-alpha, which is significantly greater than for pegylated derivatives. BELEROFON(R) is a non-pegylated, non-chemically modified, highly active, long-lasting in serum and orally available human interferon alpha.
IFN-alpha is commonly used to treat patients with chronic Hepatitis C infection. Currently, IFN-alpha, whether the native protein or its pegylated derivatives, are administered by subcutaneous injection. The market for IFN-alpha is in the order of US$3bn.
About VITATROPIN(TM)
VITATROPIN(TM), is a proprietary variant of human growth hormone (hGH), with a single amino acid replacement, which has significantly improved pharmacokinetics and pharmacodynamics profiles and has therefore, the potential to require less frequent injections of the drug. VITATROPIN(TM) has been validated in animal models for hGH deficiency.
The single point mutation introduced to create VITATROPIN(TM) has been specifically designed to increase the resistance of the entire molecule to proteolysis in blood, tissues and in the intestine. The increased resistance to proteolysis leads to a significantly improved pharmacokinetics and pharmacodynamics profile. Resistance to intestinal proteases allows VITATROPIN(TM) to survive in the intestine and to reach the blood stream when administered through the digestive tract.
Whilst long-lasting in serum and orally available, VITATROPIN(TM) also shows the high biological activity associated with native hGH.
Human growth hormone is commonly used to treat children of pathologically short stature, and has been used by some to enhance athletic performance. Currently, all forms of hGH are administered by subcutaneous daily injection, which represents a very poor patient compliance, especially for children. The market for hGH is in the order of US$2 billion.
About Genopole(R)
Genopole(R), leading French Science Park dedicated to life sciences, welcomes public research units specialising in genetics, genomics and related sciences as well as biotechnology companies by accompanying project developers from day one to the first round of financing.
www.genopole.fr At Nautilus Biotech: Dr Manuel Vega, CEO Nautilus Biotech SA 1 rue Pierre Fontaine 91000 Evry, France Tel: +33-1-60-87-54-60 Fax: +33-1-60-87-54-61 Email: mvega@nautilusbiotech.com Media relations: At Northbank Communications Lorna Watson, Senior Account Manager Northbank Communications Ltd The Media Village, 131-151 Great Titchfield Street, London, W1W 5BB, UK Tel: +44-207-886-8157 Fax: +44-207-886-8151 Email: l.watson@northbankcommunications.com
Nautilus BiotechCONTACT: Nautilus Biotech: Dr Manuel Vega, CEO, Tel: +33-1-60-87-54-60,Fax: +33-1-60-87-54-61, Email: mvega@nautilusbiotech.com. Media relations:Lorna Watson, Senior Account Manager, Northbank Communications Ltd, Tel:+44-207-886-8157, Fax: +44-207-886-8151, Email:l.watson@northbankcommunications.com
