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Compatible Permeation Enhancement Excipients: Enhancing Transmucosal and Transdermal Drug Delivery

Compatible Permeation Enhancement Excipients: Enhancing Transmucosal and Transdermal Drug Delivery

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Introduction/Background

Bentley Pharmaceuticals was formed in 1974 and became a public company in 1988. The company specialises in the development of products based upon innovative and proprietary delivery systems and has a commercial presence in Europe where it markets branded and generic products. Bentley's two Spanish subsidiaries, Laboratorios Belmac and Laboratorios Davur, have collaboration with TEVA Pharmaceutical Industries for marketing products in Spain. In 1999, Bentley acquired permeation enhancer and hydrogel drug delivery technologies and opened a research facility in New Hampshire.

Aims/Hypothesis

Bentley is developing a series of GRAS excipients that facilitate the permeability of drugs administered topically and orally into and through physiological barriers such as skin, nails, mucosa, cornea etc. in a variety of independent pharmaceutical formats. The excipient most advanced and validated in facilitating absorption is designated as CPE-215®, although there are a number of other related compounds that have similar permeation enhancement characteristics. These excipients are chemically classified as cyclic lactones and cyclic ketones. Chemical compatibility with various chemical and peptide therapeutic molecules has not been an issue to date.

Research

Lead products in development using this technology include: (1). The NDA for CPE-215® containing topical testosterone gel (Testim®) for male hormone replacement therapy was approved in November 2002 and the product was launched in the US in 2003, by licensee Auxilium A2, and recently approved in the UK. Testim® is rapidly absorbed with the competitive advantages of a high payload delivery, only a small volume of gel and a 30% increase in plasma area under the curve (AUC) vs. a non-CPE 215® containing formulation. (2). Clotrimazole paint on lacquer is in phase III for treating nail bed fungal infections (onychomycosis). Two clinical trials, at the University of Alabama, were completed and showed statistically significant clear nail growth in finger and toenails. (3). Intranasal Insulin for diabetes is in phase I clinical testing. Animal models show the intranasal formulation consistently achieves 30-33% bioavailability with no irritation. Proof-of-concept human and formulation studies are ongoing. (4). Intranasal oxycodone for pain management. Preclinical testing is underway with partner Auxilium A2. (5). Transdermal dihydrotestosterone for treating osteoporosis in men. Preclinical testing is underway with partner Auxilium A2. (6). In December 2001, Bentley signed research collaboration with Pfizer Inc. for the development of a number of nasally administered proprietary molecules (excluding insulin). (7). In November 2000, Bentley licensed a patent from Dartmouth College concerning the delivery of androgens plus CPE-215, for the treatment of fibromyalgia and chronic fatigue syndrome. Proof-of-concept studies are completed.

Bentley has achieved positive results for Testim®, which utilises Bentley's CPE-215 technology, in treating HIV positive hypogonadal men. Bentley receives a royalty on sales of Testim®. The Auxilium study explored the effect of Testim® 5g therapy in 48 hypogonadal, HIV positive men who reported that they did not have adequate symptom relief with AndroGel 5g. Auxilium reported that, compared to AndroGel treated men, at the 4-week follow-up, men treated with Testim® reported a statistically and clinically significant improvement in their sex drive, erectile function, and satisfaction with sex life as well as being more satisfied with androgen therapy. Additionally, the investigators rated their overall satisfaction with androgen therapy significantly higher in the Testim® treated group as compared to the AndroGel treated group. Auxilium reported that these improvements in sexual function resulted in significantly fewer Testim® treated men requiring titration to a higher dose compared to men treated with AndroGel (30% vs 74%, respectively).

An initial Phase II intranasal insulin study shows more rapid absorption and higher peak levels than subcutaneous insulin. Bentley's intranasal formulation demonstrated more rapid absorption and higher peak levels than subcutaneous insulin. It blunted post-prandial hyperglycaemia for over two hours. Calculated relative bioavailability (amount of total dose absorbed) as compared to subcutaneous insulin was 15-20%, which is greater than that of most reported studies of inhaled insulin formulations.

Conclusion

CPEX continues to strengthen its intellectual property portfolio across the Company's broader drug delivery business as additional applications of CPE-215 are pursued.

Relevance/Opportunity

The technology, validated with the marketed product Testim and very promising data for Nasulin, has broad applications to the universe of therapeutic peptides where a non-injectable formulation would provide considerable market potential. Access to CPEX's permeation enhancement technology with the key excipient, CPE-215, is currently being offered to pharmaceutical and biotechnology companies whose products could potentially benefit from its permeation enhancement properties – either as new product launches, as part of product lifecycle management or line-extension strategies. Our strategy includes out-licensing of our CPE-215 permeation technology and in-licensing of drug targets. If you would like to explore a possible partnership with CPEX Pharmaceuticals, please contact below.

Development status

Phase II

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