TheraQuest Announces a Safer, Abuse Deterrent, Long-acting, Once-Daily Tramadol for Pain Management

Phase 3 Clinical Trials Slated for 2005

Blue Bell, Pennsylvania – February 14, 2005 – PRNewswire – TheraQuest Biosciences, a pain management company today announced that it has developed a safer, long-acting, once-a-day formulation of the pain drug, tramadol. The formulation, TQ-1017, is designed to deter recreational use, prescription abuse or accidental misuse of tramadol. TheraQuest believes its unique formulation, slated for Phase 3 clinical trials in 2005 may have significant safety advantages over other formulations currently in development.

Tramadol’s pain relieving effects are due to serotonin and norepinephrine reuptake inhibition, and through a narcotic (opioid) effect similar to oxycodone, the active ingredient in OxyContin®. Tramadol is an unscheduled narcotic and is therefore readily available like any ordinary prescription drug. Commercially available short-acting tramadol (Ultram®) releases 50 mg of tramadol per tablet into the bloodstream over several hours. New, long-acting formulations in development are designed to gradually release their much larger tramadol content over a 24-hour period. Najib Babul, PharmD, President and Chief Executive Officer of TheraQuest stated “A formulation with a secure timed-release mechanism is especially needed because if the release mechanism is defeated, the entire 24-hour drug supply can be released into the bloodstream, with resulting potential for toxic effects.”

Dr. Gregory Skipper, Medical Director of the Alabama Physician Health Program and principle investigator of a recent JAMA report regarding drugs abused by physicians noted “In our study, tramadol was the third most frequently mentioned abused opioid. Surprisingly, it was more frequently mentioned than was fentanyl, oxycodone or hydromorphone. Tramadol definitely has abuse potential. An abuse deterrent slow release formulation would greatly reduce the likelihood of abuse.” He adds “Secure slow release mechanisms are very important because rapid absorption of tramadol from the intentional or inadvertent crushing of once-daily tramadol tablets would likely produce neurological toxicity. In addition, high concentrations of tramadol, especially in combination with many popular antidepressants may produce serotonin syndrome. If not properly treated, serotonin syndrome can lead to life-threatening complications.”

According to the Drug Enforcement Agency (DEA), Tramadol is a “drug of concern because it can be abused for its opioid effects”. DEA cites the Drug Abuse Warning Network (DAWN) data for drug related hospital emergency room episodes. In 2002, there were 1,714 episodes for tramadol and a total of 7,890 episodes from 1998 through 2002. DAWN medical examiners reported that tramadol was involved in 95 drug-related deaths in 2002 and a total of 382 deaths from 1998 through 2002. In the two most recent annual reports of the American Association of Poison Control Centers Toxic Exposure Surveillance System (TESS), tramadol ranked second to oxycodone in the number of opioid exposure cases.

Babul noted that “TQ-1017 is a formulation of once-daily tramadol that cannot be crushed for inhalation or to obtain rapid euphoria from high blood levels when swallowed. It is also difficult to extract tramadol from our once-daily formulation using common solvents.” Babul further noted “TheraQuest believes that these features, combined with other innovations embedded in the design of our formulation will provide for greater tolerability in patients with pain and a larger margin of safety in the event of intentional or inadvertent attempts to defeat the timed release mechanism”.

“We believe TheraQuest’s once-daily tramadol formulation, with its abuse deterrent technology and an optimized pharmacokinetic profile will be an attractive product for clinicians and their patients”, noted Babul “Given a choice, we believe physicians will prescribe a less abusable once-daily tramadol formulation” added Babul.

About TheraQuest Biosciences

TheraQuest Biosciences, LLC is a private, development-stage pain management company building a diversified portfolio of pharmaceutical products to address a critical area of unmet medical need. Despite their limitations, current treatments for acute and chronic pain yield worldwide sales in excess of $30 billion. The TheraQuest team has contributed to the development of numerous analgesics approved in the U.S. over the past 20 years. TheraQuest’s strategy is to use its expertise to identify, develop and commercialize product candidates with strong market potential that have lower development costs and reduced regulatory risk than new chemical entities. TheraQuest is headquartered in Blue Bell, Pennsylvania.

TheraQuest is funded in part by BioAdvance, the Biotechnology Greenhouse of Southeastern Pennsylvania and Ben Franklin Technology Partners of Southeastern Pennsylvania. Additional information is available at www.theraquestinc.com.

OxyContin® and Ultram® are trademarks of Purdue Pharma L.P. and Johnson & Johnson, respectively.