TheraQuest Unveils New Pain Management Product Pipeline

BLUE BELL, Pa., June 22 /PRNewswire/ -- TheraQuest Biosciences, Inc., a clinical stage pain management company today unveiled its analgesic product pipeline. TheraQuest also announced the launch of its new corporate website at http://www.theraquestinc.com.

Najib Babul, PharmD, President and Chief Executive Officer, said, "After a careful strategic review of our pipeline, we have realigned our development efforts to focus on chronic pain products with the largest market potential and greatest probability for timely FDA approval."  Babul further noted, "Going forward, we will focus our development resources on drugs to treat chronic musculoskeletal conditions such as osteoarthritis and low back pain, and on neuropathic pain."

Overview of Pain Pipeline

TQ-1020 (Levorphanol Extended Release) is a proprietary once-a-day extended release levorphanol in an abuse deterrent drug delivery system. It has activity at both opioid and non-opioid receptors and monoamine reuptake inhibition comparable to Nucynta® and Ultram®.

TQ-1021 (Topical Mepivacaine) is a proprietary topical dosage form of the local anesthetic, mepivacaine for the treatment of neuropathic pain. It has been granted Orphan Drug Designations for the treatment of postherpetic neuralgia and painful HIV neuropathy.

TQ-1028 (Oral, Buprenorphine Extended Release) is a proprietary once-a-day extended release oral dosage form of the C-III opioid buprenorphine. According to the DEA and FDA, buprenorphine has a lower abuse potential than oxycodone, oxymorphone, morphine and hydromorphone, the C-II opioids in OxyContin®, Opana® ER, Embeda® and Exalgo®.

Pain Pipeline Details

TQ-1020 (Levorphanol Extended Release)

TQ-1020 is a proprietary once-a-day extended release dosage form of the opioid analgesic levorphanol in an abuse deterrent drug delivery system (Levorphanol ER). It has activity at both opioid and non-opioid receptors, thus providing unique pharmacologic advantages over currently marketed strong opioids. Levorphanol is significantly more potent than morphine at the mu, delta and kappa opioid receptor.

Unlike OxyContin, Opana ER, Embeda and Exalgo, Levorphanol's norepinephrine and serotonin reuptake inhibition is comparable to tapentadol (Nucynta) and tramadol (Ultram ER). Consequently, levorphanol ER targets both opioid modulated ascending pathways and norepinephrine modulated descending pathways of pain in one centrally acting analgesic. Levorphanol also exerts NMDA antagonism which may partly explain its efficacy in neuropathic pain and its ability to reverse tolerance to morphine.

Levorphanol ER is being developed for chronic moderate to severe pain. It will compete in the same opioid market segment as OxyContin, Opana ER, Embeda and Exalgo (2009 U.S. opioid sales $8.5 billion).

TQ-1021 (Topical Mepivacaine)

TQ-1021 is a proprietary topical dosage form of the local anesthetic, mepivacaine for the treatment of neuropathic pain states such as painful diabetic neuropathy, postherpetic neuralgia and painful HIV-associated neuropathy. TQ-1021 has been granted Orphan Drug Designations by the FDA for the treatment of postherpetic neuralgia and painful HIV neuropathy.

In the United States, only Lidoderm®, Neurontin®, Lyrica® and Qutenza® are approved for treating postherpetic neuralgia, and only Lyrica and Cymbalta® are approved for treating painful diabetic neuropathy. Presently, no treatments are approved for the treatment of painful HIV neuropathy.

As a result of the success of Pfizer's Neurontin, neuropathic pain has become one of the most sought-after indications. According to Datamonitor, the market for neuropathic pain drugs is expected to grow to $5.5 billion by 2015. We expect that TQ-1021 will be used alone or with oral therapies such as Lyrica and Cymbalta. TQ-1021 will compete in the same market segment as Lidoderm patch, which had U.S. sales of $770 million in 2009.

TQ-1028 (Oral, Buprenorphine Extended Release)

TQ-1028 is a proprietary once-a-day extended release oral dosage form of the C-III opioid, buprenorphine. It is being developed for the treatment of chronic moderate to moderately severe pain and for the treatment of opioid dependence. Buprenorphine has been widely used by the sublingual and transdermal routes but not by the oral route. There are currently no marketed C-III extended release opioids in the United States.

According to FDA and DEA, buprenorphine has a lower potential for abuse relative to C-II opioids such as oxycodone, oxymorphone, morphine and hydromorphone, the opioids in OxyContin, Opana ER, Embeda and Exalgo, respectively. In addition, prescriptions for buprenorphine may transmitted by phone or fax and refilled up to 5 times in 6 months, while prescriptions for C-II opioids must be written and cannot be refilled.

Buprenorphine's unique pharmacology also distinguishes it from oxycodone, oxymorphone, morphine and hydromorphone. Among its advantages are: (i) reduced reinforcing properties and risk of physical dependence; (ii)) reduced drug liking by recreational drug users; and (iii) reduced risk of respiratory depression in overdose.

TQ-1028 will compete in the same opioid pain market segment as OxyContin, Opana ER, Embeda and Exalgo (2009 U.S. opioid sales $8.5 billion), with the advantage of C-III prescribing status and reduced risk of drug abuse. Given a choice, clinicians are more likely to use C-III pain relievers over C-II pain relievers, particularly for moderate to moderately severe pain. Additionally, TQ-1028 will compete with sublingual buprenorphine (Suboxone®/Subutex®) and methadone for the treatment of opioid dependence (2009 sales for sublingual buprenorphine were $970 million).

About TheraQuest Biosciences, Inc.

TheraQuest (http://www.theraquestinc.com) is a clinical-stage pain management company building a diversified portfolio of pain products. 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 leverage its pain expertise to identify, develop to an early stage and outlicense product candidates with strong market potential that have lower development costs and reduced regulatory risk compared to new chemical entities. TheraQuest is funded in part by BioAdvance, the Biotechnology Greenhouse of Southeastern Pennsylvania and Ben Franklin Technology Partners of Southeastern Pennsylvania.

All trademarks used herein, including Cymbalta®, Embeda®, Exalgo®, Lidoderm®, Lyrica®, Nucynta®, Neurontin®, OxyContin®, Opana® ER, Qutenza®, Suboxone®, Subutex®, Ultram® ER are the property of their respective owners.

SOURCE TheraQuest Biosciences, Inc.