Pipeline Overview

We are currently developing pain medicines for the treatment of chronic pain due to cancer, musculoskeletal disorders (e.g., osteoarthritis, low back pain) and peripheral neuropathy (e.g., postherpetic neuralgia, painful HIV neuropathy).

• TQ-1020 is a proprietary once-a-day extended release dosage form of the opioid analgesic levorphanol in an abuse deterrent drug delivery system. It has activity at both opioid and non-opioid receptors. Unlike oxycodone, morphine , hydromorphone and oxymorphone, levorphanol modulates pain through both the ascending opioidergic pathways and the descending noradrenergic pathways in one centrally acting analgesic. We have demonstrated that levorphanol is significantly more potent than morphine at the μ (mu), δ (delta) and κ (kappa) receptor and its norepinephrine and serotonin reuptake inhibition is comparable to tapentadol (Nucynta®) and tramadol (Ultram® ER, Ryzolt®). Levorphanol also exerts NMDA antagonism, which may explain its efficacy in neuropathic pain and its ability to partially reverse tolerance to morphine. TQ-1020 will compete in the same opioid market segment as OxyContin®, Opana® ER, Embeda®, Kadian®, Avinza® and Exalgo® (2009 U.S. opioid sales $8.5 billion).
  
  
• TQ-1021 is a proprietary topical dosage form of the local anesthetic mepivacaine for the treatment of painful peripheral neuropathies, such as painful diabetic neuropathy, postherpetic neuralgia and painful HIV-associated neuropathy. TQ-1021 has been granted two Orphan Drug Designations by the FDA, for the treatment of postherpetic neuralgia and for the painful HIV neuropathy. We expect TQ-1021 to be used alone and in combination with oral therapies for neuropathic pain such as Lyrica® and Cymbalta®. TQ-1020 will compete in the same market segment as Lidoderm® patch, which had U.S. sales of $770 million for 2009.
  
  
• TQ-1028 is a proprietary once-a-day extended release dosage form of oral buprenorphine. It is being developed for the treatment of chronic moderate to moderately severe pain and opioid dependence. Buprenorphine has been widely used by by the sublingual and transdermal, but not by the oral route. Buprenorphine’s unique pharmacology distinguishes it from other opioids. Among its advantages over oxycodone, oxymorphone, morphine and hydromorphone (the active opioids in OxyContin®, Opana® ER, Embeda®, and Exalgo®, respectively) are: (i) schedule III [C-III-]) controlled substance status; (ii) reduced risk of physical dependence; (iii) reduced reinforcing properties; (iv) reduced drug liking by recreational drug users; and (v) reduced risk of respiratory depression in overdose. TQ-1028 will compete in the same opioid pain market segment as OxyContin®, Opana® ER, Embeda®, Kadian®, Avinza® and Exalgo® (2009 U.S. opioid sales $8.5 billion), with the advantage of C-III prescribing status and reduced risk of drug abuse. 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).