New Drug Application Submitted to FDA for Investigational Analgesic Tapentadol Immediate Release Tablets

January 23, 2008 /PRNewswire-USNewswire/ -- Johnson & Johnson Pharmaceutical Research & Development, L.L.C. announced that it has submitted a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) for tapentadol hydrochloride immediate release (IR) tablets, an investigational oral analgesic for the relief of moderate to severe acute pain.

According to the American Pain Foundation, more than 25 million Americans experience acute pain each year as a result of injuries or surgeries, and a recent study estimated that 42 percent of U.S. hospital emergency department visits were due to pain-related problems.

Tapentadol is a novel investigational, centrally acting oral analgesic. It has a unique profile with two mechanisms of action, combining mu-opioid receptor agonism and norepinephrine reuptake inhibition in a single molecule. It is being developed in immediate-release and extended-release formulations.

Mu-opioid agonists are drugs that bind to mu-opioid receptors in the central nervous system. These drugs modify sensory and affective (mood) aspects of pain, inhibit the transmission of pain at the spinal cord and affect activity at parts of the brain that control how pain is perceived. Norepinephrine reuptake inhibitors are a type of central nervous system medication that increase the level of norepinephrine in the brain by inhibiting its re-absorption into nerve cells; these compounds have analgesic properties.

The submission is based on a full clinical development program for tapentadol. The program includes two Phase 3 multi-center studies that explored the efficacy and safety of multiple doses of the tapentadol IR formulation either for the treatment of acute pain in patients undergoing bunionectomy surgery or for patients with degenerative, end-stage joint disease of the hip or knee. The data from these clinical trials suggest that tapentadol has efficacy comparable to strong opioids.

Bunionectomy is a standard foot surgery. The predictable level of moderate to severe pain for several days following this surgery makes bunionectomy an appropriate model for assessing the efficacy of potent analgesics.

Data also were submitted to the FDA from an additional Phase 3 study that supported the safety profile of multiple doses of tapentadol IR in the treatment of outpatients with low back pain or pain from osteoarthritis of the hip or knee.

More than 1,800 patients have been treated with tapentadol IR tablets in clinical trials to date.
The most common adverse reactions in tapentadol Phase 2/3 multiple dose, placebo- and active-controlled efficacy and safety studies (10%) were nausea, dizziness, vomiting, somnolence (sleepiness) and headache.