Pipex Pharmaceuticals Inc, a specialty pharmaceutical company developing innovative late-stage drug candidates for the treatment of neurologic and fibrotic diseases, said that the United States FDA has opened an Investigational New Drug Application (IND) to conduct a double-blind, randomised, placebo-controlled phase II clinical trial of oral flupirtine for the treatment of fibromyalgia, a rheumatic pain disease which affects an estimated 6 million Americans.
Lyrica, the only FDA-approved medication for the treatment of fibromyalgia amongst other indications, recorded $1.8 billion in sales during 2007, with 47 per cent annual growth.
Oral flupirtine has been approved as a treatment of pain in Europe since 1981 but has never been approval for any indication in the US Flupirtine, a non-opiate analgesic, has been used in Europe for more than 25 years for post-surgical pain, cancer pain, trauma pain, pain associated with liver disease, and other nocioceptive pain states. Preclinical data and clinical experience suggests that flupirtine should also be effective for neuropathic pain since it acts in the central nervous system. Flupirtine is especially attractive because it operates through non-opiate pain pathways, exhibits no known abuse potential, and lacks withdrawal effects. In addition, no tolerance to its antinocioceptive effects has been observed. One common link between neuroprotection, nocioception, and flupirtine may be the NMDA (N-methyl-D-aspartate) glutamate system, a major receptor subtype for the excitotoxic neurotransmitter, glutamate. Flupirtine has strong inhibitory actions on NMDA-mediated neurotransmission.
Dr. Andrew L. Stoll, director of the Psychopharmacology Research Laboratory at McLean Hospital, a Harvard University-affiliated teaching hospital and inventor of this programme, said, "Due to its rapid onset of action and high response rate in treatment-refractory fibromyalgia patients, I believe flupirtine may represent a new therapeutic modality for the treatment of this debilitating disease which affects more than six million Americans. There is a strong scientific rationale supporting the development of flupirtine for the treatment of fibromyalgia."
Steve H. Kanzer, chairman and chief executive officer, said, "Oral flupirtine has been marketed for more than two decades in Europe for the treatment of pain-related diseases. As we enter this phase II clinical trial of oral flupirtine for treatment of fibromyalgia, the product's substantial human experience coupled with the promising human data already generated in refractory fibromyalgia patients, represents an exciting new approach to treating this widespread often debilitating disease".
This phase II clinical trial is designed as a double-blind, placebo controlled phase II clinical trial which would evaluate safety and efficacy of oral flupirtine vs. placebo in fibromyalgia patients. This phase II clinical trial is intended to enroll up to 90 subjects and treat subjects for up to 90 days and the primary endpoint will be a reduction in musculoskeletal pain and the overall symptoms of fibromyalgia. Secondary outcomes of the study will be a reduction in the severity of mood, fatigue, cognitive symptoms, and sleep disturbance, as well as improve the overall level of functioning.
Fibromyalgia is an arthritis-related condition that is characterized by generalized muscular pain and fatigue. It is a chronic and debilitating condition characterized by widespread pain and stiffness throughout the body, accompanied by severe fatigue, insomnia and mood symptoms. It is estimated to affect between two and four percent of the world's population and after, osteoarthritis, is the most commonly diagnosed disorder in rheumatology clinics.