What is it about?

Pain control in chronic diseases, such as osteoarthritis, is a major challenge. In these diseases the therapeutic repertoire, even, if large (from NSAIDs to opiates) does not grant either a sufficient efficacy or an acceptable long-term safety. CR4056 is a fist-in-class compound that binds imidazoline I2 sites and is endowed with a pain killer effect in a surprisingly broad paradigm of pain models in animals (from acute inflammatory to neuropathic pain, passing through post-surgical pain). Our aim was to demonstrate if this compound was able to show a relevant analgesic effect also in two well-established models of osteoarthritis pain in animals.

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Why is it important?

The demonstration that CR4056 is able to counteract pain behaviours in animal models of osteoarthritis allows proposing this imidazoline I2 binding compound as the founder of a new class of, hopefully, safer and more effective in the control of chronic pain conditions in humans.

Perspectives

Having spent more than 30 years in the research and development of innovative drugs, to me the discovery of CR4056 represents a great achievement, both scientifically and personally, pointing out the pioneering activity of the research group of Rottapharm Biotech.

dr gianfranco caselli
Rottapharm Biotech

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This page is a summary of: Efficacy of CR4056, a first-in-class imidazoline-2 analgesic drug, in comparison with naproxen in two rat models of osteoarthritis, Journal of Pain Research, May 2017, Dove Medical Press,
DOI: 10.2147/jpr.s132026.
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