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Osteoarthritis and Cathepsin K

Osteoarthritis (“OA”) is a chronic age-related degenerative disease caused by localised low-level joint inflammation eventually resulting in the abnormal wearing of the cartilage that covers and cushions the joints.  Destruction of the joint results in loss of lubrication resulting in chronic and severe pain as well as joint disability.  Osteoarthritis affects nearly twenty-one million people in the United States, accounting for 25% of visits to primary care physicians, and half of all NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) prescriptions. It is estimated that 80% of the population will have radiographic evidence of osteoarthritis by age sixty-five, although only 60% of those will be symptomatic.

 

General information on osteoarthritis: link here

Osteoarthritis Research Society International: link here

Current osteoarthritis treatments focus on symptomatic relief from inflammation and pain and there is a significant unmet therapeutic need for prophylactic treatments. Amura has developed low nanomolar inhibitors of cathepsin K with excellent selectivity against other cathepsins and attractive drug-like properties, with AM-3701 identified as the development candidate. In an in vivo surgical menisectomy model of osteoarthritis, our inhibitors have shown significant beneficial effects on tibial cartilage degeneration and total joint score compared to the control group. Additionally, our inhibitors demonstrated a significant decrease in synovial fluid CTxI collagen marker (CTxI).

 

 

In addition to this in vivo PoC data, the quality of the molecules is confirmed by a comprehensive pre-clinical package which includes pharmacokinetic data, selectivity and safety assessment.  The lead molecule and a first rate back-up molecule are now available for partnering.

These drugs are the product of Amura’s AMcore™  platform which  has reproducibly provided ‘fast-on, slow-off rate’ enzyme inhibitors with good pharmacokinetic half-lives and a very strong IP position. 

Full Compound Information Summaries are available under Confidentiality Agreement. 

Amura has licensing opportunities for its AMcore-based programmes.

 

 
     
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