Rheumatology

Rottapharm is leader in the field of rheumatic diseases, with different successful products and brands. In particular, the company developed the original, prescription formulation of glucosamine sulfate, which was shown in repeated and prestigious clinical trials to be the first putative disease-modifying agent in osteoarthritis (DMOAD). Logically, the R&D pipeline includes therefore a number of potential follow-on strategies for DMOADs. Glucosamine sulfate targets joint homeostasis, by inhibiting IL-1 induced gene expression via blockade of the cytokine intracellular signalling pathway ( through NFkB modulation). Large international clinical trials are ongoing for efficacy and safety in new therapeutic indications.
Current discovery approaches target:
a)Cartilage metabolism, by inhibiting the matrix metalloproteinases possibly responsible for cartilage degradation in OA: aggrecanase (ADAMTS-4 and 5) inhibitors;
b) Articular inflammation (and metabolism), searching for novel anti-inflammatories and analgesics inhibiting selective prostaglandin receptors also involved in cartilage catabolism: EP4 receptor antagonists;
c) Biomechanical responses: addressing the effects of excitatory mediators that may modulate chondrocyte responses following mechanical stimulation: peripheral NMDA receptor antagonists.