Exploration of possible innovative targets for osteoarthritis, along with the increasing knowledge on the human kinome, has led to the identification of protein kinases that may independently control pain pathways and joint degeneration. Rottapharm Biotech is engaged in target validation, discovery and development of new inhibitors of selected kinases for OA. The precise targets are undisclosed for the moment, for confidentiality reasons while waiting for intellectual property protection. In the meantime, Rottapharm Biotech has obtained validation of the targets by appropriate gene knock-out studies or pharmacological tools.
The company is currently screening different small molecule series developed for their ability to selectively inhibit the identified protein kinases. Lead compounds showing potent analgesic activity in animal models of nociceptive pain are being optimized. In parallel, preliminary investigations in rodent models of osteoarthritis have highlighted features of joint structure modification.
The potent, immediate and long-lasting symptomatic activity in general pain models with joint structure modification in specific osteoarthritis models is unprecedented in osteoarthritis drug discovery.