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The ROCK2 inhibitor has been independently developed by Genosco and has generated candidates that selectively inhibit ROCK2 kinase. Research has revealed that the signal transduction processes activated by ROCK are involved in various signaling processes, such as cell proliferation, prevention of apoptosis, cell migration, and secretion of cytokines and chemokines, and according to recent reports, it is also involved in inflammation and fibrosis. Therefore, ROCK2 is a substance that is getting attention as a new treatment target.

Genosco’s ROCK2 candidates are highly potent compared to published inhibitors and possess exceptionally high selectivity, mitigating the toxicity inherent to many pan-ROCK inhibitors developed to date. Furthermore, Genosco’s ROCK2 candidates have exhibited excellent pharmacological efficacy (Ashcroft score) in an animal model of idiopathic pulmonary fibrosis (IPF) and superior inhibition on the expression of αSMA, a representative marker of IPF, compared to the competing drug Nintedanib.

ROCK2 inhibitor is in the lead optimization stage.

Idiopathic Pulmonary Fibrosis (IPF) is a type of chronic interstitial lung disease (ILDs), and refers not to any one disease, but to all diseases that mainly cause problems with interstices in the lung. The exact cause of the onset of IPF is still unknown.
When tissues between alveoli are damaged, the inflammatory cells penetrate the area repeatedly and the inflammatory state persists, which leads to fibrosis that hardens the lungs. Subsequently, severe structural changes occur in the lung tissues and the lung function gradually decreases, causing death. So far, there are no drugs that have been proven effective for the treatment of IPF. Anti-inflammatory drugs and immunomodulators have been widely used for the treatment of IPF, but their effectiveness has not been proven. IPF is a rare refractory disease, for which a few drugs have been approved by the US FDA, but these drugs have only limited effects of delaying the decline of the lung function without stopping the disease itself.

Currently, Genosco is engaged in a rapid development of an orphan drug for IPF and is also considering the expansion of indications for other diseases with large markets, such as cerebral cavernous malformation (CCM).