RXC007 is a novel and selective Rho Associated Coiled-Coil Containing Protein Kinase 2 (ROCK2) inhibitor, an enzyme which sits at a nodal point in cell signalling pathways believed to be central to fibrosis. Fibrosis is a key pathogenic factor in multiple diseases with high unmet medical need. ROCK2 is therefore an important emerging drug target and RXC007 will be developed as a best-in-class drug to target several fibrotic diseases. These include the orphan disease, idiopathic pulmonary fibrosis (IPF), a severe and life-threatening chronic lung condition with very poor prognosis and limited treatment options; non-alcoholic steatohepatitis (NASH), an inflammatory and fibrotic disease of the liver and diabetic nephropathy, a serious diabetic kidney disease.
Preclinical data with compounds from Redx's ROCK2 programme have demonstrated robust anti-fibrotic effects in a range of industry-standard in vivo models. Specifically, RXC007, which is orally bioavailable, met fibrosis endpoints in disease models of liver and lung fibrosis. Furthermore, RXC007's selective inhibition of ROCK2 over other enzyme isoforms should enable a safe cardiovascular profile in patients. Dr Nicolas Guisot, Research Fellow at
The Company aims to initiate a phase 1 study with RXC007 in H1 2021, whilst evaluating clinical development pathways in IPF and potentially in other disease areas. This is the second development candidate that Redx has progressed in the area of fibrosis following the nomination of RXC006, a novel, orally available porcupine inhibitor, that the Company is developing as a first-in-class treatment for IPF.
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About ROCK2 (Rho-associated protein kinase 2) inhibitors
ROCK2 is an intracellular kinase with multiple cellular functions. ROCK2 signalling plays a key role in both the inflammatory component and the tissue re-modelling that drives disease progression in many fibrotic conditions. ROCK2 expression and activity has been shown to be up-regulated in acute inflammatory injury and in chronic diseases such as diabetes, metabolic syndrome and IPF. Furthermore, ROCK2 activity is also upregulated in liver, lung and kidney models of fibrosis. ROCK2 has been shown to modulate activation of the hepatic stellate cells - the central drivers of fibrosis in the liver and mesangial cells - important drivers of fibrosis in the kidney. ROCK2 has also been shown to play important roles in the pro-fibrotic response of lung epithelial cells in IPF. Targeting ROCK2 in fibrosis is a clinically validated approach with KD025, a ROCK2 inhibitor in clinical development for IPF, chronic Graft vs Host Disease (cGvHD) and systemic sclerosis.
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