ContraVir Pharmaceuticals (NASDAQ:CTRV) provided new insights into the mechanism of action of its hepatitis B (HBV) cyclophilin inhibitor, CRV431, showing that it effectively blocks a critical interaction between HBV X protein (HBx) and host cyclophilin A, with nanomolar potency.
CRV431 is believed to be the first antiviral drug with the potential to selectively block the HBx pathway, which is known to play several significant roles in HBV infection, including protecting infected liver cells from immune destruction, and promoting the development of liver cancer.
CRV431 has demonstrated synergistic activity in vitro with ContraVir’s tenofovir prodrug CMX157, currently in Phase 2 clinical trials.
In a statement, CEO, James Sapirstein, said that identifying this mechanism of action for CRV431 places ContraVir at the very forefront of HBV research, with a compound that can effectively target the HBx pathway.
“Further development of this novel compound, and ultimately layering it on top of CMX157 and potentially other HBV drugs, dovetails with our overall development strategy which is focused on finding a functional cure for HBV,” he added.
In addition, he said the pathogenic effects of HBx are many, and “we would therefore expect the anti-HBx activity of CRV431 to be equally robust. We will continue to work on characterizing the activity of CRV431 and its impact on HBx and HBV within our company, and through our peers in North America and Europe.”