NTCP: An Emerging Drug Target for A Variety of Diseases
NTCP (sodium taurocholate cotransporting polypeptide)
Bulevirtide is the first drug in clinical development specifically targeting an important liver protein – NTCP, or sodium taurocholate co-transporting polypeptide. NTCP transports bile acids in the form of their sodium salts from portal blood into the liver and thus serves as an essential component of enterohepatic circulation.
It was recently discovered that Hepatitis B and Delta viruses enter hepatocytes through the binding to NTCP with HBV preS1 surface protein domain. As a mimetic of the preS1 domain, Myrcludex B specifically blocks the corresponding NTCP binding site, thereby inhibiting the entry of the viruses into the liver cells.
The blockade of NTCP is not only relevant to antiviral drug development. The effect of this mechanism on lipid metabolism and specifically the elevation of bile acid levels may have positive implications for the treatment of a variety of other diseases. MYR Pharma is currently exploring therapeutic potential of NTCP targeting with Myrcludex B in hypercholesteromia and nonalcoholic steatohepatitis (NASH), among other indications.