ABSTRACT

Telbivudine (beta-l-2′-deoxythymidine, LdT) is the unmodified beta-l-enantiomer of the natural nucleoside d-thymidine. This nucleoside analog is a potent inhibitor of the replication of hepadnaviruses, including human hepatitis B virus (HBV) and specifically chronic hepatitis B infection (CHB) and woodchuck hepatitis virus (WHV). After triphosphorylation by cellular enzymes, telbivudine triphosphate inhibits the HBV polymerase enzyme. Telbivudine was developed by Idenix/Norvatis and was approved for registration by the US Food and Drug Administration (FDA) in 2006 and by European Medicines Agency (EMEA) in the European Union in April 2007. It is marketed under the trade name Tyzeka in the USA and Sebivo in the European Union and is available as both tablets (600 mg) and oral solution (100 mg/5 ml) for oral administration.