brincidofovir

Brincidofovir is an oral lipid conjugate prodrug of cidofovir, developed as a broad-spectrum antiviral agent. It is primarily indicated for the treatment of human smallpox disease caused by the variola virus. The drug was developed by Chimerix and is marketed under the brand name Tembexa. Brincidofovir’s design as a lipid conjugate allows it to mimic natural lipids, improving cellular uptake and oral bioavailability while reducing nephrotoxicity compared to intravenous cidofovir. Once inside cells, brincidofovir is cleaved to release cidofovir, which is then phosphorylated to its active form (cidofovir diphosphate). This active metabolite selectively inhibits orthopoxvirus DNA polymerase-mediated viral DNA synthesis by acting as an acyclic nucleotide analog of deoxycytidine monophosphate, leading to chain termination during viral DNA replication[1][2][4][5]. Brincidofovir was approved in June 2021 in the United States for smallpox under the FDA Animal Rule due to ethical constraints on human efficacy trials[1][5][6]. It has also been investigated for other double-stranded DNA viruses such as cytomegalovirus (CMV), BK virus (BKV), adenovirus (AdV), and Epstein-Barr virus (EBV)[1].

Brand names

Tembexa

Other names

cidofovir hexadecyloxypropyl esterhexadecyloxypropyl cidofovir