baloxavir

Description: Baloxavir (trade name Xofluza; also known as Baloxavir acid, BXA, or S-033447), derived from the prodrug baloxavir marboxil (BXM), is an orally available small molecule inhibitor of the cap-dependent endonuclease. It is an antiviral drug developed by Roche and Shionogi as an anti-influenza agent for treatment of influenza A andinfluenza B flu. As of 2018, it was approved for clinical use in Japan and inthe United States. Baloxavir was discovered by rational molecular design based on the two-metal pharmacophore concept for dolutegravir (DTG), a strand transfer inhibitor of human immunodeficiency virus (HIV) integrase. Baloxavir potently and selectively inhibits the cap-dependent endonuclease within the polymerase PA subunit of influenza A and B viruses. In February 2018, baloxavir received its first global approval in Japan for the treatment of influenza A or B virus infections. Phase III development is underway in the USA, EU and other countries for this indication.The drug blocks influenza virus proliferation by inhibiting the initiation of mRNA synthesis. In clinical trials, single doses of Baloxavir profoundly decrease viral titers as well as alleviating influenza symptoms.

References: Sci Rep. 2018 Jun 25; 8(1):9633; Drugs. 2018 Apr; 78(6):693-697; WO 2017104691 A1.

Related CAS: 1985606-14-1 (baloxavir marboxil) 1985605-59-1 (Baloxavir)