New Drug Approvals

({[(S)-1-(4-amino-2-oxo-1,2-dihydropyrimidin-1-yl)-3-hydroxypropan-2-yl]oxy}methyl)phosphonic acid

Cidofovir

Cidofovir is an injectable antiviral medication for the treatment of cytomegalovirus (CMV)retinitis[1] in patients with AIDS. It suppresses CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription.[2] It is an acyclic nucleoside phosphonate, and is therefore independent of phosphorylation by viral enzymes,[3] in contrast to, for instance, acyclovir.

Maintenance therapy with cidofovir involves an infusion only once every two weeks, making it a convenient treatment option. Because dosing is relatively infrequent, a permanent catheter is not necessary for infusions.

Cidofovir was discovered at the Institute of Organic Chemistry and Biochemistry, Prague, by Antonín Holý, and developed by Gilead Sciences and is marketed with the brand name Vistide by Gilead in the USA, and by Pfizer elsewhere.

Synthesis

Cidofovir syn.png

Brodfuehrer, P; Howell, Henry G.; Sapino, Chester; Vemishetti, Purushotham (1994). “A practical synthesis of (S)-HPMPC”.Tetrahedron Letters 35 (20): 3243. doi:10.1016/S0040-4039(00)76875-4.

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