Ganciclovir

Abstract

Ganciclovir is synthetic nucleoside analog of guanine closely related to acyclovir but has greater activity against cytomegalovirus. This comprehensive profile on ganciclovir starts with a description of the drug: nomenclature, formulae, chemical structure, elemental composition, and appearance. The uses and application of the drug are explained. The methods that were used for the preparation of ganciclovir are described and their respective schemes are outlined. The methods which were used for the physical characterization of the dug are: ionization constant, solubility, X-ray powder diffraction pattern, crystal structure, melting point, and differential scanning calorimetry. The chapter contains the spectra of the drug: ultraviolet spectrum, vibrational spectrum, nuclear magnetic resonance spectra, and the mass spectrum. The compendial methods of analysis of ganciclovir include the United States Pharmacopeia methods. Other methods of analysis that were reported in the literature include: high-performance liquid chromatography alone or with mass spectrometry, electrophoresis, spectrophotometry, voltammetry, chemiluminescence, and radioimmunoassay. Biological investigation on the drug includes: pharmacokinetics, metabolism, bioavailability, and biological analysis. Reviews on the methods used for preparation or for analysis of the drug are provided. The stability of the drug in various media and storage conditions is reported. More than 240 references are listed at the end of the chapter.

Bright and Early: Inhibiting Human Cytomegalovirus by Targeting Major Immediate-Early Gene Expression or Protein Function

“…Inside cells, GCV is converted to the active triphosphate via initial phosphorylation by the HCMV phosphotransferase (pUL97) and subsequent phosphorylation steps by cellular kinases. GCV inhibits the HCMV DNA polymerase (pUL54) by competing with deoxyguanosine triphosphate for the enzyme's active site, thus preventing nucleotide incorporation into the elongating viral DNA [60,64]. A closely related nucleoside analogue, Acyclovir, is potent against members of the Alphaherpesvirinae but exhibits very modest antiviral activity for HCMV [60,65].…”

Neural Progenitor Cells Expressing Herpes Simplex Virus-Thymidine Kinase for Ablation Have Differential Chemosensitivity to Brivudine and Ganciclovir

“…A possible explanation for why the two prodrugs have an additive effect when introduced to the cells together is that they are analogues of different nucleoside bases; ganciclovir is an analogue for guanine and brivudine is an analogue of thymidine (Keam et al, 2004 ; Al-Badr and Ajarim, 2018 ). When introduced together, their triphosphate forms compete for integration into the host DNA during replication with the host nucleotides but not with each other, increasing the frequency of chain termination and double stranded DNA breaks due to more targets being available.…”

Paediatric ganciclovir dosing in extracorporeal membrane oxygenation: Is standard dosing good enough?

“…Ganciclovir concentrations were determined by high‐performance liquid chromatography in the Special Chemistry Laboratory at Cincinnati Children's Hospital Medical Center. A one‐compartment model was used to characterize the pharmacokinetic profile of ganciclovir based upon reported literature . Sawchuk‐Zaske equations were used to estimate the AUC based on two concentrations.…”