生物活性

• 描述Cytomegalovirus (CMV) is a herpes virus that causes disease in severely immunocompromized patients. The ganciclovir prodrug valganciclovir, avalyl ester of ganciclovir, is rapidly converted to ganciclovir during the first pass process in the gut wall and is used to treat CMV infection. In vitro, valganciclovir inhibited the uptake of glycylsarcosine in a dose-dependent manner with IC₅₀ values of 1.69 ± 0.30 mM in Caco-2 cells and 0.046 ± 0.005 mM in SKPT cells, respectively. Likewise, it inhibited the uptake of the dipeptide in a dose-dependent manner with IC₅₀ values of 2.84 ± 0.42 mM in PEPT1-expressing cells and 0.176 ± 0.012 mM in PEPT2-expressing cells^[3]. For patients with CMV viremia, valganciclovir (900 mg b.i.d. for 7 days) was effective as pre-emptive therapy with rate of viral clearance at 28 days of 89.5%^[4].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02227641	Patients Undergoing Allogeneic... more >> Stem Cell Transplantation Collapse <<	Phase 1 Phase 2	Unknown	March 2017	Germany ... more >> Medical Center Augsburg Recruiting Augsburg, Germany, 86156 Contact: Christoph Schmid, MD, PhD    0049 821 4002736       Principal Investigator: Christoph Schmid, MD, PhD          Charité University Hospital Berlin Recruiting Berlin, Germany, 13353 Contact: Armin H Gerbitz, MD, PhD    ++49 30 450565256    armin.gerbitz@charite.de    Contact: Lutz Uharek, MD, PhD       lutz.uharek@charite.de    Sub-Investigator: Lutz Uharek, MD, PhD          Principal Investigator: Armin Gerbitz, MD, PhD          Universitiy Hospital Erlangen Recruiting Erlangen, Germany, 91054 Contact: Anita Kremer, MD, PhD    ++49 9131 8543183    anita.kremer@uk-erlangen.de    Contact: Bernd Spriewald, MD, PhD    ++49 9131 8543116    bernd.spriewald@uk-erlangen.de    Sub-Investigator: Katja San Niccolo, MD          University of Mainz Recruiting Mainz, Germany, 55131 Contact: Eva Wagner, MD          Principal Investigator: Eva Wagner, MD          University of Munich LMU Recruiting Munich, Germany, 81377 Contact: Johanna Tischer, MD    0049 89 70954240       Principal Investigator: Johanna Tischer, MD          University of Regensburg Not yet recruiting Regensburg, Germany, 93053 Contact: Ernst Holler, MD, PhD    0049 941 9445570       Principal Investigator: Ernst Holler, MD, PhD Collapse <<
  NCT00078559	Kidney Transplantation ... more >> Kidney Disease Collapse <<	Phase 1 Phase 2	Completed	-	United States, Wisconsin ... more >> University of Wisconsin - Department of Medicine Madison, Wisconsin, United States, 53792-1735 Collapse <<
  NCT02188719	Liver Transplantation	Phase 1	Recruiting	January 2022	United States, California ... more >> University of California, San Francisco Recruiting San Francisco, California, United States, 94143 Contact: Monique Koenigsberg    415-502-3016    Monique.Koenigsberg@ucsf.edu    Principal Investigator: Sandy Feng, MD, PhD          United States, Illinois Northwestern University Recruiting Chicago, Illinois, United States, 55905 Contact: Patrice Al-Saden    312-503-1058    palsaden@northwestern.edu    Principal Investigator: Josh Levitsky, MD          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Julie Gecox Hanson, CCRP    507-293-6592    Gecox.Julie@mayo.edu    Principal Investigator: Timucin Taner, MD, PhD Collapse <<

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• 参考文献

• [1] Chawla JS, Ghobadi A, et al. Oral valganciclovir versus ganciclovir as delayed pre-emptive therapy for patients after allogeneic hematopoietic stem cell transplant: a pilot trial (04-0274) and review of the literature. Transpl Infect Dis. 2012 Jun;14(3):259-67.

  [2] Sugawara M, Huang W, et al. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9.

  [3] Sugawara M, Huang W, Fei YJ, Leibach FH, Ganapathy V, Ganapathy ME. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9

  [4] Chawla JS, Ghobadi A, et al. Oral valganciclovir versus ganciclovir as delayed pre-emptive therapy for patients after allogeneic hematopoietic stem cell transplant: a pilot trial (04-0274) and review of the literature. Transpl Infect Dis. 2012 Jun;14(3):259-67