"目錄號(hào): HY-13637
Ganciclovir是皰疹家族病毒的有效抑制劑，包括巨細(xì)胞病毒（CMV），對(duì)于FHV-1的IC50值為5.2 μM 。
相關(guān)產(chǎn)品
Acyclovir-Penciclovir-Vidarabine-Valacyclovir hydrochloride-Idoxuridine-BAY 57-1293-Famciclovir-Fiacitabine-1-Docosanol-Tromantadine-
生物活性
Description
Ganciclovir is a potent inhibitor of viruses of the herpes family, including cytomegalovirus (CMV), with anIC50of 5.2 μM for feline herpesvirus type-1 (FHV-1).
IC50& Target
IC50: 5.2 μM (FHV-1)[1]
In Vitro
Ganciclovir is an acyclic deoxyguanosine analog structurally similar to acyclovir but with superior activity against CMV. The median ganciclovir concentration required to inhibit viral replication by 50 percent is 2.15 mumol versus 72 mumol for acyclovir[2].The primary mechanism of ganciclovir action against CMV is inhibition of the replication of viral DNA by ganciclovir-5'-triphosphate (ganciclovir-TP). This inhibition includes a selective and potent inhibition of the viral DNA polymerase.Ganciclovir is metabolized to the triphosphate form by primarily three cellular enzymes: a deoxyguanosine kinase induced by CMV-infected cells; guanylate kinase; and phosphoglycerate kinase[3].
In Vivo
In adult rats, the intracochlear diffusion of ganciclovir is shown to achieve the same concentration as in blood. In gestating mice, transplacental diffusion is observed, with a fetal-to-maternal blood ratio of 0.5. In newborn mice, the plasma concentration profile of ganciclovir shows a peak at 2 h followed by a gradual decrease. In adult mice, the concentration peaked at 1 h, but becomes undetectable by 2 h after injection. Counts of white blood cells, red blood cells and platelets decreases significantly in ganciclovir-treated newborn mice[4].
Clinical Trial
National Institute of Neurological Disorders and Stroke (NINDS)-National Institutes of Health Clinical Center (CC)
Brain Neoplasm-Neoplasm Metastasis
August 21, 1992
Phase 1
Singapore National Eye Centre
Cytomegalovirus Anterior Segment Infection-Anterior Uveitis-Endotheliitis
July 2012
Singapore National Eye Centre
Cytomegalovirus Infections
August 2016
Phase 4
Adapt Produtos Oftalmológicos Ltda.
Conjunctivitis-Adenovirus.
May 2012
Phase 3
Pierrel Research Europe GmbH-Roche Pharma AG
Allogeneic Stem Cell Transplantation
September 2010
Phase 3
Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Lymphoma-Lymphoproliferative Disorder
March 2005
Phase 1
Nuria Lloberas-Ministerio de Sanidad, Servicios Sociales e Igualdad-Hospital Universitari de Bellvitge
Infection in Solid Organ Transplant Recipients
December 2011
Phase 4
Federal University of S?o Paulo
Conjunctivitis, Viral-Adenoviridae Infections
August 2009
Salvador Gil-Vernet-Roche Pharma AG-Hospital Universitari de Bellvitge
Cytomegalovirus Infection
March 2004
Phase 4
Johns Hopkins Bloomberg School of Public Health
Cytomegalovirus Retinitis-HIV Infections
May 1997
Phase 3
Washington University School of Medicine
Cytomegalovirus Infections
June 2004
Phase 3
Johns Hopkins Bloomberg School of Public Health-National Eye Institute (NEI)-Johns Hopkins University-University of Wisconsin, Madison-Baylor College of Medicine-Louisiana State University Health Sciences Center in New Orleans-New York Presbyterian Hospital-Icahn School of Medicine at Mount Sinai-New York University School of Medicine-Northwestern University-University of California, Los Angeles-University of California, San Diego-University of California, San Francisco-University of Miami-University of Massachusetts, Worcester-Memorial Sloan Kettering Cancer Center
HIV Infections-Cytomegalovirus Retinitis
March 1990
Phase 3
Fred Hutchinson Cancer Research Center-National Heart, Lung, and Blood Institute (NHLBI)-Genentech, Inc.
Acute Lung Injury-Acute Respiratory Distress Syndrome-Respiratory Failure
September 2011
Phase 2
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections-HIV Infections
Phase 1
National Institute of Allergy and Infectious Diseases (NIAID)-Hoffmann-La Roche
Cytomegalovirus Retinitis-HIV Infections
Phase 1
National Institute of Allergy and Infectious Diseases (NIAID)-Hoffmann-La Roche
Cytomegalovirus Retinitis-HIV Infections
Phase 3
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Infections-HIV Infections
Roche Global Development-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Roche Global Development-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Infections-HIV Infections
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Roche Global Development-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Retinitis-HIV Infections
Phase 1
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Infections-Cytomegalovirus Retinitis-HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Retinitis-HIV Infections
Phase 3
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Infections-HIV Infections
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Hoffmann-La Roche-NIH AIDS Clinical Trials Information Service
Colitis-HIV Infections
Lower Saxony Center for Nephrology
DNA Virus Infection-Herpesviridae Infections-Cytomegalovirus Infection
August 2000
Phase 4
National Institute of Allergy and Infectious Diseases (NIAID)-Hoffmann-La Roche
Cytomegalovirus Retinitis-HIV Infections-Gastrointestinal Diseases
Phase 2
City of Hope Medical Center-National Cancer Institute (NCI)
Chronic Myeloproliferative Disorders-Leukemia-Lymphoma-Multiple Myeloma and Plasma Cell Neoplasm-Myelodysplastic Syndromes-Myelodysplastic/Myeloproliferative Diseases
March 1999
Phase 2
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Retinitis-HIV Infections
Phase 1
Hoffmann-La Roche
Cytomegalovirus Infections
April 2004
Phase 4
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections
July 2002
Phase 1-Phase 2
Schering-Plough-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Phase 3
University of Oslo School of Pharmacy
Acute Renal Failure-Cytomegalovirus Infections-Multi Organ Failure
December 2005
Phase 4
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections
Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)-Hoffmann-La Roche
Colitis-HIV Infections
Phase 1
HemaQuest Pharmaceuticals Inc.-Boston University
EBV Lymphomas-Lympho-proliferative Diseases
September 2008
Phase 2
National Institute of Allergy and Infectious Diseases (NIAID)-Johns Hopkins University
Cytomegalovirus Retinitis-HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)
Encephalopathy-HIV Infections-Radiculitis
Phase 1
Ionis Pharmaceuticals, Inc.-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Phase 2
National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections-HIV Infections
Boston Medical Center
Leukemia-Lymphoma-Precancerous Condition-Small Intestine Cancer
December
