valacyclovir profile

Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	135398742
CHEMBL ID	1349
CHEBI ID	35854
SCHEMBL ID	28644
MeSH ID	M0224608

Synonym
l-valine ester with 9-((2-hydroxyethoxy)methyl)guanine
CHEBI:35854 ,
2-[(2-amino-6-oxo-1,6-dihydro-9h-purin-9-yl)methoxy]ethyl l-valinate
MLS001304747
smr000752514
BRD-K46435977-003-01-2
talavir
256u87
bw-256u
valacv
virval
valaciclovir
zelitrex
2-{[(2-amino-6-oxo-1,6-dihydro-9h-purin-9-yl)methyl]oxy}ethyl l-valinate
BSPBIO_002474
valacyclovir
124832-26-4
valtrex (tm)
acyclovir-valine
vacv
l-valine, 2-((2-amino-1,6-dihydro-6-oxo-9h-purin-9-yl)methoxy)ethyl ester
valaciclovir, valtrex
2-[(2-amino-6-oxo-1h-purin-9-yl)methoxy]ethyl (2s)-2-amino-3-methyl-butanoate
bw256u87
DB00577
valaciclovir [inn:ban]
HMS2090D20
AC-11128
2-[(2-amino-6-oxo-3h-purin-9-yl)methoxy]ethyl (2s)-2-amino-3-methylbutanoate
bdbm50162073
(s)-2-((2-amino-6-oxo-3h-purin-9(6h)-yl)methoxy)ethyl 2-amino-3-methylbutanoate
(s)-2-amino-3-methyl-butyric acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-ethyl ester
D08664
valaciclovir (inn)
CHEMBL1349 ,
2-[(2-amino-6-oxo-3h-purin-9-yl)methoxy]ethyl 2-amino-3-methyl-butanoate;l-valine 2-(guanin-9-ylmethoxy)ethyl ester
A805302
AKOS005622706
AKOS007930693
HMS2234I15
valcyclovir [inn:ban]
valcyclovir
unii-mz1iw7q79d
hsdb 8084
valcivir
mz1iw7q79d ,
val-acv
valacyclover hydrochloric
HY-17425
CS-1356
txc ,
NCGC00178638-04
l-valine 2-((2-amino-1,6-dihydro-6-oxo-9h-purin-9-yl)methoxy)ethyl ester
valaciclovir [inn]
valacyclovir [mi]
valaciclovir [who-dd]
l-valine, ester with 9-((2-hydroxyethoxy)methyl)guanine
valacyclovir [vandf]
2-[(2-amino-6-oxo-6,9-dihydro-3h-purin-9-yl)methoxy]ethyl (2s)-2-amino-3-methylbutanoate
256u87 hcl
gtpl4824
valacyclovir hydrochloride (monohydrate)
AB00698497-11
SCHEMBL28644
AB01275525-01
HDOVUKNUBWVHOX-QMMMGPOBSA-N
MLS006011776
smr004703478
W-200980
AKOS025149468
AB01275525_03
AB01275525_02
DTXSID1023732 ,
2-[(2-amino-1,6-dihydro-6-oxo-9h-purin-9-yl)methoxy]ethyl-l-valinate
SBI-0206711.P001
(s)-2-((2-amino-6-oxo-1h-purin-9(6h)-yl)methoxy)ethyl 2-amino-3-methylbutanoate
ZB0748
AKOS037496964
Q418594
(s)-2-[(2-amino-6-oxo-6,9-dihydro-3h-purin-9-yl)methoxy]ethyl-2-amino-3-methylbutanoate
valaciclovir;val-acv; valtrex; zelitrex
BCP28415
BRD-K46435977-003-03-8
2-[(2-amino-6-oxo-1h-purin-9-yl)methoxy]ethyl (2s)-2-amino-3-methylbutanoate
NCGC00178638-05
l-valine, 2-[(2-amino-1,6-dihydro-6-oxo-9h-purin-9-yl)methoxy]ethyl ester
EN300-150220
valaciclovirum
2-((2-amino-6-oxo-1,6-dihydro-9h-purin-9-yl)methoxy)ethyl l-valinate
dtxcid403732
j05ab11
l-valine ester with 9-

Excerpt	Reference	Relevance
" There were no valaciclovir-related changes or abnormalities in safety parameters and no reports of serious adverse experiences in these elderly volunteers."	( Pharmacokinetics and safety of multiple-dose valaciclovir in geriatric volunteers with and without concomitant diuretic therapy. Blum, MR; Schultz, M; Smiley, ML; Wang, LH; Weller, S, 1996)	0.29
" Although acyclovir and its analogues are generally safe drugs, they should be used with caution in patients with end-stage renal disease."	( Neurotoxicity caused by valacyclovir in a patient on hemodialysis. Feith, GW; Linssen-Schuurmans, CD; Uges, DR; van Kan, EJ, 1998)	0.3
" Toxic events were recorded in 16 of 29 patients (55."	( Suicide gene therapy toxicity after multiple and repeat injections in patients with localized prostate cancer. Adler, HL; Aguilar-Cordova, E; Butler, EB; Herman, JR; Kadmon, D; Miles, BJ; Scardino, PT; Shalev, M; Teh, BS; Thompson, TC, 2000)	0.31
"Direct injection into the prostate of a replication defective adenovirus containing the HSV-tk gene followed by intravenous ganciclovir is safe even in repeat cycles."	( Suicide gene therapy toxicity after multiple and repeat injections in patients with localized prostate cancer. Adler, HL; Aguilar-Cordova, E; Butler, EB; Herman, JR; Kadmon, D; Miles, BJ; Scardino, PT; Shalev, M; Teh, BS; Thompson, TC, 2000)	0.31
" Tolerance was also assessed on the incidence and types of adverse effects and changes in laboratory parameters."	( Comparison of the efficacy and safety of valaciclovir and acyclovir for the treatment of herpes zoster ophthalmicus. Cochener, B; Colin, J; Hoang-Xuan, T; Lescale, O; Prisant, O; Rolland, B, 2000)	0.31
" The most frequent adverse events were vomiting and edema of the eyelids or face (3%-5%)."	( Comparison of the efficacy and safety of valaciclovir and acyclovir for the treatment of herpes zoster ophthalmicus. Cochener, B; Colin, J; Hoang-Xuan, T; Lescale, O; Prisant, O; Rolland, B, 2000)	0.31
" There was no clinically significant difference in the nature, frequency or severity of adverse events between these two groups, although one and three adverse events were reported in the acyclovir and valaciclovir group, respectively."	( Comparative study of the efficacy and safety of valaciclovir versus acyclovir in the treatment of herpes zoster. Chen, YS; Chiang, SC; Huang, CK; Lee, SS; Lin, HH; Lin, WR; Liu, YC; Tsai, HC; Wann, SR; Yen, MY, 2001)	0.31
" Valaciclovir was well tolerated, with gastrointestinal disturbances and headache being the most common adverse effects in a small number of subjects."	( Pharmacokinetics and safety of valaciclovir in children with Epstein-Barr virus illness. Deeter, RG; Fish, DN; Simon, MW, 2002)	0.31
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."	( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004)	0.32
" It is concluded, that continuous suppressive therapy of HSV infections with valacyclovir is safe and effective treatment, which strongly prevents reoccurrence or transmissions of HSV infections to sexual partners."	( Evaluation of safety and efficacy of prolonged suppressive therapy of genital herpes with valacyclovir. Durglishvili, N; Kvirkvelia, V; Shishniashvili, D, )	0.13
" Although we could treat the patient only by continuation of peritoneal dialysis, hemodialysis seems to be an effective treatment method in the case of unstable general condition or severe adverse effects, because it can eliminate the serum acyclovir."	( [Neurotoxicity of valacyclovir in a peritoneal dialysis patient]. Kyoda, Y; Maehana, T; Takayanagi, A; Yanase, M, 2010)	0.36
" No clinically significant adverse effects occurred."	( Safety of short-term valacyclovir as an anti-sickling agent in sickle-cell anemia. Billote, GB; Brittenham, GM; DeBellis, RH; Ender, KL; Erlanger, BF, 2011)	0.37
" Valacyclovir was not associated with infant or maternal toxicities or adverse events, and no congenital malformations were observed."	( Infant safety during and after maternal valacyclovir therapy in conjunction with antiretroviral HIV-1 prophylaxis in a randomized clinical trial. Drake, AL; Farquhar, C; John-Stewart, G; Kiarie, J; Richardson, BA; Roxby, AC; Wald, A, 2012)	0.38
"Exposure to PMTCT ARVs and acyclovir after maternal administration of valacyclovir during pregnancy and postpartum to women co-infected with HIV-1/HSV-2 was not associated with an increase in infant or maternal toxicities or adverse events."	( Infant safety during and after maternal valacyclovir therapy in conjunction with antiretroviral HIV-1 prophylaxis in a randomized clinical trial. Drake, AL; Farquhar, C; John-Stewart, G; Kiarie, J; Richardson, BA; Roxby, AC; Wald, A, 2012)	0.38
"To report a case of Acute Retinal Necrosis (ARN)-developed nephrotoxicity during intravenous acyclovir treatment and toxic hepatitis during oral valacyclovir treatment."	( Systemic side effects of antiviral therapy in a patient with acute retinal necrosis. Akcay, BI; Bozkurt, K; Erdogan, G; Guney, E; Onur, U; Unlu, C, 2014)	0.4
" After switching to oral valacyclovir, toxic hepatitis developed."	( Systemic side effects of antiviral therapy in a patient with acute retinal necrosis. Akcay, BI; Bozkurt, K; Erdogan, G; Guney, E; Onur, U; Unlu, C, 2014)	0.4
" Valacyclovir was not associated with toxicity or adverse events."	( A pilot study examining the safety and tolerability of valacyclovir in veterans with hepatitis C virus/herpes simplex virus type 2 coinfection. Burton, MJ; Hook, EW; McGuire, BM; Penman, A; Sunesara, I, 2014)	0.4
" As valacyclovir induces renal dysfunction, which raises the serum acyclovir level to the toxic range, special attention must be paid when administering this drug in elderly subjects."	( [Acyclovir-induced neurotoxicity and acute kidney injury in an elderly diabetic patient treated with valacyclovir: report of a case]. Kondo, M; Miyao, M; Mizuno, Y; Nomura, K; Okuyama, T; Sagawa, N; Sata, A; Tsurutani, Y, 2014)	0.4
"To determine whether antiviral therapy is safe and effective for preventing CMV reactivation in a general population of critically ill patients."	( Safety and Efficacy of Antiviral Therapy for Prevention of Cytomegalovirus Reactivation in Immunocompetent Critically Ill Patients: A Randomized Clinical Trial. Bion, JF; Cowley, NJ; Ives, N; Millar, J; Moss, P; Osman, H; Owen, A; Shiels, SC; Woolley, R, 2017)	0.46
" The objective of the study was to investigate reports of acute kidney injury (AKI) events associated with the concomitant use of oral acyclovir or valacyclovir with an NSAID by using the United States Food and Drug Administration (FDA) Adverse Event Reporting System (AERS) database between January 2004 and June 2012."	( Association between Concomitant Use of Acyclovir or Valacyclovir with NSAIDs and an Increased Risk of Acute Kidney Injury: Data Mining of FDA Adverse Event Reporting System. Li, H; Shi, J; Yue, Z, 2018)	0.48
" In terms of safety, letermovir was at least similar in comparison with placebo and most agents while both letermovir and acyclovir showed significantly reduced risk for serious adverse events compared with ganciclovir, with RRs of ."	( Comparative Efficacy and Safety of Different Antiviral Agents for Cytomegalovirus Prophylaxis in Allogeneic Hematopoietic Cell Transplantation: A Systematic Review and Meta-Analysis. Gagelmann, N; Kröger, N; Ljungman, P; Styczynski, J, 2018)	0.48
" Despite their good safety profile, they can cause systemic adverse effects, such as neurotoxicity, which are less frequent and known."	( Neurotoxicity associated with acyclovir and valacyclovir: A systematic review of cases. Brandariz-Nuñez, D; Correas-Sanahuja, M; Martín Herranz, I; Maya-Gallego, S, 2021)	0.62
"The neurotoxicity induced by acyclovir and its derivative valacyclovir is a poorly known and rare adverse effect that can occur mainly in patients with advanced age and impaired renal function."	( Neurotoxicity associated with acyclovir and valacyclovir: A systematic review of cases. Brandariz-Nuñez, D; Correas-Sanahuja, M; Martín Herranz, I; Maya-Gallego, S, 2021)	0.62
" The primary outcome was an incidence of biopsy-proven acute rejection, whereas the secondary outcome was a composite of major adverse drug reactions."	( Efficacy and Safety of Antiviral Agents in Preventing Allograft Rejection Following CMV Prophylaxis in High-Risk Kidney Transplantation: A Systematic Review and Network Meta-Analysis of Randomized Controlled Trials. Chaiyakittisopon, K; Ngamprasertchai, T; Phoompoung, P; Ruenroengbun, N; Sapankaew, T, 2022)	0.72
" The role of valacyclovir therapy in reducing the risk of vertical transmission, symptomatic congenital CMV infection and adverse outcome is controversial."	( Effectiveness and safety of prenatal valacyclovir for congenital cytomegalovirus infection: systematic review and meta-analysis. D'Antonio, F; Khalil, A; Marinceu, D; Prasad, S, 2023)	0.91
" The secondary outcomes were symptomatic and asymptomatic infection, perinatal death, termination of pregnancy, anomalies detected on follow-up ultrasound, on fetal magnetic resonance imaging or at birth, severe and mild-to-moderate symptoms due to congenital CMV infection, neurological, visual and hearing symptoms, and adverse events related to valacyclovir."	( Effectiveness and safety of prenatal valacyclovir for congenital cytomegalovirus infection: systematic review and meta-analysis. D'Antonio, F; Khalil, A; Marinceu, D; Prasad, S, 2023)	0.91
"The purpose of this study was to compare the efficacy and adverse events of various antiviral agents used for the treatment of HZ-associated pain through a network meta-analysis."	( A Network Meta-Analysis of Randomized Clinical Trials to Assess the Efficacy and Safety of Antiviral Agents for Immunocompetent Patients with Herpes Zoster-Associated Pain. Li, J; Li, X; Liu, Y; Long, X; Xiao, S; Zhang, Y, 2023)	0.91
" The primary outcome was the presence of acute pain at the end of anti-virus treatment, and the secondary outcomes included the presence of pain at 28-30 days after the onset of the acute herpetic rash, the presence of postherpetic neuralgia (PHN), and any other adverse events."	( A Network Meta-Analysis of Randomized Clinical Trials to Assess the Efficacy and Safety of Antiviral Agents for Immunocompetent Patients with Herpes Zoster-Associated Pain. Li, J; Li, X; Liu, Y; Long, X; Xiao, S; Zhang, Y, 2023)	0.91

Excerpt	Reference	Relevance
"hr, respectively) and Cmax (8 and 23 microM, respectively) increasing nearly in proportion to the dose."	( Metabolic fate and pharmacokinetics of the acyclovir prodrug valaciclovir in cynomolgus monkeys. Burnette, TC; de Miranda, P, )	0.13
" Pharmacokinetic findings for valaciclovir and acyclovir were consistent in the two studies."	( Pharmacokinetics of the acyclovir pro-drug valaciclovir after escalating single- and multiple-dose administration to normal volunteers. Blum, MR; Burnette, T; Cederberg, DM; de Miranda, P; Doucette, M; Smiley, ML; Weller, S, 1993)	0.29
" Pharmacokinetic evaluation was performed for three groups: normotensive subjects given 500-mg doses of valaciclovir (n = 11), normotensive subjects given, 1,000-mg doses of valaciclovir (n = 9), and thiazide diuretic-treated hypertensive subjects given 500-mg doses of valaciclovir (n = 9)."	( Pharmacokinetics and safety of multiple-dose valaciclovir in geriatric volunteers with and without concomitant diuretic therapy. Blum, MR; Schultz, M; Smiley, ML; Wang, LH; Weller, S, 1996)	0.29
"The objective was to obtain preliminary pharmacokinetic data for acyclovir from gravid women receiving herpes simplex virus suppressive therapy with the acyclovir prodrug valacyclovir."	( Pharmacokinetics of oral valacyclovir and acyclovir in late pregnancy. Andrews, WW; Hauth, JC; Kimberlin, DF; Lakeman, F; Miller, G; Weller, S; Whitley, RJ, 1998)	0.3
" Acyclovir pharmacokinetic profiles were obtained after the initial dose (36 weeks) and at steady state (38 weeks)."	( Pharmacokinetics of oral valacyclovir and acyclovir in late pregnancy. Andrews, WW; Hauth, JC; Kimberlin, DF; Lakeman, F; Miller, G; Weller, S; Whitley, RJ, 1998)	0.3
" There was no significant difference in drug elimination half-life or in time to peak concentration between valacyclovir and acyclovir recipients at either sampling interval."	( Pharmacokinetics of oral valacyclovir and acyclovir in late pregnancy. Andrews, WW; Hauth, JC; Kimberlin, DF; Lakeman, F; Miller, G; Weller, S; Whitley, RJ, 1998)	0.3
" The pharmacokinetic analysis was performed by pharmacokinetic modelling."	( Pharmacokinetics of acyclovir in immunocompromized children with leukopenia and mucositis after chemotherapy: can intravenous acyclovir be substituted by oral valacyclovir? Eksborg, S; Kalin, M; Pal, N; Palm, C; Söderhäll, S, 2002)	0.31
"Valacyclovir was administered to 28 immunocompromised children (ages 5-12 years) to obtain preliminary pharmacokinetic and safety information."	( An investigation of the steady-state pharmacokinetics of oral valacyclovir in immunocompromised children. Floret, D; Leibundgut, K; Leverger, G; Nadal, D; Perel, Y; Sokal, EM; Weller, S, 2002)	0.31
" Doses of either suspension or tablets were administered every 8 hours for four doses, and pharmacokinetic studies were performed to determine aciclovir serum concentrations."	( Pharmacokinetics and safety of valaciclovir in children with Epstein-Barr virus illness. Deeter, RG; Fish, DN; Simon, MW, 2002)	0.31
" In this article, we describe correlations of pharmacokinetic parameters following oral valacyclovir or acyclovir administration with expression levels of intestinal genes in humans."	( Gene expression in the human intestine and correlation with oral valacyclovir pharmacokinetic parameters. Amidon, GL; Barnett, JL; Foster, DR; Landowski, CP; Menon, SS; Ramachandran, C; Sun, D; Welage, LS, 2003)	0.32
"To investigate a potential pharmacokinetic interaction between mycophenolate mofetil (MMF) and aciclovir or valaciclovir."	( Evaluation of pharmacokinetic interactions after oral administration of mycophenolate mofetil and valaciclovir or aciclovir to healthy subjects. Bidault, R; Bourdon, O; Foeillet, E; Garret, C; Gimenez, F; Singlas, E; Weller, S, 2004)	0.32
" The following pharmacokinetic parameters were estimated for aciclovir, mycophenolic acid (MPA) and its inactive glucuronide metabolite (MPAG) from the plasma concentration-time data using noncompartmental methods: area under the concentration-time curve from zero to infinity (AUC infinity), terminal elimination half-life (t1/2z), peak concentration (Cmax) and time to Cmax (tmax)."	( Evaluation of pharmacokinetic interactions after oral administration of mycophenolate mofetil and valaciclovir or aciclovir to healthy subjects. Bidault, R; Bourdon, O; Foeillet, E; Garret, C; Gimenez, F; Singlas, E; Weller, S, 2004)	0.32
"The purpose of the study was to evaluate the pharmacokinetic effects obtained by gastroretentive dosage form (GRDF) for drugs absorbed by passive paracellular diffusion (atenolol, acyclovir) or active transport (valacyclovir)."	( Selection of drug candidates for gastroretentive dosage forms: pharmacokinetics following continuous intragastric mode of administration in a rat model. Hoffman, A; Kagan, L, 2008)	0.35
" This report describes acyclovir pharmacokinetics following valacyclovir administration in immunocompromised pediatric patients, compares pharmacokinetic parameters following oral valacyclovir and IV acyclovir, and provides a limited assessment of efficacy in the setting of active herpes zoster infection."	( Valacyclovir and acyclovir pharmacokinetics in immunocompromised children. Aleksic, A; Berg, S; Blaney, S; Bomgaars, L; Serabe, B; Thompson, P, 2008)	0.35
" Pharmacokinetic data are available for 32 patients following valacyclovir (15 mg/kg) administration, 11 of whom also had pharmacokinetic sampling following IV acyclovir administration."	( Valacyclovir and acyclovir pharmacokinetics in immunocompromised children. Aleksic, A; Berg, S; Blaney, S; Bomgaars, L; Serabe, B; Thompson, P, 2008)	0.35
" A one-compartment pharmacokinetic model with first-order elimination best described the acyclovir concentration-time data."	( Population pharmacokinetics of acyclovir in children and young people with malignancy after administration of intravenous acyclovir or oral valacyclovir. Blair, EY; Coakley, JC; Earl, JW; McLachlan, AJ; Nath, CE; Shaw, PJ; Stephen, K; Zeng, L, 2009)	0.35
" Acyclovir pharmacokinetic parameters do not correlate with response metrics."	( Valacyclovir pharmacokinetics and exploratory pharmacodynamics in young adults with Epstein-Barr virus infectious mononucleosis. Anderson, BJ; Balfour, HH; Brundage, RC; Vezina, HE; Weller, DR, 2010)	0.36
" Blood samples for pharmacokinetic analysis were collected during the 6 h after the first dose."	( Pharmacokinetics and safety of extemporaneously compounded valacyclovir oral suspension in pediatric patients from 1 month through 11 years of age. Bradley, JS; Heitman, CK; Jacobs, RF; Kimberlin, DW; Man, CY; van der Walt, JS; Weller, S, 2010)	0.36
" Blood samples for pharmacokinetic profiling were taken up to 24 h post-dose."	( Pharmacokinetics and bioequivalence study of valacyclovir hydrochloride capsules after single dose administration in healthy Chinese male volunteers. Lin, H; Mao, GG; Tian, JX; Tian, Y; Zhang, ZJ, 2010)	0.36
"The study was an open label, one-sequence cross-over pharmacokinetic study in HIV-negative adults."	( Lack of a pharmacokinetic interaction between steady-state tipranavir/ritonavir and single-dose valacyclovir in healthy volunteers. Castles, MA; Cong, XJ; Kraft, MF; MacGregor, TR; Mauss, S; Sabo, JP; Wallace, L, 2011)	0.37
" The time to peak concentration of acyclovir was 3- to 10-fold longer in KO compared with WT mice."	( Impact of peptide transporter 1 on the intestinal absorption and pharmacokinetics of valacyclovir after oral dose escalation in wild-type and PepT1 knockout mice. Hu, Y; Smith, DE; Yang, B, 2013)	0.39
"A preliminary population pharmacokinetic (PopPK) model of valacyclovir in children was developed from non-compartmental analysis (NCA) parameter values from literature, including several age groups, combined with Bayesian priors from a PopPK model of acyclovir, the active metabolite of valacyclovir, from literature too."	( Development of a paediatric population pharmacokinetic model for valacyclovir from literature non-compartmental values originating from sparse studies and Bayesian priors: a simulation study. Dokoumetzidis, A; Kechagia, IA, 2015)	0.42
" The aim of the study was to extrapolate the approved dosages of acyclovir, to valacyclovir dosages, in children using Monte Carlo simulations based on the population pharmacokinetic (PopPK) models of valacyclovir and acyclovir."	( Extrapolation of Valacyclovir Posology to Children Based on Pharmacokinetic Modeling. Dokoumetzidis, A; Kalantzi, L; Kechagia, IA, 2015)	0.42
" We performed a pharmacokinetic modeling and simulation study by integrating the existing understanding of physiology with previously published data to evaluate the vitreal penetration of oral valacyclovir for the treatment of ARN, under various dosing scenarios."	( Valacyclovir as Initial Treatment for Acute Retinal Necrosis: A Pharmacokinetic Modeling and Simulation Study. Fung, M; Ivaturi, V; Jain, A; Liu, T; Vinnard, C, 2017)	0.46
"In this study, a physiologically based pharmacokinetic (PBPK) model was established for valacyclovir based on absolute expression quantity of hPEPT1 along the entire length of the human intestine and other reliable in vitro, in vivo observed data."	( A physiologically based pharmacokinetic model for valacyclovir established based on absolute expression quantity of hPEPT1 and its application. Sun, L; Wang, C; Zhang, Y, 2018)	0.48

Excerpt	Reference	Relevance
"Two methods are presented for the determination of 'respectively' the plasma protein unbound and total concentration of acyclovir in horse plasma and body fluids: first, a liquid-liquid extraction was performed on plasma, combined with HPLC-fluorescence detection for the total plasma concentration; second a more sensitive method using high-performance liquid chromatography combined with heated electrospray ionization tandem mass spectrometry (LC-HESI-MS/MS) was described for plasma and for body fluids analysis."	( Determination of acyclovir in horse plasma and body fluids by high-performance liquid chromatography combined with fluorescence detection and heated electrospray ionization tandem mass spectrometry. Croubels, S; De Backer, P; Desmet, N; Garré, B; Maes, A; Nauwynck, H; van der Meulen, K, 2009)	0.35
"We report a case of a potential drug-drug interaction in a woman treated by a first injection of high-dose methotrexate for a T-lymphoblastic lymphoma."	( Suspicion of drug-drug interaction between high-dose methotrexate and proton pump inhibitors: a case report - should the practice be changed? Bouafia, F; Franchon, E; Gouraud, A; Pham, BN; Ranchon, F; Rioufol, C; Salles, G; Schwiertz, V; Vantard, N; Vial, T; You, B, 2011)	0.37
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."	( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012)	0.38
" The drug-drug interactions (DDIs) between simotinib and other drugs in combination and the underlying mechanism of its gastrointestinal toxicity remain unclear."	( Drug interaction studies reveal that simotinib upregulates intestinal absorption by increasing the paracellular permeability of intestinal epithelial cells. Cheng, Z; Li, P; Liu, Z; Zhu, Q, 2014)	0.4
"Little is known about the effects of drug-drug interactions between valacyclovir and non-steroidal anti-inflammatory drugs (NSAIDs)."	( Acute kidney injury during concomitant use of valacyclovir and loxoprofen: detecting drug-drug interactions in a spontaneous reporting system. Jiang, P; Shi, J; Sun, H; Yue, Z, 2014)	0.4
"05) were reduced in mice treated with VACV combined with ART versus VACV alone."	( Valacyclovir combined with artesunate or rapamycin improves the outcome of herpes simplex virus encephalitis in mice compared to antiviral therapy alone. Boivin, G; Canivet, C; Menasria, R; Piret, J; Rhéaume, C, 2015)	0.42
"Despite peptide transporter 1 (PEPT1) being responsible for the bioavailability for a variety of drugs, there has been little study of its potential involvement in drug-drug interactions."	( In Vitro and Clinical Evaluations of the Drug-Drug Interaction Potential of a Metabotropic Glutamate 2/3 Receptor Agonist Prodrug with Intestinal Peptide Transporter 1. Annes, WF; Ayan-Oshodi, MA; Hillgren, KM; Knadler, MP; Leese, P; Long, AJ; Mitchell, MI; Pak, YA; Witcher, JW, 2017)	0.46

Excerpt	Reference	Relevance
" The limited oral bioavailability of acyclovir necessitates frequent dosing."	( Valaciclovir compared with acyclovir for improved therapy for herpes zoster in immunocompetent adults. Andersen, PL; Beutner, KR; Forszpaniak, C; Friedman, DJ; Wood, MJ, 1995)	0.29
" The oral bioavailability of acyclovir derived from valaciclovir in cynomolgus monkey was 67 +/- 13%, representing a significant improvement over the limited bioavailability after acyclovir administration to primates."	( Metabolic fate and pharmacokinetics of the acyclovir prodrug valaciclovir in cynomolgus monkeys. Burnette, TC; de Miranda, P, )	0.13
" The first approach was directed towards improving the bioavailability of acyclovir by examining the potential of a variety of prodrugs, leading to the new compound valaciclovir hydrochloride."	( Review of research leading to new anti-herpesvirus agents in clinical development: valaciclovir hydrochloride (256U, the L-valyl ester of acyclovir) and 882C, a specific agent for varicella zoster virus. Beauchamp, LM; Darby, G; de Miranda, P; Ertl, P; Krenitsky, TA; Lacey, S; Powell, KL; Purifoy, DJ; Rahim, SG; Roberts, G, 1993)	0.29
" Valaciclovir is well absorbed and is rapidly converted to acyclovir, resulting in three- to fourfold higher acyclovir levels than can be achieved with oral acyclovir, even in patients with advanced HIV disease."	( Valaciclovir (BW256U87): the L-valyl ester of acyclovir. Jacobson, MA, 1993)	0.29
" Valaciclovir was rapidly and extensively converted to acyclovir, resulting in significantly greater acyclovir bioavailability (approximately threefold to fivefold) compared with that historically observed with high-dose (800 mg) oral acyclovir."	( Pharmacokinetics of the acyclovir pro-drug valaciclovir after escalating single- and multiple-dose administration to normal volunteers. Blum, MR; Burnette, T; Cederberg, DM; de Miranda, P; Doucette, M; Smiley, ML; Weller, S, 1993)	0.29
" The absolute bioavailability of acyclovir from valaciclovir and the metabolic disposition of valaciclovir were investigated with healthy volunteers in two separate studies."	( Absolute bioavailability and metabolic disposition of valaciclovir, the L-valyl ester of acyclovir, following oral administration to humans. On, N; Posner, J; Rolan, P; Seaber, E; Soul-Lawton, J; Wootton, R, 1995)	0.29
"Oral administration of the prodrug valacyclovir results in enhanced bioavailability and significantly greater plasma concentrations of acyclovir than can be achieved with oral doses of acyclovir itself."	( Valacyclovir: a review of its antiviral activity, pharmacokinetic properties, and clinical efficacy. Beutner, KR, 1995)	0.29
"Valaciclovir, the 1-valyl ester of acyclovir, has provided a peroral acyclovir bioavailability 3 to 5 times that of acyclovir itself and is rapidly and completely converted to acyclovir by the liver."	( A large-scale, placebo-controlled, dose-ranging trial of peroral valaciclovir for episodic treatment of recurrent herpes genitalis. Valaciclovir HSV Study Group. Beutner, K; DeGregorio, B; Miller, C; Spruance, SL; Tyring, SK, )	0.13
" The bioavailability of valacyclovir is 54% compared to approximately 20% for oral acyclovir."	( Valacyclovir. Acosta, EP; Fletcher, CV, 1997)	0.3
"Valacyclovir has improved bioavailability over acyclovir and is at least as efficacious."	( Valacyclovir. Acosta, EP; Fletcher, CV, 1997)	0.3
" Much of the current antiviral research focuses on providing drugs with (i) improved oral bioavailability and pharmacokinetics which permit less frequent oral or topical dosing for suppressive treatment of herpes simplex virus (HSV) infections, (ii) different mechanisms of action for synergic effects in treating resistant HSV infections in the immunocompromised host and (iii) improved efficacy."	( New therapeutic approaches to the alphaherpesvirus infections. Cassady, KA; Whitley, RJ, 1997)	0.3
" The bioavailability of aciclovir from oral valaciclovir is considerably greater than that achieved after oral aciclovir administration."	( Valaciclovir. A review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in herpesvirus infections. Faulds, D; Perry, CM, 1996)	0.29
"To determine whether the improved bioavailability of valaciclovir and a more convenient, less frequent dose regimen can maintain the clinical efficacy previously demonstrated for acyclovir."	( Valaciclovir versus acyclovir in the treatment of first-episode genital herpes infection. Results of an international, multicenter, double-blind, randomized clinical trial. The Valaciclovir International Herpes Simplex Virus Study Group. Barbarash, RA; Degregorio, B; Fife, KH; Roth, R; Rudolph, T, 1997)	0.3
" VACV demonstrates an oral bioavailability that is three to five time greater than acyclovir, concentration dependent, and saturable in humans."	( Carrier-mediated intestinal absorption of valacyclovir, the L-valyl ester prodrug of acyclovir: 1. Interactions with peptides, organic anions and organic cations in rats. Balimane, PV; Sinko, PJ, 1998)	0.3
" Valacyclovir, a water soluble amino acid ester prodrug of acyclovir has been reported to increase the oral bioavailability of acyclovir but its absorption mechanism is unknown."	( 5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter. Amidon, GL; Covitz, KM; de Vrueh, RL; Han, H; Lee, CP; Oh, DM; Rhie, JK; Sadée, W; Smith, PL, 1998)	0.3
"2-Amino-6-fluoro-9-(2-hydroxyethoxymethyl)purine (2) and its ester derivatives 4a-d were synthesized as potential prodrugs of acyclovir, and were evaluated for their oral acyclovir bioavailability in rats and in vivo antiviral efficacy in HSV-1-infected mice."	( Synthesis and evaluation of 2-amino-6-fluoro-9-(2-hydroxyethoxymethyl)purine esters as potential prodrugs of acyclovir. Im, GJ; Kim, DK; Kim, HT; Kim, KH; Lee, N, 1998)	0.3
" New antiviral drugs with improved oral bioavailability (famciclovir and valaciclovir) allow a better efficacy."	( [Drug clinics. How I treat zona]. Nikkels, AF; Piérard, GE, 1999)	0.3
" Our results suggest that L-valine is a desirable L-amino acid for the esterification of poorly permeable drugs to enhance their oral bioavailability targeting intestinal PEPT1."	( Recognition of L-amino acid ester compounds by rat peptide transporters PEPT1 and PEPT2. Hashimoto, Y; Inui, KI; Saito, H; Sawada, K; Terada, T, 1999)	0.3
" The interindividual variations of the bioavailability were 48."	( Bioavailability of aciclovir after oral administration of aciclovir and its prodrug valaciclovir to patients with leukopenia after chemotherapy. Eksborg, S; Grimfors, G; Gruber, A; Kalin, M; Palm, C; Steingrimsdottir, H, 2000)	0.31
" Famciclovir and valacyclovir offer improved oral bioavailability and convenient oral dosing schedules but are more expensive than acyclovir."	( Treatment of common cutaneous herpes simplex virus infections. Emmert, DH, 2000)	0.31
" The higher oral bioavailability of newer antiviral agents allows part of the extended treatment period of patients with herpes simplex encephalitis to be carried out as an ambulatory oral regimen."	( Use of oral valaciclovir in a 12-year-old boy with herpes simplex encephalitis. Chan, PK; Chow, PC; Huen, KF; Mak, AW; Peiris, JS, 2000)	0.31
" Oral valaciclovir provides significantly better oral bioavailability than oral aciclovir itself, contributing to the need for less frequent administration."	( Valaciclovir: a review of its long term utility in the management of genital herpes simplex virus and cytomegalovirus infections. Ormrod, D; Perry, CM; Scott, LJ, 2000)	0.31
" However, the low oral bioavailability of aciclovir has to some extent limited its efficacy in the treatment of herpes zoster and has prompted the development of the more readily absorbed oral prodrug valaciclovir."	( Valaciclovir: a review of its use in the management of herpes zoster. Goa, K; Ormrod, D, 2000)	0.31
" The bioavailability of valacyclovir is 54% compared to approximately 20% for oral acyclovir and may account for unexpected overdoses, which may lead to serious neurological toxicity."	( [Neurologic toxicity caused by zelitrex (valaciclovir) in 3 patients with renal failure. Is overdose associated with improvement of product bioavailability improvement?]. Bengler, C; Blayac, JP; Branger, B; Hillaire-Buys, D; Peyrière, H; Pinzani, V; Vécina, F, 2001)	0.31
" The mean absolute bioavailability of aciclovir from oral valaciclovir was 60 +/- 21%."	( Comparable aciclovir exposures produced by oral valaciclovir and intravenous aciclovir in immunocompromised cancer patients. Höglund, M; Ljungman, P; Weller, S, 2001)	0.31
" Its limited oral bioavailability and short half-life, however, necessitates frequent dosing."	( Comparative study of the efficacy and safety of valaciclovir versus acyclovir in the treatment of herpes zoster. Chen, YS; Chiang, SC; Huang, CK; Lee, SS; Lin, HH; Lin, WR; Liu, YC; Tsai, HC; Wann, SR; Yen, MY, 2001)	0.31
" There was no effect of sex on acyclovir bioavailability with either drug."	( Comparative bioavailability of acyclovir from oral valacyclovir and acyclovir in patients treated for recurrent genital herpes simplex virus infection. Aoki, FY; Bras, AP; Sitar, DS, 2001)	0.31
" The treatment of these conditions has been advanced over the past two decades by the introduction of guanosine nucleoside antivirals such as valacyclovir (Valtrex), Glaxo Wellcome), the highly bioavailable prodrug of acyclovir (Zovirax), Glaxo Wellcome)."	( Valacyclovir in the treatment of genital herpes and herpes zoster. Baker, DA, 2002)	0.31
" Valacyclovir has good bioavailability and has not been studied for prophylaxis of HSV among PCT patients."	( Valacyclovir prophylaxis for the prevention of Herpes simplex virus reactivation in recipients of progenitor cells transplantation. Desmery, P; Dignani, MC; Intile, D; Mammana, L; Michelet, M; Milone, G; Mykietiuk, A; Pavlovsky, S, 2002)	0.31
" The bioavailability of acyclovir after oral administration of valacyclovir was 45% (median value; 95% CI: 37-55%)."	( Pharmacokinetics of acyclovir in immunocompromized children with leukopenia and mucositis after chemotherapy: can intravenous acyclovir be substituted by oral valacyclovir? Eksborg, S; Kalin, M; Pal, N; Palm, C; Söderhäll, S, 2002)	0.31
" In view of the high oral bioavailability of valaciclovir (the L-valyl ester of acyclovir) the risk of neurotoxicity becomes more prominent."	( Evaluation of valaciclovir dosage reduction in continuous ambulatory peritoneal dialysis patients. Dhillon, S; Stathakis, C; Stathoulopoulou, F; Thodis, H; Vargemezis, V, 2002)	0.31
" The mean absolute bioavailability of aciclovir is of 54."	( [Valaciclovir]. Lebrun-Vignes, B, 2002)	0.31
" The peptide transporter on the corneal epithelium may be targeted to improve the ocular bioavailability of poorly absorbed drugs."	( Mechanism of corneal permeation of L-valyl ester of acyclovir: targeting the oligopeptide transporter on the rabbit cornea. Anand, BS; Mitra, AK, 2002)	0.31
" Valacyclovir has greater oral bioavailability and requires less frequent dosing."	( Valacyclovir versus acyclovir for HSV prophylaxisin neutropenic patients. Barnett, MJ; Campbell, LM; Cox, VC; Epstein, JB; Marra, F; Ransier, A; Warkentin, DI; Yip, JG, 2002)	0.31
" Valacyclovir enhances acyclovir bioavailability compared with orally administered acyclovir."	( Valacyclovir for herpes simplex virus infection: long-term safety and sustained efficacy after 20 years' experience with acyclovir. Baker, D; Snowden, W; Tyring, SK, 2002)	0.31
" By using historical data for intravenous acyclovir as reference, the overall estimate of acyclovir bioavailability from valacyclovir was 48%, 2- to 4-fold greater than for oral acyclovir."	( An investigation of the steady-state pharmacokinetics of oral valacyclovir in immunocompromised children. Floret, D; Leibundgut, K; Leverger, G; Nadal, D; Perel, Y; Sokal, EM; Weller, S, 2002)	0.31
" The relative bioavailability of the valaciclovir tablets compared with the suspension was 115 +/- 32%."	( Pharmacokinetics and safety of valaciclovir in children with Epstein-Barr virus illness. Deeter, RG; Fish, DN; Simon, MW, 2002)	0.31
"Oral valacyclovir is better absorbed than oral acyclovir, increasing acyclovir bioavailability three- to fivefold."	( High-dose, short-duration, early valacyclovir therapy for episodic treatment of cold sores: results of two randomized, placebo-controlled, multicenter studies. Barber, J; Blatter, MM; Goldstein, D; Hill, J; Jones, TM; Schultz, M; Spruance, SL; Vargas-Cortes, M, 2003)	0.32
" Oral valacyclovir, which is converted in the body to acyclovir, has greater oral bioavailability than oral acyclovir and compared with oral acyclovir yields similar acyclovir plasma concentrations with less frequent (twice-daily) dosing."	( Clinical utility of oral valacyclovir compared with oral acyclovir for the prevention of herpes simplex virus mucositis following autologous bone marrow transplantation or stem cell rescue therapy. Broun, ER; DeVoe, M; Eisen, D; Essell, J; Sigmund, D, 2003)	0.32
" Valacyclovir, a prodrug of acyclovir with a higher level of bioavailability than acyclovir, has also been shown to be effective in preventing CMV disease when given as prophylactic treatment."	( Comparative study of prophylactic oral ganciclovir and valacyclovir in high-risk kidney transplant recipients. Beaulieu, J; Dworkin, L; Gohh, R; Monaco, A; Morrissey, P; Shemin, D; Yango, A; Zanabli, A, 2003)	0.32
"The plasma bioavailability for acyclovir, valacyclovir and val-valacyclovir were similar with area under curve values being 896."	( Ocular penetration of acyclovir and its peptide prodrugs valacyclovir and val-valacyclovir following systemic administration in rabbits: An evaluation using ocular microdialysis and LC-MS. Atluri, H; Dias, C; Mitra, A; Nashed, Y, 2002)	0.31
" The increased bioavailability of valacyclovir is attributed to carrier-mediated intestinal absorption, via the hPEPT1 peptide transporter, followed by the rapid and complete conversion to acyclovir."	( Identification of a human valacyclovirase: biphenyl hydrolase-like protein as valacyclovir hydrolase. Amidon, GL; Chu, XY; Kim, I; Kim, S; Lee, KD; Provoda, CJ, 2003)	0.32
"A series of dipeptide prodrugs of antiviral nucleoside acyclovir (ACV) were designed to target the oligopeptide transporter on the cornea with an aim of improving the ocular bioavailability and therapeutic activity of ACV."	( Novel dipeptide prodrugs of acyclovir for ocular herpes infections: Bioreversion, antiviral activity and transport across rabbit cornea. Anand, B; Mitra, A; Nashed, Y, )	0.13
"Variability in valacyclovir bioavailability and the potential for cephalexin-valacyclovir interaction were evaluated."	( Intra- and interindividual variabilities of valacyclovir oral bioavailability and effect of coadministration of an hPEPT1 inhibitor. Anderle, P; Chin-Hong, P; Guglielmo, BJ; Lin, ET; Phan, DD; Sadee, W, 2003)	0.32
" We conclude that the improved bioavailability previously reported for valacyclovir in plasma results in higher concentrations in CSF, while the CSF/serum AUC ratio remains constant."	( Acyclovir levels in serum and cerebrospinal fluid after oral administration of valacyclovir. Lycke, J; Malmeström, C; Ståhle, L, 2003)	0.32
" Over the past two decades, the treatment of these conditions has been transformed by guanosine nucleoside antivirals such as valacyclovir (Valtrex, a highly bioavailable prodrug of acyclovir (Zovirax, and famciclovir (Famvir), a highly bioavailable prodrug of penciclovir (Denavir)."	( Valacyclovir in the treatment of herpes simplex, herpes zoster, and other viral infections. Brentjens, MH; Lee, P; Torres, G; Tyring, SK; Wu, JJ; Yeung-Yue, K, )	0.13
" Enhanced bioavailability of VACV has been attributed to its carrier-mediated intestinal absorption via hPEPT1 peptide transporter followed by rapid and complete conversion to ACV."	( Pharmacokinetics of novel dipeptide ester prodrugs of acyclovir after oral administration: intestinal absorption and liver metabolism. Anand, BS; Katragadda, S; Mitra, AK, 2004)	0.32
" This drug's short serum half-life and low oral bioavailability make frequent dosing necessary, however, and we therefore sought to determine if the pro-drug valacyclovir, which has improved bioavailability, could be successfully substituted for this indication."	( Oral valacyclovir as prophylaxis against herpes simplex virus reactivation during high dose chemotherapy for leukemia. Ambinder, RF; Gore, SD; Hartley, EE; Miller, CB; Mills, SR; Orlowski, RZ; Piantadosi, S; Ye, X, 2004)	0.32
"The absolute bioavailability of the prodrug valacyclovir, the l-valyl ester of acyclovir, after oral administration is approximately 54."	( Stability of valacyclovir: implications for its oral bioavailability. Amidon, GL; Granero, GE, 2006)	0.33
" While there is no cure for these conditions, treatment to alleviate symptoms, suppress recurrences and reduce transmission has been drastically improved over the past 20 years with the use of guanine nucleoside antivirals, such as valacyclovir hydrochloride (Valtrex), GlaxoSmithKline) the highly bioavailable prodrug of acyclovir (Zovirax((R)), GlaxoSmithKline), and famciclovir (Famvir, Novartis), a highly bioavailable prodrug of penciclovir (Denavir, Novartis)."	( Valacyclovir for the treatment of genital herpes. Brantley, JS; Hicks, L; Sra, K; Tyring, SK, 2006)	0.33
" Absorption rate constants of all the compounds were found to be lower than the elimination rate constants."	( In vivo ocular pharmacokinetics of acyclovir dipeptide ester prodrugs by microdialysis in rabbits. Anand, BS; Gunda, S; Katragadda, S; Mitra, AK, )	0.13
"The effect of colitis induced with dextran sodium sulfate (DSS) in rats on the bioavailability of drugs transported by the oligopeptide transporter PepT-1 was analyzed by studying the pharmacokinetics of PepT-1 substrates: cephalexin and valacyclovir, the prodrug of antiviral acyclovir."	( Regulation of the oligopeptide transporter, PEPT-1, in DSS-induced rat colitis. Bado, A; Beaufils, B; Buyse, M; Farinotti, R; Hindlet, P; Radeva, G; Walker, F, 2007)	0.34
" The first aim was to evaluate the oral bioavailability and pharmacokinetics (PKs) of acyclovir in horses after intravenous (i."	( Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses. Baert, K; Croubels, S; De Backer, P; Deprez, P; Garré, B; Gryspeerdt, A; Nauwynck, H; Shebany, K; van der Meulen, K, 2007)	0.34
" For atenolol (highly soluble drug), GInf resulted in a prolonged Tmax and reduced Cmax in comparison to PO, whereas bioavailability was similar."	( Selection of drug candidates for gastroretentive dosage forms: pharmacokinetics following continuous intragastric mode of administration in a rat model. Hoffman, A; Kagan, L, 2008)	0.35
" The mean bioavailability of acyclovir from valacyclovir was 64%."	( Valacyclovir and acyclovir pharmacokinetics in immunocompromised children. Aleksic, A; Berg, S; Blaney, S; Bomgaars, L; Serabe, B; Thompson, P, 2008)	0.35
"Valacyclovir provides enhanced acyclovir bioavailability in adults, but limited data are available in children."	( Pharmacokinetics and safety of extemporaneously compounded valacyclovir oral suspension in pediatric patients from 1 month through 11 years of age. Bradley, JS; Heitman, CK; Jacobs, RF; Kimberlin, DW; Man, CY; van der Walt, JS; Weller, S, 2010)	0.36
"The aim of the present study was to compare the bioavailability of valacyclovir (CAS 124832-26-4; INN: valaciclovir) from two valacyclovir hydrochloride (CAS 214832-27-5) capsules (150 mg/capsule as test preparation and 150 mg/capsule commercially available original capsule of the drug as reference preparation) in 20 Chinese healthy male volunteers, aged between 20 and 27."	( Pharmacokinetics and bioequivalence study of valacyclovir hydrochloride capsules after single dose administration in healthy Chinese male volunteers. Lin, H; Mao, GG; Tian, JX; Tian, Y; Zhang, ZJ, 2010)	0.36
" The Herpetic Eye Disease Study has guided the management of herpetic eye disease for almost twenty years, but newer medications such as valacyclovir are now available and are considered to have better bioavailability than acyclovir."	( Herpes simplex virus keratitis: an update of the pathogenesis and current treatment with oral and topical antiviral agents. Anderson, D; Athanasiadis, I; Hossain, P; MacGregor, C; Moschos, MM; Tsatsos, M, 2016)	0.43
" Although it is known that valacyclovir has an improved bioavailability and steadier plasma concentration, it is currently unclear as to whether this leads to better treatment results and less ocular complications."	( Valacyclovir versus acyclovir for the treatment of herpes zoster ophthalmicus in immunocompetent patients. Harder, BC; Jarczok, MN; Schlichtenbrede, FC; Schuster, AK; Tesarz, J, 2016)	0.43
"Despite peptide transporter 1 (PEPT1) being responsible for the bioavailability for a variety of drugs, there has been little study of its potential involvement in drug-drug interactions."	( In Vitro and Clinical Evaluations of the Drug-Drug Interaction Potential of a Metabotropic Glutamate 2/3 Receptor Agonist Prodrug with Intestinal Peptide Transporter 1. Annes, WF; Ayan-Oshodi, MA; Hillgren, KM; Knadler, MP; Leese, P; Long, AJ; Mitchell, MI; Pak, YA; Witcher, JW, 2017)	0.46
" Bioavailability was 40% after single oral administration."	( Absorption, Distribution, Metabolism, and Excretion of the Novel Helicase-Primase Inhibitor, Amenamevir (ASP2151), in Rodents. Noguchi, K; Ohtsu, Y; Susaki, Y, 2018)	0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
"The objective of this study was to investigate the processability of hot-melt extrusion (HME) to formulate ocular inserts of valacyclovir hydrochloride and evaluate the in vivo bioavailability of the formulation."	( Novel Application of Hot Melt Extrusion Technology for Preparation and Evaluation of Valacyclovir Hydrochloride Ocular Inserts. Bandari, S; Joshi, R; Majumdar, S; Marathe, S; Patil, A; Repka, M; Shadambikar, G, 2021)	0.62

Excerpt	Relevance	Reference
" In a randomized, double-blind, multicenter study, the safety and efficacy of oral valaciclovir given at a dosage of 1,000 mg three times daily for 7 or 14 days and oral acyclovir given at a dosage of 800 mg five times daily for 7 days were compared in immunocompetent adults aged > or = 50 years with herpes zoster."	( Valaciclovir compared with acyclovir for improved therapy for herpes zoster in immunocompetent adults. Andersen, PL; Beutner, KR; Forszpaniak, C; Friedman, DJ; Wood, MJ, 1995)	0.29
" When dosing was reduced to once per day, both compounds were less effective at controlling the infection."	( Comparison of efficacies of famciclovir and valaciclovir against herpes simplex virus type 1 in a murine immunosuppression model. Field, HJ; Sutton, D; Tewari, D; Thackray, AM, 1995)	0.29
"4 micrograms/ml and 120 h micrograms/ml, respectively, after a dosage of 2,000 mg of valaciclovir four times daily."	( Phase I trial of valaciclovir, the L-valyl ester of acyclovir, in patients with advanced human immunodeficiency virus disease. Blum, MR; Coakley, D; Feinberg, J; Gallant, J; Gary, D; Jacobson, MA; Smiley, ML; Squires, L; Wang, LH; Weller, S, 1994)	0.29
" This new drug produces enhanced plasma levels of acyclovir following oral dosing, which will not only allow more convenient dosing for the treatment of herpes simplex virus and varicella zoster virus (VZV) infections, but also mean that valaciclovir has the potential for superior clinical efficacy over acyclovir."	( Acyclovir--and beyond. Darby, G, 1994)	0.29
" Dosage adjustment is required in the presence of renal impairment."	( Pharmacokinetics of new antiherpetic agents. Rolan, P, 1995)	0.29
" Because optimal levels of acyclovir are achieved with a simpler dosing regimen of valacyclovir, compliance may be improved in many patients, thus reducing the incidence of resistant virus."	( Valacyclovir: a review of its antiviral activity, pharmacokinetic properties, and clinical efficacy. Beutner, KR, 1995)	0.29
" Therefore, there is no need for restriction of valaciclovir dosing in patients receiving antacid medication."	( Lack of interaction between valaciclovir, the L-valyl ester of acyclovir, and Maalox antacid. Bidault, R; de Bony, F; Peck, R; Posner, J, 1996)	0.29
"micrograms/ml) following dosing of valaciclovir (500 and 1,000 mg) three times a day were two to three times greater than those expected after high-dose oral acyclovir treatment (800 mg, five times daily)."	( Pharmacokinetics and safety of multiple-dose valaciclovir in geriatric volunteers with and without concomitant diuretic therapy. Blum, MR; Schultz, M; Smiley, ML; Wang, LH; Weller, S, 1996)	0.29
" Much of the current antiviral research focuses on providing drugs with (i) improved oral bioavailability and pharmacokinetics which permit less frequent oral or topical dosing for suppressive treatment of herpes simplex virus (HSV) infections, (ii) different mechanisms of action for synergic effects in treating resistant HSV infections in the immunocompromised host and (iii) improved efficacy."	( New therapeutic approaches to the alphaherpesvirus infections. Cassady, KA; Whitley, RJ, 1997)	0.3
" Thus, valaciclovir delivers therapeutic aciclovir concentrations when administered in a less frequent oral dosage regimen than is required for aciclovir."	( Valaciclovir. A review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in herpesvirus infections. Faulds, D; Perry, CM, 1996)	0.29
" Famciclovir and valacyclovir demonstrate superior pharmacokinetics compared with acyclovir and allow for less frequent daily dosing with higher achievable serum drug concentrations."	( Management of herpes simplex and varicella-zoster virus infections. Erlich, KS, 1997)	0.3
" With the completion of the first efficacy trials for each of these agents it has become apparent that, whilst less frequent dosing can he accomplished, it is not easy to significantly improve on the efficacy of aciclovir."	( Antiviral drugs in development for herpes zoster. Fiddian, AP, 1996)	0.29
" Once daily dosing with valaciclovir provides a more convenient dosing regimen than the more frequent aciclovir regimens."	( Valaciclovir for the suppression of recurrent genital HSV infection: a placebo controlled study of once daily therapy. International Valaciclovir HSV Study Group. Bodsworth, NJ; Gibb, A; Patel, R; Peters, B; Robinson, J; Saari, S; Vejlsgaard, G; Woolley, P, 1997)	0.3
" Valaciclovir maintains the established efficacy and safety of aciclovir but offers a much more convenient twice daily dosing regimen."	( Valaciclovir versus aciclovir in patient initiated treatment of recurrent genital herpes: a randomised, double blind clinical trial. International Valaciclovir HSV Study Group. Bodsworth, NJ; Borelli, S; Crooks, RJ; Esmann, J; Gibb, A; Ingamells, AJ; Paavonen, J; Strand, A; Uexkull, N; Vejlsgaard, G; Worm, AM, 1997)	0.3
" Valaciclovir provides a useful alternative to acyclovir with the advantage of a more convenient dosing regimen and the potential for improved compliance."	( Valaciclovir versus acyclovir in the treatment of first-episode genital herpes infection. Results of an international, multicenter, double-blind, randomized clinical trial. The Valaciclovir International Herpes Simplex Virus Study Group. Barbarash, RA; Degregorio, B; Fife, KH; Roth, R; Rudolph, T, 1997)	0.3
" Therefore, valacyclovir could prove a useful alternative to acyclovir when convenience of dosing or compliance issues are the prime considerations in treatment."	( A randomized, placebo-controlled comparison of oral valacyclovir and acyclovir in immunocompetent patients with recurrent genital herpes infections. The Valaciclovir International Study Group. Corey, L; Douglas, JM; Esmann, J; Spruance, SL; Tyring, SK, 1998)	0.3
"No dosage adjustment is required when valaciclovir and digoxin are coadministered."	( Lack of interaction between valaciclovir, the L-valyl ester of aciclovir, and digoxin. Layton, G; Peck, RW; Posner, J; Soul-Lawton, JH; Weatherley, BC, 1998)	0.3
" There was a dose-response relationship (P < ."	( Valaciclovir for the suppression of recurrent genital herpes simplex virus infection: a large-scale dose range-finding study. International Valaciclovir HSV Study Group. Borelli, S; Chambers, LO; Corey, L; Lang, W; Reitano, M; Robinson, JM; Thoming, C; Tyring, S; Worm, AM, 1998)	0.3
" Further studies need to be performed to determine proper dosing regimen for suppression of outbreaks in patients with a disease duration of less than 2 years."	( The effectiveness of valacyclovir in preventing reactivation of herpes gladiatorum in wrestlers. Anderson, BJ, 1999)	0.3
" Current recommendations regarding the dosing of antivirals used prophylactically are based mostly on anecdotal experience."	( Use of valacyclovir for herpes simplex virus-1 (HSV-1) prophylaxis after facial resurfacing: A randomized clinical trial of dosing regimens. Gilbert, S; McBurney, E, 2000)	0.31
" Famciclovir and valacyclovir offer improved oral bioavailability and convenient oral dosing schedules but are more expensive than acyclovir."	( Treatment of common cutaneous herpes simplex virus infections. Emmert, DH, 2000)	0.31
" Tolerability of the two drugs is similar, but the dosing schedule of valaciclovir is simpler."	( Comparison of the efficacy and safety of valaciclovir and acyclovir for the treatment of herpes zoster ophthalmicus. Cochener, B; Colin, J; Hoang-Xuan, T; Lescale, O; Prisant, O; Rolland, B, 2000)	0.31
" Prophylaxis with intraperitoneal valacyclovir decreases the recurrence rate in a dose-response fashion."	( Valacyclovir for the prevention of recurrent herpes simplex virus eye disease after excimer laser photokeratectomy. Asbell, PA, 2000)	0.31
" The advantage observed with the valaciclovir is the dosing comfort and the facility of completing the treatment."	( [Valaciclovir in the treatment of initial infection by genital herpes virus: comparative study]. García, A; García, I; García, S; Lanchares, JL; Sánchez, JA, 2001)	0.31
" She developed neurotoxicity with an adjustment dosage of valacyclovir for a cutaneous zoster infection."	( Neurotoxicity of valacyclovir in peritoneal dialysis: a pharmacokinetic study. Aymard, G; Deray, G; Issad, B; Izzedine, H; Launay-Vacher, V; Martinez, V; Mercadal, L, )	0.13
" Valaciclovir allows less frequent dosing and maintains the safety profiles of the parent drug."	( Comparative study of the efficacy and safety of valaciclovir versus acyclovir in the treatment of herpes zoster. Chen, YS; Chiang, SC; Huang, CK; Lee, SS; Lin, HH; Lin, WR; Liu, YC; Tsai, HC; Wann, SR; Yen, MY, 2001)	0.31
" We hypothesised that a lower dosage of VACV would prevent CMV disease with fewer CNS side effects."	( CMV disease in CMV-mismatched renal transplant recipients with prophylactic low dose valaciclovir. Eriksson, BM; Sund, F; Wahlberg, J, 2001)	0.31
" Valacyclovir is the only antiviral shown to be effective with a short (3-day) course in the episodic treatment of recurrent genital herpes, as well as with once-daily dosing for daily suppressive therapy."	( Valacyclovir in the treatment of genital herpes and herpes zoster. Baker, DA, 2002)	0.31
" However, the amount of acyclovir in breast milk after valaciclovir administration is considerably less (2%) than that used in therapeutic dosing of neonates."	( Acyclovir concentrations in human breast milk after valaciclovir administration. Cadematori, S; Fish, DN; Hollier, LM; Nobles, BJ; Sheffield, JS; Wendel, GD, 2002)	0.31
" No significant differences were detected between the 2 dosing schedules for any of the end points measured."	( Valacyclovir for episodic treatment of genital herpes: a shorter 3-day treatment course compared with 5-day treatment. Leone, PA; Miller, JM; Trottier, S, 2002)	0.31
" However, dosage simulations confirmed supratherapeutic acyclovir concentrations for all participants when following the recommended dose of 1,000 mg valaciclovir/24 h for varicella zoster infections."	( Evaluation of valaciclovir dosage reduction in continuous ambulatory peritoneal dialysis patients. Dhillon, S; Stathakis, C; Stathoulopoulou, F; Thodis, H; Vargemezis, V, 2002)	0.31
" The prodrugs valacyclovir and famciclovir offer easier, less-frequent dosing than required for acyclovir."	( Progress in meeting today's demands in genital herpes: an overview of current management. Patel, R, 2002)	0.31
" Dosage options for using valacyclovir in children are discussed."	( An investigation of the steady-state pharmacokinetics of oral valacyclovir in immunocompromised children. Floret, D; Leibundgut, K; Leverger, G; Nadal, D; Perel, Y; Sokal, EM; Weller, S, 2002)	0.31
" No studies to date have evaluated the efficacy, safety or proper dosing of valaciclovir in children for the treatment of EBV infection."	( Pharmacokinetics and safety of valaciclovir in children with Epstein-Barr virus illness. Deeter, RG; Fish, DN; Simon, MW, 2002)	0.31
" We concluded that the 16 CFS patients (included in both phases of this study) with EBV-persistent infection (EBV single-virus subset) are improved after 6 months of continuous pharmacokinetic dosing with valacyclovir."	( A six-month trial of valacyclovir in the Epstein-Barr virus subset of chronic fatigue syndrome: improvement in left ventricular function. Beqaj, SH; Chang, CH; Deeter, RG; Dworkin, HJ; Fitzgerald, JT; Goldstein, J; Lerner, AM; O'Neill, W; Zervos, M, 2002)	0.31
" The 1-day valacyclovir regimen offers patients a unique and convenient dosing alternative compared to available topical therapies."	( High-dose, short-duration, early valacyclovir therapy for episodic treatment of cold sores: results of two randomized, placebo-controlled, multicenter studies. Barber, J; Blatter, MM; Goldstein, D; Hill, J; Jones, TM; Schultz, M; Spruance, SL; Vargas-Cortes, M, 2003)	0.32
" The less frequent dosing schedule with valacyclovir compared with acyclovir offers a potential advantage for patients undergoing BMT who frequently suffer with severe mucositis and have difficulty taking oral medications."	( Clinical utility of oral valacyclovir compared with oral acyclovir for the prevention of herpes simplex virus mucositis following autologous bone marrow transplantation or stem cell rescue therapy. Broun, ER; DeVoe, M; Eisen, D; Essell, J; Sigmund, D, 2003)	0.32
" Inflammation was stabilized, and steroid dosage could be significantly reduced."	( Nonnecrotizing herpetic retinopathies masquerading as severe posterior uveitis. Bodaghi, B; Cassoux, N; Fardeau, C; LeHoang, P; Rozenberg, F, 2003)	0.32
"Valacyclovir is the only oral antiviral agent approved for therapy of herpes labialis, the only antiviral drug approved for a 3-day course in the episodic treatment of recurrent genital herpes, as well as the only antiviral drug approved for once daily dosing for suppressive therapy."	( Valacyclovir in the treatment of herpes simplex, herpes zoster, and other viral infections. Brentjens, MH; Lee, P; Torres, G; Tyring, SK; Wu, JJ; Yeung-Yue, K, )	0.13
" Choice of therapy would then depend on convenience of dosing and cost."	( Antiviral treatment of genital herpes. Apoola, A; Radcliffe, K, 2004)	0.32
" This drug's short serum half-life and low oral bioavailability make frequent dosing necessary, however, and we therefore sought to determine if the pro-drug valacyclovir, which has improved bioavailability, could be successfully substituted for this indication."	( Oral valacyclovir as prophylaxis against herpes simplex virus reactivation during high dose chemotherapy for leukemia. Ambinder, RF; Gore, SD; Hartley, EE; Miller, CB; Mills, SR; Orlowski, RZ; Piantadosi, S; Ye, X, 2004)	0.32
" The factors influencing the choice of therapy, such as cost, ease of dosing and acyclovir resistance are also discussed."	( Genital herpes: antiviral therapy for symptom relief and prevention of transmission. Gupta, R; Wald, A, 2006)	0.33
"Intravenous acyclovir at a dosage of 10 mg/kg every 8 hours for 14 days followed by oral valacyclovir at a dosage of 1000 mg 3 times per day for 1 month."	( Improvement of postherpetic neuralgia after treatment with intravenous acyclovir followed by oral valacyclovir. Gilden, DH; Hammack, BN; Kittelson, J; Quan, D, 2006)	0.33
" The less frequent dosing regimen makes it an attractive option in the treatment of genital herpes and other viral infections, and may contribute to increased patient adherence to therapy."	( Valacyclovir for the treatment of genital herpes. Brantley, JS; Hicks, L; Sra, K; Tyring, SK, 2006)	0.33
" Satisfaction with treatment is important since daily dosing with suppressive therapy is necessary in the absence of symptoms."	( Validation of the genital herpes treatment satisfaction questionnaire (GHerpTSQ) in status and change versions. Bradley, C; Taback, NA, 2006)	0.33
" A questionnaire was applied to 31 physicians working in hospital- or community-based settings in Santiago, Chile in order to characterize their dosing and timing preferences for aciclovir or valaciclovir prescriptions."	( [Erroneous prescriptions of aciclovir and valaciclovir in herpes zoster treatment]. Donaire R, L; Fica C, A; Jadue A, C, 2007)	0.34
" The dosing schedule of bid versus three times daily is desirable for enhancing patient compliance and to subsequently reduce the incidence of viral resistance."	( Open-label study of valacyclovir 1.5 g twice daily for the treatment of uncomplicated herpes zoster in immunocompetent patients 18 years of age or older. Aboutlabeti, S; Arora, A; Babb-Tarbox, M; Madkan, VK; Tyring, S, )	0.13
" The results showed that twice-daily dosing was as safe and effective as three times daily dosing for the reduction of ZAP and ZAAS."	( Open-label study of valacyclovir 1.5 g twice daily for the treatment of uncomplicated herpes zoster in immunocompetent patients 18 years of age or older. Aboutlabeti, S; Arora, A; Babb-Tarbox, M; Madkan, VK; Tyring, S, )	0.13
" Twice-daily dosing may help increase patient compliance and therefore increase the effectiveness of treatment of the acute herpes zoster rash and the prevention of ZAP."	( Open-label study of valacyclovir 1.5 g twice daily for the treatment of uncomplicated herpes zoster in immunocompetent patients 18 years of age or older. Aboutlabeti, S; Arora, A; Babb-Tarbox, M; Madkan, VK; Tyring, S, )	0.13
", 50% effective concentrations (EC(50) values) from in vitro studies, to design an optimal dosage schedule."	( Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses. Baert, K; Croubels, S; De Backer, P; Deprez, P; Garré, B; Gryspeerdt, A; Nauwynck, H; Shebany, K; van der Meulen, K, 2007)	0.34
"The purpose of the study was to evaluate the pharmacokinetic effects obtained by gastroretentive dosage form (GRDF) for drugs absorbed by passive paracellular diffusion (atenolol, acyclovir) or active transport (valacyclovir)."	( Selection of drug candidates for gastroretentive dosage forms: pharmacokinetics following continuous intragastric mode of administration in a rat model. Hoffman, A; Kagan, L, 2008)	0.35
"A dosage of 1 g of valacyclovir 3 times per day (TID) for 7 days has already been shown to be superior to an oral dosage of 800 mg acyclovir 5 times per day for 7 days in immunocompetent individuals."	( Double-blind study comparing 2 dosages of valacyclovir hydrochloride for the treatment of uncomplicated herpes zoster in immunocompromised patients 18 years of age and older. Arora, A; Brantley, J; Dix, L; Mendoza, N; Tyring, S; Yates, B, 2008)	0.35
" Whereas the diagnosis of this condition is often straightforward, choosing an appropriate drug (eg, acyclovir, valacyclovir hydrochloride, or famciclovir) and dosing regimen can be confusing in view of (1) competing clinical approaches to therapy; (2) evolving dosing schedules based on new research; (3) approved regimens of the Food and Drug Administration that may not match recommendations of the Centers for Disease Control and Prevention or of other experts; and (4) dissimilar regimens for oral and genital infections."	( The treatment of herpes simplex infections: an evidence-based review. Brodell, RT; Cernik, C; Gallina, K, 2008)	0.35
" The tolerability of the two drugs is similar, but the dosing for VAL might be more comfortable for patients."	( Comparison of oral antiviral therapy with valacyclovir or acyclovir after penetrating keratoplasty for herpetic keratitis. Bachmann, C; Frueh, BE; Garweg, J; Goldblum, D; Tappeiner, C, 2008)	0.35
" The methods were successfully used to perform pharmacokinetic and clinical studies in horses after intravenous and oral dosage of acyclovir and its prodrug valacyclovir."	( Determination of acyclovir in horse plasma and body fluids by high-performance liquid chromatography combined with fluorescence detection and heated electrospray ionization tandem mass spectrometry. Croubels, S; De Backer, P; Desmet, N; Garré, B; Maes, A; Nauwynck, H; van der Meulen, K, 2009)	0.35
" Four ponies were treated with valacyclovir at a dosage of 40mg/kg bodyweight, 3 times daily, for 5 (n=2) or 7 (n=2) consecutive days, while the other four ponies served as untreated controls."	( Evaluation of orally administered valacyclovir in experimentally EHV1-infected ponies. Croubels, S; De Backer, P; Garré, B; Gryspeerdt, A; Nauwynck, H, 2009)	0.35
"1 million genome-copies/ml, and thereafter declined precipitously, coinciding with an increase in the dosage of valaciclovir given; HHV-8 DNA was detected most often in WMS compared with parotid saliva, and buccal and palatal exfoliates."	( Extensive oral shedding of human herpesvirus 8 in a renal allograft recipient. Al-Otaibi, LM; Al-Sulaiman, MH; Porter, SR; Teo, CG, 2009)	0.35
" This validated population pharmacokinetic model for acyclovir may be used to develop dosing guidelines for safe and effective antiviral therapy in young people with malignancy."	( Population pharmacokinetics of acyclovir in children and young people with malignancy after administration of intravenous acyclovir or oral valacyclovir. Blair, EY; Coakley, JC; Earl, JW; McLachlan, AJ; Nath, CE; Shaw, PJ; Stephen, K; Zeng, L, 2009)	0.35
"The aim of the current study was to investigate whether multiple oral dosing of valacyclovir could result in plasma concentrations exceeding the EC(50)-value of acyclovir against equine herpesvirus 1 (EHV1) during the majority of the treatment period."	( Multiple oral dosing of valacyclovir in horses and ponies. Baert, K; Croubels, S; De Backer, P; Deprez, P; Garré, B; Nauwynck, H, 2009)	0.35
" A dosing recommendation cannot be made for infants <3 months of age because of decreased clearance in this age group."	( Pharmacokinetics and safety of extemporaneously compounded valacyclovir oral suspension in pediatric patients from 1 month through 11 years of age. Bradley, JS; Heitman, CK; Jacobs, RF; Kimberlin, DW; Man, CY; van der Walt, JS; Weller, S, 2010)	0.36
" Indwelling intrathecal catheters allowed serial CSF sampling throughout the dosing interval."	( Pharmacokinetics of acyclovir and its metabolites in cerebrospinal fluid and systemic circulation after administration of high-dose valacyclovir in subjects with normal and impaired renal function. Haas, DW; Johnson, B; Luther, JM; Nicotera, J; Smith, JP; Weller, S, 2010)	0.36
" Short-course (<1 year) prophylaxis with acyclovir has been shown to be effective, but compliance with five times daily dosing may be problematic."	( A randomized, double-blind, placebo-controlled trial of valacyclovir prophylaxis to prevent zoster recurrence from months 4 to 24 after BMT. DesJardin, JA; Klein, A; Miller, KB; Snydman, DR; Sprague, K, 2011)	0.37
" Valacyclovir was discovered in 1988 and revolutionized the treatment of these infections by virtue of its less frequent dosing regimen, which promotes patient adherence."	( Valacyclovir: approved and off-label uses for the treatment of herpes virus infections in immunocompetent and immunocompromised adults. Chemaly, RF; Vigil, KJ, 2010)	0.36
" Of the 10 D+/R- patients who developed CMV disease, six were inadvertently on a dose of valaciclovir below that dictated by protocol arising from a failure to increase dosage in parallel with improving recipient renal function."	( Low-dose valaciclovir and cytomegalovirus immunoglobulin to prevent cytomegalovirus disease in high-risk renal transplant recipients. Cohney, SJ; Nicholls, K; Tan, MB; Toussaint, ND; Walker, RG, 2011)	0.37
" Furthermore, the superior pharmacokinetics and more convenient dosing regimens with the use of valaciclovir and famciclovir clearly make them the preferred treatment option."	( Antivirals for management of herpes zoster including ophthalmicus: a systematic review of high-quality randomized controlled trials. de Kock, J; McDonald, EM; Ram, FS, 2012)	0.38
" Protection against mucocutaneous lesions was observed, but the dosage was probably inappropriate for the prevention of HSV activation in the central nervous system."	( Long-term valacyclovir suppressive treatment after herpes simplex virus type 2 meningitis: a double-blind, randomized controlled trial. Akre, O; Aurelius, E; Franzen-Röhl, E; Glimåker, M; Grillner, L; Jorup-Rönström, C; Studahl, M, 2012)	0.38
"Randomization within 72 hours in a factorial fashion to placebo plus placebo (n = 206); prednisolone, 60 mg/d for 5 days, with the dosage then tapered for 5 days, plus placebo (n = 210); valacyclovir hydrochloride, 1000 mg 3 times daily for 7 days, plus placebo (n = 207); or prednisolone plus valacyclovir (n = 206)."	( The effect of prednisolone on sequelae in Bell's palsy. Berg, T; Bylund, N; Engström, M; Hultcrantz, M; Jonsson, L; Kanerva, M; Marsk, E, 2012)	0.38
" Six of 16 patients (37%) receiving long-term oral acyclovir had recurrent HSV, at least one case of which followed a growth spurt that caused the baseline dosage of acyclovir to become subtherapeutic."	( Pediatric herpes simplex of the anterior segment: characteristics, treatment, and outcomes. Colby, KA; Liu, S; Pavan-Langston, D, 2012)	0.38
" Oral acyclovir is effective, but the dosage must be adjusted as the child grows."	( Pediatric herpes simplex of the anterior segment: characteristics, treatment, and outcomes. Colby, KA; Liu, S; Pavan-Langston, D, 2012)	0.38
" In analyzing parallel-group trials by daily dose, no clear evidence was found of a dose-response relationship for any drug."	( Oral antiviral therapy for prevention of genital herpes outbreaks in immunocompetent and nonpregnant patients. Chosidow, O; Do, G; Le Cleach, L; Lebrun-Vignes, B; Maruani, A; Ravaud, P; Trinquart, L, 2014)	0.4
" This preliminary valacyclovir model can be used in simulations to provide dosage recommendations for children of various ages and to help design more efficiently prospective clinical trials."	( Development of a paediatric population pharmacokinetic model for valacyclovir from literature non-compartmental values originating from sparse studies and Bayesian priors: a simulation study. Dokoumetzidis, A; Kechagia, IA, 2015)	0.42
" Then a PopPK model of valacyclovir was used to determine by simulations, dosage regimens that fulfill the criteria for both targets."	( Extrapolation of Valacyclovir Posology to Children Based on Pharmacokinetic Modeling. Dokoumetzidis, A; Kalantzi, L; Kechagia, IA, 2015)	0.42
" Finally, valacyclovir at this high dosage was extremely well tolerated."	( In utero treatment of congenital cytomegalovirus infection with valacyclovir in a multicenter, open-label, phase II study. Aegerter, P; Benoist, G; Bussières, L; Couderc, S; Ghout, I; Guilleminot, T; Jacquemard, F; Leruez-Ville, M; Magny, JF; Picone, O; Salomon, LJ; Stirnemann, J; Ville, Y; Winer, N, 2016)	0.43
" We performed a pharmacokinetic modeling and simulation study by integrating the existing understanding of physiology with previously published data to evaluate the vitreal penetration of oral valacyclovir for the treatment of ARN, under various dosing scenarios."	( Valacyclovir as Initial Treatment for Acute Retinal Necrosis: A Pharmacokinetic Modeling and Simulation Study. Fung, M; Ivaturi, V; Jain, A; Liu, T; Vinnard, C, 2017)	0.46
"We compared different oral valacyclovir dosing regimens with intravenous acyclovir."	( Valacyclovir as Initial Treatment for Acute Retinal Necrosis: A Pharmacokinetic Modeling and Simulation Study. Fung, M; Ivaturi, V; Jain, A; Liu, T; Vinnard, C, 2017)	0.46
"Modeling and simulation data support oral valacyclovir for the treatment of ARN, although the required dosing exceeds the recommended FDA dose size for herpes zoster."	( Valacyclovir as Initial Treatment for Acute Retinal Necrosis: A Pharmacokinetic Modeling and Simulation Study. Fung, M; Ivaturi, V; Jain, A; Liu, T; Vinnard, C, 2017)	0.46
" The recommended dosage for valaciclovir is 1g×2/d and treatment duration is identical to that for aciclovir."	( [Diagnostic and therapeutic recommendations for sexually transmitted diseases: Genital herpes]. Caumes, E; Chosidow, O; Janier, M; Milpied, B; Senat, MV; Sentilhes, L; Spenatto, N; Timsit, J, 2019)	0.51
" While on maintenance dosing of oral valacyclovir, he experienced reactivation in the form of bilateral vasculitis, which was successfully managed once restarting therapeutic oral dosing."	( Case Report: Varicella-zoster Encephalitis with Acute Retinal Necrosis and Oculomotor Nerve Palsy. Quan, SC; Skondra, D, 2019)	0.51
" Chronic suppression with oral antiviral therapy after ARN is recommended to prevent involvement of the contralateral eye, though there is no consensus on the duration and dosage of antivirals."	( Acute retinal necrosis in a patient with remote severe herpes simplex encephalitis. Kobayashi, T; Meier, J; Sekar, P; Streit, J, 2019)	0.51
" In contrast, the animals dosed orally once daily with the HPI compounds at 10 or 4 mg/kg/day showed a significantly increased survival (70% and 100% for 10 mg/kg/day; 90% and 100% for 4 mg/kg/day, respectively) compared to the vehicle treatment (0-10%), when therapy was initiated 6 h post HSV-1 inoculation."	( Helicase primase inhibitors (HPIs) are efficacious for therapy of human herpes simplex virus (HSV) disease in an infection mouse model. Donner, AK; Gege, C; Grunwald, T; Kleymann, G; Lange, F; Uhlig, N, 2021)	0.62
"This was a retrospective, multicenter study evaluating the rate of maternal-fetal CMV transmission in pregnancies with maternal primary CMV infection treated with VCV at a dosage of 8 g per day (VCV group) compared with a control group of untreated women."	( New data on efficacy of valacyclovir in secondary prevention of maternal-fetal transmission of cytomegalovirus. Benachi, A; Biquard, F; Bouthry, E; Egloff, C; Hawkins-Villarreal, A; Houhou-Fidouh, N; Mandelbrot, L; Picone, O; Sibiude, J; Vauloup-Fellous, C; Vivanti, AJ, 2023)	0.91
" Recently, valaciclovir at the dosage of 8 g/day was also reported to be capable of decreasing the rates of congenital infection and disease."	( Prevention of Congenital Cytomegalovirus Infection: Review and Case Series of Valaciclovir versus Hyperimmune Globulin Therapy. Muselli, M; Nigro, G, 2023)	0.91

Role	Description
antiviral drug	A substance used in the prophylaxis or therapy of virus diseases.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
L-valyl ester	Any alpha-amino acid ester that has L-valine as the amino acid component.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathway	Proteins	Compounds
Metabolism	1496	1108
Biological oxidations	150	276
Phase I - Functionalization of compounds	69	175

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	2.8184	0.0447	17.8581	100.0000	AID485294
TDP1 protein	Homo sapiens (human)	Potency	2.3725	0.0008	11.3822	44.6684	AID686978; AID686979
thioredoxin glutathione reductase	Schistosoma mansoni	Potency	0.2512	0.1000	22.9075	100.0000	AID485364
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	21.3174	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	17.2471	0.0013	10.1577	42.8575	AID1259252; AID1259256
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	0.8913	0.0355	20.9770	89.1251	AID504332
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	0.7079	0.2512	15.8432	39.8107	AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Solute carrier family 15 member 1	Homo sapiens (human)	IC50 (µMol)	1,350.2000	0.1800	0.1900	0.2000	AID242368; AID456673; AID679008; AID680835; AID680836
Solute carrier family 15 member 1	Homo sapiens (human)	Ki	1,770.0000	0.1800	3.3933	9.8000	AID680838; AID680840; AID680842
Solute carrier family 15 member 2	Rattus norvegicus (Norway rat)	Ki	260.0000	3.0000	6.4778	8.5000	AID678858; AID678860; AID679307
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Solute carrier family 22 member 8	Homo sapiens (human)	Km	57.9000	0.3450	1.3217	3.1000	AID679673
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
monoatomic ion transport	Solute carrier family 15 member 1	Homo sapiens (human)
protein transport	Solute carrier family 15 member 1	Homo sapiens (human)
peptide transport	Solute carrier family 15 member 1	Homo sapiens (human)
dipeptide import across plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
tripeptide import across plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
proton transmembrane transport	Solute carrier family 15 member 1	Homo sapiens (human)
amino acid metabolic process	Valacyclovir hydrolase	Homo sapiens (human)
xenobiotic metabolic process	Valacyclovir hydrolase	Homo sapiens (human)
response to toxic substance	Valacyclovir hydrolase	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 8	Homo sapiens (human)
response to toxic substance	Solute carrier family 22 member 8	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 8	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 8	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
proton-dependent oligopeptide secondary active transmembrane transporter activity	Solute carrier family 15 member 1	Homo sapiens (human)
peptide:proton symporter activity	Solute carrier family 15 member 1	Homo sapiens (human)
tripeptide transmembrane transporter activity	Solute carrier family 15 member 1	Homo sapiens (human)
dipeptide transmembrane transporter activity	Solute carrier family 15 member 1	Homo sapiens (human)
alpha-amino-acid esterase activity	Valacyclovir hydrolase	Homo sapiens (human)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
brush border	Solute carrier family 15 member 1	Homo sapiens (human)
membrane	Solute carrier family 15 member 1	Homo sapiens (human)
apical plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
apical plasma membrane	Solute carrier family 15 member 1	Homo sapiens (human)
mitochondrion	Valacyclovir hydrolase	Homo sapiens (human)
mitochondrial outer membrane	Valacyclovir hydrolase	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1857434	Antiviral activity against HSV-1 infected in po dosed BALB/c mouse administered twice on infection day and three times daily from day 1 to 4 post infection	2022	Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20	Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Treatment Option for Acyclovir-Resistant Herpes Simplex Virus Infections.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID680665	TP_TRANSPORTER: transepithelial transport (apical to basal), L-form in Caco-2 cells	1998	Pharmaceutical research, Aug, Volume: 15, Issue:8	5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
AID404304	Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID679307	TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT2-expressing LLC-PK1 cells	1999	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2	Recognition of L-amino acid ester compounds by rat peptide transporters PEPT1 and PEPT2.
AID615024	Half life in human plasma	2009	Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10	QSAR models for predicting enzymatic hydrolysis of new chemical entities in 'soft-drug' design.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID679972	TP_TRANSPORTER: uptake in PEPT1-expressing CHO cells	1999	The Journal of pharmacology and experimental therapeutics, Apr, Volume: 289, Issue:1	Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1857435	Antiviral activity against HSV-2 infected in po dosed BALB/c mouse administered twice on infection day and three times daily from day 1 to 4 post infection	2022	Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20	Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Treatment Option for Acyclovir-Resistant Herpes Simplex Virus Infections.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID456668	Stability in human HeLa cell homogenate assessed as half life of hydrolysis	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID456675	Stability in human HeLa cells expressing hPEPT1 after 60 mins	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID456680	Activity of human recombinant VACVase assessed as hydrolysis measured per ug of protein	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID679008	TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	1998	Pharmaceutical research, Aug, Volume: 15, Issue:8	5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID243132	Relative inhibition of [3H]glycylsarcosine uptake in HeLa cells expressing human Intestinal peptide transporter PepT1 compared to BDCRB; na=Not applicable	2005	Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4	Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
AID680836	TP_TRANSPORTER: inhibition of Gly-Sar uptake, D-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	1998	Pharmaceutical research, Aug, Volume: 15, Issue:8	5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
AID1055694	Prodrug conversion assessed as dipeptidyl peptidase 4-mediated ACV formation in bovine serum at 50 uM after 24 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID481444	Octanol-water partition coefficient, log P of the compound	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID679673	TP_TRANSPORTER: uptake in OAT3-expressing S2 cells	2002	The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3	Human organic anion transporters and human organic cation transporters mediate renal antiviral transport.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID456671	Activity of human recombinant VACVase assessed as hydrolysis	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID1055700	Prodrug conversion in PBS buffer assessed as ACV formation at 50 uM after 24 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID678860	TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT2-expressing HeLa cells	1998	Biochemical and biophysical research communications, May-19, Volume: 246, Issue:2	Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.
AID680660	TP_TRANSPORTER: uptake (pH 7.5) in PEPT1-expressing CHO cells	2000	Biopharmaceutics & drug disposition, Jul, Volume: 21, Issue:5	Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID425257	Total Cmax in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID481446	Effective permeability across human jejunum	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1055695	Prodrug conversion assessed as dipeptidyl peptidase 4-mediated ACV formation in human serum at 50 uM after 24 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID456676	Drug uptake in human HeLa cells after 60 mins	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID425258	fCmax in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID456672	Ratio of Kcat to Km of human recombinant VACVase assessed as hydrolysis	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID592683	Apparent permeability from basolateral side to apical side of human Caco2 cells by LC/MS/MS analysis	2011	Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8	QSAR-based permeability model for drug-like compounds.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID588970	Substrates of transporters of clinical importance in the absorption and disposition of drugs, PEPT1	2010	Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3	Membrane transporters in drug development.
AID456678	Drug uptake in human HeLa cells expressing hPEPT1 after 60 mins relative ro control	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID425265	Total oral bioavailability in horse at 20 mg/kg administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID680835	TP_TRANSPORTER: inhibition of Gly-Sar uptake, L-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	1998	Pharmaceutical research, Aug, Volume: 15, Issue:8	5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
AID456665	Chemical stability assessed as half life of hydrolysis in pH 7.4 buffer	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1055696	Prodrug conversion assessed as human dipeptidyl peptidase 4-mediated ACV formation at 50 uM after 24 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID679328	TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT1-expressing LLC-PK1 cells	1999	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2	Recognition of L-amino acid ester compounds by rat peptide transporters PEPT1 and PEPT2.
AID425259	Total Tmax in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID481439	Absolute bioavailability in human	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID370992	Cellular uptake in human HeLa cells after 45 mins	2009	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3	Design and synthesis of vidarabine prodrugs as antiviral agents.
AID680840	TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT1-expressing HeLa cells	1998	Biochemical and biophysical research communications, May-19, Volume: 246, Issue:2	Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.
AID680662	TP_TRANSPORTER: uptake (pH 6.2) in PEPT1-expressing CHO cells	2000	Biopharmaceutics & drug disposition, Jul, Volume: 21, Issue:5	Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells.
AID236916	Percentage of mass balance in hexadecane membranes model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID456670	Stability in human Caco-2 cell homogenate assessed as half life of hydrolysis	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID236914	Permeability Coefficient in hexadecane membranes model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID456673	Inhibition of human PEPT1-mediated [3H]Gly-Sar uptake in human HeLa cells	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID481440	Dissociation constant, pKa of the compound	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID680838	TP_TRANSPORTER: inhibition of Gly-Sar uptake in Xenopus laevis oocytes	1998	Biochemical and biophysical research communications, Sep-18, Volume: 250, Issue:2	Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.
AID456677	Stability in human HeLa cells after 60 mins	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID680661	TP_TRANSPORTER: uptake (pH 6.8) in PEPT1-expressing CHO cells	2000	Biopharmaceutics & drug disposition, Jul, Volume: 21, Issue:5	Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1055702	Prodrug conversion assessed as dipeptidyl peptidase 4-mediated ACV formation in human serum at 50 uM after 2 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID425261	Total elimination half life in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID242368	Inhibitory concentration against [3H]glycylsarcosine uptake in HeLa cells expressing human Intestinal peptide transporter PepT1	2005	Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4	Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
AID456679	Stability in apical side in human Caco-2 cells at 120 mins by permeability study	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID425263	Total AUC in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID678858	TP_TRANSPORTER: inhibition of Gly-Sar uptake in SKPT cells	1998	Biochemical and biophysical research communications, May-19, Volume: 246, Issue:2	Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID425262	Free elimination half life in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID456674	Drug uptake in human HeLa cells expressing hPEPT1 after 60 mins	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID425264	fAUC in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID481441	Aqueous diffusivity at 37C	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID680659	TP_TRANSPORTER: uptake (pH 7.9) in PEPT1-expressing CHO cells	2000	Biopharmaceutics & drug disposition, Jul, Volume: 21, Issue:5	Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells.
AID1055701	Prodrug conversion assessed as dipeptidyl peptidase 4-mediated ACV formation in bovine serum at 50 uM after 2 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID236268	Fraction absorbed in human intestine after oral administration compound was measured	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID592682	Apparent permeability from apical to basolateral side of human Caco2 cells after 2 hrs by LC/MS/MS analysis	2011	Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8	QSAR-based permeability model for drug-like compounds.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1055703	Prodrug conversion in PBS buffer assessed as ACV formation at 50 uM after 2 hrs by HPLC analysis	2013	European journal of medicinal chemistry, , Volume: 70	Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.
AID236913	Permeability Coefficient in Caco-2 cell culture model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID425268	Oral bioavailability in human	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID481442	Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells	2010	Journal of medicinal chemistry, May-13, Volume: 53, Issue:9	How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID425260	fTmax in horse at 20 mg/kg, po administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID588971	Substrates of transporters of clinical importance in the absorption and disposition of drugs, PEPT2	2010	Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3	Membrane transporters in drug development.
AID456664	Chemical stability in pH 6 buffer after 2 hrs	2010	Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2	Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
AID680842	TP_TRANSPORTER: inhibition of Gly-Sar uptake in Caco-2 cells	1998	Biochemical and biophysical research communications, May-19, Volume: 246, Issue:2	Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID236912	Permeability Coefficient in 2/4/A1 cell model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID370991	Cellular uptake in human HeLa cells expressing human PEPT1 transporter after 45 mins	2009	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3	Design and synthesis of vidarabine prodrugs as antiviral agents.
AID680663	TP_TRANSPORTER: uptake (pH 5.5) in PEPT1-expressing CHO cells	2000	Biopharmaceutics & drug disposition, Jul, Volume: 21, Issue:5	Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID425266	Free oral bioavailability in horse at 20 mg/kg administered as single dose	2007	Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12	Pharmacokinetics of acyclovir after intravenous infusion of acyclovir and after oral administration of acyclovir and its prodrug valacyclovir in healthy adult horses.
AID680651	TP_TRANSPORTER: uptake in Xenopus laevis oocytes	1998	Biochemical and biophysical research communications, Sep-18, Volume: 250, Issue:2	Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.
AID1745854	NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855	NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	123 (10.64)	18.2507
2000's	469 (40.57)	29.6817
2010's	425 (36.76)	24.3611
2020's	139 (12.02)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	221 (17.87%)	5.53%
Reviews	213 (17.22%)	6.00%
Case Studies	384 (31.04%)	4.05%
Observational	7 (0.57%)	0.25%
Other	412 (33.31%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (122)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Randomized, Cross-Over Study to Evaluate the Suppressive Effect of High-Dose Acyclovir Versus Once Daily Valacyclovir on Herpes Simplex Virus Type 2 Genital Shedding in Herpes Simplex Virus-2 Seropositive Adults [NCT00362297]	Phase 4	31 participants (Actual)	Interventional	2006-09-30	Completed
An Open Label, Balanced, Randomized, Two-treatment, Two-period,Two-sequence,Single-dose, Crossover, Bioequivalence Study Comparing Valacyclovir Hydrochloride Tablets 1 Gram of Ohm Laboratories Inc. (a Subsidiary of Ranbaxy Pharmaceuticals Inc., USA) With [NCT01222910]		36 participants (Actual)	Interventional	2009-05-31	Completed
The Effect of Valacyclovir 1g Once Daily on HSV-2 Viral Shedding in Subjects Newly Diagnosed With Genital Herpes Infection [NCT00306293]	Phase 4	70 participants (Actual)	Interventional	2006-02-20	Completed
A Single Dose, 2-Period, 2-Treatment 2-Way Crossover Bioequivalency Study of Valacyclovir Caplets Under Fed Conditions [NCT01132716]		48 participants (Actual)	Interventional	2006-09-30	Completed
An Open Label, Balanced, Randomized, Two Treatment, Two-sequence, Two-period, Single-dose Crossover Comparative Bioavailability Study of 1000 mg Valacyclovir HCl Tablets of Dr. Reddys's and Valtrex (R) 1 gm Caplets of GlaxoSmithkline in Healthy Volunteers [NCT01136538]	Phase 1	34 participants (Actual)	Interventional	2007-02-28	Completed
The Efficacy of Systemic Valacyclovir (Valtrex) to Arrest Further Progression of Severe Periodontitis [NCT05712343]	Early Phase 1	40 participants (Anticipated)	Interventional	2023-05-25	Recruiting
VZV in the Enteric Nervous System: Pathogenesis and Consequences [NCT05550194]	Phase 4	40 participants (Anticipated)	Interventional	2023-03-27	Recruiting
A Randomised, Double-blind, Placebo-controlled Trial to Evaluate the Effect of Epstein-Barr Virus Suppression in Chronic Obstructive Pulmonary Disease (EViSCO). [NCT03699904]	Phase 2	85 participants (Actual)	Interventional	2018-10-11	Terminated(stopped due to In light of the evolving Covid19 pandemic ongoing study recruitment was felt to pose an unacceptable risk to patient safety.)
Evaluation of the Pharmacokinetics and Pharmacodynamics of Valacyclovir in Neonates With Neonatal Herpes Simplex Virus Disease Who Have Completed Standard of Care Treatment With Acyclovir [NCT04448392]	Phase 1	10 participants (Anticipated)	Interventional	2021-07-01	Recruiting
A Randomized Trial of Topical Corticosteroid Use in Addition to Oral Antivirals for Prevention of Recurrence of Herpes Simplex Virus (HSV) Keratitis [NCT03626376]	Phase 4	0 participants (Actual)	Interventional	2019-12-10	Withdrawn(stopped due to Unable to enroll participants)
A Randomized, Double-Blind, Double-Dummy Phase II Study of Single Dose HDIT101 Versus Standard of Care Valaciclovir in Patients With Chronic Recurrent Anogenital HSV-2 Infection [NCT04165122]	Phase 2	122 participants (Actual)	Interventional	2019-11-15	Completed
A Randomized, Cross-Over Study to Evaluate the Suppressive Effect of High-Dose Valacyclovir Versus Once Daily Valacyclovir on Herpes Simplex Virus Type 2 Genital Shedding in Herpes Simplex Virus-2 Seropositive Adults [NCT01346475]	Phase 4	50 participants (Actual)	Interventional	2008-11-30	Completed
Aciclovir for HSV-2 Meningitis: A Double-blind Randomised Controlled Trial (AMEN) [NCT05452928]	Phase 4	150 participants (Anticipated)	Interventional	2024-01-01	Not yet recruiting
Phase II Study Evaluating HSV-tk + Valacyclovir Gene Therapy in Combination With Androgen Deprivation Therapy, Brachytherapy, External Beam Radiotherapy, and Prostatectomy for High-Risk Prostate Cancer [NCT03541928]	Phase 2	60 participants (Anticipated)	Interventional	2018-08-02	Recruiting
Valacyclovir for the Suppression of HSV-2 Viral Shedding in HSV-2 Seropositive Individuals With No History of Symptomatic GH [NCT00116844]	Phase 4	73 participants (Actual)	Interventional	2005-03-29	Completed
A Phase II, Multicenter, Randomized, Double-Blind, Parallel-Group, Comparative Study of FV-100 vs. Valacyclovir in Patients With Herpes Zoster [NCT00900783]	Phase 2	350 participants (Actual)	Interventional	2009-05-31	Completed
Valacyclovir to Prevent Vertical Transmission of Cytomegalovirus After Maternal Primary Infection During Pregnancy [NCT02351102]	Phase 2/Phase 3	100 participants (Actual)	Interventional	2015-11-30	Completed
An International, Randomized, Double-Blind, Placebo-Controlled, Multicenter, 6-Month Study of the Efficacy and Safety of Valtrex 1g QD vs. Placebo for the Suppression of HSV-2 Genital Herpes in Newly Diagnosed Immunocompetent Patients [NCT00158860]	Phase 4	384 participants (Actual)	Interventional	2004-06-21	Completed
A Multicenter, Open-label Study to Evaluate Preventive Efficacy for Herpes Simplex Virus Infection and Safety of 256U87 (Valaciclovir Hydrochloride) in Adult and Pediatric Hematopoietic Stem Cell Transplantation Patients [NCT01602562]	Phase 3	40 participants (Actual)	Interventional	2012-05-07	Completed
A Phase II, Dose-Finding Study With ASP2151 in Subjects With Recurrent Episodes of Genital HErpes [NCT00486200]	Phase 2	695 participants (Actual)	Interventional	2007-06-21	Completed
A Study of Vacyless® Versus Valtrex® in Patients With Herpes Zoster [NCT02152800]	Phase 4	25 participants (Actual)	Interventional	2011-04-30	Completed
An Open-label One-sequence Cross-over Pharmacokinetic Interaction Study of Steady-state Tipranavir/Ritonavir 500/200 mg With Single-dose Valaciclovir (500 mg) in Healthy Volunteers [NCT02226978]	Phase 1	29 participants (Actual)	Interventional	2007-02-28	Completed
Long-term Suppressive Valacyclovir Treatment for Herpes Zoster Ophthalmicus [NCT03134196]	Phase 4	652 participants (Actual)	Interventional	2017-08-23	Active, not recruiting
The Interaction of HSV-2 Co-infection in Veterans With Chronic Hepatitis C: the Effect of Valacyclovir on HCV Viral Load [NCT01037621]	Phase 1	50 participants (Anticipated)	Interventional	2010-04-30	Active, not recruiting
An Open Label, Balanced, Randomized, Two-treatment, Two-period, Two-sequence, Single-dose, Crossover, Bioequivalence Study Comparing Valacyclovir Hydrochloride Tablets 1 Gram of Ohm Laboratories Inc. (A Subsidiary of Ranbaxy Pharmaceuticals Inc., USA) Wit [NCT01222897]		40 participants (Actual)	Interventional	2009-05-31	Completed
Anti Viral Treatment in Mild Cognitive Impairment [NCT04710030]	Phase 2	50 participants (Anticipated)	Interventional	2021-02-01	Active, not recruiting
A Single Dose, 2-Period, 2-Treatment 2-Way Crossover Bioequivalency Study of Valacyclovir Caplets Under Fasting Conditions [NCT01132729]		48 participants (Actual)	Interventional	2006-09-30	Completed
A Double Blind Placebo Controlled Study of Valaciclovir in Treatment of Psychosis in Patients With Schizophrenia [NCT01364792]	Phase 2	24 participants (Actual)	Interventional	2011-04-30	Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Valacyclovir 1000 mg Tablet and Valtrex Following a 1 x 1000 mg Dose in Healthy Subjects Under Fasting Conditions [NCT01149499]	Phase 1	60 participants (Actual)	Interventional	2005-01-31	Completed
VALacyclovir for Inflammation AttenuatioN Trial Pilot (VALIANT Pilot) [NCT01176409]	Phase 3	60 participants (Actual)	Interventional	2010-09-30	Completed
An Open Label, Balanced, Randomized, Two Treatment, Two-sequence, Two-period, Single-dose Crossover Comparative Bioavailability Study of 1000 mg Valacyclovir HCl Tablets of Dr. Reddys's and Valtrex (R) 1 gm Caplets of GlaxoSmithkline in Healthy Volunteers [NCT01136525]	Phase 1	41 participants (Actual)	Interventional	2007-02-28	Completed
[NCT01250561]		133 participants (Actual)	Interventional	2002-02-28	Completed
A Randomized, Open-label, Crossover Trial of the Effect of High-dose Daily HSV-2 Suppressive Therapy on Plasma HIV-1 Levels Among HIV-1/HSV-2 Co-infected Persons [NCT01026454]	Phase 4	32 participants (Actual)	Interventional	2010-02-28	Completed
ValGanciclovir Versus ValAcyclovir for Viral Prophylaxis in Kidney Transplantation [NCT01972035]	Phase 2	137 participants (Actual)	Interventional	2014-08-01	Completed
Pharmacokinetics of a New Paediatric Formulation of Valacyclovir Used for Prophylaxis and Treatment of Varicella Zoster Virus (VZV) and Herpes Simplex Virus (HSV) Infections in Children, Phase II (VALID II) [NCT04081480]		7 participants (Actual)	Interventional	2019-12-10	Terminated(stopped due to Interim analysis showed positive results, it was difficult to include patients and also the fact that the grant for this project has ended, we have decided to complete the study before we had included the total number of 16 patients.)
An Open-label Trial of the Effect of Valacyclovir on Plasma HIV-1 Levels Among HIV-1 Seropositive and HSV-1/2 Seronegative Persons [NCT01059084]		0 participants (Actual)	Interventional	2010-01-31	Withdrawn(stopped due to We were unable to enroll any participants into this study.)
A Randomized, Double-blind, Active-controlled, Multi-center, Parallel-group Dose-ranging Study Assessing the Safety and Efficacy of EPB-348 Versus Valacyclovir Among Immunocompetent Patients With an Acute Episode of Herpes Zoster [NCT00831103]	Phase 2	373 participants (Actual)	Interventional	2007-11-30	Completed
VALacyclovir In Delaying Antiretroviral Treatment Entry [NCT00860977]	Phase 3	202 participants (Actual)	Interventional	2010-03-31	Completed
Time-limited Triplet Combination of Pirtobrutinib, Venetoclax, and Obinutuzumab for Patients With Treatment-naïve Chronic Lymphocytic Leukemia (CLL) or Richter Transformation (RT) [NCT05536349]	Phase 2	60 participants (Anticipated)	Interventional	2022-12-20	Recruiting
A Randomized Double-blind Controlled Trial of Valacyclovir Add-on Treatment of HSV Positive Early Course Schizophrenia Patients [NCT00514449]	Phase 2	31 participants (Actual)	Interventional	2007-06-30	Completed
Examining the Ability of HSV2 Therapy to Reduce HIV Target Cell Numbers in the Cervix. [NCT00946556]		30 participants (Actual)	Interventional	2010-04-30	Completed
A New Clinical Therapy for Bell's Palsy [NCT01686464]		882 participants (Actual)	Interventional	1998-06-30	Completed
A Phase III Double-Blind, Placebo-Controlled Trial of Long Term Therapy of Herpes Simplex Encephalitis (HSE): An Evaluation of Valacyclovir (CASG-204) [NCT00031486]	Phase 3	91 participants (Actual)	Interventional	2000-09-30	Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Valacyclovir Hydrochloride Tablets (1000 mg; Mylan) to Valtrex® Tablets (1000 mg; GlaxoSmithKline) in Healthy Volunteers [NCT00649974]	Phase 1	28 participants (Actual)	Interventional	2005-05-31	Completed
A Randomized, Open-label, Crossover Trial of the Effect of Dosing of Daily HSV-2 Suppressive Therapy on HSV Reactivation and Plasma HIV-1 Levels Among HIV-1/ HSV-2 Co-infected Persons [NCT00527618]	Phase 4	28 participants (Actual)	Interventional	2007-12-31	Completed
A Phase I Adaptive, Multiple Dose Pharmacokinetic and Safety Assessment of Valacyclovir in Infants at Risk of Acquiring Neonatal Herpes Simplex Virus Disease [NCT05468619]	Phase 1	16 participants (Anticipated)	Interventional	2022-09-23	Recruiting
Valacyclovir Suppression to Improve the Stability of Vaginal Flora Among HSV-2 Seropositive Women [NCT00682721]		0 participants (Actual)	Interventional	2009-02-28	Withdrawn(stopped due to Sponsor has withdrawn support for this study and it will not be performed)
Role of Herpesviruses as a Causative Factor in Acute Apical Abscess [NCT05266040]	Phase 2	250 participants (Anticipated)	Interventional	2023-05-01	Recruiting
Single-Dose Food in Vivo Bioequivalence Study of Valacyclovir Hydrochloride Tablets (1000 mg; Mylan) to Valtrex® Tablets (1000 mg; GlaxoSmithKline) in Healthy Volunteers [NCT00650494]	Phase 1	66 participants (Actual)	Interventional	2005-08-31	Completed
Open Label, Phase II Randomized Study of Oral Valganciclovir Versus Valacyclovir for Prophylaxis of Cytomegalovirus Reactivation in Patients Receiving Alemtuzumab (Campath). [NCT00562770]	Phase 2	46 participants (Actual)	Interventional	2003-09-30	Completed
A Phase 1, Randomized, Double-Blind, Multiple Dose, Multi-Center Study to Compare the Safety of ASP2151 to Valacylcovir and Placebo in Healthy Male and Female Subjects [NCT00870441]	Phase 1	442 participants (Actual)	Interventional	2009-03-31	Terminated(stopped due to Study terminated due to treatment-emergent serious adverse events)
Special Drug Use Investigation for VALTREX (Valaciclovir) (Suppression Prophylaxis) [NCT01390805]		462 participants (Actual)	Observational	2006-11-30	Completed
A Multicenter, Randomized, Double-blind Study to Compare the Efficacy and Safety of Patient-initiated Famciclovir 1000 mg b.i.d. x 1 Day to Valacyclovir 500 mg b.i.d. x 3 Days in Immunocompetent Adults With Recurrent Genital Herpes [NCT00306787]	Phase 3	1,179 participants (Actual)	Interventional	2006-03-31	Completed
Phase I-II Study HSV-tk + Valacyclovir Therapy in Combination With Brachytherapy for Recurrent Prostate Cancer With or Without Metastatic Disease [NCT01913106]	Phase 1/Phase 2	25 participants (Anticipated)	Interventional	2007-06-30	Recruiting
Clinical Evaluation of Valaciclovir Hydrochloride: 256U87 in Patients With Chickenpox - Open Uncontrolled Study. [NCT00169416]	Phase 3	43 participants (Actual)	Interventional	2005-03-31	Completed
HSV-2 Suppression to Reduce Maternal HIV-1 RNA Levels During Pregnancy and Breastfeeding [NCT00530777]	Phase 2	148 participants (Actual)	Interventional	2008-04-30	Completed
In UTERO Treatment of Cytomegalovirus Congenital Infection With Valacyclovir: Prospective Multicenter Randomized Trial Versus Placebo [NCT01037712]	Phase 4	6 participants (Actual)	Interventional	2009-09-30	Terminated(stopped due to not enough inclusion)
Should We Use Oral Valacyclovir in Acute Herpetic Gingivostomatitis in Children? A Randomized Controlled Trial [NCT02738229]	Phase 2	80 participants (Actual)	Interventional	2016-07-31	Completed
A Multicenter, Randomized, Active-controlled, Dose-finding Phase II Clinical Study Evaluating the Safety and Efficacy of Peginterferon α1b for Injection in Patients With Herpes Zoster [NCT05492591]	Phase 2	50 participants (Actual)	Interventional	2022-10-11	Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Valacyclovir 1000 mg Tablet and Valtrex Administered as 1 x 1000 mg Tablet in Healthy Subjects Under Fed Conditions [NCT01149460]	Phase 1	36 participants (Actual)	Interventional	2004-09-30	Completed
A 30-Day Double-Masked Study to Determine the Effect of Oral Valacyclovir or Oral Valacyclovir Plus Aspirin on the Shedding of Herpes Simplex Virus DNA in the Tears and Saliva of Volunteers Without Clinical Signs of Ocular Herpetic Disease [NCT00587496]	Phase 1	60 participants (Anticipated)	Interventional	2006-04-30	Recruiting
Palatability Testing of a New Paediatric Formulation of Valacyclovir for the Prophylaxis and Treatment of VZV and HSV Infections in Children [NCT01682109]	Phase 4	41 participants (Actual)	Interventional	2012-09-30	Completed
ENSIGN: Phase II Window of Opportunity Trial of Stereotactic Body Radiation Therapy and In Situ Gene Therapy Followed by Nivolumab in Metastatic Squamous or Non-Squamous Non-Small Cell Lung Carcinoma and Metastatic Uveal Melanoma [NCT02831933]	Phase 2	11 participants (Actual)	Interventional	2017-02-15	Terminated(stopped due to Lack of funding)
Bioequivalence Study in Healthy Volunteers of a New Paediatric Formulation of Valacyclovir Used for Prophylaxis and Treatment of VZV and HSV Infections in Children, Phase I (VALID-I) [NCT01689285]	Phase 1	16 participants (Actual)	Interventional	2013-12-31	Completed
Phase I Study of the Genital Immune Response to Live, Attenuated HSV529 Vaccine in HSV-2 Seropositive Adults [NCT02571166]	Phase 1	10 participants (Actual)	Interventional	2015-11-30	Completed
Phase 2/3 Multi-Center, Double-Blind, Controlled Trial Comparing Topical ARYS-01 (Sorivudine) Cream 3%, Oral Valaciclovir, and Combination Topical ARYS-01 Cream /Oral Valaciclovir for Treatment of Herpes Zoster in Immunocompetent Patients 18 Years of Age [NCT00652184]	Phase 2	300 participants (Anticipated)	Interventional	2008-03-31	Active, not recruiting
Single-Dose Food In Vivo Bioequivalence Study of Valacyclovir Hydrochloride Tablets (1000 mg; Mylan) to Valtrex® Tablets (1000 mg; GlaxoSmithKline) in Healthy Volunteers [NCT00649870]	Phase 1	26 participants (Actual)	Interventional	2005-05-31	Completed
Clinical and Immunological Study of the Efficacy and Safety of Combined Treatment of Patients With Severe Herpes Simplex (HSV) Infection) by Acyclic Nucleoside Valacyclovir and Interferon Inducer Kagocel [NCT04664127]		45 participants (Actual)	Observational	2017-10-30	Completed
[NCT00006131]		66 participants (Anticipated)	Interventional	1997-01-31	Completed
Anti-viral Therapy in Alzheimer's Disease [NCT03282916]	Phase 2	120 participants (Actual)	Interventional	2018-02-12	Active, not recruiting
Treatment Bell´s Palsy: Prednisone vs Prednisone Valacyclovir [NCT00561106]		42 participants (Actual)	Interventional	2002-12-31	Completed
Primary Treatment of Waldenstrom's Macroglobulinemia With Bortezomib (Velcade) and Rituximab (Rituxan) Followed by Autologous Stem Cell Collection [NCT00492050]	Phase 2	46 participants (Actual)	Interventional	2006-08-02	Active, not recruiting
Dose-finding Study of ASP2151 in Subjects With Herpes Zoster- A Multicenter, Randomized, Double-blind, Valacyclovir Hydrochloride-controlled, Parallel-group, Comparative Study [NCT00487682]	Phase 2	403 participants (Actual)	Interventional	2007-11-13	Completed
A Phase IIa Study of AdV-tk + Valacyclovir Gene Therapy in Combination With Standard Radiation Therapy for Malignant Gliomas [NCT00589875]	Phase 2	52 participants (Actual)	Interventional	2007-03-31	Completed
A Randomized, Double-Blind, Placebo Controlled Crossover Trial Using Valacyclovir to Suppress HSV and HIV Shedding in HIV-1, HSV-2 Coinfected Persons [NCT00161434]	Phase 4	60 participants (Actual)	Interventional	2003-03-31	Completed
"A Double-blind, Double Dummy, Randomized Crossover Trial to Compare the Effect of AIC316 (Pritelivir) 100 mg Once Daily Versus Valacyclovir 500 mg Once Daily on Genital HSV Shedding in HSV-2 Seropositive Adults." [NCT01658826]	Phase 2	91 participants (Actual)	Interventional	2012-10-31	Terminated
A Randomized,Double-Blind , Placebo-Controlled Crossover Trial of Antivirals for Suppression of HSV and HIV Shedding in HIV-1, HSV-2 Co-infected Persons [NCT00465205]	Phase 3	20 participants (Actual)	Interventional	2005-01-31	Completed
A Double Blind Placebo Controlled Study of Valacyclovir in Cognitive Impairment and Mood Symptoms of Bipolar Disorder [NCT00428298]	Phase 2	60 participants (Actual)	Interventional	2007-03-31	Completed
A Randomized, Double-Blind Trial of Valacyclovir Hydrochloride (BW 256U87) Prophylaxis for Opportunistic Cytomegalovirus End-Organ Disease in Patients With Advanced HIV Infection (< 100 CD4+ Lymphocytes) [NCT00001038]	Phase 3	1,200 participants	Interventional		Completed
A Multicentre Placebo-Controlled Evaluation of Prednisolone and/or Valaciclovir for the Treatment of Bell's Palsy [NCT00510263]	Phase 4	839 participants (Actual)	Interventional	2001-05-31	Completed
A Comparative Trial of Valacyclovir Hydrochloride ( 256U87 ) and Acyclovir for the Suppression of Anogenital Herpes Infections in HIV-Infected Patients [NCT00002084]		0 participants	Interventional		Completed
A Pharmacokinetic Study of Valacyclovir in Pediatric Oncology Patients [NCT00042328]	Phase 2	30 participants	Interventional	2001-08-31	Completed
A Randomized, Double-Blind, Placebo-Controlled Evaluation of Valaciclovir for the Prevention of Herpes Simplex Virus Transmission in Heterosexual Couples [NCT00001649]	Phase 3	180 participants	Interventional	1997-08-31	Completed
A Phase III Multicenter Study of Cytomegalovirus Prophylaxis With Valacyclovir for the Prevention of Serious Fungal and Bacterial Infections Among Cytomegalovirus Seronegative Recipients of Cytomegalovirus Seropositive Sx Stem Cell Transplants [NCT00045292]	Phase 3	0 participants	Interventional	2002-04-30	Completed
Valacyclovir in Immunocompromised Children [NCT00059592]	Phase 1	37 participants (Actual)	Interventional	1998-04-07	Completed
An International, Randomized, Double-Blind, Placebo-Controlled Study of Valaciclovir for the Suppression and Episodic Treatment of Genital HSV Infection in HIV-Infected Persons With CD4+ Lymphocyte Count <100 Cells/mm3. [NCT00079911]	Phase 4	7 participants (Actual)	Interventional	2004-03-12	Terminated(stopped due to Terminated)
Efficacy of an HSV2 Genital Herpes Suppressive Treatment on HIV and HSV2 Genital Shedding Among Co-Infected Patients Receiving or Not Antiretroviral Drugs [NCT00158509]	Phase 2	215 participants	Interventional	2004-08-31	Completed
V3: Vancouver-Victoria Valacyclovir Trial for Early Psychosis [NCT00175513]	Phase 2	100 participants (Anticipated)	Interventional	2005-09-30	Completed
Seroprevalence of HSV-2 in HIV Infected Subjects and the Effect of Daiy Valacyclovir in the Reduction of HSV-2 Recurrences and Viral Shedding [NCT00803543]		103 participants (Actual)	Interventional	2009-01-31	Completed
Evaluating Three Grams Daily Valacyclovir in Patients With Chronic Hepatitis C and Herpes Simplex Virus 2 (HSV-2) Infection (Phase I) [NCT01453075]	Phase 1	31 participants (Actual)	Interventional	2011-11-30	Completed
Randomized Study Assessing the Antiviral Activity and Safety of Valacyclovir in Primary Infectious Mononucleosis [NCT00274404]	Phase 1/Phase 2	20 participants	Interventional	2004-02-29	Completed
Valacyclovir+Temovate Gel for the Episodic Treatment of Herpes Labialis: A Patient-Initiated Double-Blind, Placebo-Controlled Study, Randomized Study. [NCT00297011]	Phase 2	300 participants	Interventional	2004-09-30	Completed
An Open-label, Single-dose, Multicenter, Pharmacokinetic, Safety and Tolerability Study of Valaciclovir Oral Suspension in Infants and Children. [NCT00297206]	Phase 1	36 participants (Actual)	Interventional	2003-01-25	Completed
Post-Marketing Clinical Study of Valaciclovir Hydrochloride Tablets -Single Oral Dose Study in Hemodialysis Patients- [NCT00343278]	Phase 4	18 participants	Interventional	2005-07-31	Completed
Anti-viral Prophylaxis for Prevention of Cytomegalovirus (CMV) Reactivation in Immunocompetent Patients in Critical Care [NCT01503918]	Phase 2	124 participants (Actual)	Interventional	2012-01-31	Completed
Does CMV Reactivation Cause Functional Impairment of CMV Specific CD4+ T-cells? The Potential for Valaciclovir to Prevent CMV-mediated Adverse Modulation of the Immune System in Patients With ANCA-associated Vasculitis [NCT01633476]	Phase 2	38 participants (Actual)	Interventional	2013-07-31	Active, not recruiting
In Utero Treatment of Cytomegalovirus congénitale Infection With Valacyclovir : Prospective Multicenter Nonrandomized Trial [NCT01651585]	Phase 4	41 participants (Actual)	Interventional	2011-07-31	Completed
Valacyclovir Augmentation for Cognitive and Functional Remediation in Schizophrenia [NCT01794897]	Phase 4	134 participants (Actual)	Interventional	2013-02-28	Completed
A Randomized Controlled Trial of ProstAtak® as Adjuvant to Up-front Radiation Therapy For Localized Prostate Cancer [NCT01436968]	Phase 3	711 participants (Anticipated)	Interventional	2011-09-30	Active, not recruiting
A Randomized, Double-blind, Placebo-controlled Crossover Trial of Valacyclovir for Suppression of HSV and HIV Shedding in HIV-1, HSV-2 Coinfected Men Who Have Sex With Men (MSM). [NCT00378976]	Phase 3	20 participants (Actual)	Interventional	2003-08-31	Completed
A Phase I Trial to Evaluate the Pharmacokinetics, Safety, and Tolerance of Valacyclovir HCl in HIV-1 Infected Children With Herpes Simplex Infections or Varicella/Zoster Infections [NCT00001054]	Phase 1	0 participants (Actual)	Interventional		Withdrawn
Prenatal Treatment of Congenital Cytomegalovirus Infection With Letermovir Randomized Against Valaciclovir (Step 2) [NCT05446571]	Phase 3	46 participants (Anticipated)	Interventional	2023-04-30	Not yet recruiting
The Effect of Treatment With Valacyclovir 500 mg BID on the Detection of HIV From Genital HSV Lesions in HIV-Infected Patients: A Double-Blind Crossover Study [NCT00002404]		30 participants	Interventional		Completed
Intratumoral Gene Mediated Cytotoxic Immunotherapy (GMCI) For Resectable Non-Small Cell Lung Cancer [NCT03131037]	Phase 1	12 participants (Actual)	Interventional	2017-05-04	Active, not recruiting
A Randomized Controlled Trial Of AdV-tk + Valacyclovir Administered During Active Surveillance For Newly Diagnosed Prostate Cancer [NCT02768363]	Phase 2	187 participants (Actual)	Interventional	2016-05-31	Active, not recruiting
Special Drug Use Investigation for VALTREX (Valaciclovir) (Pediatrics Chickenpox) [NCT01390857]		379 participants (Actual)	Observational	2007-11-30	Completed
A Study to Compare the Efficacy and Safety of Valacyclovir Hydrochloride ( 256U87 ) Versus Acyclovir in the Treatment of Recurrent Anogenital Herpes Infections in HIV Infected Patients [NCT00002000]		0 participants	Interventional		Completed
Phase II Window of Opportunity Trial of Stereotactic Body Radiation Therapy and In Situ Oncolytic Virus Therapy in Metastatic Triple Negative Breast Cancer and Metastatic Non-Small Cell Lung Cancer Followed by Pembrolizumab [NCT03004183]	Phase 2	57 participants (Actual)	Interventional	2017-07-01	Active, not recruiting
HSV-1 Suppression in HCV Infected Veterans Who Are Seronegative for HSV-2 [NCT01580995]	Phase 2	19 participants (Actual)	Interventional	2012-04-30	Completed
Phase I Study of Neoadjuvant GMCI Plus Immune Checkpoint Inhibitor Combined With Standard of Care for Newly Diagnosed High-Grade Gliomas [NCT03576612]	Phase 1	36 participants (Anticipated)	Interventional	2018-02-27	Active, not recruiting
A Multicenter, Randomized, Double-Blind, Parallel-Group, Comparative Study of FV-100 vs. Valacyclovir for the Prevention of Post-Herpetic Neuralgia and Treatment of Acute Herpes Zoster Associated Pain [NCT02412917]	Phase 3	237 participants (Actual)	Interventional	2015-06-30	Terminated
Urology Department, Hualien Tzu Chi Hospital, Hualien, Taiwan [NCT05094414]	Phase 1	30 participants (Anticipated)	Interventional	2021-07-01	Recruiting
Feasibility and Effects on Markers in Spinal Fluid in Persons With Early Alzheimer's Disease When Treated With Valaciclovir - Open Fas II Pilot Study (VALZ-Pilot) [NCT02997982]	Phase 2	33 participants (Actual)	Interventional	2016-12-31	Completed
AdV-tk + Valacyclovir Therapy in Combination With Surgery and Chemoradiation for Pancreas Cancer [NCT00638612]	Phase 1	27 participants (Actual)	Interventional	2008-08-31	Completed
A Phase I Study of AdV-tk + Prodrug Therapy in Combination With Radiation Therapy for Pediatric Brain Tumors [NCT00634231]	Phase 1	8 participants (Actual)	Interventional	2010-10-31	Completed
An International, Randomized, Double-Blind, Placebo-Controlled Study of Valacyclovir for the Suppression of Recurrent Ano-Genital HSV Infections in HIV-Infected Subjects [NCT00005663]	Phase 3	0 participants	Interventional	1999-06-30	Active, not recruiting
Early Non-Ablative Fractional Laser Resurfacing for Acne Scars After Treatment With Oral Isotretinoin [NCT03514771]		15 participants (Actual)	Interventional	2016-01-28	Completed
Impact of Metformin and Polysorbate 80 on Drug Absorption and Disposition [NCT04640571]	Phase 4	18 participants (Actual)	Interventional	2021-04-01	Completed
A Phase I Study of Intrapleural AdV-tk Therapy in Patients With Malignant Pleural Effusion [NCT01997190]	Phase 1	19 participants (Actual)	Interventional	2013-10-31	Completed
A Phase 1b Study of AdV-tk + Valacyclovir Gene Therapy in Combination With Standard Radiation Therapy for Malignant Gliomas [NCT00751270]	Phase 1	15 participants (Actual)	Interventional	2005-11-30	Completed
Phase III Study of ASP2151 in Herpes Zoster Patients- A Double-blind, Valaciclovir-controlled Study [NCT01959841]	Phase 3	751 participants (Actual)	Interventional	2013-08-31	Completed
A Double-Blind Trial of Adjunctive Valacyclovir to Improve Cognition in Early Phase Schizophrenia [NCT02008773]	Phase 2	170 participants (Actual)	Interventional	2014-03-26	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00031486 (6) [back to overview]	Survival With no or Mild Neuropsychological Impairment at 12 Months After Initiation of Study Medication as Measured by the Mattis Dementia Rating Scale (MDRS)
NCT00031486 (6) [back to overview]	Survival With no or Mild Neuropsychological Impairment at 90 Days, and at 6 and 12 Months, as Measured by the Mini-Mental Status Examination (MMSE).
NCT00031486 (6) [back to overview]	Survival With no or Mild Neuropsychological Impairment at 90 Days and at 6 and 12 Months, as Measured by the Mattis Dementia Rating Scale (MDRS)
NCT00031486 (6) [back to overview]	Survival With no or Mild Neuropsychological Impairment at 90 Days and at 6 and 12 Months, as Measured by the Glasgow Coma Scale (GCS).
NCT00031486 (6) [back to overview]	Median Number of Reported AEs Describing Safety and Tolerance of Valacyclovir (VACV), Evaluated by the Number Adverse Events, Administered at a Dose of 2.0 Grams Given Orally 3 Times a Day for 90 Days.
NCT00031486 (6) [back to overview]	Effect of Study Medication on Quality of Life Measurements.
NCT00116844 (6) [back to overview]	Mean Log HSV-2 DNA Copy Number Per Day on Days With Total Shedding
NCT00116844 (6) [back to overview]	Mean Log HSV-2 DNA Copy Number Per Day on Days With Subclinical Shedding
NCT00116844 (6) [back to overview]	Mean Percent Days of Subclinical Shedding as Determined by Type-specific Polymerase Chain Reaction (PCR) Assay for HSV-2
NCT00116844 (6) [back to overview]	Mean Percent Days of Total HSV-2 Shedding
NCT00116844 (6) [back to overview]	Number of Participants With no Shedding
NCT00116844 (6) [back to overview]	Percent Overall Study Population Who Have Recognized Clinical Signs/Symptoms of Genital Herpes Infection During the Study
NCT00158860 (5) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00158860 (5) [back to overview]	Mean Number of GH Recurrences Per Month Within the 6-month Study Period
NCT00158860 (5) [back to overview]	Number of Isolates With Resistance to Acyclovir (ACV)
NCT00158860 (5) [back to overview]	Percentage of Participants With Time to First GH Recurrence
NCT00158860 (5) [back to overview]	Percentage of Participants With Time to First Oral Herpes Simplex Virus (HSV) Outbreak Within 6-months
NCT00306293 (7) [back to overview]	Mean Percent Days Clinical Shedding (Presence of Genital Lesions)
NCT00306293 (7) [back to overview]	Mean Percent Days of Total Shedding (Clinical and Subclinical) as Determined by Type-specific Polymerase Chain Reaction (PCR) Assay for Herpes Simplex Virus Type 2 (HSV-2)
NCT00306293 (7) [back to overview]	Mean Percent Days Subclinical Shedding (no Genital Lesions Present)
NCT00306293 (7) [back to overview]	Median Time to First Genital Herpes Recurrence (Days)
NCT00306293 (7) [back to overview]	Percentage of Participants With at Least One Genital Herpes Recurrence
NCT00306293 (7) [back to overview]	Percentage of Participants With no Shedding
NCT00306293 (7) [back to overview]	Number of Participants With Any Adverse Event (AE) and Serious Adverse Event (SAE)
NCT00306787 (6) [back to overview]	Time to Resolution of Symptoms Associated With Recurrent Genital Herpes
NCT00306787 (6) [back to overview]	Time to a Second Recurrence of Genital Herpes
NCT00306787 (6) [back to overview]	Percentage of Participants With Aborted Genital Herpes Lesions
NCT00306787 (6) [back to overview]	Number of Patients With a Second Recurrence of Genital Herpes
NCT00306787 (6) [back to overview]	Investigator-assessed Time to Healing of All Non-aborted Genital Herpes Lesions
NCT00306787 (6) [back to overview]	Investigator-assessed Time to Healing of All (Non-aborted and Aborted) Genital Herpes Lesions
NCT00362297 (1) [back to overview]	Frequency of HSV-2 Total Shedding From the Genital Tract as Measured by PCR, Calculated Using a Per-day Shedding Rate in Participants Treated With High-dose Acyclovir as Compared to Once-daily Valacyclovir.
NCT00428298 (3) [back to overview]	Change From Baseline in Young Mania Rating Scale (YMRS) at 16 Weeks
NCT00428298 (3) [back to overview]	Change From Baseline in Montgomery Asberg Depression Score at 16 Weeks
NCT00428298 (3) [back to overview]	Percent Change From Baseline in Repeatable Battery for the Assessment of Neuropsychological Status at 16 Weeks
NCT00492050 (3) [back to overview]	Response Rate After 3 Cycles of Treatment With Bortezomib and Rituximab
NCT00492050 (3) [back to overview]	Response Rate After 2 Cycles of Treatment With Bortezomib and Rituximab
NCT00492050 (3) [back to overview]	Participants Ability to Collect Stem Cells After Treatment With Bortezomib and Rituximab
NCT00514449 (3) [back to overview]	PANSS Positive and Negative Syndrome Scale for Schizophrenia
NCT00514449 (3) [back to overview]	Cognitive Function Neuropsychological Battery (Gur Battery)
NCT00514449 (3) [back to overview]	Changes in Grey Matter Deficit
NCT00527618 (5) [back to overview]	The Effect of Valacyclovir 1 Gram Twice Daily Compared to Acyclovir 400 mg Twice Daily on the Percentage of Days With Genital Herpes Lesions.
NCT00527618 (5) [back to overview]	The Genital HSV Shedding Rate While on 400 mg Twice Daily of Acyclovir Versus 1000 mg Twice Daily of Valacyclovir.
NCT00527618 (5) [back to overview]	The Quantity of HIV-1 RNA in Plasma While on 400 mg Twice Daily of Acyclovir Versus 1000 mg Twice Daily of Valacyclovir.
NCT00527618 (5) [back to overview]	Sub-Study: To Evaluate the Kinetics of Plasma HIV-1 Decline Over the First Three Days of High-dose Valacyclovir Administration.
NCT00527618 (5) [back to overview]	The Effect of Valacyclovir 1 g Twice Daily Compared With Acyclovir 400 mg Twice Daily on the Quantity of Genital HSV Detected During Shedding Episodes.
NCT00530777 (2) [back to overview]	Mean Change in HIV-1 Levels in Plasma Between 34 and 38 Weeks Gestation
NCT00530777 (2) [back to overview]	Vertical HIV-1 Transmission
NCT00803543 (4) [back to overview]	Number of Participants With an HIV Viral Load of <500 Copies/ml
NCT00803543 (4) [back to overview]	CD4 Count
NCT00803543 (4) [back to overview]	Herpes Simplex Virus Type 2 Recurrence
NCT00803543 (4) [back to overview]	Rate of Asymptomatic HSV-2 Genital Shedding
NCT01026454 (1) [back to overview]	Mean Level of HIV-1 RNA in Plasma of Participants While on Acyclovir or Valacyclovir.
NCT01149460 (6) [back to overview]	AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity) - Valacyclovir
NCT01149460 (6) [back to overview]	AUC0-t (Area Under Concentration-time Curve From Time Zero to Time of Last Measurable Concentration) - Acyclovir
NCT01149460 (6) [back to overview]	AUC0-t (Area Under the Concentration-time Curve From Time Zero to Time of Last Measurable Concentration) - Valacyclovir
NCT01149460 (6) [back to overview]	Cmax (Maximum Observed Concentration of Drug Substance in Plasma) - Acyclovir
NCT01149460 (6) [back to overview]	Cmax (Maximum Observed Concentration of Drug Substance in Plasma) - Valacyclovir
NCT01149460 (6) [back to overview]	AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity) - Acyclovir
NCT01346475 (4) [back to overview]	Frequency of HSV-2 Total Shedding From the Genital Tract as Measured by PCR, Calculated Using a Per-day Shedding Rate in Participants Treated With High-dose Valacyclovir as Compared to Once-daily Valacyclovir.
NCT01346475 (4) [back to overview]	Number of Genital HSV Shedding Episodes
NCT01346475 (4) [back to overview]	Quantity of HSV Detected, Median
NCT01346475 (4) [back to overview]	Duration of Genital HSV Shedding Episodes
NCT01390857 (4) [back to overview]	Number of Participants With Any Serious Adverse Event
NCT01390857 (4) [back to overview]	Number of Participants With Any Unexpected Adverse Drug Reactions
NCT01390857 (4) [back to overview]	Number of Participants Classified as Effective and Not Effective
NCT01390857 (4) [back to overview]	Number of Participants With the Indicated Adverse Drug Reactions
NCT01453075 (1) [back to overview]	Effect of HSV-2 Suppression on HCV Viral Load.
NCT01580995 (1) [back to overview]	Change in HCV RNA Viral Load
NCT01602562 (15) [back to overview]	Mean Urine Specific Gravity Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Red Blood Cell Count at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Albumin and Total Protein Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Platelet Count and White Blood Cell (WBC) Count at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Hemoglobin Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Direct Bilirubin, Total Bilirubin, Creatinine, and Uric Acid Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Cholesterol, Chloride, Glucose, Potassium, Sodium, Triglyceride, and Urea/Blood Urea Nitrogen (BUN) Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Basophil, Eosinophil, Lymphocyte, Monocyte, and Total Neutrophil Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Mean Alkaline Phosphatase (ALP), Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Creatine Phosphokinase (CPK), Gamma Glutamyl Transferase (GGT), and Lactate Dehydrogenase (LD) Values at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Number of Participants With a Herpes Simplex Virus (HSV) Infection
NCT01602562 (15) [back to overview]	Change From Baseline in Heart Rate at Days 0, 7, 14, 21, and 35
NCT01602562 (15) [back to overview]	Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at Days 0, 7, 14, 21, and 35
NCT01602562 (15) [back to overview]	Number of Participants With the Indicated Result for the Indicated Urinalysis Parameters Tested by Dipstick at Screening, Day 14, and Day 35
NCT01602562 (15) [back to overview]	Number of Participants With the Indicated Electrocardiogram (ECG) Findings at Screening and Day 35
NCT01602562 (15) [back to overview]	Number of Participants With Any Adverse Event (AE) or Any Serious Adverse Event (SAE)
NCT01658826 (2) [back to overview]	Within-subject Genital HSV Mucocutaneous Shedding Rate
NCT01658826 (2) [back to overview]	Overall Shedding Rate
NCT01959841 (6) [back to overview]	Time to Pain Resolution
NCT01959841 (6) [back to overview]	The Percentage of Participants Achieving Cessation of New Lesion Formation by Day 4 of Study Treatment
NCT01959841 (6) [back to overview]	Time to Cessation of New Lesion Formation
NCT01959841 (6) [back to overview]	Time to Complete Crusting
NCT01959841 (6) [back to overview]	Time to Healing
NCT01959841 (6) [back to overview]	Time to Virus Disappearance
NCT02008773 (6) [back to overview]	Working Memory
NCT02008773 (6) [back to overview]	Cognitive Performance
NCT02008773 (6) [back to overview]	Functional Performance
NCT02008773 (6) [back to overview]	Functional Performance
NCT02008773 (6) [back to overview]	Psychosis Symptoms
NCT02008773 (6) [back to overview]	Visual Memory
NCT02831933 (2) [back to overview]	Overall Survival (OS) Rate
NCT02831933 (2) [back to overview]	Progression Free Survival (PFS) Rate
NCT03004183 (6) [back to overview]	Clinical Benefit Rate
NCT03004183 (6) [back to overview]	Duration of Response
NCT03004183 (6) [back to overview]	Number of Participants With Treatment-related Adverse Events
NCT03004183 (6) [back to overview]	Overall Survival Rate
NCT03004183 (6) [back to overview]	Antitumor Activity
NCT03004183 (6) [back to overview]	Objective Response Rate

Survival With no or Mild Neuropsychological Impairment at 12 Months After Initiation of Study Medication as Measured by the Mattis Dementia Rating Scale (MDRS)

Number of subjects who were assessed to have no or mild neuropsychological impairment at 12 months using the Mattis Dementia Rating Scale. (A score of 121 or higher refects no or mild neuropsychological impairment.) Scale is: 139-144 normal; 121-139 mild; 114-120 moderate; 87-113 severe; and <=86 very severe. (NCT00031486)
Timeframe: One year post therapy.

Intervention	Participants (Number)
	MDRS Score >= 121 (positive)	MDRS score < 121 (negative)
Placebo	34	2
Total	62	7
Valacyclovir	28	5

Intervention	Participants (Number)
	MMSE score >= 23 (90 days)	MMSE score < 23 (90 days)	MMSE score >= 23 (6 months)	MMSE score < 23 (6 months)	MMSE score >= 23 (12 months)	MMSE score < 23 (12 months)
Placebo	31	5	29	4	30	5
Total	57	8	52	8	58	9
Valacyclovir	26	3	23	4	28	4

Intervention	Participants (Number)
	MDRS score >= 121 (90 days)	MDRS score < 121 (90 days)	MDRS score >= 121 ( 6 months)	MDRS score < 121 (6 months)	MDRS score >= 121 (12 months)	MDRS score < 121 (12 months)
Placebo	31	5	31	4	34	2
Total	59	8	55	9	62	7
Valacyclovir	28	3	24	5	28	5

Intervention	Participants (Number)
	GCS score >= 12 (90 days)	GCS score < 12 (90 days)	GCS score >= 12 (6 months)	GCS score < 12 (6 months)	GCS score >= 12 (12 months)	GCS score < 12 (12 months)
Placebo	37	0	36	0	37	0
Total	67	0	67	0	70	0
Valacyclovir	30	0	31	0	33	0

Intervention	Scores on a scale Change in SF-36 (Median)
	SF-36 score difference from day 0 to 90	SF-36 score difference from day 0 to 6 months	SF-36 score difference from day 0 to 12 months
Placebo	307.5	475	985
Total	355	635	985
Valacyclovir	465	722.5	1095

Intervention	Percentage of participants (Number)
	No Signs/Symptoms	Signs/symptoms Present
Placebo	77	23
VALTREX 1 g Once Daily	88	13

Intervention	Days (Median)
VALTREX 1 g First Then Placebo	NA
Placebo First Then VALTREX 1 g	61

Intervention	hours (Median)
	Pain (n = 220, 228)	Burning (n = 221, 218)	Itching (n = 309, 297)	Tingling (n = 266, 275)	Tenderness (n = 298, 311)
Famciclovir	18.0	16.1	43.9	23.8	55.2
Valacyclovir	20.3	12.6	43.5	23.0	48.0

Intervention	days (Median)
	From treatment initiation	From date of healing /confirmation
Famciclovir	33.5	27.5
Valacyclovir	38.0	32.0

Intervention	Percentage of participants (Number)
	Aborted Lesions	Non-Aborted lesions
Famciclovir	32.7	67.3
Valacyclovir	33.6	66.4

Intervention	participants (Number)
	Patients continued in follow up period	Patients with 2nd recurrence in follow up period
Famciclovir	324	226
Valacyclovir	342	231

Intervention	units on a scale (Mean)
	Baseline YMRS	Final YMRS 16 weeks
Active Treatment Group - Valcyclovir	7.88	5.19
Inactive Treatment Group - Placebo	8.84	4.84

Intervention	units on a scale (Mean)
	Baseline MADRS	Final MADRS 16 weeks
Active Treatment Group - Valcyclovir	27.94	11.5
Inactive Treatment Group - Placebo	19.74	14.89

Intervention	Participants (Count of Participants)
	Stable Disease	Partial Response	No Response
All Participants	7	16	2

Intervention	Participants (Count of Participants)
	Stable Disease	Partial Response	Progressive Disease	No Response
All Participants	20	11	2	3

Intervention	Participants (Count of Participants)
	Participants Collected Successfully	Participants Unable to Collect
All Participants	30	7

Intervention	Scores on the scale (Mean)
	Scores at Baseline of the trial	Scores at week 2 of the trial	Scores at week 4 of the trial	Scores at week 6 of the trial	Scores at week 10 of the trial	Scores at week 14 of the trial	Scores at the end of the trial
Sugar Pill	83.92	77	75.2	74.3	73.2	69.6	67.125
Valacyclovir	70.08	72.25	67.36	65.583	65.2	57.1	56.5

Intervention	units on a scale (Mean)
	Working Memory: 2-Back Test Accuracy	Immediate Verbal Memory Reaction Accuracy
Sugar Pill	0.13	-0.49
Valacyclovir	2.13	2.44

Intervention	percentage of swabs with HSV detected (Number)
Standard-dose Valacyclovir (500 mg Daily)	5
High-dose Valacyclovir (1 gm Three Times Daily)	3

Intervention	ratio (Mean)
	SCR, n=21, 19	Day 14, n=18, 17	Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	1.0146	1.0158	1.0137
Pediatric Participants: VACV 500 mg Granules/Tablets	1.0188	1.0155	1.0153

Intervention	tera (10^12) per liter (TI/L) (Mean)
	SCR, n=21,19	Day 14, n=18, 17	Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	3.165	2.932	3.297
Pediatric Participants: VACV 500 mg Granules/Tablets	3.293	2.908	3.073

valacyclovir

Description

Cross-References

Synonyms (92)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (1)

Drug Classes (1)

Pathways (3)

Protein Targets (12)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (14)

Molecular Functions (9)

Ceullar Components (8)

Bioassays (164)

Research

Studies (1,156)

Study Types

Clinical Trials (122)

Trial Overview

Trial Outcomes

Survival With no or Mild Neuropsychological Impairment at 12 Months After Initiation of Study Medication as Measured by the Mattis Dementia Rating Scale (MDRS)

Survival With no or Mild Neuropsychological Impairment at 90 Days, and at 6 and 12 Months, as Measured by the Mini-Mental Status Examination (MMSE).

Survival With no or Mild Neuropsychological Impairment at 90 Days and at 6 and 12 Months, as Measured by the Mattis Dementia Rating Scale (MDRS)

Survival With no or Mild Neuropsychological Impairment at 90 Days and at 6 and 12 Months, as Measured by the Glasgow Coma Scale (GCS).

Median Number of Reported AEs Describing Safety and Tolerance of Valacyclovir (VACV), Evaluated by the Number Adverse Events, Administered at a Dose of 2.0 Grams Given Orally 3 Times a Day for 90 Days.

Effect of Study Medication on Quality of Life Measurements.

Mean Log HSV-2 DNA Copy Number Per Day on Days With Total Shedding

Mean Log HSV-2 DNA Copy Number Per Day on Days With Subclinical Shedding

Mean Percent Days of Subclinical Shedding as Determined by Type-specific Polymerase Chain Reaction (PCR) Assay for HSV-2

Mean Percent Days of Total HSV-2 Shedding

Number of Participants With no Shedding

Percent Overall Study Population Who Have Recognized Clinical Signs/Symptoms of Genital Herpes Infection During the Study

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Mean Number of GH Recurrences Per Month Within the 6-month Study Period

Number of Isolates With Resistance to Acyclovir (ACV)

Percentage of Participants With Time to First GH Recurrence

Percentage of Participants With Time to First Oral Herpes Simplex Virus (HSV) Outbreak Within 6-months

Mean Percent Days Clinical Shedding (Presence of Genital Lesions)

Mean Percent Days of Total Shedding (Clinical and Subclinical) as Determined by Type-specific Polymerase Chain Reaction (PCR) Assay for Herpes Simplex Virus Type 2 (HSV-2)

Mean Percent Days Subclinical Shedding (no Genital Lesions Present)

Median Time to First Genital Herpes Recurrence (Days)

Percentage of Participants With at Least One Genital Herpes Recurrence

Percentage of Participants With no Shedding

Number of Participants With Any Adverse Event (AE) and Serious Adverse Event (SAE)

Time to Resolution of Symptoms Associated With Recurrent Genital Herpes

Time to a Second Recurrence of Genital Herpes

Percentage of Participants With Aborted Genital Herpes Lesions

Number of Patients With a Second Recurrence of Genital Herpes

Investigator-assessed Time to Healing of All Non-aborted Genital Herpes Lesions

Investigator-assessed Time to Healing of All (Non-aborted and Aborted) Genital Herpes Lesions

Frequency of HSV-2 Total Shedding From the Genital Tract as Measured by PCR, Calculated Using a Per-day Shedding Rate in Participants Treated With High-dose Acyclovir as Compared to Once-daily Valacyclovir.

Change From Baseline in Young Mania Rating Scale (YMRS) at 16 Weeks

Change From Baseline in Montgomery Asberg Depression Score at 16 Weeks

Percent Change From Baseline in Repeatable Battery for the Assessment of Neuropsychological Status at 16 Weeks

Response Rate After 3 Cycles of Treatment With Bortezomib and Rituximab

Response Rate After 2 Cycles of Treatment With Bortezomib and Rituximab

Participants Ability to Collect Stem Cells After Treatment With Bortezomib and Rituximab

PANSS Positive and Negative Syndrome Scale for Schizophrenia

Cognitive Function Neuropsychological Battery (Gur Battery)

Changes in Grey Matter Deficit

The Effect of Valacyclovir 1 Gram Twice Daily Compared to Acyclovir 400 mg Twice Daily on the Percentage of Days With Genital Herpes Lesions.

The Genital HSV Shedding Rate While on 400 mg Twice Daily of Acyclovir Versus 1000 mg Twice Daily of Valacyclovir.

The Quantity of HIV-1 RNA in Plasma While on 400 mg Twice Daily of Acyclovir Versus 1000 mg Twice Daily of Valacyclovir.

Sub-Study: To Evaluate the Kinetics of Plasma HIV-1 Decline Over the First Three Days of High-dose Valacyclovir Administration.

The Effect of Valacyclovir 1 g Twice Daily Compared With Acyclovir 400 mg Twice Daily on the Quantity of Genital HSV Detected During Shedding Episodes.

Mean Change in HIV-1 Levels in Plasma Between 34 and 38 Weeks Gestation

Vertical HIV-1 Transmission

Number of Participants With an HIV Viral Load of <500 Copies/ml

CD4 Count

Herpes Simplex Virus Type 2 Recurrence

Rate of Asymptomatic HSV-2 Genital Shedding

Mean Level of HIV-1 RNA in Plasma of Participants While on Acyclovir or Valacyclovir.

AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity) - Valacyclovir

Intervention	Grams per liter (G/L) (Mean)
	Albumin, SCR, n=21, 19	Albumin, Day 14, n=18, 17	Albumin, Day 35, n=16, 16	Total protein, SCR, n=21, 19	Total protein, Day 14, n=18, 17	Total protein, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	41.0	34.6	40.8	64.2	57.6	62.9
Pediatric Participants: VACV 500 mg Granules/Tablets	41.5	39.1	40.9	66.2	62.7	65.3

Intervention	giga (10^9) per liter (GI/L) (Mean)
	Platelet count, SCR, n=21,19	Platelet count, Day 14, n=18, 17	Platelet count, Day 35, n=16, 16	WBC count, SCR, n=21,19	WBC count, Day 14, n=16, 12	WBC count, Day 35, n=16, 14
Adult Participants: VACV 500 mg Tablet	190.2	40.3	139.4	4.01	3.46	5.00
Pediatric Participants: VACV 500 mg Granules/Tablets	167.7	58.2	119.0	3.03	2.23	3.71

Intervention	Micromoles per liter (µmol/L) (Mean)
	Direct bilirubin, SCR, n=21, 19	Direct bilirubin, Day 14, n=18, 17	Direct bilirubin, Day 35, n=16, 16	Total bilirubin, SCR, n=21, 19	Total bilirubin, Day 14, n=18, 17	Total bilirubin, Day 35, n=16, 16	Creatinine, SCR, n=21, 19	Creatinine, Day 14, n=18, 17	Creatinine, Day 35, n=16, 16	Uric acid, SCR, n=21, 19	Uric acid, Day 14, n=18, 17	Uric acid, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	2.931	7.410	2.351	8.224	12.540	6.306	62.6798	46.7047	58.7860	276.1571	133.1691	255.0205
Pediatric Participants: VACV 500 mg Granules/Tablets	2.970	3.923	2.565	8.190	9.858	6.733	30.1025	25.5320	33.3710	259.5206	137.5038	238.6635

Intervention	Millimoles per liter (mmol/L) (Mean)
	Cholesterol, SCR, n=21, 19	Cholesterol, Day 14, n=18, 17	Cholesterol, Day 35, n=16, 16	Chloride, SCR, n=21, 19	Chloride, Day 14, n=18, 17	Chloride, Day 35, n=16, 16	Glucose, SCR, n=21, 19	Glucose, Day 14, n=18, 17	Glucose, Day 35, n=16, 16	Potassium, SCR, n=21, 19	Potassium, Day 14, n=18, 17	Potassium, Day 35, n=16, 16	Sodium, SCR, n=21, 19	Sodium, Day 14, n=18, 17	Sodium, Day 35, n=16, 16	Triglycerides, SCR, n=21, 19	Triglycerides, Day 14, n=18, 17	Triglycerides, Day 35, n=16, 16	Urea/BUN, SCR, n=21, 19	Urea/BUN, Day 14, n=18, 17	Urea/BUN, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	4.8149	4.0255	5.5324	105.2	104.4	106.0	5.8127	7.2656	6.4808	4.08	3.93	4.31	142.0	140.3	141.8	2.0760	1.8789	2.9486	4.2721	4.8274	3.7619
Pediatric Participants: VACV 500 mg Granules/Tablets	4.1703	3.5504	4.1279	103.3	105.0	104.0	6.0214	6.0996	5.7800	4.01	4.34	4.09	140.2	139.2	139.3	1.3489	1.4185	1.6646	3.6903	3.1332	4.1657

Intervention	Percentage of cells in blood (Mean)
	Basophils, SCR, n=21,19	Basophils, Day 14, n=16, 16	Basophils, Day 35, n=16, 15	Eosinophils, SCR, n=21, 19	Eosinophils, Day 14, n=16, 16	Eosinophils, Day 35, n=16, 15	Lymphocytes, SCR, n=21,19	Lymphocytes, Day 14, n=16, 16	Lymphocytes, Day 35, n=16, 15	Monocytes, SCR, n=21,19	Monocytes, Day 14, n=16, 16	Monocytes, Day 35, n=16, 15	Total neutrophils, SCR, n=21,19	Total neutrophils, Day 14, n=16, 16	Total neutrophils, Day 35, n=16, 15
Adult Participants: VACV 500 mg Tablet	1.05	0.69	1.09	3.67	0.79	4.10	32.72	13.61	37.08	7.90	15.32	14.54	54.46	63.53	42.76
Pediatric Participants: VACV 500 mg Granules/Tablets	0.49	0.14	0.59	2.06	0.59	7.51	38.94	16.73	30.85	10.99	17.33	13.33	47.52	62.21	47.63

Intervention	International units per liter (IU/L) (Mean)
	ALP, SCR, n=21, 19	ALP, Day 14, n=18, 17	ALP, Day 35, n=16, 16	ALT, SCR, n=21, 19	ALT, Day 14, n=18, 17	ALT, Day 35, n=16, 16	AST, SCR, n=21, 19	AST, Day 14, n=18, 17	AST, Day 35, n=16, 16	CPK, SCR, n=21, 19	CPK, Day 14, n=18, 17	CPK, Day 35, n=16, 16	GGT, SCR, n=21, 19	GGT, Day 14, n=18, 17	GGT, Day 35, n=16, 16	LD, SCR, n=21, 19	LD, Day 14, n=18, 17	LD, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	247.1	358.7	314.9	23.7	53.2	58.9	23.2	39.8	45.1	65.1	20.5	42.1	47.2	118.4	90.3	251.8	215.4	256.7
Pediatric Participants: VACV 500 mg Granules/Tablets	598.8	456.7	519.9	20.7	62.1	62.0	27.1	35.0	54.0	72.0	27.4	38.4	24.8	27.5	50.7	213.3	210.6	255.9

Intervention	Beats per minute (Mean)
	Day 0, n=21, 19	Day 7, n=19, 17	Day 14, n=18, 17	Day 21, n=17, 17	Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	1.1	13.3	12.5	16.4	19.2
Pediatric Participants: VACV 500 mg Granules/Tablets	-1.0	3.8	3.6	1.8	3.6

Intervention	Millimeters of mercury (Mean)
	SBP, Day 0, n=21, 19	SBP, Day 7, n=19, 17	SBP, Day 14, n=18, 17	SBP, Day 21, n=17, 17	SBP, Day 35, n=16, 16	DBP, Day 0, n=21, 19	DBP, Day 7, n=19, 17	DBP, Day 14, n=18, 17	DBP, Day 21, n=17, 17	DBP, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	-1.8	0.9	4.3	-1.4	2.8	-2.7	1.6	3.4	1.5	4.7
Pediatric Participants: VACV 500 mg Granules/Tablets	-4.7	-6.1	-7.6	-7.0	-4.5	-1.8	0.3	-5.9	-1.2	-1.1

Intervention	Participants (Number)
	UB, Neg, SCR, n=21, 19	UB, Neg, Day 14, n=18, 17	UB, Neg, Day 35, n=16, 16	UOB, Neg, SCR, n=21, 19	UOB, 2+, SCR, n=21, 19	UOB, Neg, Day 14, n=18, 17	UOB, Trace, Day 14, n=18, 17	UOB, 1+, Day 14, n=18, 17	UOB, 3+, Day 14, n=18, 17	UOB, Neg, Day 35, n=16, 16	UOB, Trace, Day 35, n=16, 16	UOB, 1+, Day 35, n=16, 16	UOB, 3+, Day 35, n=16, 16	UG, Neg, SCR, n=21, 19	UG, Trace, SCR, n=21, 19	UG, Neg, Day 14, n=18, 17	UG, Trace, Day 14, n=18, 17	UG, 1+, Day 14, n=18, 17	UG, 2+, Day 14, n=18, 17	UG, 3+, Day 14, n=18, 17	UG, Neg, Day 35, n=16, 16	UG, Trace, Day 35, n=16, 16	UK, Neg, SCR, n=21, 19	UK, Neg, Day 14, n=18, 17	UK, 1+, Day 14, n=18, 17	UK, Neg, Day 35, n=16, 16	UK, 1+, Day 35, n=16, 16	UP, Neg, SCR, n=21, 19	UP, Trace, SCR, n=21, 19	UP, 1+, SCR, n=21, 19	UP, 2+, SCR, n=21, 19	UP, Neg, Day 14, n=18, 17	UP, Trace, Day 14, n=18, 17	UP, 1+, Day 14, n=18, 17	UP, 2+, Day 14, n=18, 17	UP, Neg, Day 35, n=16, 16	UP, Trace, Day 35, n=16, 16	UP, 1+, Day 35, n=16, 16	UUG, Trace, SCR, n=21, 19	UUG, 2+, SCR, n=21, 19	UUG, Trace, Day 14, n=18, 17	UUG, 1+, Day 14, n=18, 17	UUG, 2+, Day 14, n=18, 17	UUG, 3+, Day 14, n=18, 17	UUG, Trace, Day 35, n=16, 16	UUG, 3+, Day 35, n=16, 16
Adult Participants: VACV 500 mg Tablet	21	18	16	19	2	14	2	2	0	12	1	2	1	19	2	14	1	1	1	1	15	1	21	17	1	16	0	19	0	0	2	9	5	2	2	13	2	1	19	2	17	1	0	0	16	0
Pediatric Participants: VACV 500 mg Granules/Tablets	19	17	16	19	0	14	2	0	1	16	0	0	0	19	0	17	0	0	0	0	16	0	19	17	0	15	1	14	4	1	0	12	4	0	1	13	1	2	19	0	15	0	1	1	15	1

Intervention	Participants (Number)
	SCR, Normal, n=21, 19	SCR, NCS, n=21, 19	SCR, CS, n=21, 19	SCR, NR, n=21, 19	Day 35, Normal, n=16, 16	Day 35, NCS, n=16, 16	Day 35, CS, n=16, 16	Day 35, NR, n=16, 16
Adult Participants: VACV 500 mg Tablet	16	5	0	0	15	1	0	0
Pediatric Participants: VACV 500 mg Granules/Tablets	19	0	0	0	13	2	0	1