Page last updated: 2024-12-05

brl 42810

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Cross-References

ID SourceID
PubMed CID3324
CHEMBL ID880
CHEBI ID4974
SCHEMBL ID2949
MeSH IDM0168273

Synonyms (151)

Synonym
AKOS005556609
HMS3393G22
AB00639952-08
BRD-K45033733-001-02-3
oravir
ak-120
2-(acetoxymethyl)-4-(2-amino-4,5-dihydro-9h-purin-9-yl)butyl acetate
1,3-propanediol, 2-(2-(2-amino-9h-purin-9-yl)ethyl)-, diacetate (ester)
brl-42810
c14h19n5o4
SPECTRUM_000466
2-[2-(2-amino-9h-purin-9-yl)ethyl]-1,3-propanediol diacetate
9-(4-acetoxy-3-(acetoxymethyl)but-1-yl)-2-aminopurine
famciclovirum [inn-latin]
2-(2-(2-amino-9h-purin-9-yl)ethyl)-1,3-propanediol diacetate (ester)
SPECTRUM5_001548
BSPBIO_003489
MLS001424115
104227-87-4
famciclovir ,
[2-(acetoxymethyl)-4-(2-aminopurin-9-yl)butyl] acetate
brl 42810
diacetyl 6-deoxy-9-(4-hydroxy-3-hydroxymethyl-but-1-yl)guanine
FCV ,
famvir
MLS000759505
smr000466375
9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurine
acetic acid 2-acetoxymethyl-4-(2-amino-purin-9-yl)-butyl ester
2-(2-(2-amino-9h-purin-9-yl)ethyl)-1,3-propanediol diacetate
DB00426
D00317
famciclovir (jan/usp/inn)
famvir (tn)
NCGC00095133-02
NCGC00095133-01
KBIOSS_000946
KBIO2_006082
KBIO2_003514
KBIO3_002709
KBIOGR_001162
KBIO2_000946
SPECTRUM3_001675
SPBIO_001202
SPECTRUM2_001101
SPECTRUM4_000611
SPECTRUM1505201
NCGC00095133-03
HMS2093K12
HMS2051G22
HMS2090G10
CHEMBL880
nsc-758921
famciclovirum
CHEBI:4974 ,
2-[(acetyloxy)methyl]-4-(2-amino-9h-purin-9-yl)butyl acetate
FT-0668461
HMS1922L09
[2-(acetyloxymethyl)-4-(2-aminopurin-9-yl)butyl] acetate
STK623204
A19583
[2-(acetyloxymethyl)-4-(2-aminopurin-9-yl)-butyl] acetate
HMS3262O08
nsc758921
pharmakon1600-01505201
cas-104227-87-4
dtxsid0023038 ,
dtxcid403038
tox21_111442
F0842
2-(2-(2-amino-9h-purin-9-yl)ethyl)propane-1,3-diyl diacetate
HMS2232H09
CCG-39277
unii-qic03ani02
qic03ani02 ,
famciclovir [usan:inn:ban]
nsc 758921
hsdb 8121
HY-17426
CS-1357
FT-0602549
NCGC00095133-04
AB07547
famciclovir [jan]
famciclovir [vandf]
famciclovir [inn]
famciclovir [usp-rs]
famciclovir [mart.]
famciclovir [usp monograph]
2-[2-(2-amino-9h-purin-9-yl)ethyl]-1,3-propanediol diacetate (ester)
famciclovir [mi]
famciclovir [orange book]
famciclovir [who-dd]
famciclovir [usan]
S2467
HMS3370D14
AB00639952-06
NC00156
SCHEMBL2949
tox21_111442_1
NCGC00095133-06
KS-5020
tox21_500793
NCGC00261478-01
9-[4-acetoxy-3-(acetoxymethyl)butyl]-2-amino-9h purine
9-(4-acetoxy-3-acetoxymethylbut-1-yl)-2-aminopurine
MLS006011896
AB00639952_10
AB00639952_09
mfcd00866964
2-(2-(2-amino-9h-purin-9-yl)ethyl)-1,3-propanediol diacetate ester
J-001134
sr-01000759358
SR-01000759358-5
SR-01000759358-4
AC-8066
famciclovir, united states pharmacopeia (usp) reference standard
famciclovir, >=98% (hplc)
HMS3656A04
famciclovir, pharmaceutical secondary standard; certified reference material
SBI-0206743.P001
HMS3715F03
SW197536-3
2-[2-(2-amino-9h-purin-9-yl)ethyl]trimethylene diacetate;2-[2-(2-amino-9h-purin-9-yl)ethyl]trimethylene diacetate
bdbm50248001
BCP21312
brl-42810;brl42810;brl 42810;famciclovirum
Q420186
famciclovir (famvir)
2-(2-(2-amino-9h-purin-9-yl)ethyl)propane-
famciclovir,(s)
1,3-diyl diacetate
BRD-K45033733-001-05-6
NCGC00095133-15
brl42810
gtpl11629
famciclovir 100 microg/ml in acetonitrile
2-(2-(2-amino-9h-purin-9-yl)ethyl)-propane-1,3-diyl diacetate
EN300-120645
BF164441
famciclovir, bio-x
Z1530532759
j05ab09
2-((acetyloxy)methyl)-4-(2-amino-9h-purin-9-yl)butyl acetate
famciclovir (usp monograph)
famciclovir (mart.)
famciclovir (usp-rs)
9-(4-acetoxy-3-acetoxymethyl-1-butyl)-2-aminopurine
famciclovirum (inn-latin)
famciclovirum (latin)
s01ad07

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most common adverse experiences reported as related to study medication (famciclovir and placebo) were headache, nausea, and diarrhea."( Safety of famciclovir in patients with herpes zoster and genital herpes.
Boon, R; Jurewicz, R; Saltzman, R, 1994
)
0.29
" There were no differences between groups in the incidence of adverse events."( Efficacy and safety of famciclovir for treating mucocutaneous herpes simplex infection in HIV-infected individuals. Collaborative Famciclovir HIV Study Group.
Aoki, FY; Lavender, EA; Martel, AY; Parsons, JE; Romanowski, B; Saltzman, RL, 2000
)
0.31
" Four patients in the acyclovir plus placebo group did not complete the study protocol due to adverse events (n = 2), deviation from the protocol (n = 1), or loss to follow-up (n = 1)."( Double-blind, randomized, acyclovir-controlled, parallel-group trial comparing the safety and efficacy of famciclovir and acyclovir in patients with uncomplicated herpes zoster.
Chen, YS; Chiang, PC; Lee, SS; Lin, HH; Liu, YC; Shen, MC, 2004
)
0.32
"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
"3%) VZV-infected patients who received famciclovir three times a day experienced at least one adverse event."( Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
Abrams, B; Arguedas, A; Bomgaars, L; De León Castrejón, T; Hamed, K; Kaiser, G; Looby, M; Roberts, M; Rodriguez, A; Sáez-Llorens, X; Spigarelli, MG; Yogev, R; Zhou, W, 2009
)
0.35
" Adverse events were generally mild and transient."( Safety and pharmacokinetics of a single 1500-mg dose of famciclovir in adolescents with recurrent herpes labialis.
Block, SL; Hamed, K; Waldmeier, F; Yogev, R, 2011
)
0.37
"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

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic profile of penciclovir was determined after a single 500-mg dose of its oral precursor, famciclovir, in 9 healthy volunteers and in 14 patients with chronic hepatic disease."( Pharmacokinetics of famciclovir in subjects with chronic hepatic disease.
Audet, PR; Boike, SC; Fairless, A; Freed, MI; Ilson, BE; Jorkasky, DK; Pue, M; Zariffa, N, 1994
)
0.29
" The possibility of a pharmacokinetic interaction between the anti-viral agent, famciclovir and allopurinol has been investigated in twelve healthy male volunteers following a single oral dose of famciclovir (500 mg) in the presence and absence of steady-state levels of allopurinol (300 mg)."( Lack of a pharmacokinetic interaction between oral famciclovir and allopurinol in healthy volunteers.
Fowles, SE; Laroche, J; Pratt, SK; Prince, WT, 1994
)
0.29
" Plasma and urine concentrations of penciclovir and its 6-deoxy precursor, BRL 42359, were determined and penciclovir plasma concentration-time data submitted to model-independent pharmacokinetic analysis."( Linear pharmacokinetics of penciclovir following administration of single oral doses of famciclovir 125, 250, 500 and 750 mg to healthy volunteers.
Fairless, AJ; Fowles, S; Georgiou, P; Laroche, J; Pratt, SK; Prince, W; Pue, MA, 1994
)
0.29
" In paediatric patients this may be difficult to achieve due to lack of pharmacokinetic studies, administration of small doses, changes in body composition, continuous growth, and development and maturation of organs and systems."( The pharmacokinetics of antiviral therapy in paediatric patients.
Eksborg, S, 2003
)
0.32
" Several phase I studies were conducted in healthy volunteers over the course of clinical development to evaluate whether pharmacokinetic drug-drug interactions exist between emtricitabine and other nucleoside antivirals that are extensively eliminated by renal excretion."( Pharmacokinetic evaluation of emtricitabine in combination with other nucleoside antivirals in healthy volunteers.
Begley, JA; Blum, MR; Chittick, GE; Hui, J; Wang, LH; Zong, J, 2007
)
0.34
" Pooled pharmacokinetic data were generated after single doses in 51 participants (approximately 12."( Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
Abrams, B; Arguedas, A; Bomgaars, L; De León Castrejón, T; Hamed, K; Kaiser, G; Looby, M; Roberts, M; Rodriguez, A; Sáez-Llorens, X; Spigarelli, MG; Yogev, R; Zhou, W, 2009
)
0.35
"To develop a population pharmacokinetic model for penciclovir (famciclovir is a prodrug of penciclovir) in adults and children and suggest an appropriate dose for children."( Population pharmacokinetics and optimal design of paediatric studies for famciclovir.
Aarons, L; Graham, G; Kaiser, G; Looby, M; Matthews, I; Ogungbenro, K, 2009
)
0.35
" Population pharmacokinetic modelling was undertaken in NONMEM version VI."( Population pharmacokinetics and optimal design of paediatric studies for famciclovir.
Aarons, L; Graham, G; Kaiser, G; Looby, M; Matthews, I; Ogungbenro, K, 2009
)
0.35
"A population pharmacokinetic model of penciclovir in adults and children has been developed."( Population pharmacokinetics and optimal design of paediatric studies for famciclovir.
Aarons, L; Graham, G; Kaiser, G; Looby, M; Matthews, I; Ogungbenro, K, 2009
)
0.35
" The concentrations of penciclovir declined in a biphasic manner after the peak concentration was attained."( Pharmacokinetics of penciclovir after oral administration of its prodrug famciclovir to horses.
Kondo, T; Kurosawa, M; Matsumura, T; Nagata, S; Nemoto, M; Tsujimura, K; Yamada, M; Yamanaka, T, 2010
)
0.36
" Seventeen infants were included in the pharmacokinetic analysis; one infant experienced immediate emesis and was excluded."( Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
Blumer, J; Hamed, K; Kaiser, G; Rodriguez, A; Sallas, W; Sánchez, PJ, 2010
)
0.36
"OBJECTIVES To determine, following oral administration of famciclovir, pharmacokinetic (PK) parameters for 2 of its metabolites (penciclovir and BRL42359) in plasma and tears of healthy cats so that famciclovir dosage recommendations for the treatment of herpetic disease can be optimized."( Pharmacokinetic modeling of penciclovir and BRL42359 in the plasma and tears of healthy cats to optimize dosage recommendations for oral administration of famciclovir.
Knych, HK; Maggs, DJ; Sebbag, L; Thomasy, SM; Woodward, AP, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
"Emtricitabine is a potent nucleoside reverse transcriptase inhibitor approved as a once-daily drug in combination with other antiretroviral agents for the treatment of HIV infection."( Pharmacokinetic evaluation of emtricitabine in combination with other nucleoside antivirals in healthy volunteers.
Begley, JA; Blum, MR; Chittick, GE; Hui, J; Wang, LH; Zong, J, 2007
)
0.34

Bioavailability

ExcerptReferenceRelevance
"Potential oral prodrugs of the antiherpesvirus acyclonucleoside 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (1, BRL 39123) have been synthesized and evaluated for bioavailability of 1 in the blood of mice."( Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.28
"Famciclovir, a synthetic acyclic guanine derivative, is a prodrug which, after oral administration, is rapidly metabolised to the highly bioavailable antiviral compound penciclovir."( Famciclovir. A review of its pharmacological properties and therapeutic efficacy in herpesvirus infections.
Perry, CM; Wagstaff, AJ, 1995
)
0.29
"Famciclovir is the well-absorbed oral form of penciclovir, an antiviral agent with potent activity against varicella-zoster virus (VZV) and herpes simplex virus (HSV-1) and 2 (HSV-2)."( Famciclovir: review of clinical efficacy and safety.
Cirelli, R; Herne, K; Lee, P; McCrary, M; Tyring, SK, 1996
)
0.29
" The bioavailability of penciclovir, measured by urinary recovery, is approximately 60% and is not affected by food."( The clinical pharmacokinetics of famciclovir.
Gill, KS; Wood, MJ, 1996
)
0.29
"Famciclovir is the well-absorbed oral form of penciclovir, a potent and selective antiviral agent, with activity against members of the herpesvirus family, including varicella-zoster virus (VZV), and herpes simplex virus-1 (HSV-1) and HSV-2."( The pharmacological profile of famciclovir.
Crumpacker, C, 1996
)
0.29
" When administered orally, faMciclovir, the oral prodrug of PCV, is better absorbed than acyclovir, yielding an absolute bioavailability of PCV of 77%."( Famciclovir for treatment of herpesvirus infections.
Flaherty, JF; Luber, AD, 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
"A series of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines (4-10) and 2-amino-9-(2-(2-oxo-1,3-dioxan-5-yl)ethyl)purine (1) were synthesized as potential prodrugs of penciclovir and evaluated for their oral penciclovir bioavailability in mice and rats."( Synthesis and evaluation of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir.
Chang, K; Cho, YB; Choi, WS; Hwang, YY; Im, GJ; Jung, I; Kim, DK; Kim, JS; Kim, KH; Kim, TS; Kim, YW; Lee, N; Min, DS; Um, KA, 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
" 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
" Its bioavailability means that it can be taken less frequently than acyclovir, the only other approved herpes treatment."( Drug effective against herpes.
, 1996
)
0.29
" 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
"Famciclovir, the well absorbed oral pro-drug of penciclovir, is effective in the treatment of herpes zoster when given three times daily."( Once, twice, or three times daily famciclovir compared with aciclovir for the oral treatment of herpes zoster in immunocompetent adults: a randomized, multicenter, double-blind clinical trial.
Ashton, R; Candaele, D; Decroix, J; Forszpaniak, C; Paulet, C; Shafran, SD; Tyring, SK; Wade, A, 2004
)
0.32
" Subsequently, the orally bioavailable prodrugs valaciclovir and famciclovir have been introduced."( Recent clinical experience with famciclovir--a "third generation" nucleoside prodrug.
Beutner, K; Chakrabarty, A; Rauser, M; Tyring, SK, 2004
)
0.32
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"4 hours, respectively; and penciclovir bioavailability was 12."( Pharmacokinetics of penciclovir in healthy cats following oral administration of famciclovir or intravenous infusion of penciclovir.
Bales, JL; Ferrone, M; Maggs, DJ; Stanley, SD; Thomasy, SM; Whittem, T, 2012
)
0.38
"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

Dosage Studied

ExcerptRelevanceReference
" These subsequent studies confirmed that, after oral dosing with famciclovir, more than half the dose was absorbed and rapidly converted to penciclovir."( Selection of an oral prodrug (BRL 42810; famciclovir) for the antiherpesvirus agent BRL 39123 [9-(4-hydroxy-3-hydroxymethylbut-l-yl)guanine; penciclovir].
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.57
" Both 5 and its esters (14-17, 21, 22) and also 18 were well absorbed after oral administration and converted efficiently to 1, the diacetyl (14) and dipropionyl (16) esters providing concentrations of 1 in the blood that were more than 15-fold higher than those observed after dosing either 1 or its esters (25-27)."( Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.28
" 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
" On oral dosing of famciclovir to humans, only penciclovir and BRL 42359 can be detected consistently in the plasma; thus, attention was focused on the oxidation reaction."( Role of aldehyde oxidase in the in vitro conversion of famciclovir to penciclovir in human liver.
Chenery, RJ; Clarke, SE; Harrell, AW, 1995
)
0.29
"Consideration should be given to modification of the dosing schedule of famciclovir from the usual 8-hour interval to a 12-hour interval for patients with moderate renal impairment (CLCR 30 to 59 ml/min/1."( Pharmacokinetics of famciclovir in subjects with varying degrees of renal impairment.
Audet, PR; Boike, SC; Fairless, A; Freed, MI; Ilson, BE; Jorkasky, DK; Pue, MA; Zariffa, N, 1994
)
0.29
" Thus, famciclovir is now established as an effective treatment of immunocompetent patients with herpes zoster or genital herpes infection, particularly as famciclovir is administered in a convenient dosage regimen that may improve compliance compared with aciclovir."( Famciclovir. A review of its pharmacological properties and therapeutic efficacy in herpesvirus infections.
Perry, CM; Wagstaff, AJ, 1995
)
0.29
" Dosage adjustment is required in the presence of renal impairment."( Pharmacokinetics of new antiherpetic agents.
Rolan, P, 1995
)
0.29
" Dosage adjustment is not required for famciclovir in elderly patients with normal or mildly impaired renal function, and the extent of penciclovir availability is not affected by food."( The pharmacological profile of famciclovir.
Crumpacker, C, 1996
)
0.29
" The dosage of famciclovir for herpes zoster in immunocompetent individuals is 500 mg po tid for 7 days; for recurrent genital herpes a dosage of 125 mg po bid for 5 days is recommended."( Famciclovir for treatment of herpesvirus infections.
Flaherty, JF; Luber, AD, 1996
)
0.29
"Given its comparable efficacy, similar adverse effect profile, and less frequent dosing schedule than acyclovir, famciclovir represents a viable alternative for treatment of herpes zoster and for episodic therapy of recurrent genital herpes in immunocompetent adults."( Famciclovir for treatment of herpesvirus infections.
Flaherty, JF; Luber, AD, 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
" 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
" The pharmacokinetics of famciclovir allow a more convenient dosing schedule than the schedule used with acyclovir."( Famciclovir: a new systemic antiviral agent for herpesvirus infections.
Stott, GA, 1997
)
0.3
" New areas of retinitis developed within the posterior pole despite treatment with the maximum dosage of acyclovir; thus, we used a new antiviral agent, famciclovir."( Famciclovir for the treatment of acute retinal necrosis (ARN) syndrome.
Figueroa, MS; Fortun, J; Garabito, I; Gutierrez, C, 1997
)
0.3
" Famciclovir is effective in the suppression and treatment of HSV infections; however, no studies have examined the optimum dosing regimen for HSV prophylaxis in laser resurfacing."( Famciclovir prophylaxis of herpes simplex virus reactivation after laser skin resurfacing.
Alster, TS; Nanni, CA, 1999
)
0.3
" 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 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
"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
" Prophylactic oral antiviral agents are administered routinely to patients undergoing laser resurfacing to prevent postoperative HSV-1 eruptions; however, dosage and duration of treatment vary in the literature."( Herpes simplex virus prophylaxis with famciclovir in patients undergoing aesthetic facial CO2 laser resurfacing.
Bisaccia, E; Scarborough, D, 2003
)
0.32
" The treatment for recurrent hepatitis B after liver transplantation includes increased dosage of lamivudine, application of famciclovir, and other liver protection measures."( Prophylaxis and treatment of hepatitis B virus reinfection following liver transplantation.
Huang, DS; Liang, TB; Wang, WL; Wu, J; Xu, X; Zheng, SS, 2002
)
0.31
" Choice of therapy would then depend on convenience of dosing and cost."( Antiviral treatment of genital herpes.
Apoola, A; Radcliffe, K, 2004
)
0.32
" These compounds offer high oral bioavailabilty and deliver acyclovir and penciclovir, respectively, to the target cells by means of more convenient dosing schedules."( Recent clinical experience with famciclovir--a "third generation" nucleoside prodrug.
Beutner, K; Chakrabarty, A; Rauser, M; Tyring, SK, 2004
)
0.32
"In immunocompetent adults with recurrent genital herpes, a 5-day course of famciclovir at a dosage of 125 mg, 250 mg, or 500 mg twice per day was significantly more effective than was placebo in reducing the duration of viral shedding and symptoms and in accelerating lesion healing."( Clinic-initiated, twice-daily oral famciclovir for treatment of recurrent genital herpes: a randomized, double-blind, controlled trial.
Aoki, FY; Lassonde, M; Martel, AY; Sacks, SL; Shafran, SD, 2005
)
0.33
" Although traditional therapy for a recurrent episode for healthy adults has consisted of twice-daily dosing for 5 days, recent studies have indicated that shorter courses of antiviral therapy are effective."( Single-day, patient-initiated famciclovir therapy for recurrent genital herpes: a randomized, double-blind, placebo-controlled trial.
Aoki, FY; Diaz-Mitoma, F; Gao, J; Gross, G; Hamed, K; Tyring, S, 2006
)
0.33
" 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
" single-day bid famciclovir and placebo in the treatment of herpes labialis demonstrated single-dose famciclovir to be as efficacious as single-day bid dosing in time to healing of lesions and more efficacious than single-day bid famciclovir in time to resolution of pain and tenderness."( Single-dose famciclovir for the treatment of herpes labialis.
Hamed, K; Hull, C; Spruance, S; Tyring, S, 2006
)
0.33
" Its pharmacokinetics allow for administration in a convenient dosing regimen compared with acyclovir, which may improve compliance."( Famciclovir for the treatment of recurrent genital herpes: a clinical and pharmacological perspective.
Aoki, FY; Vinh, DC, 2006
)
0.33
" Convenient patient-initiated single-day (for recurrent genital herpes) and single-dose (for orolabial herpes) dosage regimens may contribute to treatment compliance, patient acceptability and subsequent treatment outcomes."( Famciclovir: a review of its use in herpes zoster and genital and orolabial herpes.
Lyseng-Williamson, KA; Simpson, D, 2006
)
0.33
" Famciclovir has received single-day dosing indications for both of these entities."( Famciclovir for cutaneous herpesvirus infections: an update and review of new single-day dosing indications.
Chacko, M; Weinberg, JM, 2007
)
0.34
"Penciclovir pharmacokinetics following oral famciclovir administration in cats appeared complex within the dosage range studied."( Pharmacokinetics and safety of penciclovir following oral administration of famciclovir to cats.
Maggs, DJ; Moulin, NK; Stanley, SD; Thomasy, SM, 2007
)
0.34
" 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
" More rigorous clinical trials are required to optimise the dosing regimen for safe and effective specific anti-herpes treatment in feline clinical medicine."( Treatment of feline herpesvirus-1 associated disease in cats with famciclovir and related drugs.
Graham, PG; Lessels, NS; Malik, R; Meek, M; Norris, JM; Power, H; Vitale, C; Webb, S, 2009
)
0.35
" An eight-step weight-based dosing regimen was developed to optimize exposure in smaller children and was used in the 7-day multiple-dose safety phases of both studies, which enrolled 100 patients with confirmed/suspected viral infections."( Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
Abrams, B; Arguedas, A; Bomgaars, L; De León Castrejón, T; Hamed, K; Kaiser, G; Looby, M; Roberts, M; Rodriguez, A; Sáez-Llorens, X; Spigarelli, MG; Yogev, R; Zhou, W, 2009
)
0.35
" An eight-step dosing regimen was derived that targeted exposure in infants and children 6 months to 12 years of age to match the penciclovir AUC seen in adults after a 500-mg dose of famciclovir."( Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
Blumer, J; Hamed, K; Kaiser, G; Rodriguez, A; Sallas, W; Sánchez, PJ, 2010
)
0.36
" 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
"Penciclovir pharmacokinetics following oral administration of famciclovir were nonlinear within the dosage range studied, likely because of saturation of famciclovir metabolism."( Pharmacokinetics of penciclovir in healthy cats following oral administration of famciclovir or intravenous infusion of penciclovir.
Bales, JL; Ferrone, M; Maggs, DJ; Stanley, SD; Thomasy, SM; Whittem, T, 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
" However, drug concentrations were noninhibitory during 42% of the dosing cycle."( Rapid viral expansion and short drug half-life explain the incomplete effectiveness of current herpes simplex virus 2-directed antiviral agents.
Corey, L; Schiffer, JT; Swan, DA; Wald, A, 2013
)
0.39
" 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
"OBJECTIVES To determine, following oral administration of famciclovir, pharmacokinetic (PK) parameters for 2 of its metabolites (penciclovir and BRL42359) in plasma and tears of healthy cats so that famciclovir dosage recommendations for the treatment of herpetic disease can be optimized."( Pharmacokinetic modeling of penciclovir and BRL42359 in the plasma and tears of healthy cats to optimize dosage recommendations for oral administration of famciclovir.
Knych, HK; Maggs, DJ; Sebbag, L; Thomasy, SM; Woodward, AP, 2016
)
0.43
" Further studies are needed to assess whether a famciclovir dosage of 90 versus 40 mg/kg, PO, 3 times/d would result in increased efficacy and shorter treatment time."( Oral administration of famciclovir for treatment of spontaneous ocular, respiratory, or dermatologic disease attributed to feline herpesvirus type 1: 59 cases (2006-2013).
Freeman, KS; Kass, PH; Lim, CC; Maggs, DJ; Outerbridge, CA; Shull, O; Strom, AR; Thomasy, SM, 2016
)
0.43
" Both dosing groups were statistically consistent with each other in reducing pain at 2, 4 and 12 weeks follow up."( Comparison Of Efficacy Of Two Different Doses Of Famciclovir In The Prevention And Treatment Of Postherpetic Neuralgia.
Aslam, F; Faisal, LR; Saleem, MA; Sharif, S,
)
0.13
"This study found substantial variation in famciclovir content in the compounded products evaluated, which, in turn, raises concerns that substandard dosing could result in lack of efficacy or a failed treatment trial."( Drug content on receipt and over time for compounded formulations of famciclovir.
Forsythe, LE; Johnson, LR; Knych, HK; Thomasy, SM; Weaver, PG, 2021
)
0.62
"Although proximal tubular secretion is the primary mechanism of kidney drug elimination, current kidney drug dosing strategies are on the basis of eGFR."( Prediction of Kidney Drug Clearance: A Comparison of Tubular Secretory Clearance and Glomerular Filtration Rate.
Brauchla, CC; Chen, Y; de Boer, I; Heckbert, SR; Himmelfarb, J; Hoofnagle, AN; Kestenbaum, BR; Manahan, L; Phillips, B; Shireman, LM; Yeung, CK; Zelnick, LR, 2021
)
0.62
" Once daily famciclovir may provide an effective and convenient once daily dosing regimen for antiviral prophylaxis in CMV low-risk SOT recipients."( Evaluation of low dose famciclovir as herpes simplex virus and varicella zoster virus prophylaxis in cytomegalovirus low-risk solid organ transplant recipients.
Crouch, A; Kotton, C; Le, M; Rogers, C; Shao, S, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
antiviral drugA 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]

Drug Classes (2)

ClassDescription
2-aminopurinesAny aminopurine having the amino substituent at the 2-position.
acetate esterAny carboxylic ester where the carboxylic acid component is acetic acid.
[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]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency29.90330.177814.390939.8107AID2147
Chain A, CruzipainTrypanosoma cruziPotency15.84890.002014.677939.8107AID1476
acetylcholinesteraseHomo sapiens (human)Potency3.89020.002541.796015,848.9004AID1347395
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.37580.006038.004119,952.5996AID1159521
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.84930.000229.305416,493.5996AID743091
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency22.38720.001815.663839.8107AID894
relaxin receptor 1 isoform 1Homo sapiens (human)Potency17.78280.038814.350143.6206AID2676
Interferon betaHomo sapiens (human)Potency23.57030.00339.158239.8107AID1347407
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (71)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (140)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347411qHTS 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) Libary2020ACS 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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588215FDA HLAED, alkaline phosphatase increase2004Current 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.
AID520604Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID14358The total amount of penciclovir recovered in the urine over a 48-h period was determined by HPLC using a C18 reversed-phase column in mouse.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Synthesis and evaluation of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir.
AID554900Half life in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID554888Cmax in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID523080Cmax in 6 to 12 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current 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.
AID523079Tmax in 6 to 12 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current 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.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079931Moderate 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]
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current 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.
AID217408Compound was tested for cytotoxicity in Vero cells (concentration required to reduce the OD value by 50% of the control)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Synthesis and evaluation of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir.
AID1079935Cytolytic 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]
AID109692Concentration of 9-[4-Hydroxy-3-(hydroxymethyl)but-1-yl)guanine in blood of mice after 1 hour upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID28660Aqueous solubility at 25 degrees Centigrade1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID523073Tmax in 1 to <3 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID109691Concentration of 9-[4-Hydroxy-3-(hydroxymethyl)but-1-yl)guanine in blood of mice after 0.25 hours upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID1079938Chronic 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]
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current 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.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID109687Concentration of 2-Amino-9-(4-hydroxy-3-hydroxymethyl)but-1-yl)purine in blood of mice after 0.25 hours upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1079936Choleostatic 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]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID523085Toxicity in 1 to 12 months old infant assessed as severe adverse events at 13.5 mg/kg, po single dose within 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID523081AUC (0 to 6 hrs) in 6 to 12 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID554892AUC (0 to last) in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID523078AUC (0 to 6 hrs) in 2 to <6 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID523075AUC (0 to 6 hrs) in 1 to <3 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID85890Compound was tested for in vitro antiviral activity against herpes viruses of type 1 (HSV-1,KOS strain) (concentration required to reduce the OD value by 50% of the virus infected control)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Synthesis and evaluation of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID523084Toxicity in 1 to 12 months old infant assessed as moderate adverse events at 13.5 mg/kg, po single dose within 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID14359The total amount of penciclovir recovered in the urine over a 48-h period was determined by HPLC using a C18 reversed-phase column in rat.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Synthesis and evaluation of 2-amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as potential prodrugs of penciclovir.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID520606Selectivity index, ratio of CC50 for human WI38 cells to EC50 for BK polyomavirus ATCC VR8372008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID523083Toxicity in 1 to 12 months old infant assessed as mild adverse events at 13.5 mg/kg, po single dose within 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID369218Antiviral activity against woodchuck hepatitis virus infected woodchucks assessed as log reduction of serum viral DNA per ml of serum after 4 weeks2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Antiviral effect of orally administered (-)-beta-D-2-aminopurine dioxolane in woodchucks with chronic woodchuck hepatitis virus infection.
AID1079933Acute 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
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID520605Cytotoxicity against human WI38 cells by neutral red assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID109688Concentration of 2-Amino-9-(4-hydroxy-3-hydroxymethyl)but-1-yl)purine in blood of mice after 1 hour upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID523074Cmax in 1 to <3 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID523076Tmax in 2 to <6 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID554884Tmax in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID554896AUC (0 to infinity) in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID523077Cmax in 2 to <6 months old infant assessed as penciclovir at 6.6 +/- 1.4 mg/kg, po single dose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID122589Concentration of 9-[4-Hydroxy-3-(hydroxymethyl)but-1-yl)guanine in blood of mice after 3 hours upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID109690Concentration of 2-Amino-9-(4-hydroxy-3-hydroxymethyl)but-1-yl)purine in blood of mice after 3 hours upon oral administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID523082Toxicity in 1 to 12 months old infant assessed as adverse events at 13.5 mg/kg, po single dose within 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Single-dose pharmacokinetics of famciclovir in infants and population pharmacokinetic analysis in infants and children.
AID28838Solubility in water1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
AID554904Apparent oral clearance in healthy human at 500 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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]

Research

Studies (542)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (0.37)18.7374
1990's166 (30.63)18.2507
2000's239 (44.10)29.6817
2010's110 (20.30)24.3611
2020's25 (4.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.39

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.39 (24.57)
Research Supply Index6.51 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials93 (16.01%)5.53%
Reviews156 (26.85%)6.00%
Case Studies102 (17.56%)4.05%
Observational1 (0.17%)0.25%
Other229 (39.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]