pradefovir mesylate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

pradefovir: a HepDirect prodrug of adefovir; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9604653
CHEMBL ID	3989658
MeSH ID	M0482044

Synonyms (29)

Synonym
625095-61-6
pradefovir mesylate (usan)
D05588
remofovir mesylate
icn-2001-3
mb-6866
pradefovir mesylate
hepavir b
mb-06866 ,
mb-06866q
9-(2-(4-(3-chlorophenyl)-2-oxo-1,3,2-dioxaphosphorinan-2-yl)methoxyethyl)adenine
pradefovir mesylate [usan]
9h-purin-6-amine, 9-(2-(((2r,4s)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphorinan-2-yl)-methoxy)ethyl)-, monomethanesulfonate;
unii-0d5204zsix
mb 06866q
0d5204zsix ,
pradefovir
pradefovir mesilate [who-dd]
pradefovir mesilate
DB05478
DTXSID00211558
mb6866
CHEMBL3989658
Q27095685
HY-112690A
CS-0062746
pradefovir mesylate (remofovir mesylate)
EX-A1921
9-[2-[[(2r,4s)-4-(3-chlorophenyl)-2-oxo-1,3,2lambda5-dioxaphosphinan-2-yl]methoxy]ethyl]purin-6-amine;methanesulfonic acid

Research Excerpts

Toxicity

Excerpt	Reference	Relevance
" No subject experienced a serious adverse event or nephrotoxicity."	( Safety, efficacy, and pharmacokinetics of pradefovir for the treatment of chronic hepatitis B infection. Chen, H; Ding, Y; Jin, W; Li, C; Li, X; Liu, C; Liu, J; Niu, J; Wu, M; Zhang, D; Zhang, H; Zhu, X, 2020)	0.56

Pharmacokinetics

Excerpt	Reference	Relevance
" The half-life of PMEA in the pradefovir group was 11."	( Safety, efficacy, and pharmacokinetics of pradefovir for the treatment of chronic hepatitis B infection. Chen, H; Ding, Y; Jin, W; Li, C; Li, X; Liu, C; Liu, J; Niu, J; Wu, M; Zhang, D; Zhang, H; Zhu, X, 2020)	0.56

Bioavailability

Excerpt	Reference	Relevance
" Oral absorption and bioavailability were 29."	( Single-dose pharmacokinetics and metabolism of [14C]remofovir in rats and cynomolgus monkeys. Lin, CC; Lourenco, D; Xu, C; Yeh, LT; Zhu, N, 2005)	0.33
" The lead prodrug (14, MB06866, pradefovir), identified from a variety of in vitro and in vivo assays, exhibited good oral bioavailability (F = 42%, mesylate salt, rat) and rate of prodrug conversion to ADV-DP."	( Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B. Boyer, SH; Colby, TJ; Craigo, W; DaRe, J; Erion, MD; Fujitaki, JM; Gómez-Galeno, JE; Matelich, MC; Ollis, K; Reddy, KR; Sun, Z; Ugarkar, BG; van Poelje, PD, 2008)	0.35

Dosage Studied

Excerpt	Relevance	Reference
" Dose-limiting nephrotoxicity necessitates suboptimal dosing at 10 mg/day."	( Remofovir mesylate: a prodrug of PMEA with improved liver-targeting and safety in rats and monkeys. Erion, MD; Hong, Z; Lin, CC; Vitarella, D; Yeh, LT, 2004)	0.32
" dosing of [(14)C]remofovir, fecal excretion of radioactivity accounted for 37."	( Single-dose pharmacokinetics and metabolism of [14C]remofovir in rats and cynomolgus monkeys. Lin, CC; Lourenco, D; Xu, C; Yeh, LT; Zhu, N, 2005)	0.33
"The pharmacokinetics of pradefovir and adefovir, 9-(2-phosphonylmethoxyethyl) adenine (PMEA), was evaluated in healthy male volunteers after oral dosing of pradefovir (10, 30, or 60 mg)."	( Pharmacokinetics of pradefovir and PMEA in healthy volunteers after oral dosing of pradefovir. Lin, CC; Peterson, J; Teng, A; Xu, C; Yeh, LT, 2005)	0.33
" The enzyme induction potential of pradefovir was evaluated in rats following multiple oral dosing and in primary cultures of human hepatocytes."	( Metabolic activation of pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Benetton, S; Fang, C; Lin, CC; Xu, GF; Yeh, LT, 2006)	0.33
"Adefovir dipivoxil, a marketed drug for the treatment of hepatitis B, is dosed at submaximally efficacious doses because of renal toxicity."	( Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B. Boyer, SH; Colby, TJ; Craigo, W; DaRe, J; Erion, MD; Fujitaki, JM; Gómez-Galeno, JE; Matelich, MC; Ollis, K; Reddy, KR; Sun, Z; Ugarkar, BG; van Poelje, PD, 2008)	0.35

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	8 (66.67)	29.6817
2010's	2 (16.67)	24.3611
2020's	2 (16.67)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.63

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.

Metric	This Compound (vs All)
Research Demand Index	11.63 (24.57)
Research Supply Index	2.83 (2.92)
Research Growth Index	4.46 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.63)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	4 (33.33%)	5.53%
Reviews	1 (8.33%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	7 (58.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
adenine [no description available]	8.51	12	4	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.	2.02	1	0	acetamides; phenols	antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.03	1	0	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
cytarabine [no description available]	2.02	1	0	beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside	antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent
adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection.	6.95	8	3	6-aminopurines; ether; phosphonic acids	antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent
adefovir dipivoxil bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.	2.02	1	0	6-aminopurines; carbonate ester; ether; organic phosphonate	antiviral drug; DNA synthesis inhibitor; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent; prodrug
organophosphonates hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.	7.05	9	3	divalent inorganic anion; phosphite ion
9-(2-(phosphonomethoxy)ethyl)adenine diphosphate 9-(2-(phosphonomethoxy)ethyl)adenine diphosphate: structure in first source	2.02	1	0
tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.	6.13	3	3	nucleoside analogue; phosphonic acids	antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Chronic Hepatitis B [description not available]	0	5.86	4	2
Hepatitis B, Chronic INFLAMMATION of the LIVER in humans caused by HEPATITIS B VIRUS lasting six months or more. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	1	7.86	4	2
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	3.51	1	1
Hepatitis B Virus Infection [description not available]	0	2.94	1	0
Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	0	2.94	1	0

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