Page last updated: 2024-12-08

taribavirin

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

Cross-References

ID SourceID
PubMed CID451448
CHEMBL ID2111108
CHEBI ID134989
SCHEMBL ID40670
MeSH IDM0088029

Synonyms (31)

Synonym
icn 3142
prodrug of ribavirin
viramidine
119567-79-2
taribavirin
ribavirin amidine
1-.beta.-d-ribofuranosyl-1,2,4-triazole-3-carboximidine hydrochloride
ribamidine
nsc627433
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1,2,4-triazole-3-carboxamidine
CHEBI:134989
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,4-triazole-3-carboximidamide
unii-r3b1994k2e
r3b1994k2e ,
1h-1,2,4-triazole-3-carboximidamide, 1-beta-d-ribofuranosyl-
taribavirin [inn]
1-beta-d-ribofuranosyl-1,2,4-triazole-3-carboximidine
taribavirin [mi]
taribavirin [who-dd]
SCHEMBL40670
CHEMBL2111108
1-beta-d-ribofuranosyl-1h-1,2,4-triazole-3-carboximidamide
DTXSID80894181
HY-10545
taribavirin free base
DB06408
1-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1h-1,2,4-triazole-3-carboximidamide
Q7686009
CS-0002635
R1Y ,
AKOS040742679

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" There were no serious adverse events, and most adverse events were mild."( Pharmacokinetics and safety of viramidine, a prodrug of ribavirin, in healthy volunteers.
Lin, CC; Philips, L; Xu, C; Yeh, LT, 2004
)
0.32
" Adverse event rates were similar between groups except for diarrhea (viramidine 29."( Safety and efficacy of viramidine versus ribavirin in ViSER2: randomized, double-blind study in therapy-naive hepatitis C patients.
Chun, E; Gish, RG; Gitlin, N; Halliman, DG; Heise, J; Marcellin, P; Rodriguez-Torres, M, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
"The current study was carried out to evaluate pharmacokinetic profiles of viramidine and ribavirin in patients (n = 8 per dose group) with compensated hepatitis C infection following oral dosing of viramidine (400, 600, or 800 mg bid for 4 weeks)."( Ascending multiple-dose pharmacokinetics of viramidine, a prodrug of ribavirin, in adult subjects with compensated hepatitis C infection.
Aora, S; Gish, R; Lau, D; Lin, CC; Peterson, J; Rossi, S; Teng, A; Xu, C; Yeh, LT, 2005
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
" ribavirin combined with pegylated interferon in patients with chronic hepatitis C (CHC)."( Virological response and safety outcomes in therapy-nai ve patients treated for chronic hepatitis C with taribavirin or ribavirin in combination with pegylated interferon alfa-2a: a randomized, phase 2 study.
Arora, S; Gish, RG; Murphy, B; Nelson, DR; O'Brien, C; Rajender Reddy, K; Xu, Y, 2007
)
0.34

Dosage Studied

Weight-based dosing of taribavirin at 25 mg/kg demonstrates lower rates of hemolytic anemia with comparable rates of sustained virologic response (SVR) A recent Phase II trial investigating early and sustained virological response showed no statistically significant differences between ribavirin 1000/1200 mg and taribAvirin at 800-, 1200-, or 1600-mg dosing.

ExcerptRelevanceReference
" The imidates 4 and 6 differed greatly in solubility and dosing requirements."( Synthesis and antitumor activity of ribavirin imidates. A new facile synthesis of ribavirin amidine (1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride).
Avery, TL; Kini, GD; Robins, RK, 1989
)
0.28
" In a whole body autoradiography study in rats following oral dosing (30 mg/kg) of [14C]ribavirin or [14C]viramidine to monkeys, viramidine produced 32% higher radioactivity in the liver than ribavirin, indicating a better liver-targeting properties."( Viramidine, a prodrug of ribavirin, shows better liver-targeting properties and safety profiles than ribavirin in animals.
Hong, Z; Lin, CC; Vitarella, D; Yeh, LT, 2003
)
0.32
" Rats were dosed orally with 120 mg kg(-1) day(-1) of ribavirin and viramidine and 2000 mg kg(-1) day(-1) of levovirin for 8 days."( Effect of ribavirin, levovirin and viramidine on liver toxicological gene expression in rats.
Fang, C; Lin, CC; Srivastava, P,
)
0.13
" Viramidine dosing yielded 50% higher ribavirin levels in the monkey liver but only half in plasma and red blood cells compared to ribavirin dosing."( Pharmacokinetics and safety of viramidine, a prodrug of ribavirin, in healthy volunteers.
Lin, CC; Philips, L; Xu, C; Yeh, LT, 2004
)
0.32
" In the 1-month study in rats, viramidine or ribavirin dosing at 120 mg/kg/day reduced Hgb concentrations (12-16% and 13-20% compared to controls, respectively) and caused slight erythroid hyperplasia in the bone marrow."( Viramidine demonstrates better safety than ribavirin in monkeys but not rats.
Dadgostari, S; Lin, CC; Vitarella, D; Xu, C; Yeh, LT, 2004
)
0.32
"The current study was carried out to evaluate pharmacokinetic profiles of viramidine and ribavirin in patients (n = 8 per dose group) with compensated hepatitis C infection following oral dosing of viramidine (400, 600, or 800 mg bid for 4 weeks)."( Ascending multiple-dose pharmacokinetics of viramidine, a prodrug of ribavirin, in adult subjects with compensated hepatitis C infection.
Aora, S; Gish, R; Lau, D; Lin, CC; Peterson, J; Rossi, S; Teng, A; Xu, C; Yeh, LT, 2005
)
0.33
" The method has been used to simultaneously determine the total concentrations of ribavirin and viramidine in monkey RBC following 5, 15, and 36 weeks dosing of viramidine or ribavirin (60 mg/kg)."( LC-MS/MS method for simultaneous determination of viramidine and ribavirin levels in monkey red blood cells.
Bu, W; Dadgostari, S; Lin, CC; Nguyen, M; Yeh, LT, 2007
)
0.34
" A recent Phase II trial investigating early and sustained virological response showed no statistically significant differences between ribavirin 1000/1200 mg and taribavirin at 800-, 1200-, or 1600-mg dosing, while illustrating a lesser degree of anemia in 800- and 1200-mg dosing of taribavirin."( Taribavirin for the treatment of chronic hepatitis C.
Kearney, KR; Navarro, VJ; Thornton, JJ, 2008
)
0.35
" These results suggest fixed-dose VRD given 600 mg BID is insufficient to treat patients with chronic hepatitis C; a weight-based dosing trial of viramidine is currently under way."( A phase III study of the safety and efficacy of viramidine versus ribavirin in treatment-naïve patients with chronic hepatitis C: ViSER1 results.
Afdhal, NH; Benhamou, Y; Chun, E; Halliman, DG; Heise, J; Nelson, DR; Pockros, PJ; Shiffman, ML, 2009
)
0.35
" Determination of a viramidine dosage that would yield superior efficacy over ribavirin is needed."( Safety and efficacy of viramidine versus ribavirin in ViSER2: randomized, double-blind study in therapy-naive hepatitis C patients.
Chun, E; Gish, RG; Gitlin, N; Halliman, DG; Heise, J; Marcellin, P; Rodriguez-Torres, M, 2010
)
0.36
" The study aimed to determine if weight-based dosing of taribavirin (TBV), an oral prodrug of ribavirin (RBV), demonstrated efficacy comparable to RBV while maintaining its previously demonstrated anemia advantage with fixed dose administration."( Virologic response rates of weight-based taribavirin versus ribavirin in treatment-naive patients with genotype 1 chronic hepatitis C.
Bacon, BR; Chun, E; Halliman, D; Hammond, J; Hassanein, T; Heise, J; Lawitz, E; Muir, AJ; Poordad, F; Shiffman, ML, 2010
)
0.36
" The literature suggests that weight-based dosing of taribavirin at 25 mg/kg demonstrates lower rates of hemolytic anemia with comparable rates of sustained virologic response (SVR) and is the optimum dose for further studies comparing the efficacy of taribavirin with weight-based dosing of ribavirin."( Taribavirin in the treatment of hepatitis C.
Arora, S; Deming, P, 2011
)
0.37
" The dosing strategy of taribavirin favors concentration within the liver to reduce treatment-limiting rates of anemia but may be insufficient to prevent virologic relapse."( Taribavirin in the treatment of hepatitis C.
Arora, S; Deming, P, 2011
)
0.37
"Therapy-naïve patients with chronic hepatitis C virus (HCV) genotype 1 (G1) were randomised to receive (i) TBV 600 mg BID monotherapy for 4 weeks followed by combination therapy with PIFN [pre-dosing arm (n = 23)] or (ii) TBV administered concurrently with PIFN [standard dosing arm (n = 19)]."( Randomised clinical trial: pre-dosing with taribavirin before starting pegylated interferon vs. standard combination regimen in treatment-naïve patients with chronic hepatitis C genotype 1.
Palmer, M; Rubin, R; Rustgi, V, 2012
)
0.38
" the standard dosing arm [33% vs."( Randomised clinical trial: pre-dosing with taribavirin before starting pegylated interferon vs. standard combination regimen in treatment-naïve patients with chronic hepatitis C genotype 1.
Palmer, M; Rubin, R; Rustgi, V, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
nucleobase-containing molecular entityAny compound that has a nucleobase as a part.
[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]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID199875Virus rating against rhinovirus type 1A1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Analysis of the in vitro antiviral activity of certain ribonucleosides against parainfluenza virus using a novel computer aided receptor modeling procedure.
AID155596Virus rating against parainfluenza virus type 31989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Analysis of the in vitro antiviral activity of certain ribonucleosides against parainfluenza virus using a novel computer aided receptor modeling procedure.
AID87045Virus rating of against herpes simplex virus type 21989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Analysis of the in vitro antiviral activity of certain ribonucleosides against parainfluenza virus using a novel computer aided receptor modeling procedure.
AID34142Virus rating against adenovirus type 21989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Analysis of the in vitro antiviral activity of certain ribonucleosides against parainfluenza virus using a novel computer aided receptor modeling procedure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (52)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (7.69)18.7374
1990's2 (3.85)18.2507
2000's35 (67.31)29.6817
2010's9 (17.31)24.3611
2020's2 (3.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (12.73%)5.53%
Reviews12 (21.82%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other36 (65.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 2 Comparison of Weight-based Doses of Taribavirin Combined With Peginterferon Alfa-2b Versus Ribavirin Combined With Peginterferon Alfa-2b in Therapy-naïve Patients With Chronic Hepatitis C Virus Genotype 1 Infection [NCT00446134]Phase 2278 participants (Actual)Interventional2007-03-31Completed
Randomized, Double-Blind, Multicenter Study to Compare the Safety and Efficacy of Viramidine to Ribavirin in Treatment-Naive Patients With Chronic Hepatitis C [NCT00230958]Phase 3900 participants Interventional2003-12-31Completed
Analysis of Hepatitis C Viral Kinetics and Viramidine Pharmacokinetics Utilizing Two Treatment Regimens in Therapy-Naive Patients With Chronic Hepatitis C [NCT00305383]Phase 2100 participants Interventional2005-11-30Terminated(stopped due to Dose levels were determined to be subtherapeutic)
Randomized, Double-Blind, Multicenter Study to Compare the Safety and Efficacy of Viramidine to Ribavirin in Treatment-Naive Patients With Chronic Hepatitis C [NCT00093093]Phase 3900 participants Interventional2004-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00446134 (4) [back to overview]Patients With Anemia (Hemoglobin <10 g/dL) Up to Follow-up Week 24
NCT00446134 (4) [back to overview]Relapsers at Follow-Up Visit 24
NCT00446134 (4) [back to overview]Patients With Either Undetectable Serum HCV RNA (<100 Copies/ml) or at Least a 2-log Decrease From Baseline in Serum Hepatitis C Virus (HCV) Ribonucleic Acid (RNA) at Treatment Week 12.
NCT00446134 (4) [back to overview]Patients With Undetected Hepatitis C Virus (HCV) Ribonucleic Acid (RNA) (<100 Copies/mL) at Treatment Week Follow-Up 24

Patients With Anemia (Hemoglobin <10 g/dL) Up to Follow-up Week 24

The primary safety endpoint will be the numbers of patients with hemoglobin <10 g/dL (anemia) at any time during the treatment period. The comparison of anemia rates between taribavirin and ribavirin groups will be carried out using the Fisher's exact test or Chi-square test. The 95% confidence interval of the difference in proportion will be analyzed. (NCT00446134)
Timeframe: Treatment Week Follow-Up 24

InterventionParticipants (Number)
Taribavirin 20 mg/kg/Day11
Taribavirin 25 mg/kg/Day11
Taribavirin 30 mg/kg/Day19
Ribavirin 800 mg/Day23

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Relapsers at Follow-Up Visit 24

Includes patients who had undetectable Hepatitis Virus C (HVC) Ribonucleic Acid (RNA) at their last visit on drug. (NCT00446134)
Timeframe: Follow-Up Week 24

InterventionParticipants (Number)
Taribavirin 20 mg/kg/Day10
Taribavirin 25 mg/kg/Day5
Taribavirin 30 mg/kg/Day3
Ribavirin 800 mg/Day5

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Patients With Either Undetectable Serum HCV RNA (<100 Copies/ml) or at Least a 2-log Decrease From Baseline in Serum Hepatitis C Virus (HCV) Ribonucleic Acid (RNA) at Treatment Week 12.

The primary efficacy endpoint was the numbers of responders at Treatment Week (TW) 12. Responders are defined as patients achieving either viral negativity or a partial response (PR). Viral negativity is defined as <100 copies/mL serum HCV RNA. A PR is defined as < 100 copies/mL serum HCV RNA and at least a 2-log decrease from baseline in serum HCV RNA levels. Responder rates with corresponding 95% confidence intervals were estimated for each treatment group. (NCT00446134)
Timeframe: Treatment Week 12

,,,
InterventionParticipants (Number)
Early Virologic Response (EVR) (less than 100)No EVR (non-responder, Total)Detectable (greater than 100 copies/mL at TW 12)Discontinued (Prior to TW 12)Missing (No value at TW 12)
Ribavirin 800 mg/Day363419150
Taribavirin 20 mg/kg/Day43241770
Taribavirin 25 mg/kg/Day403017121
Taribavirin 30 mg/kg/Day373121100

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Patients With Undetected Hepatitis C Virus (HCV) Ribonucleic Acid (RNA) (<100 Copies/mL) at Treatment Week Follow-Up 24

(NCT00446134)
Timeframe: Treatment Week Follow-Up 24

,,,
InterventionParticipants (Number)
Responder Follow-Up Week 24Non-Responder Follow-Up Week 24Detectable HCV RNA Follow-Up Week 24Discontinued Week Follow-Up Week 24
Ribavirin 800 mg/Day19511437
Taribavirin 20 mg/kg/Day19481434
Taribavirin 25 mg/kg/Day19511536
Taribavirin 30 mg/kg/Day19491633

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