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ru 66647

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Description

telithromycin: a ketolide; semisynthetic derivative of erythromycin with cycling of the C11-12 positions to form a carbamate ring to avoid acquired resistance to macrolides; binds 70S bacterial rRNA, specifically to the 23S part (23S RIBOSOMAL RNA), preventing protein synthesis; [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11693521
CHEMBL ID1215848
MeSH IDM0278119

Synonyms (19)

Synonym
CHEMBL1215848
levviax
telithromycin
191114-48-4
hmr-3647
ru66647
ru-66647
HMS2052B11
MLS001424285
smr000469222
CCG-101183
AKOS016339661
173838-31-8
NC00433
MRF-0000457
mfcd00943561
(1s,2s,5s,7r,8r,9r,11r,13s,14r)-8-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone
(1s,2r,5r,7r,8r,9r,11r,13r,14s)-8-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone
gtpl10878

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Telithromycin was generally well tolerated, with gastro-intestinal adverse events observed most frequently (diarrhea 4/218 [1."( Efficacy and safety of telithromycin in community-acquired pneumonia.
Leroy, B; Matthews, PA; Van Rensburg, DJ, 2002
)
0.31
" Adverse events were generally mild in severity, and no serious drug-related adverse events were reported."( Pharmacokinetics and safety of the ketolide telithromycin in patients with renal impairment.
Barrett, JS; Bhargava, VO; Chapel, S; Hardy, P; Leclerc, V; Leroy, B; Marbury, T; Montay, G; Sack, M; Shi, J; Swan, SK; Vargas, R, 2004
)
0.32
" Most treatment-emergent adverse events were mild to moderate in intensity with most commonly reported adverse events involving the gastrointestinal system."( Clinical and bacteriological efficacy and safety of 5 and 7 day regimens of telithromycin once daily compared with a 10 day regimen of clarithromycin twice daily in patients with mild to moderate community-acquired pneumonia.
Lavin, B; Niederman, MS; Nusrat, R; Patel, M; Tellier, G, 2004
)
0.32
"Telithromycin 800 mg administered once a day for 5 or 7 days was as effective and safe as clarithromycin 500 mg administered twice a day for 10 days in treating patients with CAP caused by common respiratory pathogens, including macrolide-resistant isolates, and pneumococcal bacteraemia."( Clinical and bacteriological efficacy and safety of 5 and 7 day regimens of telithromycin once daily compared with a 10 day regimen of clarithromycin twice daily in patients with mild to moderate community-acquired pneumonia.
Lavin, B; Niederman, MS; Nusrat, R; Patel, M; Tellier, G, 2004
)
0.32
" Overall treatment-emergent adverse events for both drugs (mostly gastrointestinal) were mild to moderate in intensity."( Efficacy and safety of oral telithromycin once daily for 5 days versus moxifloxacin once daily for 10 days in the treatment of acute bacterial rhinosinusitis.
Ferguson, BJ; Guzzetta, RV; Hadley, JA; Spector, SL, 2004
)
0.32
" No serious adverse event related to the study drug was reported."( [Efficacy and safety of telithromycin in the treatment of acute maxillary sinusitis].
Dubreuil, C; Ebbo, D; Goldstein, F, 2005
)
0.33
" In the 430 patients evaluable for safety, the most common drug-related adverse events were diarrhea (8."( Efficacy and safety of telithromycin 800 mg once daily for 7 days in community-acquired pneumonia: an open-label, multicenter study.
Dunbar, LM; Fogarty, CM; Leroy, BP; Patel, TC, 2005
)
0.33
"4%) experienced at least one treatment-related adverse event (P=0."( [Efficacy and safety of extended-release clarithromycin (5-day short-course) vs telithromycin, in acute bacterial exacerbation of chronic bronchitis].
Drugeon, H; Filipecki, J; Goldfarb, G; Léophonte, P; Perronne, C; Vincent-Lacaze, N; Zuck, P, 2005
)
0.33
" No treatment-related serious adverse events were observed."( [Efficacy and safety of telithromycin in the treatment of acute exacerbation of chronic obstructive pulmonary disease].
Benhamou, D; Piperno, D; Tremolieres, F; Zuck, P, 2005
)
0.33
" This drug interaction-determined as probable according to the Naranjo adverse drug reaction probability scale-may be mediated by P-glycoprotein."( Telithromycin-induced digoxin toxicity and electrocardiographic changes.
Laberge, P; Nenciu, LM; Thirion, DJ, 2006
)
0.33
"We conducted a spontaneous-report case-control study of hepatotoxicity in telithromycin recipients using reports from the US FDA Adverse Event Reporting System."( Telithromycin use and spontaneous reports of hepatotoxicity.
DiBello, JR; Dore, DD; Lapane, KL, 2007
)
0.34
"Based on the Adverse Events Reporting System (AERS) database of the Food and Drug Administration, 4 DMAs, including the reporting odds ratio (ROR), the proportional reporting ratio (PRR), the information component (IC), and the Gamma Poisson Shrinker (GPS), were applied to examine the association between the reporting of hepatotoxicity and the use of telithromycin."( Risk of hepatotoxicity associated with the use of telithromycin: a signal detection using data mining algorithms.
Chen, Y; Guo, JJ; Healy, DP; Lin, X; Patel, NC, 2008
)
0.35
" In addition, further observational studies are required to evaluate the utility of signal detection systems for early recognition of serious, life-threatening, low-frequency drug-induced adverse events."( Risk of hepatotoxicity associated with the use of telithromycin: a signal detection using data mining algorithms.
Chen, Y; Guo, JJ; Healy, DP; Lin, X; Patel, NC, 2008
)
0.35
" To address these reports, an ad hoc group with expertise in spontaneous adverse events reporting and experience in evaluating drug-induced liver injury was formed, including members of the FDA, other federal agencies, and academia."( Telithromycin-associated hepatotoxicity: Clinical spectrum and causality assessment of 42 cases.
Avigan, M; Brinker, AD; Lee, WM; Lyndly, J; Seeff, LB; Serrano, J; Wassel, RT, 2009
)
0.35
" In early 2014, we reviewed its adverse effect profile using data from periodic safety update reports, drug regulatory agencies, and detailed published case reports."( Telithromycin: review of adverse effects.
, 2014
)
0.4

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacodynamic properties of a novel ketolide (a new class of macrolide), HMR 3647, were investigated by studying time-kill kinetics and postantibiotic effect (PAE)."( Pharmacodynamic properties of HMR 3647, a novel ketolide, on respiratory pathogens, enterococci and Bacteroides fragilis demonstrated by studies of time-kill kinetics and postantibiotic effect.
Andrews, JM; Boswell, FJ; Wise, R, 1998
)
0.3
" Blood, saliva and faecal specimens were collected at defined intervals before, during and after administration for pharmacokinetic and microbiological analyses."( Pharmacokinetics and comparative effects of telithromycin (HMR 3647) and clarithromycin on the oropharyngeal and intestinal microflora.
Alván, G; Barkholt, L; Edlund, C; Nord, CE; Vacheron, F, 2000
)
0.31
" The aim of the present study was to investigate different basic pharmacodynamic properties of this new compound."( Pharmacodynamics of telithromycin In vitro against respiratory tract pathogens.
Cars, O; Löwdin, E; Odenholt, I, 2001
)
0.31
" Blood and urine samples were taken throughout the study for determination of pharmacokinetic parameters for telithromycin and RU 76363, its main metabolite."( Pharmacokinetics of the new ketolide telithromycin (HMR 3647) administered in ascending single and multiple doses.
Lenfant, B; Namour, F; Pascual, MH; Reynolds, D; Sultan, E; Wessels, DH, 2001
)
0.31
"The pharmacodynamic properties of the ketolides HMR 3647 (telithromycin) and HMR 3004 were studied against Helicobacter pylori."( In vitro pharmacodynamic studies of activities of ketolides HMR 3647 (Telithromycin) and HMR 3004 against extracellular or intracellular Helicobacter pylori.
Cars, O; Engstrand, L; Gustafsson, I, 2001
)
0.31
" Pharmacokinetic and pharmacodynamic profiling of antimicrobial agents is increasingly being used to select the most appropriate treatment and dosage schedules for RTIs."( Pharmacodynamic and pharmacokinetic considerations in antimicrobial selection: focus on telithromycin.
Drusano, G, 2001
)
0.31
" Neither microbiologic activity nor antibacterial pharmacokinetic data alone can adequately describe the complex interaction between pathogen, host and antibacterial during the disease process."( Predicting antibacterial response from pharmacodynamic and pharmacokinetic profiles.
Nicolau, DP, 2001
)
0.31
" Neither microbiological nor pharmacokinetic (PK) data alone can determine whether a drug is suitable for short-duration therapy."( Pharmacodynamic rationale for short-duration antibacterial therapy.
Nicolau, DP, 2002
)
0.31
" The plasma concentrations and pharmacokinetic parameters of telithromycin and its major metabolite, RU 76363, were determined."( Pharmacokinetics and absolute oral bioavailability of an 800-mg oral dose of telithromycin in healthy young and elderly volunteers.
Lenfant, B; Montay, G; Perret, C; Scholtz, HE; Sultan, E; Weinling, E; Wessels, DH, 2002
)
0.31
"The pharmacokinetic profiles of single and repeated oral doses of telithromycin 800 mg/day were compared in patients with hepatic impairment and healthy subjects in two open-label, non-randomized, parallel-group, multicentre studies."( Pharmacokinetics of the ketolide telithromycin after single and repeated doses in patients with hepatic impairment.
Batista, I; Bhargava, V; Cantalloube, C; Montay, G; Sultan, E; Vacheron, F, 2003
)
0.32
", minimum inhibitory concentrations [MICs]) with the pharmacokinetic profile."( Optimizing outcomes with antimicrobial therapy through pharmacodynamic profiling.
Nicolau, DP, 2003
)
0.32
" Therapeutic drug monitoring and quantitative assessment of antibacterial potency are not always feasible in daily practice, but the pharmacodynamic profiles of antibacterials - which integrate pharmacokinetic profiles and microbiological properties - can be used to predict clinical success."( Clinical use of antimicrobial pharmacodynamic profiles to optimise treatment outcomes in community-acquired bacterial respiratory tract infections: application to telithromycin.
Nicolau, DP, 2004
)
0.32
" Only subjects with a single pathogen isolated at baseline, a telithromycin MIC determination and at least one plasma pharmacokinetic sample were included."( Pharmacodynamic analysis of the microbiological efficacy of telithromycin in patients with community-acquired pneumonia.
Barrett, JS; Chapel, S; Howard, D; Jenkins, SG; Pfister, M; Port, RE; Shi, J, 2005
)
0.33
"To determine whether coadministration of the cytochrome P450 3A4 (CYP3A4) inhibitors itraconazole or grapefruit juice will modify the pharmacokinetic profile of telithromycin, and to assess the safety of telithromycin."( Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin.
Bhargava, VO; Leroy, B; Montay, G; Shi, J, 2005
)
0.33
"Standard pharmacokinetic and safety measurements were performed."( Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin.
Bhargava, VO; Leroy, B; Montay, G; Shi, J, 2005
)
0.33
"The present study, using an in vitro model, assessed telithromycin pharmacodynamic activity at simulated clinically achievable free-drug concentrations in serum (S) and epithelial lining fluid (ELF) against efflux (mefE)-producing macrolide-resistant Streptococcus pneumoniae."( Pharmacodynamic activity of telithromycin at simulated clinically achievable free-drug concentrations in serum and epithelial lining fluid against efflux (mefE)-producing macrolide-resistant Streptococcus pneumoniae for which telithromycin MICs vary.
Hisanaga, T; Hoban, DJ; Johanson, C; Laing, N; Wierzbowski, A; Zhanel, GG, 2005
)
0.33
" Pharmacokinetic parameters were determined, and exposure was linked to microbiological outcome using logistic regression analysis."( Pharmacodynamics of an 800-mg dose of telithromycin in patients with community-acquired pneumonia caused by extracellular pathogens.
Bhargava, V; Bryskier, A; Chapel, S; Drusano, GL; Lodise, TP; Nusrat, R; Preston, S; Rangaraju, M, 2005
)
0.33
" The purpose of this article is to review the main pharmacokinetic properties of telithromycin and their application to the treatment of these infections."( Pharmacokinetics of telithromycin: application to dosing in the treatment of community-acquired respiratory tract infections.
Ciervo, CA; Shi, J, 2005
)
0.33
" At the recommended 800 mg once-daily oral dosing regimen, telithromycin reaches a steady-state concentration of approximately 2 microg/mL in plasma and has an elimination half-life of approximately 10 hours."( Pharmacokinetics of telithromycin: application to dosing in the treatment of community-acquired respiratory tract infections.
Ciervo, CA; Shi, J, 2005
)
0.33
"Bronchoscopic microsampling (BMS) is a new technique for repeated sampling of bronchial epithelial lining fluid (ELF) to obtain the pharmacokinetic profile of drugs."( Pharmacokinetics of telithromycin using bronchoscopic microsampling after single and multiple oral doses.
Ishizaka, A; Kikuchi, E; Kikuchi, J; Nishimura, M; Yamazaki, K, 2007
)
0.34
" Hence, the pharmacokinetic parameters of telithromycin were compared after both intravenous and oral administration at a dose of 50 mg/kg to control rats and a rat model of U-ARF."( Effects of acute renal failure on the pharmacokinetics of telithromycin in rats: negligible effects of increase in CYP3A1 on the metabolism of telithromycin.
Lee, JH; Lee, MG, 2007
)
0.34
" To assess this, the pharmacokinetic parameters of telithromycin were compared after intravenous and oral administration (50 mg/kg)."( Effects of Escherichia coli lipopolysaccharide on telithromycin pharmacokinetics in rats: inhibition of metabolism via CYP3A.
Cho, YK; Jung, YS; Kim, YC; Lee, JH; Lee, MG, 2008
)
0.35
" Thus, the pharmacokinetic changes of telithromycin in both models of diabetes mellitus compared with those in the control rats were evaluated."( Telithromycin pharmacokinetics in rat model of diabetes mellitus induced by alloxan or streptozotocin.
Lee, JH; Lee, MG, 2008
)
0.35
"The pharmacokinetic parameters of telithromycin were compared after intravenous and oral administration at a dose of 50mg/kg to control, 24-h KPLPS, and 96-h KPLPS rats."( Time-dependent effects of Klebsiella pneumoniae endotoxin on the telithromycin pharmacokinetics in rats; restoration of the parameters in 96-hour KPLPS rats to the control levels.
Cho, YK; Jung, YS; Kim, YC; Lee, JH; Lee, MG, 2008
)
0.35
" However, in 96-h KPLPS rats, the pharmacokinetic parameters of telithromycin restored fully to those in control rats due to restoration of the protein expression of the hepatic CYP3A subfamily to that in control rats."( Time-dependent effects of Klebsiella pneumoniae endotoxin on the telithromycin pharmacokinetics in rats; restoration of the parameters in 96-hour KPLPS rats to the control levels.
Cho, YK; Jung, YS; Kim, YC; Lee, JH; Lee, MG, 2008
)
0.35
" To clarify this clinically important issue, the present investigation was carried out to measure the pharmacokinetic profile of TEL in the interstitial space fluid (ISF) of skeletal muscle and subcutaneous adipose tissue by means of the microdialysis technique in 10 healthy subjects following repetitive daily doses of 800 mg TEL."( Multiple-dose pharmacokinetics of telithromycin in peripheral soft tissues.
Fille, M; Joukhadar, C; Thallinger, C; Traunmüller, F, 2009
)
0.35
" Plasma concentrations of oxycodone and its oxidative metabolites were measured for 48 hours, and pharmacodynamic effects were evaluated."( Effect of telithromycin on the pharmacokinetics and pharmacodynamics of oral oxycodone.
Grönlund, J; Hagelberg, N; Laine, K; Martikainen, IK; Neuvonen, PJ; Olkkola, KT; Saari, T, 2010
)
0.36
" We constructed physiologically based pharmacokinetic (PBPK) models for 3 nonrenally eliminated drugs (sildenafil, repaglinide, and telithromycin)."( Evaluation of exposure change of nonrenally eliminated drugs in patients with chronic kidney disease using physiologically based pharmacokinetic modeling and simulation.
Abernethy, DR; Arya, V; Atkinson, AJ; Berglund, EG; Grillo, JA; Huang, SM; Lesko, LJ; Pang, KS; Reynolds, KS; Song, P; Sugiyama, Y; Vieira, Mde L; Wu, TC; Zhang, L; Zhao, P; Zheng, JH, 2012
)
0.38
"Clinical pharmacokinetic profiles of clarithromycin and telithromycin in bronchopulmonary sites have not been fully characterized."( Pharmacokinetic modelling of serum and bronchial concentrations for clarithromycin and telithromycin, and site-specific pharmacodynamic simulation for their dosages.
Derendorf, H; Ikawa, K; Kikuchi, E; Kikuchi, J; Morikawa, N; Nishimura, M, 2014
)
0.4
"Previously reported drug concentration data for serum and ELF were simultaneously fitted to a three-compartment pharmacokinetic model using nonmem program."( Pharmacokinetic modelling of serum and bronchial concentrations for clarithromycin and telithromycin, and site-specific pharmacodynamic simulation for their dosages.
Derendorf, H; Ikawa, K; Kikuchi, E; Kikuchi, J; Morikawa, N; Nishimura, M, 2014
)
0.4
" Clarithromycin achieved a ≥ 90% probability of attaining a pharmacodynamic target [AUC/minimum inhibitory concentration (MIC) = 100] in ELF against bacterial isolates for which MICs were ≤0·5 and ≤1 mg/L for twice-daily doses of 250 and 500 mg, respectively."( Pharmacokinetic modelling of serum and bronchial concentrations for clarithromycin and telithromycin, and site-specific pharmacodynamic simulation for their dosages.
Derendorf, H; Ikawa, K; Kikuchi, E; Kikuchi, J; Morikawa, N; Nishimura, M, 2014
)
0.4
"These results should provide a better understanding of the bronchial pharmacokinetics of clarithromycin and telithromycin, while also providing useful information about their dosages for respiratory tract infections based on site-specific pharmacodynamic evaluation."( Pharmacokinetic modelling of serum and bronchial concentrations for clarithromycin and telithromycin, and site-specific pharmacodynamic simulation for their dosages.
Derendorf, H; Ikawa, K; Kikuchi, E; Kikuchi, J; Morikawa, N; Nishimura, M, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
" The same dose protected 100% of infected mice when administered in combination with non-protective doses of atovaquone, clindamycin or sulphadiazine."( Use of ketolides in combination with other drugs to treat experimental toxoplasmosis.
Araujo, FG; Bryskier, A; Khan, AA; Remington, JS, 1998
)
0.3
" In the absence of in vitro TDI data, a PBPK model can be used to incorporate TDI mechanisms based on nonlinear PK data to predict clinical drug-drug interactions."( Predicting drug interaction potential with a physiologically based pharmacokinetic model: a case study of telithromycin, a time-dependent CYP3A inhibitor.
Berglund, EG; Huang, SM; Lesko, LJ; Reynolds, KS; Vieira, ML; Zhang, L; Zhao, P, 2012
)
0.38
"A previous attempt to accurately quantify the increased simvastatin acid exposure due to drug-drug interaction (DDI) with coadministered telithromycin, using a mechanistic static model, substantially underpredicted the magnitude of the area under the plasma concentration-time curve ratio (AUCR) based on reversible inhibition of CYP3A4 and organic anion transporting polypeptide 1B1 (OATP1B1)."( Mechanistic In Vitro Studies Indicate that the Clinical Drug-Drug Interaction between Telithromycin and Simvastatin Acid Is Driven by Time-Dependent Inhibition of CYP3A4 with Minimal Effect on OATP1B1.
Butler, P; Elsby, R; Gill, RU; Hare, V; Neal, H; Outteridge, S; Pearson, C; Plant, K; Riley, RJ, 2019
)
0.51
"The clinical impact of drug-drug interactions based on time-dependent inhibition of cytochrome P450 (CYP) 3A4 has often been overpredicted, likely due to use of improper inhibitor concentration estimates at the enzyme."( Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations.
Artursson, P; Baranczewski, P; Filppula, AM; Mateus, A; Parvizi, R, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
"This two-way, randomized, single-dose, crossover study determined the pharmacokinetics and absolute oral bioavailability of telithromycin in young and elderly healthy subjects."( Pharmacokinetics and absolute oral bioavailability of an 800-mg oral dose of telithromycin in healthy young and elderly volunteers.
Lenfant, B; Montay, G; Perret, C; Scholtz, HE; Sultan, E; Weinling, E; Wessels, DH, 2002
)
0.31
" Absolute oral bioavailability was calculated using the area under the plasma concentration-time curve (AUC) from zero hours to infinity."( Pharmacokinetics and absolute oral bioavailability of an 800-mg oral dose of telithromycin in healthy young and elderly volunteers.
Lenfant, B; Montay, G; Perret, C; Scholtz, HE; Sultan, E; Weinling, E; Wessels, DH, 2002
)
0.31
"The absolute oral bioavailability of telithromycin was 57% in both young and elderly subjects."( Pharmacokinetics and absolute oral bioavailability of an 800-mg oral dose of telithromycin in healthy young and elderly volunteers.
Lenfant, B; Montay, G; Perret, C; Scholtz, HE; Sultan, E; Weinling, E; Wessels, DH, 2002
)
0.31
"Telithromycin has an absolute oral bioavailability of 57% in young and elderly subjects and is well tolerated."( Pharmacokinetics and absolute oral bioavailability of an 800-mg oral dose of telithromycin in healthy young and elderly volunteers.
Lenfant, B; Montay, G; Perret, C; Scholtz, HE; Sultan, E; Weinling, E; Wessels, DH, 2002
)
0.31
" This study assessed the effect of food on the bioavailability of a single oral dose of telithromycin 800 mg in healthy male subjects."( Lack of effect of food on the bioavailability of a new ketolide antibacterial, telithromycin.
Bhargava, V; Lenfant, B; Montay, G; Pascual, MH; Perret, C; Sultan, E, 2002
)
0.31
" Its absolute bioavailability is 57% and is unaffected by food."( Clinical pharmacokinetics of telithromycin, the first ketolide antibacterial.
Bhargava, VO; Montay, G; Shi, J, 2005
)
0.33
"The absolute oral bioavailability of telithromycin is approximately 57%, which is unaffected by food intake."( Pharmacokinetics of telithromycin: application to dosing in the treatment of community-acquired respiratory tract infections.
Ciervo, CA; Shi, J, 2005
)
0.33
" Combined with an advantageous pharmacokinetic profile (good oral bioavailability and penetration in the respiratory tract tissues and fluids; prolonged half-life allowing for once-a-day administration), these antimicrobial properties make ketolides an attractive alternative for the treatment of severe respiratory tract infections such as pneumonia in areas with significant resistance to conventional macrolides."( Ketolides: pharmacological profile and rational positioning in the treatment of respiratory tract infections.
Harms, JM; Tulkens, PM; Van Bambeke, F; Van Laethem, Y, 2008
)
0.35
"The aim of this study was to compare the roles of gastrointestinal absorption and hepatic extraction as barriers to oral bioavailability for macrolide antibiotics erythromycin, clarithromycin, roxithromycin and telithromycin."( Investigating the barriers to bioavailability of macrolide antibiotics in the rat.
Bencetić Mihaljević, V; Letfus, V; Milić, A; Padovan, J; Ralić, J, 2012
)
0.38
"Population mean parameters for clarithromycin were as follows: distribution volumes of central, peripheral and ELF compartments (V1 /F, V2 /F and V3 /F) = 204·7, 168·9 and 67·1 L; clearance (CL/F) = 34·4 L/h; absorption rate constant (Ka ) = 0·680 1/h; transfer rate constants connecting compartments (K12 , K21 , K13 and K31  = 0·0193, 0·434, 0·667 and 0·260 1/h, respectively)."( Pharmacokinetic modelling of serum and bronchial concentrations for clarithromycin and telithromycin, and site-specific pharmacodynamic simulation for their dosages.
Derendorf, H; Ikawa, K; Kikuchi, E; Kikuchi, J; Morikawa, N; Nishimura, M, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" A dosage of 100 mg of HMR 3647 per kg of body weight per day administered for 10 days protected 50% of mice infected with tachyzoites."( The ketolide antibiotics HMR 3647 and HMR 3004 are active against Toxoplasma gondii in vitro and in murine models of infection.
Araujo, FG; Bryskier, A; Khan, AA; Remington, JS; Slifer, TL, 1997
)
0.3
" This randomized, three-period crossover study determined the dose proportionality of telithromycin pharmacokinetics after single and multiple dosing in healthy subjects."( Pharmacokinetics of the new ketolide telithromycin (HMR 3647) administered in ascending single and multiple doses.
Lenfant, B; Namour, F; Pascual, MH; Reynolds, D; Sultan, E; Wessels, DH, 2001
)
0.31
" At the recommended dosage of 800 mg orally once daily, telithromycin reaches maximal plasma concentrations of about 2 mg/L."( Telithromycin.
Balfour, JA; Figgitt, DP, 2001
)
0.31
" Pharmacokinetic and pharmacodynamic profiling of antimicrobial agents is increasingly being used to select the most appropriate treatment and dosage schedules for RTIs."( Pharmacodynamic and pharmacokinetic considerations in antimicrobial selection: focus on telithromycin.
Drusano, G, 2001
)
0.31
" The concentration of telithromycin in alveolar macrophages markedly exceeded that in plasma, reaching up to 146 times the concentration in plasma 8 h after dosing (median concentration, 81 mg/liter)."( Bronchopulmonary disposition of the ketolide telithromycin (HMR 3647).
Andremont, A; Brunner, F; Cantalloube, C; Gia, HP; Lemaitre, F; Muller-Serieys, C; Soler, P, 2001
)
0.31
" Similar clinical and microbiologic efficacy has been demonstrated with oral dosing in comparative clinical trials for community-acquired pneumonia, acute sinusitis, acute exacerbations of chronic bronchitis, and pharyngitis."( Telithromycin: an oral ketolide for respiratory infections.
Bearden, DT; Garey, KW; Neuhauser, MM, 2001
)
0.31
" Time above MIC (T(MIC)) is therefore the parameter that best correlates with clinical efficacy for these agents and that, in turn, necessitates multiple daily dosing to optimize the duration of exposure."( Predicting antibacterial response from pharmacodynamic and pharmacokinetic profiles.
Nicolau, DP, 2001
)
0.31
" The results of these studies demonstrate that telithromycin, at a dosage of 800 mg once daily, is an effective, well-tolerated agent for the treatment of the most commonly encountered community-acquired RTIs."( Clinical management of respiratory tract infections in the community: experience with telithromycin.
Quintiliani, R, 2001
)
0.31
" Telithromycin's pharmacokinetics permit once-daily dosing for abbreviated periods and good distribution into lung tissue and phagocytic cells."( Telithromycin: the first of the ketolides.
Amsden, GW; Shain, CS, 2002
)
0.31
" Pharmacodynamics (PD) seeks to integrate PK and microbiological data into models that can then be used to predict clinical outcomes and to guide rational dosing strategies."( Pharmacodynamic rationale for short-duration antibacterial therapy.
Nicolau, DP, 2002
)
0.31
" Tonsillar and plasma concentrations exceeded the MIC(50) for GABHS throughout the 24-h dosing period."( Telithromycin (HMR 3647) achieves high and sustained concentrations in tonsils of patients undergoing tonsillectomy.
Attal, P; Danon, J; Gehanno, P; Nabet, P; Passot, V; Romanet, P; Sultan, E, 2003
)
0.32
" A once-daily dose of telithromycin 800 mg rapidly achieves high concentrations in both plasma and respiratory tissues and fluids and is maintained at effective levels throughout the 24-hour dosing period."( Telithromycin: the first ketolide antibacterial for the treatment of community-acquired respiratory tract infections.
Lorenz, J,
)
0.13
" Exposure to telithromycin was comparable in patients with hepatic impairment and healthy subjects and thus, no dosage adjustment is required in this patient group providing renal function is not severely impaired."( Pharmacokinetics of the ketolide telithromycin after single and repeated doses in patients with hepatic impairment.
Batista, I; Bhargava, V; Cantalloube, C; Montay, G; Sultan, E; Vacheron, F, 2003
)
0.32
" The low MICs for many strains as well as the PAE and PA-SME demonstrated in this study for telithromycin show promise for increasing the dosing interval of this ketolide, but will need verification by pharmacokinetic/pharmacodynamic and clinical studies."( Telithromycin post-antibiotic and post-antibiotic sub-MIC effects for 10 Gram-positive cocci.
Appelbaum, PC; Bajaksouzian, S; Jacobs, MR, 2003
)
0.32
"The pharmacokinetics and safety of the ketolide telithromycin were evaluated in two separate studies after single and repeat oral dosing in patients with varying degrees of renal impairment and in subjects with normal renal function."( Pharmacokinetics and safety of the ketolide telithromycin in patients with renal impairment.
Barrett, JS; Bhargava, VO; Chapel, S; Hardy, P; Leclerc, V; Leroy, B; Marbury, T; Montay, G; Sack, M; Shi, J; Swan, SK; Vargas, R, 2004
)
0.32
" It has a broad in vitro spectrum versus usual respiratory pathogens and oral once-daily dosing that increases patient compliance."( Telithromycin.
Spiers, KM; Zervos, MJ, 2004
)
0.32
" These data suggest that telithromycin provides effective first-line therapy for use in patients with acute maxillary sinusitis in a short and convenient once-daily dosage regimen."( Bacteriological efficacy of 5-day therapy with telithromycin in acute maxillary sinusitis.
Buchanan, P; Leroy, B; Rangaraju, M; Roos, K; Tellier, G, 2005
)
0.33
"The pharmacology, mechanisms of resistance, in vitro activity, clinical efficacy, pharmacokinetics, indications, adverse effects, dosage and administration, and place in therapy of telithromycin in the treatment of respiratory infections are reviewed."( Telithromycin: the first ketolide for the treatment of respiratory infections.
Acharya, PS; Kasbekar, N, 2005
)
0.33
" Telithromycin is 60-70% bound to serum proteins and has extensive diffusion into a range of target biological tissues, achieving concentrations above its minimum inhibitory concentration (MIC) against key respiratory pathogens throughout the dosing interval."( Clinical pharmacokinetics of telithromycin, the first ketolide antibacterial.
Bhargava, VO; Montay, G; Shi, J, 2005
)
0.33
" It is expected that TEL can become an oral antibiotic recommended for treatment of gonococcus if dosage and administration are considered."( [In vitro antibacterial activities of telithromycin against clinical isolates of Neisseria gonorrhoeae].
Arai, S; Matsumoto, T; Muratani, T, 2005
)
0.33
" Telithromycin is dosed at 800 mg (two 400-mg tablets) QD in community-acquired respiratory tract infections (RTIs)."( Telithromycin: the first ketolide antimicrobial.
Chung, EP; Nguyen, M, 2005
)
0.33
" At the recommended 800 mg once-daily oral dosing regimen, telithromycin reaches a steady-state concentration of approximately 2 microg/mL in plasma and has an elimination half-life of approximately 10 hours."( Pharmacokinetics of telithromycin: application to dosing in the treatment of community-acquired respiratory tract infections.
Ciervo, CA; Shi, J, 2005
)
0.33
"The aim of this study was to evaluate the clinical efficacy of telithromycin administered for 5 days at a dosage of 800 mg/day, in patients with acute exacerbation of chronic obstructive pulmonary disease (AECOPD) presenting with at least 2 of Anthonisen's criteria including the increase of purulence."( [Efficacy and safety of telithromycin in the treatment of acute exacerbation of chronic obstructive pulmonary disease].
Benhamou, D; Piperno, D; Tremolieres, F; Zuck, P, 2005
)
0.33
" The 3 PD parameters commonly used to predict antibiotic efficacy are (1) the ratio of maximum serum concentration to the minimum inhibitory concentration (MIC) (C(max)/MIC); (2) the ratio of the area under the plasma concentration versus time curve (AUC) versus MIC (AUC/MIC) and (3) the duration of the dosing interval that plasma concentrations exceed the MIC (T>MIC)."( Pharmacodynamics: relation to antimicrobial resistance.
Rybak, MJ, 2006
)
0.33
" The proposed method allows the quantitation of telithromycin in pharmaceutical dosage form and can be used for drug analysis in routine quality control."( Microbiological assay for the determination of telithromycin in tablets.
Breier, AR; Schapoval, EE; Vaucher, LC,
)
0.13
"Clarithromycin is commonly dosed for 7 or more days in patients with acute bacterial exacerbation of chronic bronchitis (ABECB)."( Role for 5-day, once-daily extended-release clarithromycin in acute bacterial exacerbation of chronic bronchitis.
Busman, TA; Gotfried, M; Norris, S; Notario, GF, 2007
)
0.34
" The advantages of lower antimicrobial resistance rates, once-daily short-duration dosing and reported lower health-care costs make oral telithromycin a useful option for the empiric management of mild-to-moderate RTIs."( Telithromycin versus clarithromycin for the treatment of community-acquired respiratory tract infections: a meta-analysis of randomized controlled trials.
Jin, YH; Li, XM; Wang, FC; Yang, F, 2013
)
0.39
"To evaluate the efficacy and safety of short-course versus longer-course treatment with the same antibiotic at the same daily dosage for CAP in non-hospitalised adolescents and adults (outpatients)."( Short-course versus long-course therapy of the same antibiotic for community-acquired pneumonia in adolescent and adult outpatients.
Azcoaga-Lorenzo, A; Casanova-Colominas, J; Gómez-García, M; Heras-Mosteiro, J; Hernandez Santiago, V; López-Alcalde, J; Marin-Cañada, J; Molero García, JM; Muñoz-Gutiérrez, J; Redondo-Sánchez, J; Rodriguez-Barrientos, R; Rodríguez-Fernández, C, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
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 (590)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's40 (6.78)18.2507
2000's472 (80.00)29.6817
2010's72 (12.20)24.3611
2020's6 (1.02)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.60

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 Index8.60 (24.57)
Research Supply Index6.50 (2.92)
Research Growth Index5.10 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials57 (9.39%)5.53%
Reviews85 (14.00%)6.00%
Case Studies24 (3.95%)4.05%
Observational0 (0.00%)0.25%
Other441 (72.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]