Page last updated: 2024-11-10

alatrofloxacin

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

Description

alatrofloxacin: prodrug of trovafloxacin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3086677
CHEMBL ID1201197
CHEBI ID135829
SCHEMBL ID140567
SCHEMBL ID7616277
MeSH IDM0278267

Synonyms (27)

Synonym
l-alaninamide, l-alanyl-n-(3-(6-carboxy-8-(2,4-difluorophenyl)-3-fluoro-5,8-dihydro-5-oxo-1,8-naphthyridin-2-yl)-3-azabicyclo(310)hex-6-yl)-, (1alpha,5alpha,6alpha)-
l-alaninamide, l-alanyl-n-((1alpha,5alpha,6alpha)-3-(6-carboxy-8-(2,4-difluorophenyl)-3-fluoro-5,8-dihydro-5-oxo-1,8-naphthyridin-2-yl)-3-azabicyclo(310)hex-6-yl)-
D07562
alatrofloxacin (inn)
146961-76-4
alatrofloxacin [inn]
alatrofloxacin
CHEBI:135829
7qvv6i50dt ,
unii-7qvv6i50dt
CHEMBL1201197
alatrofloxacin [vandf]
alatrofloxacin [who-dd]
7-((1r,5s,6s)-6-((s)-2-((s)-2-aminopropionamido)propionamido)-3-azabicyclo(3.1.0)hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
SCHEMBL140567
UUZPPAMZDFLUHD-VUJLHGSVSA-N
SCHEMBL7616277
DTXSID4057893
DB09335
157182-32-6
7-[(1r,5s)-6-[[(2s)-2-[[(2s)-2-aminopropanoyl]amino]propanoyl]amino]-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
7-((1r,5s,6s)-6-((s)-2-((s)-2-aminopropanamido)propanamido)-3-azabicyclo[3.1.0]hexan-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
HY-16035
CS-0006126
7-[(1r,5s,6r)-6-[(2s)-2-[(2s)-2-aminopropanamido]propanamido]-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
EN300-19997200
AKOS040745545

Research Excerpts

Overview

Alatrofloxacin is a prodrug that is rapidly hydrolyzed to trovafloxacins in the body.

ExcerptReferenceRelevance
"Alatrofloxacin is a prodrug that is rapidly hydrolyzed to trovafloxacin in the body."( Concentrations of trovafloxacin in colonic tissue and peritoneal fluid after intravenous infusion of the prodrug alatrofloxacin in patients undergoing colorectal surgery.
Dogolo, LC; Melnik, G; Schwesinger, WH; Teng, R; Vincent, J, 1998
)
1.23

Actions

ExcerptReferenceRelevance
"Alatrofloxacin may cause seizures even during slow infusion. "( Alatrofloxacin-induced seizures during slow intravenous infusion.
Melvani, S; Speed, BR, 2000
)
3.19

Toxicity

The most common treatment-related adverse events in studies were nausea, headache, insertion site reaction, and dizziness. In this large patient sample, intravenous alatrofloxacin followed by oral trovafloxacins was safe and well tolerated.

ExcerptReferenceRelevance
" The most common treatment-related adverse events in studies of intravenous alatrofloxacin followed by oral trovafloxacin were nausea, headache, insertion site reaction, and dizziness."( Safety and tolerability of intravenous-to-oral treatment and single-dose intravenous or oral prophylaxis with trovafloxacin.
Hopkins, S; Williams, DJ, 1998
)
0.53
"In this large patient sample, intravenous alatrofloxacin followed by oral trovafloxacin was safe and well tolerated."( Safety and tolerability of intravenous-to-oral treatment and single-dose intravenous or oral prophylaxis with trovafloxacin.
Hopkins, S; Williams, DJ, 1998
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" The elimination half-life (T(1/2)) for trovafloxacin was independent of the dose and the mean T(1/2)s for the 100, 200 and 300 mg equivalent doses of alatrofloxacin were 10."( Pharmacokinetics and safety of trovafloxacin in healthy male volunteers following administration of single intravenous doses of the prodrug, alatrofloxacin.
Baris, BA; Friedman, HL; Polzer, RJ; Teng, R; Venitz, J; Vincent, J; Willavize, SA, 1997
)
0.7
" The primary pharmacokinetic parameters (average +/- SD) analyzed were volume of distribution at steady state (1."( Pharmacokinetics of a fluoronaphthyridone, trovafloxacin (CP 99,219), in infants and children following administration of a single intravenous dose of alatrofloxacin.
Bradley, JS; Capparelli, EV; Kearns, GL; Reed, MD; Vincent, J, 2000
)
0.51

Bioavailability

ExcerptReferenceRelevance
"Two studies determined the oral bioavailability of trovafloxacin (CP-99,219) in healthy volunteers under fasted and fed conditions."( Oral bioavailability of trovafloxacin with and without food in healthy volunteers.
Dogolo, LC; Friedman, HL; Teng, R; Vincent, J; Willavize, SA, 1997
)
0.3
" The mean absolute bioavailability was 91%."( Oral bioavailability and pharmacokinetics of trovafloxacin in patients with AIDS.
Geffken, A; Lacy, MK; Nicolau, DP; Nightingale, CH; Quintiliani, R; Teng, R; Vincent, J, 1999
)
0.3

Dosage Studied

ExcerptRelevanceReference
"A simplified dosing algorithm for trovafloxacin was evaluated following a single-dose infusion of alatrofloxacin at trovafloxacin equivalent doses of 30, 100, 200, 300 and 400 mg (57 subjects), and multiple doses of 200, 300 and 400 mg (30 subjects)."( Single- and multiple-dose administration, dosing regimens, and pharmacokinetics of trovafloxacin and alatrofloxacin in humans.
Baris, BA; Dogolo, L; Teng, R; Vincent, J; Willavize, SA, 1998
)
0.73
"5 microg/ml) of common pediatric bacterial pathogens to trovafloxacin, dosing of 4 mg/kg/day once or twice daily should be appropriate."( Pharmacokinetics of a fluoronaphthyridone, trovafloxacin (CP 99,219), in infants and children following administration of a single intravenous dose of alatrofloxacin.
Bradley, JS; Capparelli, EV; Kearns, GL; Reed, MD; Vincent, J, 2000
)
0.51
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID625293Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (40.00)18.2507
2000's14 (46.67)29.6817
2010's4 (13.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.19

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index30.19 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index35.70 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.19)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (26.67%)5.53%
Reviews1 (3.33%)6.00%
Case Studies3 (10.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]