Page last updated: 2024-11-06

ljc 10627

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Description

biapenem: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

biapenem : A carbapenem antibiotic in which the azetidine and pyrroline rings carry 1-hydroxymethyl and pyrazolo[1,2-a][1,2,4]triazolium-6-ylthio substituents respectively. [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]

Cross-References

ID SourceID
PubMed CID71339
CHEMBL ID285347
CHEBI ID3089
SCHEMBL ID49242
MeSH IDM0179483

Synonyms (64)

Synonym
L627 ,
omegacin
l-627
cl-186815
ljc-10627
biapenem
120410-24-4
D01057
biapenem (jan/usan/inn)
omegacin (tn)
(4r,5s,6s)-3-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylthio)-6-[(1r)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
(6s)-2-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylsulfanyl)-6-[(1r)-1-hydroxyethyl]-1beta-methyl-2,3-didehydro-1-carbapenam-3-carboxylate
CHEBI:3089 ,
cli 86815
biapenem [usan:inn]
cl 186,815
ljc10,627
l 627
lj c10,627
ljc 10627
6-(((4r,5s,6s)-2-carboxy-6-((1r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo(3.2.0)hept-2-en-3-yl)thio)-6,7-dihydro-5h-pyrazolo(1,2-a)-s-triazol-4-ium hydroxide, inner salt
CHEMBL285347
lj-c10627
(4r,5s,6s)-3-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylsulfanyl)-6-[(1r)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
(4r,5s,6s)-3-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylthio)-6-((r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
A804499
cas-120410-24-4
dtxcid3026435
tox21_112180
dtxsid5046435 ,
rpx2003
biapenern
yr5u3l9zh1 ,
unii-yr5u3l9zh1
S1370
biapenem [who-dd]
biapenem [jan]
6-(((4r,5s,6s)-2-carboxy-6-((1r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo(3.2.0)hept-2-en-3-yl)thio)-6,7-dihydro-5h-pyrazolo(1,2-a)(1,2,4)triazol-4-ium inner salt
5h-pyrazolo(1,2-a)(1,2,4)triazol-4-ium, 6-((2-carboxy-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo(3.2.0)hept-2-en-3-yl)thio)-6,7-dihydro-, hydroxide, inner salt, (4r-(4.alpha.,5.beta.,6.beta.(r*)))-
biapenem [mi]
6-[[(4r,5s,6s)-2-carboxy-6-[(1r)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]thio]-6,7-dihydro-5h-pyrazolo[1,2-a]-s-triazol-4-ium hydroxide, inner salt
biapenem [inn]
biapenem [mart.]
biapenem [usan]
CS-2071
HY-13573
SCHEMBL49242
NCGC00164551-02
AKOS025149478
Q-101421
(4r,5s,6s)-3-((6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-yl)thio)-6-((r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
mfcd00864863
bipenem
biapenem, >=98% (hplc)
DB13028
(4r,5s,6s)-3-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylthio)-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
Q4902548
ljc10627
AS-14655
EX-A4945
CCG-268031
NCGC00164551-05
biapenem;(4r,5s,6s)-3-(6,7-dihydro-5h-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylthio)-6-((r)-1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
gtpl12022

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" As for the safety, a decrease in the WBC count and slight elevation of GOT and GPT were observed in 1 case as abnormal changes in the laboratory tests results, only incidence of side effect observed was the eruption in 1 case."( [Studies on the efficacy and safety of biapenem (L-627) against infections in pediatrics].
Haruta, T; Kobayashi, Y; Kuroki, S; Nikami, H; Nishio, T; Ohkura, K, 1994
)
0.29
" It is believed that biapenem (300 mg once to three times a day), even when taken by elderly people, does not accumulate and that the dosage is safe and appropriate."( Evaluation of the efficacy and safety of biapenem against pneumonia in the elderly and a study on its pharmacokinetics.
Deguchi, N; Ikawa, K; Isobe, T; Kanda, H; Karino, F; Kondo, K; Kuraki, T; Morikawa, N; Moriyama, H; Nishimura, N; Ohe, M; Tada, M, 2013
)
0.39
" Biapenem was effective in 22 of 25 patients, as assessed by the improvement in clinical symptoms and/or the eradication of the causative organisms, and caused no serious adverse events."( The efficacy, safety, and pharmacokinetics of biapenem administered thrice daily for the treatment of pneumonia in the elderly.
Betsuyaku, T; Hasegawa, N; Hayashi, T; Ishii, M; Iwata, S; Kameyama, Y; Kanayama, A; Kaneko, H; Kawashima, C; Kizu, J; Kobayashi, I; Maezawa, K; Nakayama, S; Namkoong, H; Sandoh, M; Sato, Y; Tasaka, S; Terajima, T; Yasuda, H, 2014
)
0.4
" There was no difference found between the patients with LRTIs, cUTIs, or cIAIs treated with biapenem and comparators, regarding treatment success and adverse events."( Efficacy and safety of biapenem in treatment of infectious disease: a meta-analysis of randomized controlled trials.
Mao, Y; Pei, G; Sun, Y; Wang, T; Yin, W; Zhang, Y, 2016
)
0.43
" Drug-related adverse reactions were seen in 12."( Efficacy and safety of biapenem against lower respiratory tract infections in elderly Chinese patients and optimal dosing regimen based on pharmacokinetic/pharmacodynamic analysis.
Chen, XJ; Chen, YC; Dong, J; Li, WY; Liu, YH; Lu, Y; Sun, YB; Xiong, W; Zhao, YF, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
"Clinical and pharmacokinetic studies were performed on a new carbapenem antibiotic, biapenem (L-627), in children with acute infectious diseases and the results were as follows: 1) Clinical efficacies were evaluated on the intravenous-administration at daily doses of 17-37."( [Clinical studies on and pharmacokinetics of a new carbapenem antibiotic, biapenem (L-627), in the pediatric field].
Kakizaki, Y; Tsushima, N; Yokoyama, M, 1994
)
0.29
" Pharmacokinetic studies Peak plasma concentrations of L-627 were 12."( [Pharmacokinetic, bacteriological and clinical studies on biapenem (L-627) in children].
Abe, T; Hagiwara, N; Kobayashi, M; Kobayashi-Negishi, S; Kondo, Y; Nakayama-Esaki, E; Niimi, R; Nishimura, S; Tajima, T, 1994
)
0.29
"To conduct pharmacokinetic and clinical studies on newly developed L-627 (biapenem) against various infections in pediatrics, a study group was organized and a joint research by 15 institutions and their related hospitals was undertaken."( [Pharmacokinetic and clinical studies with L-627 (biapenem) in the pediatric field. Pediatric study group of L-627].
Chiba, S; Fujii, R; Fujita, K; Inyaku, F; Maruyama, S; Murono, K; Saino, T; Sakata, H; Takahashi, S; Yoshikawa, M, 1994
)
0.29
" Results of a pharmacokinetic study in eight volunteers, 17 patients with variant degrees of renal impairment and in addition 13 haemodialysis patients, both on (n = 8) and off dialysis (n = 5), are reported."( Biapenem pharmacokinetics in healthy volunteers and in patients with impaired renal function.
Fitzen, B; Höffler, D; Koeppe, P, 1997
)
0.3
" Serial blood and urine samples were analyzed for biapenem to obtain key pharmacokinetic parameters by both two-compartment model-dependent and -independent methods."( Pharmacokinetics and safety of a new parenteral carbapenem antibiotic, biapenem (L-627), in elderly subjects.
Kanamaru, M; Kozawa, O; Matsumoto, S; Matsuno, H; Minamoto, M; Nagashima, S; Niida, Y; Niwa, M; Takiguchi, Y; Uematsu, T; Yokokawa, M, 1998
)
0.3
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
"The present study examined the pharmacokinetics of biapenem during continuous venovenous hemodiafiltration (CVVHDF) and assessed the pharmacodynamic exposure, based on a pharmacokinetic model, to consider biapenem dosage adaptation in CVVHDF."( Pharmacokinetic modeling and dosage adaptation of biapenem in Japanese patients during continuous venovenous hemodiafiltration.
Ikawa, K; Ikeda, K; Morikawa, N; Suyama, H, 2008
)
0.35
"To develop a population pharmacokinetic model for biapenem in paediatric patients and to use the parameter estimates to assess pharmacodynamic exposure of common bacterial populations."( Population pharmacokinetics and pharmacodynamics of biapenem in paediatric patients.
Ikawa, K; Ikeda, K; Kobayashi, M; Miki, M; Morikawa, N; Nishimura, S, 2008
)
0.35
" Biapenem regimens of 5 mg/kg q8h and 10 mg/kg q8h provided sufficient pharmacodynamic exposures to Pseudomonas aeruginosa and Streptococcus pneumoniae in most typical patient populations."( Population pharmacokinetics and pharmacodynamics of biapenem in paediatric patients.
Ikawa, K; Ikeda, K; Kobayashi, M; Miki, M; Morikawa, N; Nishimura, S, 2008
)
0.35
" For pharmacokinetic evaluation, antibiotics were subcutaneously administered at 3 hours after the pancreatitis induction."( Pharmacokinetic and pharmacodynamic properties of biapenem, a carbapenem antibiotic, in rat experimental model of severe acute pancreatitis.
Hikida, M; Ito, F; Kataoka, H; Kijima, K; Maebashi, K; Mikami, Y; Muto, Y; Niida, M; Sakakibara, S; Shimizu, A; Suzuki, K; Takata, T; Takeda, K; Unno, M, 2008
)
0.35
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Drug concentration data (108 plasma samples and 105 PF samples) were analysed using population pharmacokinetic modelling."( Pharmacodynamic evaluation of biapenem in peritoneal fluid using population pharmacokinetic modelling and Monte Carlo simulation.
Ikawa, K; Ikeda, K; Morikawa, N; Ohge, H; Sueda, T, 2008
)
0.35
"The present study investigated the pharmacokinetics of meropenem and biapenem in bile and estimated their pharmacodynamic target attainment at the site."( Clinical pharmacokinetics of meropenem and biapenem in bile and dosing considerations for biliary tract infections based on site-specific pharmacodynamic target attainment.
Derendorf, H; Ikawa, K; Ikeda, K; Morikawa, N; Murakami, Y; Nakashima, A; Ohge, H; Sueda, T, 2011
)
0.37
" The changes in the predicted concentrations calculated with the pharmacokinetic-pharmacodynamic (PK-PD) software, which is based on previously reported population pharmacokinetic parameters, and those in the measured concentrations approximately matched."( Evaluation of the efficacy and safety of biapenem against pneumonia in the elderly and a study on its pharmacokinetics.
Deguchi, N; Ikawa, K; Isobe, T; Kanda, H; Karino, F; Kondo, K; Kuraki, T; Morikawa, N; Moriyama, H; Nishimura, N; Ohe, M; Tada, M, 2013
)
0.39
" The pharmacokinetic profile was established based on simulations using a modeling program."( The efficacy, safety, and pharmacokinetics of biapenem administered thrice daily for the treatment of pneumonia in the elderly.
Betsuyaku, T; Hasegawa, N; Hayashi, T; Ishii, M; Iwata, S; Kameyama, Y; Kanayama, A; Kaneko, H; Kawashima, C; Kizu, J; Kobayashi, I; Maezawa, K; Nakayama, S; Namkoong, H; Sandoh, M; Sato, Y; Tasaka, S; Terajima, T; Yasuda, H, 2014
)
0.4
"In this study, a population pharmacokinetic (PPK) model of biapenem in Chinese patients with lower respiratory tract infections (LRTIs) was developed and optimal dosage regimens based on Monte Carlo simulation were proposed."( Optimal dosing regimen of biapenem in Chinese patients with lower respiratory tract infections based on population pharmacokinetic/pharmacodynamic modelling and Monte Carlo simulation.
Chen, X; Chen, Y; Dong, J; Li, W; Liu, Y; Lu, Y; Xiong, W; Zhao, D; Zhao, Y, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
"Biapenem is a carbapenem being developed in combination with RPX7009, a new inhibitor of serine β-lactamases."( In vitro activity of Biapenem plus RPX7009, a carbapenem combined with a serine β-lactamase inhibitor, against anaerobic bacteria.
Citron, DM; Goldstein, EJ; Merriam, CV; Tyrrell, KL, 2013
)
0.39
" RPX7009 is a new boron-based inhibitor of several class A and C β-lactamases and is being developed in combination with biapenem (RPX2003)."( Activity of biapenem (RPX2003) combined with the boronate β-lactamase inhibitor RPX7009 against carbapenem-resistant Enterobacteriaceae.
Livermore, DM; Mushtaq, S, 2013
)
0.39
" SIGNIFICANCE AND IMPACT OF THE STUDY: Drug combination is an effective approach for the treatment of resistant bacterial infection."( In vitro interactions of ambroxol hydrochloride or amlodipine in combination with antibacterial agents against carbapenem-resistant Acinetobacter baumannii.
Li, X; Lu, C; Sun, S; Wang, D; Wang, Y, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" Tebipenem is the active form of tebipenem pivoxil, a novel oral carbapenem antibiotic that has a high level of bioavailability in humans, in addition to the above-mentioned features."( Crystal structures of biapenem and tebipenem complexed with penicillin-binding proteins 2X and 1A from Streptococcus pneumoniae.
Baba, N; Gomi, S; Ohsawa, F; Takeuchi, Y; Watanabe, T; Yamada, M, 2008
)
0.35
"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
", significantly lowered the convulsive threshold of pentylenetetrazol (PTZ) in mice and shifted the dose-response curve of PTZ."( Correlation between in vitro and in vivo models of proconvulsive activity with the carbapenem antibiotics, biapenem, imipenem/cilastatin and meropenem.
Day, IP; Goudie, J; Nishiki, K; Williams, PD, 1995
)
0.29
" Dosage suggestions are made."( Biapenem pharmacokinetics in healthy volunteers and in patients with impaired renal function.
Fitzen, B; Höffler, D; Koeppe, P, 1997
)
0.3
" However, the magnitude of those changes does not necessitate dosage adjustment in elderly patients with normal renal function for their age."( Pharmacokinetics and safety of a new parenteral carbapenem antibiotic, biapenem (L-627), in elderly subjects.
Kanamaru, M; Kozawa, O; Matsumoto, S; Matsuno, H; Minamoto, M; Nagashima, S; Niida, Y; Niwa, M; Takiguchi, Y; Uematsu, T; Yokokawa, M, 1998
)
0.3
"The present study examined the pharmacokinetics of biapenem during continuous venovenous hemodiafiltration (CVVHDF) and assessed the pharmacodynamic exposure, based on a pharmacokinetic model, to consider biapenem dosage adaptation in CVVHDF."( Pharmacokinetic modeling and dosage adaptation of biapenem in Japanese patients during continuous venovenous hemodiafiltration.
Ikawa, K; Ikeda, K; Morikawa, N; Suyama, H, 2008
)
0.35
"These results better define the pharmacokinetics of biapenem and help in the choice of the appropriate dosage regimens for paediatric."( Population pharmacokinetics and pharmacodynamics of biapenem in paediatric patients.
Ikawa, K; Ikeda, K; Kobayashi, M; Miki, M; Morikawa, N; Nishimura, S, 2008
)
0.35
"Recently, PK/PD (pharmacokinetics/pharmacodynamics) analysis for the antimicrobial dosage method became one of the popular categories in chemotherapy and infectious disease societies world wide."( [Analysis on the effective dosage regimens for meropenem, biapenem and doripenem against P. aeruginosa infection based on pharmacokinetics and pharmacodynamics theory].
Kobayashi, Y; Sumitani, Y, 2007
)
0.34
" Thus, these results should support the clinical use of biapenem as a treatment for intra-abdominal infections and facilitate the design of the dosing regimen."( Pharmacodynamic evaluation of biapenem in peritoneal fluid using population pharmacokinetic modelling and Monte Carlo simulation.
Ikawa, K; Ikeda, K; Morikawa, N; Ohge, H; Sueda, T, 2008
)
0.35
"A pharmacokinetic-pharmacodynamic (PK-PD) target attainment analysis to build a dosing strategy for biapenem in adult patients has not been conducted."( Pharmacokinetic-pharmacodynamic target attainment analysis of biapenem in adult patients: a dosing strategy.
Doi, M; Ikawa, K; Ikeda, K; Kuwabara, M; Morikawa, N; Ohge, H; Sueda, T; Suyama, H, 2008
)
0.35
"5-h infusions) achieved a PK-PD target attainment probability of > or =90%, which varied with Cl(cr) of the patient and susceptibility of the tested bacterium; however, higher dosage with prolonged infusion time (600 mg Q8H, 3 h infusion) was required for a high probability against Pseudomonas aeruginosa and Haemophilus influenzae isolates in the case of Cl(cr) = 90 ml/min."( Pharmacokinetic-pharmacodynamic target attainment analysis of biapenem in adult patients: a dosing strategy.
Doi, M; Ikawa, K; Ikeda, K; Kuwabara, M; Morikawa, N; Ohge, H; Sueda, T; Suyama, H, 2008
)
0.35
" In conclusion, a dosing regimen of 300 mg BIPM q8h had a higher probability of therapeutic efficacy than q12h in patients with severe sepsis under CVVHDF."( Pharmacokinetics and pharmacodynamics of biapenem in critically ill patients under continuous venovenous hemodiafiltration.
Fujiue, Y; Ikawa, K; Ikeda, K; Kaneko, K; Kuwabara, M; Morikawa, N; Morikawa, S; Suyama, H; Yamanoue, T, 2008
)
0.35
"Biapenem has been used in pediatric patients as well as adult patients; however, little information is available on dosing regimens for pediatric patients."( [Dosing regimen rationalization of biapenem in pediatric patients: use of Monte Carlo simulation].
Ikawa, K; Kameda, K; Kobayashi, M; Miki, M; Morikawa, N, 2009
)
0.35
" These results help to define the clinical pharmacokinetics of the two carbapenems in bile while also helping to rationalize and optimize the dosing regimens for biliary tract infections based on site-specific pharmacodynamic target attainment."( Clinical pharmacokinetics of meropenem and biapenem in bile and dosing considerations for biliary tract infections based on site-specific pharmacodynamic target attainment.
Derendorf, H; Ikawa, K; Ikeda, K; Morikawa, N; Murakami, Y; Nakashima, A; Ohge, H; Sueda, T, 2011
)
0.37
" It is believed that biapenem (300 mg once to three times a day), even when taken by elderly people, does not accumulate and that the dosage is safe and appropriate."( Evaluation of the efficacy and safety of biapenem against pneumonia in the elderly and a study on its pharmacokinetics.
Deguchi, N; Ikawa, K; Isobe, T; Kanda, H; Karino, F; Kondo, K; Kuraki, T; Morikawa, N; Moriyama, H; Nishimura, N; Ohe, M; Tada, M, 2013
)
0.39
" One of the reasons (carba)penems are seldom used for treatment of TB is the high dosage levels required, often at the therapeutic limits."( Carbapenems and Rifampin Exhibit Synergy against Mycobacterium tuberculosis and Mycobacterium abscessus.
Kaushik, A; Lamichhane, G; Makkar, N; Pandey, P; Parrish, N; Singh, U, 2015
)
0.42
"The present study evaluated the efficacy and safety of biapenem in elderly Chinese patients with lower respiratory tract infections (LRTIs) and proposed optimal dosage regimen on the basis of pharmacokinetic/pharmacodynamic (PK/PD) analysis."( Efficacy and safety of biapenem against lower respiratory tract infections in elderly Chinese patients and optimal dosing regimen based on pharmacokinetic/pharmacodynamic analysis.
Chen, XJ; Chen, YC; Dong, J; Li, WY; Liu, YH; Lu, Y; Sun, YB; Xiong, W; Zhao, YF, 2016
)
0.43
"In this study, a population pharmacokinetic (PPK) model of biapenem in Chinese patients with lower respiratory tract infections (LRTIs) was developed and optimal dosage regimens based on Monte Carlo simulation were proposed."( Optimal dosing regimen of biapenem in Chinese patients with lower respiratory tract infections based on population pharmacokinetic/pharmacodynamic modelling and Monte Carlo simulation.
Chen, X; Chen, Y; Dong, J; Li, W; Liu, Y; Lu, Y; Xiong, W; Zhao, D; Zhao, Y, 2016
)
0.43
" The significance of using drug combination is that it can reduce drug dosage requirements, reduce the toxic effects of agents and prevent or delay the emergence of drug resistance."( In vitro interactions of ambroxol hydrochloride or amlodipine in combination with antibacterial agents against carbapenem-resistant Acinetobacter baumannii.
Li, X; Lu, C; Sun, S; Wang, D; Wang, Y, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
[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 (3)

ClassDescription
carbapenemsThe class of beta-lactam antibiotics that whose members have a carbapenem skeleton which is variously substituted at positions 3, 4, and 6.
pyrazolotriazole
organic sulfideCompounds having the structure RSR (R =/= H). Such compounds were once called thioethers.
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency6.60600.000221.22318,912.5098AID743036; AID743053
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.39140.000214.376460.0339AID720691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-lactamase class B VIM-2 Pseudomonas aeruginosaKm24.70002.00006.65009.4000AID575015
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (102)

Assay IDTitleYearJournalArticle
AID560182T>MIC in healthy human at plasma MIC of 0.5 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225787Antibacterial activity against Klebsiella pneumoniae KP1082 expressing KPC2/SHV-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID285683Antimicrobial activity against Pseudomonas aeruginosa PAO1 with rpoN mutation after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID560172AUC in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225791Antibacterial activity against Klebsiella pneumoniae KP1088 expressing KPC3/SHV-11/TEM-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID560386T>MIC in healthy human at epithelial lining fluid MIC of 0.5 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560383T>MIC in healthy human at epithelial lining fluid MIC of 1 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225790Antibacterial activity against Klebsiella pneumoniae KP1084 expressing KPC3/SHV-11/TEM-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID560183T>MIC in healthy human at plasma MIC of 0.25 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560384T>MIC in healthy human at epithelial lining fluid MIC of 1 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560162Cmax in plasma of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1311365Antibacterial activity against Enterococcus faecalis ATCC 19433 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID285682Antimicrobial activity against wild type Pseudomonas aeruginosa PAO1 after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID1883779Antibacterial activity against Mycobacterium tuberculosis in acute Mtb infection mouse model assessed as reduction in log10 CFU at 200 mg/kg for 3 weeks in presence of Rifampicin2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID560166AUC in plasma of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID560179T>MIC in healthy human at plasma MIC of 1 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID560168Cmax in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225783Antibacterial activity against Klebsiella oxytoca KX1019 expressing KPC2/OXA2 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225782Antibacterial activity against Enterobacter cloacae ECL1058 expressing KPC3/SHV-11/TEM-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225849Antibacterial activity against Klebsiella pneumoniae KP1074 in Swiss webster neutropenic mouse lung infection model assessed as change in log10 CFU in lung at 50 mg/kg, ip administered every 2 hrs starting at 2 hrs postinfection measured after 24 hrs rela2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID438298Inhibition of penicillin-resistant Streptococcus pneumoniae 5204 PBP2X preincubated for 4 hrs before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID560167Cmax in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID767189Antibacterial activity against Pseudomonas aeruginosa PAO1 pMS363 by microbroth dilution method2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Metallo-β-lactamase inhibitory activity of 3-alkyloxy and 3-amino phthalic acid derivatives and their combination effect with carbapenem.
AID560181T>MIC in healthy human at plasma MIC of 0.5 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1883727Half life in mouse2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1225788Antibacterial activity against Klebsiella pneumoniae KP1087 expressing KPC2/CTX-M-15/SHV-11/TEM-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1883778Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 14 days by CLSI protocol based assay in presence of Clavulanic acid2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID575016Ratio of Kcat to Km for Pseudomonas aeruginosa beta-lactamaseVIM-2 by UV spectrophotometric analysis2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
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]
AID1883776Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 14 days by CLSI protocol based assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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]
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1311377Antibacterial activity against Mycobacterium tuberculosis2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
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
AID575013Ratio of Kcat to Km for Pseudomonas aeruginosa beta-lactamase IMP-1 by UV spectrophotometric analysis2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
AID285684Antimicrobial activity against Pseudomonas aeruginosa PAO1 with pvdS mutation after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID560381T>MIC in healthy human at epithelial lining fluid MIC of 2 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560161Cmax in plasma of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560185T>MIC in healthy human at epithelial lining fluid MIC of 4 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560173Drug level in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225785Antibacterial activity against Klebsiella pneumoniae KP1004 expressing KPC2/TEM1/SHV11 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225781Antibacterial activity against Escherichia coli EC1007 expressing KPC3 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID560164Tmax in plasma of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
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]
AID575015Activity of Pseudomonas aeruginosa beta-lactamase VIM-2 by UV spectrophotometric analysis2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
AID560387T>MIC in healthy human at epithelial lining fluid MIC of 0.5 ug/ml and compound dose of 0.3 gm/kg, iv after 0.25 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID560175T>MIC in healthy human at plasma MIC of 4 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID560385T>MIC in healthy human at epithelial lining fluid MIC of 0.5 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560178T>MIC in healthy human at plasma MIC of 2 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560163Tmax in plasma of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID560176T>MIC in healthy human at plasma MIC of 4 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560169Tmax in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560171AUC in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1311364Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID560388T>MIC in healthy human at epithelial lining fluid MIC of 0.25 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225784Antibacterial activity against Klebsiella oxytoca KX1017 expressing KPC2/OXA2/SHV30 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1225786Antibacterial activity against Klebsiella pneumoniae KP1008 expressing KPC2 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID560170Tmax in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID560380T>MIC in healthy human at epithelial lining fluid MIC of 4 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560184T>MIC in healthy human at plasma MIC of 0.25 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID560177T>MIC in healthy human at plasma MIC of 2 ug/ml and compound dose of 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID575012Activity of Pseudomonas aeruginosa beta-lactamase IMP-1 by UV spectrophotometric analysis2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
AID560382T>MIC in healthy human at epithelial lining fluid MIC of 2 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID438297Inhibition of penicillin-sensitive Streptococcus pneumoniae R6 PBP2X preincubated for 1 hr before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID560174Drug level in epithelial lining fluid of healthy human at 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID560165AUC in plasma of healthy human at 0.3 gm/kg, iv after 0.5 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID767190Antibacterial activity against mexAB-deleted Pseudomonas aeruginosa KG5002/pMS363 by microbroth dilution method2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Metallo-β-lactamase inhibitory activity of 3-alkyloxy and 3-amino phthalic acid derivatives and their combination effect with carbapenem.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
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]
AID560180T>MIC in healthy human at plasma MIC of 1 ug/ml and compound dose of 0.3 gm/kg, iv after 3 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Comparison of the pharmacodynamics of biapenem in bronchial epithelial lining fluid in healthy volunteers given half-hour and three-hour intravenous infusions.
AID1225789Antibacterial activity against Klebsiella pneumoniae KP1083 expressing KPC3/SHV-1/TEM-1 by broth microdilution method2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
AID1883777Antibacterial activity against Mycobacterium tuberculosis in acute Mtb infection mouse model assessed as reduction in log10 CFU at 200 mg/kg for 3 weeks2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (169)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's68 (40.24)18.2507
2000's46 (27.22)29.6817
2010's43 (25.44)24.3611
2020's12 (7.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.17

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 Index9.17 (24.57)
Research Supply Index5.34 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials31 (17.61%)5.53%
Reviews6 (3.41%)6.00%
Case Studies4 (2.27%)4.05%
Observational0 (0.00%)0.25%
Other135 (76.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]