cilastatin profile

ID Source	ID
PubMed CID	6435415
CHEMBL ID	766
CHEBI ID	3697
SCHEMBL ID	37051
MeSH ID	M0023687

Synonym
BIDD:GT0782
cilastatina
AC-268
cilastatine
(2z)-7-{[(2r)-2-amino-2-carboxyethyl]sulfanyl}-2-({[(1s)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoic acid
cilastatin acid
cilastatin [inn:ban]
cilastatina [spanish]
einecs 279-875-8
cilastatinum [latin]
2-heptenoic acid, 7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyclopropyl)carbonyl)amino)-, (r-(r,s-(z)))-
cilastatine [french]
cilastatin (inn)
D07698
cilastatin ,
C01675
DB01597
(l)-7-(2-amino-2-carboxy-ethylsulfanyl)-2-[(2,2-dimethyl-cyclopropanecarbonyl)-amino]-hept-2-enoic acid
(z)-(s)-6-carboxy-6-[(s)-2,2-dimethylcyclopropanecarboxamido]hex-5-enyl-l-cysteine
(z)-7-((r)-2-amino-2-carboxy-ethylsulfanyl)-2-[((s)-2,2-dimethyl-cyclopropanecarbonyl)-amino]-hept-2-enoic acid
CHEMBL766
chebi:3697 ,
A840230
(z)-7-[(2r)-2-azanyl-3-oxidanyl-3-oxidanylidene-propyl]sulfanyl-2-[[(1s)-2,2-dimethylcyclopropyl]carbonylamino]hept-2-enoic acid
(z)-7-[[(2r)-2-amino-2-carboxyethyl]thio]-2-[[[(1s)-2,2-dimethylcyclopropyl]-oxomethyl]amino]-2-heptenoic acid
mk791
unii-141a6amn38
141a6amn38 ,
AKOS015962144
bdbm50367502
cilastatin [who-dd]
cilastatin [mi]
cilastatin [inn]
cilastatin [vandf]
(2z)-7-{[(2r)-2-amino-2-carboxyethyl]sulfanyl}-2-{[(1s)-2,2-dimethylcyclopropyl]formamido}hept-2-enoic acid
gtpl5166
SCHEMBL37051
DTXSID8048238
2-heptenoic acid, 7-[[(2r)-2-amino-2-carboxyethyl]thio]-2-[[[(1s)-2,2-dimethylcyclopropyl]carbonyl]amino]-, (2z)-
cilastin
sr-01000781260
SR-01000781260-3
(z)-7-(((r)-2-amino-2-carboxyethyl)thio)-2-((s)-2,2-dimethylcyclopropane-1-carboxamido)hept-2-enoic acid
CS-8177
cilastastin
Q418201
HY-A0166
DS-11972
EX-A4954
A16977

Excerpt	Reference	Relevance
" Adverse effects were generally mild and reversible and included diarrhea alone or with vomiting (5."	( Imipenem-cilastatin in pediatric patients: an overview of safety and efficacy in studies conducted in the United States. Ahonkhai, VI; Brown, KR; Cyhan, GM; Wilson, SE, 1989)	0.28
" In the remaining two patients treatment had to be prematurely discontinued due to adverse effects."	( Efficacy and safety of imipenem/cilastatin in the empirical treatment of septicemia. Del Valle, J; Noriega, AR; Otero, JR; Revilla, AP; Sanz, F, 1987)	0.27
" The most common clinical adverse experiences were local ones related to the site of intravenous infusion."	( The safety profile of imipenem/cilastatin: worldwide clinical experience based on 3470 patients. Aziz, M; Brown, KR; Calandra, GB; Wang, C, 1986)	0.27
" No patients experienced drug-related clinical adverse effects."	( Safety and efficacy of imipenem/cilastatin in treatment of complicated urinary tract infections. Corrado, ML; Cox, CE, 1985)	0.27
" Twenty-one patients had no adverse reaction; of the remaining 10 patients, 4 had nausea, 1 had urticaria, and 6 had mild abnormalities in hepatic function; three episodes of diarrhea included two with Clostridium difficile toxin in stool and one with pseudomembranous colitis, as determined by sigmoidoscopy."	( Safety and efficacy of high-dose treatment with imipenem-cilastatin in seriously ill patients. Fisher, MA; Gibson, GA; MacGregor, RR; Zajac, BA, 1985)	0.27
" Because VCM has the adverse reaction of nephrotoxicity, we are apprehensive about using VCM with other antibiotics, which might increase this problem."	( [Nephrotoxicity and drug interaction of vancomycin (2)]. Nakagawa, Y; Toyoguchi, T, 1996)	0.29
" Both VCM and IPM have the adverse reaction of nephrotoxicity, whereas CS restrains the nephrotoxicity of IPM."	( [Nephrotoxicity and drug interaction of vancomycin]. Nakagawa, Y; Toyoguchi, T; Watanabe, H, 1996)	0.29
" The aim of the study was to measure the possible dose-related suppressive effects or elimination by cilastatin of the adverse reactions generated by vancomycin in the kidneys of rabbits."	( Nephrotoxicity of vancomycin and drug interaction study with cilastatin in rabbits. Hosoya, J; Nakagawa, Y; Takahashi, S; Toyoguchi, T; Watanabe, H, 1997)	0.3
" The possibility of administering meropenem in intravenous infusion or bolus injection with lower volumes of fluid, without increasing the incidence of these adverse reactions, may have practical advantages in special situations."	( [Tolerance and safety of carbapenems: the use of meropenem]. Lizasoaín, M; Noriega, AR, 1997)	0.3
" Comparable incidences of adverse events, mainly mild or moderate in intensity, were experienced in each treatment group."	( Treatment of complicated intra-abdominal infections: comparison of the tolerability and safety of intravenous/oral trovafloxacin versus intravenous imipenem/cilastatin switching to oral amoxycillin/clavulanic acid. Luke, DR; Peterson, J, )	0.13
" The incidence, severity and type of adverse events were similar in both treatment groups."	( An open, randomised, multi-centre study comparing the safety and efficacy of sitafloxacin and imipenem/cilastatin in the intravenous treatment of hospitalised patients with pneumonia. Briggs, A; Feldman, C; Flitcroft, A; O'Grady, J; Richards, G; White, H, 2001)	0.31
"719]) were the most frequently reported adverse events."	( The efficacy and safety of tigecycline for the treatment of complicated intra-abdominal infections: analysis of pooled clinical trial data. Babinchak, T; Dartois, N; Ellis-Grosse, E; Loh, E; Rose, GM, 2005)	0.33
"435]) were the most frequently reported adverse events."	( A multicenter trial of the efficacy and safety of tigecycline versus imipenem/cilastatin in patients with complicated intra-abdominal infections [Study ID Numbers: 3074A1-301-WW; ClinicalTrials.gov Identifier: NCT00081744]. Babinchak, T; Campos, M; Ellis-Grosse, EJ; Loh, E; Oliva, ME; Pasternak, J; Rekha, A; Rose, GM; Yellin, A, 2005)	0.33
" Most commonly reported treatment emergent adverse events for tigecycline and imipenem/cilastatin were nausea (14."	( The efficacy and safety of tigecycline for the treatment of complicated intra-abdominal infections - the European experience. Babinchak, T; Castaing, N; Cooper, A; Dartois, N; De Vane, N; Fomin, P; Koalov, S; Tellado, J, 2008)	0.35
" Drug-induced seizures are a rare but serious adverse effect, with carbapenems being one of the most common classes of antibiotics associated with seizures."	( Safety of imipenem/cilastatin in neurocritical care patients. Brophy, GM; Hoffman, J; Trimble, J, 2009)	0.35
" The overall incidence of treatment-emergent adverse events was 80."	( Efficacy and safety of tigecycline monotherapy vs. imipenem/cilastatin in Chinese patients with complicated intra-abdominal infections: a randomized controlled trial. Bi, J; Chen, X; Chen, Z; Cooper, A; Leng, X; Li, R; Liu, D; Ma, X; Maroko, R; Quan, Z; Wei, J; Wu, J; Wu, Z; Yan, L; Yu, Y; Zhang, Y, 2010)	0.36
"Cisplatin is an anticancer agent marred by nephrotoxicity; however, limiting this adverse effect may allow the use of higher doses to improve its efficacy."	( Cilastatin protects against cisplatin-induced nephrotoxicity without compromising its anticancer efficiency in rats. Blanco-Codesido, M; Camano, S; Gomez-Gomez, MM; Humanes, B; Lara, JM; Lazaro, A; Lazaro, JA; Martín-Vasallo, P; Moreno-Gordaliza, E; Ortiz, A; Tejedor, A, 2012)	0.38
" Adverse events were observed in 67."	( Efficacy and safety of ceftazidime-avibactam versus imipenem-cilastatin in the treatment of complicated urinary tract infections, including acute pyelonephritis, in hospitalized adults: results of a prospective, investigator-blinded, randomized study. Duttaroy, DD; González Patzán, LD; Kreidly, Z; Lipka, J; Sable, C; Stricklin, D; Vazquez, JA, 2012)	0.38
" We compared the incidence of adverse events in hospitalized infants receiving meropenem versus imipenem/cilastatin."	( Adverse events associated with meropenem versus imipenem/cilastatin therapy in a large retrospective cohort of hospitalized infants. Benjamin, DK; Capparelli, EV; Clark, RH; Cohen-Wolkowiez, M; Herring, AH; Hornik, CP; Kearns, GL; Smith, PB; van den Anker, J, 2013)	0.39
" Multivariable conditional logistic regression was performed to evaluate the association between carbapenem therapy and adverse events, controlling for infant factors and severity of illness."	( Adverse events associated with meropenem versus imipenem/cilastatin therapy in a large retrospective cohort of hospitalized infants. Benjamin, DK; Capparelli, EV; Clark, RH; Cohen-Wolkowiez, M; Herring, AH; Hornik, CP; Kearns, GL; Smith, PB; van den Anker, J, 2013)	0.39
"In this cohort of infants, meropenem was associated with more frequent but less severe adverse events when compared with imipenem/cilastatin."	( Adverse events associated with meropenem versus imipenem/cilastatin therapy in a large retrospective cohort of hospitalized infants. Benjamin, DK; Capparelli, EV; Clark, RH; Cohen-Wolkowiez, M; Herring, AH; Hornik, CP; Kearns, GL; Smith, PB; van den Anker, J, 2013)	0.39
" Azithromycin was not associated with excess serious adverse events (SAEs)."	( Efficacy and safety of World Health Organization group 5 drugs for multidrug-resistant tuberculosis treatment. Butler-Laporte, G; Menzies, D; Winters, N, 2015)	0.42
"0% of patients, respectively, had treatment-emergent adverse events."	( Prospective, randomized, double-blind, Phase 2 dose-ranging study comparing efficacy and safety of imipenem/cilastatin plus relebactam with imipenem/cilastatin alone in patients with complicated urinary tract infections. Akers, W; Brown, ML; Du, J; Kartsonis, NA; Lee, YC; Mariyanovski, V; McLeroth, P; Paschke, A; Pedley, A; Sims, M, 2017)	0.46
" However, adverse effects in the kidney limit its clinical application."	( Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters. Huo, X; Liu, K; Ma, X; Meng, Q; Sun, H; Wang, C; Wu, J; Zhu, Y, 2020)	0.56
" Cilastatin can be potentially used in the clinic as a therapeutic agent to alleviate the adverse renal reaction to diclofenac."	( Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters. Huo, X; Liu, K; Ma, X; Meng, Q; Sun, H; Wang, C; Wu, J; Zhu, Y, 2020)	0.56
" Serious adverse events (AEs) occurred in 26."	( A Randomized, Double-blind, Multicenter Trial Comparing Efficacy and Safety of Imipenem/Cilastatin/Relebactam Versus Piperacillin/Tazobactam in Adults With Hospital-acquired or Ventilator-associated Bacterial Pneumonia (RESTORE-IMI 2 Study). Boucher, HW; Brown, ML; Butterton, JR; Chen, LF; David-Wang, A; Du, J; Kartsonis, NA; Kaye, KS; Losada, MC; Paschke, A; Patel, M; Rizk, ML; Rodríguez Gonzalez, D; Roquilly, A; Tipping, R; Titov, I; Wunderink, RG; Young, K, 2021)	0.62
" Adverse events (AEs) were reported in 74."	( The safety and efficacy of relebactam/imipenem/cilastatin in Japanese patients with complicated intra-abdominal infection or complicated urinary tract infection: A multicenter, open-label, noncomparative phase 3 study. Aoyama, N; Bando, H; Brown, M; Kawahara, K; Kikukawa, H; Kohno, S; Paschke, A; Shirakawa, M; Takase, A; Yoneyama, F, 2021)	0.62
" Relebactam/imipenem/cilastatin was well tolerated; mild adverse events occurred during single dosing, and one participant experienced serious adverse events after multiple doses."	( A Single- and Multiple-Dose Study To Characterize the Pharmacokinetics, Safety, and Tolerability of Imipenem and Relebactam in Healthy Chinese Participants. Boundy, KE; Colon-Gonzalez, F; Li, H; Liu, N; Patel, M; Wang, H; Wang, X; Wei, Y; Yan, B; Zang, Y; Zhang, S; Zhao, X, 2021)	0.62
" Although less toxic methods of cisplatin administration have been established, cisplatin-induced nephrotoxicity remains an unsolved problem."	( Combination therapy of cisplatin with cilastatin enables an increased dose of cisplatin, enhancing its antitumor effect by suppression of nephrotoxicity. Abe, Y; Aoki, N; Arita, M; Goto, S; Hayashi, M; Hokari, S; Hosojima, M; Ichikawa, K; Kabasawa, H; Kikuchi, T; Kondo, R; Koya, T; Kuwahara, S; Nozaki, K; Ohshima, Y; Ohtsubo, A; Saito, A; Sato, M; Shoji, S; Suzuki, R; Takahashi, M; Watanabe, S, 2021)	0.62
" No severe or life-threatening adverse events were encountered."	( Effectiveness and Safety of Intra-arterial Imipenem/Cilastatin Sodium Infusion for Patients with Hand Osteoarthritis-Related Interphalangeal Joint Pain. Huang, HH; Liang, KW; Tsao, TF; Tyan, YS; Wang, B; Wang, PH, 2023)	0.91

Excerpt	Reference	Relevance
"The pharmacokinetic profiles of imipenem after intramuscular (i."	( Pharmacokinetics of imipenem in serum and skin window fluid in healthy adults after intramuscular or intravenous administration. File, TM; Salstrom, SJ; Signs, SA; Tan, JS, 1992)	0.28
" The mean peak serum concentration was 26 mg/l, the mean half-life 55 min and the AUC 40 mg/l/h-1."	( Pharmacokinetics of imipenem in patients undergoing major colon surgery. Erttmann, M; Krausse, R; Ullmann, U, )	0.13
" Following an intravenous infusion of imipenem 500 mg, the main pharmacokinetic values for the antibiotic are: area under the plasma concentration curve 43."	( [Clinical pharmacokinetics of an imipenem-cilastatin combination]. Singlas, E, 1990)	0.28
" Intravenously administered FCE 22101 at a dose of 250 mg gave peak plasma concentrations of about 12 mg/l and the plasma half-life was about 60 min."	( Pharmacokinetics in healthy subjects of FCE 22101 and its acetoxymethyl ester, FCE 22891: effect of co-administration of imipenem/cilastatin on the renal metabolism of FCE 22101. Burman, LA; Cassinelli, G; Corigli, R; Dornbusch, K; Franceschi, G; Norrby, SR; Sassella, D, 1990)	0.28
"96 mg/l), plasma half-life (60 min), volume of distribution (0."	( Pharmacokinetics of imipenem/cilastatin in neutropenic patients with haematological malignancies. Farrell, I; Janmohamed, RM; Kelly, J; Leyland, MJ, 1990)	0.28
"76 hours, and the half-life of CS tended to be longer than that of IPM."	( [Pharmacokinetic and clinical evaluations of imipenem/cilastatin sodium in neonates and premature infants]. Fujimoto, T; Kawakami, A; Koga, T; Motohiro, T; Oda, K; Sakata, Y; Shimada, Y; Tanaka, K; Tominaga, K; Tomita, S, 1989)	0.28
" The blood half-life of CS tended to be longer than that of IPM."	( [Pharmacokinetic and clinical evaluation of imipenem/cilastatin sodium in neonates and premature infants. A study of imipenem/cilastatin sodium by a perinatal co-research group]. Fujii, R; Fujita, K; Hashira, S; Inyaku, F; Maruyama, S; Nakazawa, S; Sakata, H; Sato, H; Tajima, T; Yoshioka, H, 1989)	0.28
" Pharmacokinetic studies were performed in the 11 children and in 10 of the neonates."	( [Clinical and pharmacokinetic study of imipenem/cilastatin in children and newborn infants]. Baron, S; Bégué, P; Challier, P; Fontaine, JL; Lasfargues, G; Quinet, B, 1989)	0.28
" Drug levels in plasma and the peritoneal dialysis fluid were analyzed at frequent intervals, and various pharmacokinetic variables were calculated for a one-compartment open model."	( Pharmacokinetics of imipenem-cilastatin in patients with renal insufficiency undergoing continuous ambulatory peritoneal dialysis. Freimer, EH; Gross, ML; Higgins, JT; Somani, P, 1988)	0.27
" The mean serum half-life was 82."	( Imipenem pharmacokinetics and body fluid concentrations in patients receiving high-dose treatment for serious infections. Bland, JA; Gibson, GA; MacGregor, RR, 1986)	0.27
" Our data suggest that a minimum dosage, greater than 10 mg/kg, of cilastatin may be required to prolong the half-life of imipenem to adult values."	( Single-dose pharmacokinetics of imipenem-cilastatin in pediatric patients. Engelhard, D; Greenwood, R; Griffis, J; Marks, MI; Shalit, I; Stutman, HR, 1986)	0.27
" Pharmacokinetic studies were done in 7 patients whose ages ranged from 3 years 2 months to 13 years 1 month."	( [Clinical and pharmacokinetic evaluation of imipenem/cilastatin sodium in children]. Fujita, K; Inyaku, F; Kakehashi, H; Maruyama, S; Murono, K; Ohmi, H; Sakata, H; Sanae, N; Yoshioka, H, 1986)	0.27
" Pharmacokinetic studies Peak plasma concentrations of MK-0787/MK-0791 were 27."	( [Pharmacokinetic and clinical studies with imipenem/cilastatin sodium in the pediatric field. Pediatric Study Group for Imipenem/Cilastatin Sodium]. Arimasu, O; Fujii, R; Fujita, K; Inyaku, F; Maruyama, S; Meguro, H; Nagamatsu, I; Takase, A; Wagatsuma, Y; Yoshioka, H, 1986)	0.27
" Pharmacokinetic parameters were calculated from the results."	( Pharmacokinetic studies of imipenem/cilastatin in elderly patients. Craddock, C; Deaney, NB; Finch, RG; Kelly, J, 1986)	0.27
" Pharmacokinetic studies were performed in the 11 children and in 10 of the neonates."	( Pharmacokinetic and clinical evaluation of imipenem/cilastatin in children and neonates. Baron, S; Bégué, PC; Challier, P; Fontaine, JL; Lasfargues, G, 1987)	0.27
" Although probenecid causes only a minor effect on imipenem pharmacology, it increases the area under the curve and half-life of imipenem and decreases the renal clearance of cilastatin significantly."	( Pharmacokinetic profile of imipenem/cilastatin in normal volunteers. Drusano, GL; Standiford, HC, 1985)	0.27
" Pharmacokinetic evaluation after the first dose and again under steady-state conditions revealed biodisposition characteristics which were similar and independent of the daily dose administered."	( Pharmacokinetics of imipenem and cilastatin in patients with cystic fibrosis. Blumer, JL; Myers, CM; O'Brien, CA; Reed, MD; Stern, RC; Yamashita, TS, 1985)	0.27
" Kinetics of imipenem in plasma are less variable, and the half-life of imipenem in plasma is 1 hr."	( Pharmacokinetics of imipenem and cilastatin in volunteers. Bland, JA; Calandra, GB; Demetriades, JL; Ferber, F; Meisinger, MA; Rogers, JD, )	0.13
" The mean plasma half-life of imipenem varied from 52 min in subjects with normal renal function to 173 min in subjects with end-stage renal failure studied while off-dialysis."	( The pharmacokinetics of imipenem (thienamycin-formamidine) and the renal dehydropeptidase inhibitor cilastatin sodium in normal subjects and patients with renal failure. Buntinx, AP; De Broe, ME; Entwistle, LA; Jones, KH; Verbist, L; Verpooten, GA, 1984)	0.27
" The terminal excretion half-life was short (1."	( The plasma pharmacokinetics of high dose (1 g) imipenem coadministered with 1 g cilastatin in six normal volunteers. Bustamante, CI; Drusano, GL; Forrest, A; Rivera, G; Schimpff, SC; Standiford, HC; Tatem, B, 1984)	0.27
"We characterized the pharmacokinetic profile of imipenem-cilastatin administered intravenously to six normal volunteers in a dose of 1,000 mg of each drug every 6 h for 40 doses."	( Multiple-dose pharmacokinetics of imipenem-cilastatin. Bustamante, C; Delaportas, D; Drusano, GL; Forrest, A; Leslie, J; MacGregor, RR; Rivera, G; Schimpff, SC; Standiford, HC; Tatem, B, 1984)	0.27
"To determine the appropriate compartmental and noncompartmental pharmacokinetic parameters for intravenous piperacillin and tazobactam."	( Piperacillin-tazobactam pharmacokinetics in patients with intraabdominal infections. Burm, JP; Gill, MA; Jhee, SS; Kern, JW; Yellin, AE, )	0.13
"The estimated noncompartmental pharmacokinetic parameters (mean +/- SD) for piperacillin and tazobactam, respectively, were as follows: maximum concentration in plasma 218."	( Piperacillin-tazobactam pharmacokinetics in patients with intraabdominal infections. Burm, JP; Gill, MA; Jhee, SS; Kern, JW; Yellin, AE, )	0.13
" Therefore, knowledge of the impact of continuous haemofiltration on drug elimination and the pharmacokinetic profile of drugs is essential to good clinical management."	( Clinical pharmacokinetics during continuous haemofiltration. Bressolle, F; de la Coussaye, JE; Eledjam, JJ; Galtier, M; Kinowski, JM; Wynn, N, 1994)	0.29
" Imipenem pharmacokinetic parameters were determined in 10 anuric patients with renal failure managed by continuous venovenous hemofiltration (CVVH)."	( Comparison of imipenem pharmacokinetics in patients with acute or chronic renal failure treated with continuous hemofiltration. Macias, WL; Mueller, BA; Scarim, SK, 1993)	0.29
" Pharmacokinetic parameters were based on an open two-compartment model and a noncompartmental technique."	( Serum bactericidal activities and comparative pharmacokinetics of meropenem and imipenem-cilastatin. Borner, K; Dreetz, M; Eller, J; Hamacher, J; Koeppe, P; Lode, H; Schaberg, T, 1996)	0.29
"h/ml in the chimpanzee) and a longer half-life at beta phase (1."	( Pharmacokinetics in nonhuman primates of a prototype carbapenem active against methicillin-resistant Staphylococcus aureus. Cama, L; Kropp, H; Sasor, MW; Sundelof, JG; Thompson, R; White, KM, 1996)	0.29
" The pharmacokinetic parameters for meropenem are similar to those for imipenem/cilastatin, with the exception of meropenem's smaller volume of distribution."	( Pharmacokinetics of meropenem in animals, healthy volunteers, and patients. Chung, KC; Gill, MA; Moon, YS, 1997)	0.3
" Pharmacokinetic variables were calculated by a first-order, two-compartment pharmacokinetic model for both substances."	( Pharmacokinetics of imipenem-cilastatin in critically ill patients undergoing continuous venovenous hemofiltration. Bremer, F; Brune, K; Geisslinger, G; Oelkers, R; Schobel, H; Schüttler, J; Tegeder, I, 1997)	0.3
"Efficacy and pharmacokinetic parameters of imipenem/cilastatin (I/C) were investigated in a retrospective evaluation in 104 premature and newborn infants."	( Pharmacokinetic and clinical evaluation of serious infections in premature and newborn infants under therapy with imipenem/cilastatin. Böswald, M; Döbig, C; Guggenbichler, JP; Kändler, C; Krüger, C; Scharf, J; Soergel, F; Zink, S, 1999)	0.3
"To investigate the pharmacokinetic characteristics of Imipenem/cilastatin in burn patients during the acute phase."	( [Study on the pharmacokinetics of Imipenem cilastatin in burn patients during the acute phase]. Peng, Y; Wang, H; Xiao, G, 2000)	0.31
"Compared to those in control group, pharmacokinetic parameters of Imipenem exhibited evident difference, such as prolonged half-life [(1."	( [Study on the pharmacokinetics of Imipenem cilastatin in burn patients during the acute phase]. Peng, Y; Wang, H; Xiao, G, 2000)	0.31
"The probability of attaining lower pharmacodynamic targets for most gram-negative bacteria is similar for these carbapenems; however, differences become apparent as the pharmacodynamic requirement increases."	( Pharmacodynamics of meropenem and imipenem against Enterobacteriaceae, Acinetobacter baumannii, and Pseudomonas aeruginosa. Florea, NR; Kuti, JL; Nicolau, DP; Nightingale, CH, 2004)	0.32
" Pharmacokinetic parameters, obtained from previously published studies in healthy volunteers were used to simulate the %T > MIC for 10,000 patients receiving imipenem-cilastatin, meropenem, and piperacillin/tazobactam."	( Pharmacodynamic modeling of beta-lactam antibiotics for the empiric treatment of secondary peritonitis: a report from the OPTAMA program. Kotapati, S; Kuti, JL; Nicolau, DP, 2005)	0.33
"The bactericidal exposures necessary for positive clinical outcomes among skin and soft tissue infections are largely dependent on interpatient pharmacokinetic variability and pathogen drug susceptibility."	( Pharmacodynamic modeling of imipenem-cilastatin, meropenem, and piperacillin-tazobactam for empiric therapy of skin and soft tissue infections: a report from the OPTAMA Program. Kuti, JL; Nicolau, DP; Ong, CT, 2005)	0.33
" A two-compartment open model was employed for population pharmacokinetic modeling."	( Population pharmacokinetics and pharmacodynamics of continuous versus short-term infusion of imipenem-cilastatin in critically ill patients in a randomized, controlled trial. Bulitta, JB; Drusano, GL; Glauner, AK; Kinzig-Schippers, M; Pfister, W; Sakka, SG; Sörgel, F, 2007)	0.34
"A pharmacokinetic (PK)/pharmacodynamic (PD) modeling strategy to simulate in vivo bactericidal effects for three carbapenem antibiotics, doripenem (DRPM), meropenem (MEPM)/cilastatin (CS), and imipenem (IPM)/CS, against a Pseudomonas aeruginosa (P."	( Pharmacokinetic-pharmacodynamic modeling and simulation for in vivo bactericidal effect in murine infection model. Katsube, T; Yamano, Y; Yano, Y, 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
"This phase I study assessed the intrapulmonary pharmacokinetic profiles of relebactam (MK-7655), a novel β-lactamase inhibitor, and imipenem."	( Intrapulmonary Pharmacokinetics of Relebactam, a Novel β-Lactamase Inhibitor, Dosed in Combination with Imipenem-Cilastatin in Healthy Subjects. Bi, S; Butterton, JR; Chavez-Eng, CM; Gotfried, MH; Jumes, PA; Mangin, E; Rhee, EG; Rizk, ML; Zhang, Z; Zhao, T, 2018)	0.48
"Simulations demonstrated that the ratio of the area under the concentration-time curve for free drug to the minimum inhibitory concentration (fAUC/MIC) was the pharmacokinetic driver for relebactam, with a target fAUC/MIC=7."	( A translational pharmacokinetic/pharmacodynamic model to characterize bacterial kill in the presence of imipenem-relebactam. Bhagunde, P; Carr, D; Racine, F; Rizk, ML; Wu, J; Young, K; Zhang, Z, 2019)	0.51
" Population pharmacokinetic models with and without covariates were fit using the non-parametric adaptive grid algorithm in Pmetrics."	( Imipenem/cilastatin/relebactam pharmacokinetics in critically ill patients with augmented renal clearance. Fratoni, AJ; Kuti, JL; Mah, JW; Nicolau, DP, 2022)	0.72
" A base population pharmacokinetic model with two-compartments fitted the data best."	( Imipenem/cilastatin/relebactam pharmacokinetics in critically ill patients with augmented renal clearance. Fratoni, AJ; Kuti, JL; Mah, JW; Nicolau, DP, 2022)	0.72

Excerpt	Reference	Relevance
"In a randomised and coordinated multicentre study, 143 patients with severe infections received treatment with either imipenem/cilastatin (72; I/C group) or cefotaxime combined with metronidazole and optional cloxacillin (71; CX/M/CL group)."	( Imipenem/cilastatin as monotherapy in severe infections: comparison with cefotaxime in combination with metronidazole and cloxacillin. Report from a Norwegian Study Group. , 1987)	0.27
"Imipenem was evaluated for its in vitro and in vivo activities alone and in combination with gentamicin against a clinical isolate of Listeria monocytogenes, and the results were compared with the activities of ampicillin with and without gentamicin."	( In vitro and in vivo studies of imipenem-cilastatin alone and in combination with gentamicin against Listeria monocytogenes. Kim, KS, 1986)	0.27
"Nine severe Gram-negative septicaemias in neutropenic (less than 500 neutrophils/mm3) children with neoplastic diseases were treated with imipenem/cilastatin (75 mg/kg/day) in combination with an aminoglycoside."	( Severe gram-negative infections in neutropenic children cured by imipenem/cilastatin in combination with an aminoglycoside. Andremont, A; Baruchel, A; Hartmann, O; Tancrède, C, 1986)	0.27
" These results indicate that IPM/CS alone produces of good response in moderate to severe respiratory infections while IPM/CS combined with AMK is useful in intractable respiratory infections."	( [Imipenem/cilastatin sodium alone or combined with amikacin sulfate in respiratory infections]. Ichikawa, Y; Ishibashi, T; Oizumi, K; Takamoto, M; Tamaru, N; Tanaka, H; Tokunaga, N; Toyoshima, H; Watanabe, K; Yoshida, M, 1994)	0.29
"The synergic activity of imipenem/cilastatin combined with cefotiam was studied in a mouse bacteraemia model."	( Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus. Asahi, Y; Goto, M; Inoue, M; Kaji, Y; Kimura, S; Matsuda, K; Nakagawa, S; Oka, S; Sanada, M; Shimada, K, 1993)	0.29
" Therefore, the nephrotoxic effects and pharmacokinetics of VCM were examined in rabbits and compared with those in rabbits administered with VCM and other antibiotics."	( [Nephrotoxicity and drug interaction of vancomycin (2)]. Nakagawa, Y; Toyoguchi, T, 1996)	0.29
"Against gram-positive sepsis, vancomycin (VCM) was administered in combination with imipenem or cilastatin (IPM/CS)."	( [Two cases of gram-positive sepsis successfully treated with vancomycin in combination with imipenem or cilastatin]. Maezawa, H; Nakazawa, Y; Saitoh, A; Sakai, O; Sakamoto, M; Saruta, K; Shiba, K; Shindo, N; Yoshida, M; Yoshikawa, K, 1996)	0.29
"The nephrotoxic effects of vancomycin hydrochloride (VCM) and the potential drug-drug interaction with cilastatin sodium (CS) were examined in rabbits."	( Nephrotoxicity of vancomycin and drug interaction study with cilastatin in rabbits. Hosoya, J; Nakagawa, Y; Takahashi, S; Toyoguchi, T; Watanabe, H, 1997)	0.3
"The aim of this in vitro study was to compare the elution characteristics of vancomycin alone and in combination with imipenem-cilastatin from 3 acrylic bone-cements (CMW1 [DePuy International, Blackpool, UK], Palacos R [Schering-Plough, Wehrheim, Germany], and Simplex P [Howmedica International, London, UK])."	( The in vitro elution characteristics of vancomycin combined with imipenem-cilastatin in acrylic bone-cements: a pharmacokinetic study. Bocchi, L; Ceffa, R; Cerretani, D; Fornara, P; Ghisellini, F; Giorgi, G; Neri, L; Ritter, MA, 2002)	0.31
"Convulsant activity of pazufloxacin mesilate (PZFX mesilate), a new quinolone antibacterial agent for intravenous use, in combination with nonsteroidal anti-inflammatory drug (NSAID) was investigated in mice after intravenous or intracerebroventricular administration."	( [Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration]. Fukuda, H; Kawamura, Y, 2002)	0.31
"This randomized, double-blind, multicenter study compared the efficacy and safety of piperacillin/tazobactam (P/T) and imipenem/cilastatin (IMP), both in combination with an aminoglycoside, in hospitalized patients with acute nosocomial pneumonia (NP)."	( Comparison of piperacillin/tazobactam and imipenem/cilastatin, both in combination with tobramycin, administered every 6 h for treatment of nosocomial pneumonia. Cooper, A; Joshi, M; Kassira, W; McCarthy, M; Metzler, M; Olvey, S, 2006)	0.33
" The purpose of this study was to investigate the clinical outcomes of patients with healthcare-associated infections (HAIs) caused by MDRAB who were treated with imipenem/cilastatin and sulbactam, and TG alone or in combination with other antibiotics."	( Clinical outcomes of tigecycline alone or in combination with other antimicrobial agents for the treatment of patients with healthcare-associated multidrug-resistant Acinetobacter baumannii infections. Hsueh, PR; Lee, YT; Tsao, SM, 2013)	0.39
"β-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C β-lactamase mediated antibiotic resistance."	( Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®. Blizzard, TA; Bodner, R; Chen, H; Fitzgerald, P; Gude, C; Ha, S; Hairston, N; Hammond, ML; Hermes, J; Imbriglio, J; Kim, S; Lu, J; Ogawa, A; Painter, RE; Park, YW; Raghoobar, S; Scapin, G; Sharma, N; Wisniewski, D; Wu, J; Young, K, 2014)	0.4

Excerpt	Reference	Relevance
" Excellent tissue pharmacokinetics and oral bioavailability suggest usefulness in the treatment of complicated intra-abdominal infections."	( Trovafloxacin in the treatment of intra-abdominal infections: results of a double-blind, multicenter comparison with imipenem/cilastatin. Trovafloxacin Surgical Group. Bur, F; Donahue, PE; Luke, DR; Mintz, SJ; Smith, DL; Yellin, AE, 1998)	0.3
" Bioavailability was 93."	( Pharmacokinetics of imipenem after intravenous, intramuscular and subcutaneous administration to cats. Albarellos, GA; Denamiel, GA; Landoni, MF; Lupi, MP; Montoya, L; Quaine, PC, 2013)	0.39

Excerpt	Relevance	Reference
" One day during treatment days 2-8, multiple blood and urine samples were collected from each individual over a six hour dosing interval."	( Pharmacokinetics of imipenem/cilastatin sodium in children with peritonitis. Claesson, G; Eriksson, M; Rogers, JD, 1992)	0.28
" Microbes which appeared after its dosing amounted to 6 classes of 17 strains, 6 NFB strains of which were identified."	( [Clinical studies of efficacy of imipenem/cilastatin sodium against urinary tract infections with ureterocutaneostomy]. Ikeuchi, T; Kai, Y; Yogi, S; Yoshikawa, H, 1992)	0.28
" This was offset, however, by greater costs in the C+A group for dosage preparation, material and labor, and need for therapeutic drug monitoring of the aminoglycoside."	( Cost-analysis of imipenem-cilastatin monotherapy compared with clindamycin+aminoglycoside combination therapy for treatment of serious lower respiratory, intra-abdominal, gynecologic, and urinary tract infections. Kreter, B, )	0.13
"To report a case of Pseudomonas aeruginosa endocarditis that was successfully treated with high-dose imipenem/cilastatin and to discuss dosage modification based on individual pharmacokinetic parameters."	( Successful use of higher-than-recommended dosage of imipenem in Pseudomonas aeruginosa endocarditis. Hrdy, DB; Kailath, EJ; King, JH, 1992)	0.28
" Dosage may need to be adjusted to body size in order to obtain optimal serum concentrations and activity."	( Successful use of higher-than-recommended dosage of imipenem in Pseudomonas aeruginosa endocarditis. Hrdy, DB; Kailath, EJ; King, JH, 1992)	0.28
" (22) and other dosages (a change in dosing regimen, 2)."	( [Clinical study of intramuscular imipenem/cilastatin sodium in the field of obstetrics and gynecology]. Banzai, M; Chimura, T; Kanasugi, H; Kihara, K; Matsuo, M; Miyata, R; Oda, T; Takahashi, H; Yamazaki, K; Yokoyama, Y, 1991)	0.28
" Mean imipenem AUCss (area under the concentration-time curve over a dosage interval at steady state) values were 38."	( Steady-state pharmacokinetics of intramuscular imipenem-cilastatin in elderly patients with various degrees of renal function. Bland, JA; Graziani, AL; Lawson, LA; MacGregor, RR; Pietroski, NA; Rogers, JD, 1991)	0.28
" Dosing regimens in evaluable patients were 500 mg every 12 h (45."	( Intramuscular imipenem/cilastatin in multiple-dose treatment regimens: review of the worldwide clinical experience. Calandra, GB; Garau, J, 1991)	0.28
"Imipenem is the broadest-spectrum antibiotic currently available but requires frequent intravenous dosing for efficacy."	( Overall clinical utility of the intramuscular preparation of imipenem/cilastatin. MacGregor, RR, 1991)	0.28
" Pharmacists evaluated I/C dosage based upon culture/sensitivity results and indicators of renal function."	( Evaluation of an imipenem/cilastatin target drug program. Abel, SR; Guba, EA, 1991)	0.28
" This makes it difficult to determine a mean dosage for therapeutic uses."	( [Clinical pharmacokinetics of an imipenem-cilastatin combination]. Singlas, E, 1990)	0.28
" The mean dosage and duration of treatment were 29."	( [An imipenem-cilastatin combination in the treatment of infection at general intensive care units]. Gouin, F, 1990)	0.28
" This dose should be the starting dose for a period of 12-h dosing intervals until the next IHF procedure."	( Pharmacokinetics of intravenous imipenem/cilastatin during intermittent haemofiltration. Alarabi, AA; Cars, O; Danielson, BG; Salmonson, T; Wikström, B, 1990)	0.28
" Up to six hours after dosing the concentrations in prostatic secretions ranged between 1 and 2 mg/l."	( [Imipenem/cilastatin: in vitro activity, concentrations in plasma and prostatic adenoma and therapeutic results in patients with complicated urinary tract infections]. Adam, D; Bauernfeind, A; Hönig, E; Naber, KG, 1986)	0.27
" The concentration of IPM in plasma showed a dose-response to the 10 mg/10 mg/kg and 20 mg/20 mg/kg dosages."	( [Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium in neonates]. Iwai, N; Kasai, K; Miyazu, M; Nakamura, H; Taneda, Y, 1989)	0.28
" Our work indicates that with serum concentration of 100 mg/l, superior to those obtained in therapeutic, neither imipenem nor cilastatin interact on the creatinine dosage using either the Jaffé reaction of the enzymatic technic."	( [Do imipenem and cilastatin interfere with the determination of serum creatinine?]. Dauchy, F, 1988)	0.27
" aerogenes septicemia required pefloxacin because blood cultures remained positive (d5) despite an increased dosage (90 mg/kg/d)."	( [Use of imipenem-cilastatin in neonatal septicemias caused by gram-negative bacilli multiresistant to beta-lactam antibiotics]. Aufrant, C; Bompard, Y; Chastel, A; Gantzer, A; Lambert, T; Voinnesson, A, 1988)	0.27
" There was an association with Pseudomonas aeruginosa infection that remained statistically significant even after controlling for imipenem/cilastatin dosage as well as for the other factors indicated."	( Factors predisposing to seizures in seriously ill infected patients receiving antibiotics: experience with imipenem/cilastatin. Calandra, G; Carrigan, J; Guess, H; Lydick, E; Weiss, L, 1988)	0.27
" Plasma concentrations, half-lives, and areas under the curve of both imipenem and cilastatin was significantly greater at the 25 mg/kg dosage but the half-lives and clearances of the two drugs were similar to each other only at the larger dose."	( Single-dose pharmacokinetics of imipenem-cilastatin in pediatric patients. Engelhard, D; Greenwood, R; Griffis, J; Marks, MI; Shalit, I; Stutman, HR, 1986)	0.27
" Clinically, MK-0787/MK-0791 was used for the treatment of obstetrical and gynecological infections at a dosage of 500 mg/500 mg twice daily by intravenous drip infusion."	( [Fundamental and clinical studies of imipenem/cilastatin sodium in the field of obstetrics and gynecology]. Akagi, T; Fujiwara, A; Hara, T; Iwasaki, K; Kudo, Y; Masaoka, T; Matsuo, M; Naito, H; Urabe, T, 1986)	0.27
" In 112 patients the daily dosage ranged from 30/30 mg/kg to 59/59 mg/kg, and in 138 patients it ranged from 60/60 mg/kg to 99/99 mg/kg."	( [Pharmacokinetic and clinical studies with imipenem/cilastatin sodium in the pediatric field. Pediatric Study Group for Imipenem/Cilastatin Sodium]. Arimasu, O; Fujii, R; Fujita, K; Inyaku, F; Maruyama, S; Meguro, H; Nagamatsu, I; Takase, A; Wagatsuma, Y; Yoshioka, H, 1986)	0.27
"The chemistry, antimicrobial spectrum, mechanism of action, pharmacology and pharmacokinetics, clinical use, adverse effects, dosage and administration, place in therapy, cost-effectiveness, and formulary considerations of imipenem-cilastatin sodium are reviewed."	( Imipenem-cilastatin sodium, a broad-spectrum carbapenem antibiotic combination. Pastel, DA, 1986)	0.27
" Imipenem and cilastatin sodium in a dosage of 100 mg/kg/d was used for children 3 years of age or younger, while older ones received 60 mg/kg/d intravenously, divided in four equal doses."	( Imipenem and cilastatin in acute osteomyelitis and suppurative arthritis. Therapy in infants and children. Freij, BJ; Kusmiesz, H; Nelson, JD; Shelton, S, 1987)	0.27
" Therefore, dose adjustments will be required in patients with markedly reduced renal function and supplemental dosing will be required after hemodialysis."	( Imipenem/cilastatin: pharmacokinetic profile in renal insufficiency. Bland, JA; Demetriades, JL; Gibson, TP, 1985)	0.27
" Pure tone audiograms were performed before and after dosing in 11 of 12 subjects; no changes were noted."	( Safety and tolerability of multiple doses of imipenem/cilastatin. Bustamante, CI; Delaportas, D; Drusano, GL; Forrest, A; Leslie, J; Rivera, G; Schimpff, SC; Standiford, HC; Tatem, B, 1985)	0.27
" In view of the important increase in half-life of cilastatin as a function of increasing renal failure, a dosage reduction is proposed in patients with severe renal failure."	( The pharmacokinetics of imipenem (thienamycin-formamidine) and the renal dehydropeptidase inhibitor cilastatin sodium in normal subjects and patients with renal failure. Buntinx, AP; De Broe, ME; Entwistle, LA; Jones, KH; Verbist, L; Verpooten, GA, 1984)	0.27
"5) micrograms/ml in the 1st, 17th, and 37th dosing intervals, respectively."	( Multiple-dose pharmacokinetics of imipenem-cilastatin. Bustamante, C; Delaportas, D; Drusano, GL; Forrest, A; Leslie, J; MacGregor, RR; Rivera, G; Schimpff, SC; Standiford, HC; Tatem, B, 1984)	0.27
", 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
" Because patients undergoing continuous haemofiltration have impaired renal function, dosage reduction is often recommended so that adverse drug reactions are avoided."	( Clinical pharmacokinetics during continuous haemofiltration. Bressolle, F; de la Coussaye, JE; Eledjam, JJ; Galtier, M; Kinowski, JM; Wynn, N, 1994)	0.29
" The recommended dosage was 30 mg/kg/day and could be increased up to 50 mg/kg/day, without exceeding four grams per day, administered by four infusions per day."	( [Efficacy and tolerance of imipenem/cilastatin in the adjuvant treatment of surgery for peritonitis in patients over the age of 70 years]. Carles, J; Janvier, G, 1993)	0.29
" At the dosage used piperacillin/tazobactam was as safe as, and statistically more effective than, imipenem/cilastatin in the treatment of intra-abdominal infections caused by sensitive organisms."	( A randomized multicenter trial of piperacillin/tazobactam versus imipenem/cilastatin in the treatment of severe intra-abdominal infections. Swedish Study Group. Eklund, AE; Nord, CE, 1993)	0.29
" Current dosing recommendations for the administration of imipenem to patients with acute or chronic renal failure are based on this reduced clearance rate."	( Comparison of imipenem pharmacokinetics in patients with acute or chronic renal failure treated with continuous hemofiltration. Macias, WL; Mueller, BA; Scarim, SK, 1993)	0.29
"To develop computerized methods to monitor and recommend dosage changes for patients treated with excessive dosages of imipenem/cilastatin (I/C) and to determine the incidence of I/C-associated seizures in our patient population."	( Prospective surveillance of imipenem/cilastatin use and associated seizures using a hospital information system. Burke, JP; Classen, DC; Evans, RS; Pestotnik, SL; Stevens, LE, 1993)	0.29
" Additional computer-generated alerts identified patients who were receiving anticonvulsants concomitantly with I/C or whose therapy reflected dosage changes in the previous 24 hours."	( Prospective surveillance of imipenem/cilastatin use and associated seizures using a hospital information system. Burke, JP; Classen, DC; Evans, RS; Pestotnik, SL; Stevens, LE, 1993)	0.29
" We believe that appropriate dosing of I/C results in a low rate of associated seizures."	( Prospective surveillance of imipenem/cilastatin use and associated seizures using a hospital information system. Burke, JP; Classen, DC; Evans, RS; Pestotnik, SL; Stevens, LE, 1993)	0.29
" These results indicate that the timing of dosing of each antibiotic influences synergy, and administration of cefotiam 2 h after imipenem is more effective than the other regimens."	( Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus. Asahi, Y; Goto, M; Inoue, M; Kaji, Y; Kimura, S; Matsuda, K; Nakagawa, S; Oka, S; Sanada, M; Shimada, K, 1993)	0.29
" The convenience of use of the kit and the time required for the preparation of the dosing solution were evaluated by nurses and pharmacists at the Kitasato University East Hospital."	( [Study of the usefulness of a kit containing imipenem/cilastatin powder with diluent for injection: convenience of use and preparation]. Hirayama, T; Kuroyama, M; Shimda, S, 1996)	0.29
" The amount of imipenem/cilastatin remaining in the newly developed kit should be negligible, because the kit serves as both a vial and a dosing package."	( [Study of the usefulness of a kit containing imipenem/cilastatin powder with diluent for injection: accuracy of reconstitution]. Hirayama, T; Kuroyama, M; Shimada, S, 1996)	0.29
" If the manufacturer's dosage recommendations are followed, the risk of seizures in patients receiving this combination is minimal."	( Neurotoxicity of carbapenem antibacterials. Norrby, SR, 1996)	0.29
"In a nonblind, randomised, parallel-group study, initial empirical monotherapy with meropenem 1 g intravenously every 8 h was compared to an identical dosage of imipenem/cilastatin for the treatment of 66 febrile episodes in 61 adult neutropenic patients."	( Empirical monotherapy with meropenem versus imipenem/cilastatin for febrile episodes in neutropenic patients. Böhme, A; Fuhr, HG; Halir, S; Heller, A; Jung, B; Köhler, A; Lips-Schulte, C; Schaumann, R; Shah, PM; Stille, W; Walther, F, )	0.13
" Approximately 70% of meropenem is excreted via the kidneys, thus dosage adjustments are required for patients with renal impairment."	( Pharmacokinetics of meropenem in animals, healthy volunteers, and patients. Chung, KC; Gill, MA; Moon, YS, 1997)	0.3
" Dosage reduction is required in patients with reduced renal function; no dosage adjustment is required for patients with hepatic impairment."	( The pharmacology of meropenem, a new carbapenem antibiotic. Craig, WA, 1997)	0.3
" Dosage was reduced in patients with renal impairment."	( [Meropenem (Merrem) vs imipenem/cilastatin in hospital treatment of intra-abdominal infections. A multicenter study]. Tonelli, F, 1997)	0.3
" The dosage of prednisolone was increased, and amikacin was injected to treat pneumonia that had developed in the right lung."	( [Legionella pneumonia successfully treated despite late diagnosis]. Takazakura, E; Tsuji, H, 1997)	0.3
" Plasma and hemofiltrate samples were taken at specified times during one dosing interval, and the concentrations of imipenem and cilastatin were determined by high-performance liquid chromatography."	( Pharmacokinetics of imipenem-cilastatin in critically ill patients undergoing continuous venovenous hemofiltration. Bremer, F; Brune, K; Geisslinger, G; Oelkers, R; Schobel, H; Schüttler, J; Tegeder, I, 1997)	0.3
" To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefditoren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin."	( In vitro and in vivo antibacterial activities of CS-834, a new oral carbapenem. Domon, H; Furuya, N; Ishii, K; Matsumoto, T; Miyazaki, S; Ohno, A; Tateda, K; Yamaguchi, K, 1998)	0.3
" Cost-avoidance with meropenem is, therefore, mainly the result of less frequent dosing and the ability to administer meropenem by rapid intravenous injection."	( Formulary review of the carbapenems: comparison of imipenem/cilastatin and meropenem. Ambrose, PG; Nightingale, CH; Quintiliani, R; Richerson, MA, 1998)	0.3
" The same dosage regimen resulted in complete bacterial eradication in 88% of the kidneys."	( Comparative therapeutic efficacy of clinafloxacin in a Pseudomonas aeruginosa mouse renal abscess model. Desaty, TM; Griffin, TJ; Heifetz, CL; Sesnie, JC; Shapiro, MA, 1998)	0.3
" Under base-case conditions, our pharmacoeconomic analysis showed that I/C was a cost-effective alternative to P/T at the dosage regimens studied."	( Cost-minimization analysis of piperacillin/tazobactam versus imipenem/cilastatin for the treatment of serious infections: a Canadian hospital perspective. Bryce, EA; Frighetto, LO; Jewesson, PJ; Marra, CA; Marra, FO; Reynolds, RP; Sleigh, KM; Stiver, HG, 1999)	0.3
"All courses of IC administered to patients over age 60 during a four-month period were retrospectively assessed for appropriateness based on both dosing interval and dosage."	( Evaluation and financial impact of imipenem/cilastatin dosing in elderly patients based on renal function and body weight. Bailey, TC; Canaday, KL; Reichley, RM; Ritchie, DJ, )	0.13
" The projected annual cost savings that could have been realized by appropriately adjusting IC dosage based on estimated Cl cr and body weight was $11,500."	( Evaluation and financial impact of imipenem/cilastatin dosing in elderly patients based on renal function and body weight. Bailey, TC; Canaday, KL; Reichley, RM; Ritchie, DJ, )	0.13
" Thus, the dosing of imipenem-cilastatin 750 mg intramuscularly every 12 hours is a more cost effective method of drug delivery with equal efficacy and safety when compared to imipenem-cilastatin 500 mg given intravenously every 6 hours."	( A cost comparison of intramuscular versus intravenous imipenem. Appleman, MD; Berne, TV; Chin, A; Gill, MA; Heseltine, PN; Ito, MK; Yellin, AE, 1989)	0.28
" Cost saving may be achieved with trovafloxacin due to the lack of any need to monitor creatinine levels and the once-daily dosing regimen that allows a switch to the same orally administered drug."	( Treatment of complicated intra-abdominal infections: comparison of the tolerability and safety of intravenous/oral trovafloxacin versus intravenous imipenem/cilastatin switching to oral amoxycillin/clavulanic acid. Luke, DR; Peterson, J, )	0.13
"Tazobactam/piperacillin (total daily dosage of 13."	( Cost efficacy of tazobactam/piperacillin versus imipenem/cilastatin in the treatment of intra-abdominal infection. Daschner, F; Dietrich, ES; Ebner, W; Schubert, B, 2001)	0.31
"2%, without significant differences according to the type of pathogen or dosage schedule; however one of the two observed failures was due to a resistant Pseudomonas aeruginosa."	( Imipenem/cilastatin as empirical treatment of severe infections in compromised patients. Biglino, A; Bonasso, M; Gioannini, P, 1991)	0.28
" In addition, concurrent dosing of BPAA (1 microgram/body) did not reduce the convulsion-inducing dose of PZFX mesilate."	( [Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration]. Fukuda, H; Kawamura, Y, 2002)	0.31
" For the free drug concentrations, the percentage of the dosing interval that the drug concentrations remain above the MIC (%T>MIC) for each carbapenem-bacteria combination was calculated for 10,000 iterations, substituting a different ClT, Vdbeta, fraction of unbound drug, and MIC into the equation each time based on the probability distribution for each parameter."	( Pharmacodynamics of meropenem and imipenem against Enterobacteriaceae, Acinetobacter baumannii, and Pseudomonas aeruginosa. Florea, NR; Kuti, JL; Nicolau, DP; Nightingale, CH, 2004)	0.32
" This tendency inverse correlated to decreasing dosage of PCs."	( [The trend and susceptibility to antibacterial agents of enterococcus species from urinary tract infections]. Hoshinaga, K; Ishikawa, K; Miyakawa, S; Naide, Y; Shiroki, R; Tanaka, T, 2004)	0.32
" Pre- and postmembrane blood (plasma) and corresponding ultrafiltrate or dialysate samples were collected 1, 2, 4, and 8 or 12 h (depending on dosing interval) after completion of the drug infusion."	( Pharmacokinetics and pharmacodynamics of imipenem during continuous renal replacement therapy in critically ill patients. Abraham, E; Fish, DN; Teitelbaum, I, 2005)	0.33
"Randomized controlled trials of adult patients with severe infections treated with meropenem or imipenem plus cilastatin at an equal dose, on a gram-for-gram basis, and with the same dosing regimen."	( Systematic review comparing meropenem with imipenem plus cilastatin in the treatment of severe infections. Campbell, HE; Edwards, SJ; Emmas, CE, 2005)	0.33
") infusion at an imipenem dosage of 10 mg/kg (study 1) and 20 mg/kg (study 2)."	( Pharmacokinetics of imipenem-cilastatin following intravenous administration in healthy adult horses. Benson, CE; Boston, RC; Engiles, J; Moate, PJ; Norman, T; Orsini, JA; Poppenga, R, 2005)	0.33
" For meaningful dosage recommendations to be made, further studies are required using larger populations and with more detail regarding liver dysfunction and duration of renal failure."	( Using imipenem and cilastatin during continuous renal replacement therapy. Brett, S; Cotton, A; Franklin, BD; Holmes, A, 2005)	0.33
" The percentage of the dosing interval during which free drug concentrations exceed the MIC (fT(>MIC)) is the measure of drug exposure that best correlates with clinical outcome for beta-lactams."	( Population pharmacokinetics and pharmacodynamics of continuous versus short-term infusion of imipenem-cilastatin in critically ill patients in a randomized, controlled trial. Bulitta, JB; Drusano, GL; Glauner, AK; Kinzig-Schippers, M; Pfister, W; Sakka, SG; Sörgel, F, 2007)	0.34
"When dosed appropriately, imipenem/cilastatin may be used to treat serious infections in critically ill patients with central nervous system (CNS) disorders or injury with minimal seizure risk."	( Safety of imipenem/cilastatin in neurocritical care patients. Brophy, GM; Hoffman, J; Trimble, J, 2009)	0.35
" Sixty-four patients underwent the imipenem-cilastatin intramuscular test dosing and none of them had a clinical reaction."	( Cross-reactivity and tolerability of imipenem in patients with delayed-type, cell-mediated hypersensitivity to beta-lactams. Altomonte, G; Buonomo, A; Decinti, M; Lombardo, C; Nucera, E; Pascolini, L; Patriarca, G; Schiavino, D, 2009)	0.35
"To compare clinical outcomes of patients receiving an alternative dosage of meropenem with those of patients receiving imipenem-cilastatin or the traditional dosage of meropenem after failure of or intolerance to cefepime for treatment of febrile neutropenia."	( Assessment of an alternative meropenem dosing strategy compared with imipenem-cilastatin or traditional meropenem dosing after cefepime failure or intolerance in adults with neutropenic fever. Arnold, HM; Augustin, KM; Casabar, E; Dubberke, ER; Hladnik, LM; McKinnon, PS; Reichley, RM; Ritchie, DJ; Westervelt, P, 2009)	0.35
"Of the 127 patients, 40 received imipenem-cilastatin 500 mg every 6 hours between September 1, 2005, and August 31, 2006; 87 patients received meropenem between September 1, 2006, and August 31, 2007: 29 received a traditional dosage of meropenem 1 g every 8 hours, and 58 received an alternative dosage of meropenem 500 mg every 6 hours."	( Assessment of an alternative meropenem dosing strategy compared with imipenem-cilastatin or traditional meropenem dosing after cefepime failure or intolerance in adults with neutropenic fever. Arnold, HM; Augustin, KM; Casabar, E; Dubberke, ER; Hladnik, LM; McKinnon, PS; Reichley, RM; Ritchie, DJ; Westervelt, P, 2009)	0.35
"The alternative meropenem dosage of 500 mg every 6 hours yielded similar patient outcomes, including time to defervescence, need for additional antibiotics, duration of therapy, and mortality, when compared with the traditional meropenem dosage and imipenem-cilastatin in adults with febrile neutropenia."	( Assessment of an alternative meropenem dosing strategy compared with imipenem-cilastatin or traditional meropenem dosing after cefepime failure or intolerance in adults with neutropenic fever. Arnold, HM; Augustin, KM; Casabar, E; Dubberke, ER; Hladnik, LM; McKinnon, PS; Reichley, RM; Ritchie, DJ; Westervelt, P, 2009)	0.35
" Monte Carlo simulations using various dosage regimens at steady-state and 30-min and 3-h infusion rates were performed to evaluate the probabilities of attaining 20% (bacteriostatic), 30%, and 40% (maximum kill) time above the MIC."	( Comparison of 30-min and 3-h infusion regimens for imipenem/cilastatin and for meropenem evaluated by Monte Carlo simulation. Bertino, JS; Drusano, GL; Jones, RN; Kinzig-Schippers, M; Lee, LS; Ma, L; Nafziger, AN; Sörgel, F, 2010)	0.36
" Imipenem would be predicted to be effective for the treatment of antimicrobial resistant bacterial infections in cats at a dosage of 5 mg/kg every 6-8 h (IV, IM), or longer for the SC route."	( Pharmacokinetics of imipenem after intravenous, intramuscular and subcutaneous administration to cats. Albarellos, GA; Denamiel, GA; Landoni, MF; Lupi, MP; Montoya, L; Quaine, PC, 2013)	0.39
" Data including the dosage and duration of the drug use, occurrence of seizures and mortality outcome was collected from the electronic pharmacy records."	( A Retrospective Study on the Incidence of Seizures among Neurosurgical Patients Who Treated with Imipenem/Cilastatin or Meropenem. Chen, K; Shi, Z; Wang, Q; Wu, Y, 2014)	0.4
" There was not further risk for patients with pre-existing seizures or creatinine clearance abnormalities when dosed appropriate."	( A Retrospective Study on the Incidence of Seizures among Neurosurgical Patients Who Treated with Imipenem/Cilastatin or Meropenem. Chen, K; Shi, Z; Wang, Q; Wu, Y, 2014)	0.4
" Therapeutic drug monitoring (TDM) may aid antibiotic prescription and implementation of initial empirical antimicrobial dosage recommendations."	( Impact of the introduction of real-time therapeutic drug monitoring on empirical doses of carbapenems in critically ill burn patients. Decosterd, LA; Eggimann, P; Fournier, A; Marchetti, O; Pagani, JL; Pannatier, A; Que, YA; Revelly, JP; Voirol, P, 2015)	0.42
"Imipenem/cilastatin and meropenem use and daily empirical dosage at a five-bed burn ICU were analyzed retrospectively."	( Impact of the introduction of real-time therapeutic drug monitoring on empirical doses of carbapenems in critically ill burn patients. Decosterd, LA; Eggimann, P; Fournier, A; Marchetti, O; Pagani, JL; Pannatier, A; Que, YA; Revelly, JP; Voirol, P, 2015)	0.42
"Real-time carbapenem TDM availability significantly altered the empirical daily dosage of imipenem/cilastatin at our burn ICU."	( Impact of the introduction of real-time therapeutic drug monitoring on empirical doses of carbapenems in critically ill burn patients. Decosterd, LA; Eggimann, P; Fournier, A; Marchetti, O; Pagani, JL; Pannatier, A; Que, YA; Revelly, JP; Voirol, P, 2015)	0.42
" Study PN019 evaluated the PK of REL (250 mg) and imipenem (500 mg; dosed as IMI) with/without probenecid (1 g; OAT inhibitor) in healthy adults."	( Impact of renal impairment and human organic anion transporter inhibition on pharmacokinetics, safety and tolerability of relebactam combined with imipenem and cilastatin. Bhagunde, P; Boundy, K; Butterton, JR; Colon-Gonzalez, F; Garrett, G; Jumes, P; Lala, M; Lasseter, K; Liu, Y; Marbury, T; Rhee, EG; Rizk, ML; Wu, J; Xu, SS, 2020)	0.56
" Hence, there is a strong rationale to individualize anti-infective dosing in these patients by using therapeutic drug monitoring (TDM)."	( Determination of Total and Unbound Meropenem, Imipenem/Cilastatin, and Cefoperazone/Sulbactam in Human Plasma: Application for Therapeutic Drug Monitoring in Critically Ill Patients. Dang, ZL; Li, B; Qin, HY; Rao, Z; Wei, YH; Wu, XA; Zhu, L, 2020)	0.56
" Available clinical and pharmacokinetic data support the approved dosage of a 30-minute infusion of imipenem 500 mg-cilastatin 500 mg-relebactam 250 mg every 6 hours, along with dosage adjustments based on renal function."	( Imipenem-Cilastatin-Relebactam: A Novel β-Lactam-β-Lactamase Inhibitor Combination for the Treatment of Multidrug-Resistant Gram-Negative Infections. Claeys, KC; Rybak, JM; Smith, JR, 2020)	0.56
"This phase 3, multicenter, open-label, noncomparative study (NCT03293485) evaluated relebactam/imipenem/cilastatin (250 mg/500 mg/500 mg) dosed every 6 h for 5-14 days in Japanese patients with complicated intra-abdominal infections (cIAIs) or complicated urinary tract infections (cUTIs), including those with secondary sepsis."	( The safety and efficacy of relebactam/imipenem/cilastatin in Japanese patients with complicated intra-abdominal infection or complicated urinary tract infection: A multicenter, open-label, noncomparative phase 3 study. Aoyama, N; Bando, H; Brown, M; Kawahara, K; Kikukawa, H; Kohno, S; Paschke, A; Shirakawa, M; Takase, A; Yoneyama, F, 2021)	0.62
" At the recommended IMI/REL dosing regimens across renal categories, greater than 90% of patients in all renal function groups were predicted to achieve joint pharmacokinetic/pharmacodynamic targets at a minimum inhibitory concentration breakpoint of ≤2 μg/ml, regardless of ventilation status."	( Population pharmacokinetic/pharmacodynamic assessment of imipenem/cilastatin/relebactam in patients with hospital-acquired/ventilator-associated bacterial pneumonia. Bellanti, F; Copalu, W; Daryani, NM; Gheyas, F; Hilbert, DW; Kulkarni, P; Noormohamed, N; Patel, M; Rizk, ML; Young, K, 2022)	0.72
" IMI/REL is a therapeutic option in HAP and VAP at approved dosage imipenem 500 mg, cilastatin 500 mg and relebactam 250 mg once every 6h, by an IV infusion over 30 min."	( New evidence in severe pneumonia: imipenem/ cilastatin/relebactam. Alarcón, T; Girón, RM; Gómez-Punter, RM; Ibáñez, A, 2022)	0.72
"Despite enhanced clearance of both imipenem and relebactam, the currently approved dosing regimen for normal renal function was predicted to achieve optimal exposure in critically-ill patients with ARC sufficient to treat most susceptible pathogens."	( Imipenem/cilastatin/relebactam pharmacokinetics in critically ill patients with augmented renal clearance. Fratoni, AJ; Kuti, JL; Mah, JW; Nicolau, DP, 2022)	0.72

Role	Description
protease inhibitor	A compound which inhibits or antagonizes the biosynthesis or actions of proteases (endopeptidases).
EC 3.4.13.19 (membrane dipeptidase) inhibitor	An EC 3.4.13.* (dipeptidase) inhibitor that interferes with the action of membrane dipeptidase (EC 3.4.13.19).
xenobiotic	A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
environmental contaminant	Any minor or unwanted substance introduced into the environment that can have undesired effects.
[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]

Class	Description
non-proteinogenic L-alpha-amino acid	Any L-alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
L-cysteine derivative	A proteinogenic amino acid derivative resulting from the formal reaction of L-cysteine at the amino group, carboxy group, or thiol group, or from the replacement of any hydrogen of L-cysteine by a heteroatom.
organic sulfide	Compounds having the structure RSR (R =/= H). Such compounds were once called thioethers.
carboxamide	An amide of a carboxylic acid, having the structure RC(=O)NR2. The term is used as a suffix in systematic name formation to denote the -C(=O)NH2 group including its carbon atom.
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
phosphopantetheinyl transferase	Bacillus subtilis	Potency	79.4328	0.1413	37.9142	100.0000	AID1490
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Solute carrier family 22 member 6	Rattus norvegicus (Norway rat)	IC50 (µMol)	2,387.0000	0.5000	0.5000	0.5000	AID680339
Beta-2 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	0.0005	0.3546	1.6000	AID218702
Beta-1 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	0.0000	0.6673	10.0000	AID218702
Dipeptidase 1	Sus scrofa (pig)	Ki	0.1700	0.1100	0.1700	0.2100	AID218702
Beta-3 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	0.0005	0.3367	1.6000	AID218702
Solute carrier family 22 member 6	Homo sapiens (human)	IC50 (µMol)	2,550.0000	0.2700	4.5306	9.9000	AID682026
Solute carrier family 22 member 6	Homo sapiens (human)	Ki	1,470.0000	0.0300	3.2043	7.8200	AID678999
Solute carrier family 22 member 8	Homo sapiens (human)	IC50 (µMol)	249.0000	4.9300	7.3900	9.9200	AID678815
Solute carrier family 22 member 8	Homo sapiens (human)	Ki	231.0000	0.0400	4.2297	9.0000	AID678987
Solute carrier family 22 member 8	Rattus norvegicus (Norway rat)	IC50 (µMol)	742.0000	6.0300	6.0300	6.0300	AID678805
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
monoatomic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
response to organic cyclic compound	Solute carrier family 22 member 6	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
organic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 6	Homo sapiens (human)
alpha-ketoglutarate transport	Solute carrier family 22 member 6	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 6	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 6	Homo sapiens (human)
metanephric proximal tubule development	Solute carrier family 22 member 6	Homo sapiens (human)
renal tubular secretion	Solute carrier family 22 member 6	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 8	Homo sapiens (human)
response to toxic substance	Solute carrier family 22 member 8	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 8	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 8	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
solute:inorganic anion antiporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
protein binding	Solute carrier family 22 member 6	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
antiporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
chloride ion binding	Solute carrier family 22 member 6	Homo sapiens (human)
identical protein binding	Solute carrier family 22 member 6	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
caveola	Solute carrier family 22 member 6	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 6	Homo sapiens (human)
protein-containing complex	Solute carrier family 22 member 6	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID678999	TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	2001	European journal of pharmacology, May-11, Volume: 419, Issue:2-3	Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters.
AID409957	Inhibition of bovine liver MAOA	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug 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.
AID678962	TP_TRANSPORTER: inhibition of PGF2alpha uptake in OAT2-expressing S2 cells	2002	The Journal of pharmacology and experimental therapeutics, Jun, Volume: 301, Issue:3	Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors.
AID678805	TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells	2004	Journal of pharmacological sciences, Feb, Volume: 94, Issue:2	Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID218702	Inhibitory activity against beta-lactamase renal dipeptidase	1987	Journal of medicinal chemistry, Jun, Volume: 30, Issue:6	Inhibition of the mammalian beta-lactamase renal dipeptidase (dehydropeptidase-I) by (Z)-2-(acylamino)-3-substituted-propenoic acids.
AID540212	Mean residence time in human after iv administration	2008	Drug 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.
AID409954	Inhibition of mouse brain MAOA	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID409956	Inhibition of mouse brain MAOB	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID540213	Half life in human after iv administration	2008	Drug 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.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID680339	TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells	2004	Journal of pharmacological sciences, Feb, Volume: 94, Issue:2	Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID678815	TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells	2004	Journal of pharmacological sciences, Feb, Volume: 94, Issue:2	Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID682026	TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells	2004	Journal of pharmacological sciences, Feb, Volume: 94, Issue:2	Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID409959	Inhibition of bovine liver MAOB	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID540210	Clearance in human after iv administration	2008	Drug 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.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID540211	Fraction unbound in human after iv administration	2008	Drug 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.
AID678987	TP_TRANSPORTER: inhibition of E1S uptake in OAT3-expressing S2 cells	2001	European journal of pharmacology, May-11, Volume: 419, Issue:2-3	Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters.
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	279 (30.53)	18.7374
1990's	325 (35.56)	18.2507
2000's	158 (17.29)	29.6817
2010's	110 (12.04)	24.3611
2020's	42 (4.60)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	270 (27.03%)	5.53%
Reviews	64 (6.41%)	6.00%
Case Studies	141 (14.11%)	4.05%
Observational	0 (0.00%)	0.25%
Other	524 (52.45%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (37)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Linezolid Alone or Combined With Carbapenem Against Methicillin-resistant Staphylococcus Aureus (MRSA) in Vitro and in Ventilator-associated Pneumonia [NCT01356472]	Phase 4	60 participants (Anticipated)	Interventional	2011-06-30	Not yet recruiting
Pharmacokinetics/Pharmacodynamics and Clinical Outcomes of β-lactams in Critically Ill Patients [NCT03858387]		102 participants (Anticipated)	Observational	2018-09-01	Recruiting
A Phase III Non-randomized, Non-controlled, Open Label Clinical Trial to Study the Safety and Efficacy of Imipenem/Cilastatin/Relebactam (IMI/REL [MK-7655A]) in Japanese Subjects With Complicated Intra-Abdominal Infection (cIAI) or Complicated Urinary Tra [NCT03293485]	Phase 3	83 participants (Actual)	Interventional	2017-10-04	Completed
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]	Early Phase 1	11 participants (Actual)	Interventional	2014-03-06	Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Multicenter, Randomized, Double-Blind, Comparative, Phase 3 Study to Evaluate the Efficacy and Safety of Intravenous Imipenem/Cilastatin/XNW4107 in Comparison With Imipenem/Cilastatin/Relebactam in Adults With Hospital-Acquired Bacterial Pneumonia or Ve [NCT05204563]	Phase 3	450 participants (Anticipated)	Interventional	2022-07-31	Recruiting
A Multi-center, Randomized, Double-blind, Active Controlled, Parallel Groups, Phase II Study to Evaluate the Efficacy and Safety of Intravenous HRS-8427 in the Treatment of Adults With Complicate Urinary Tract Infection, Including Acute Pyelonephritis [NCT06144060]	Phase 2	126 participants (Anticipated)	Interventional	2023-12-31	Not yet recruiting
Short Versus Extended Antibiotic Treatment With a Carbapenem for High-risk Febrile Neutropenia in Hematology Patients With Fever of Unknown Origin: a Randomized Multicenter Non-inferiority Trial. [NCT02149329]	Phase 4	276 participants (Actual)	Interventional	2014-12-31	Completed
A Randomized, Active-controlled Study to Evaluate the Efficacy and Safety of Intravenous Sulbactam-ETX2514 in the Treatment of Patients With Infections Caused by Acinetobacter Baumannii-calcoaceticus Complex [NCT03894046]	Phase 3	207 participants (Actual)	Interventional	2019-09-05	Completed
A Phase 2, Multicenter, Randomized, Double-Blind, Comparative Study Of The Safety And Efficacy of 2 Doses Of Tigecycline Versus Imipenem/Cilastatin For The Treatment Of Subjects With Hospital-Acquired Pneumonia [NCT00707239]	Phase 2	108 participants (Actual)	Interventional	2008-12-31	Terminated(stopped due to See termination reason in detailed description.)
A Phase 3, Multi-Center, Randomized, Double-Blind Study to Evaluate the Efficacy and Safety of Cefepime/Nacubactam or Aztreonam/Nacubactam Compared to Imipenem/Cilastatin in the Treatment of Complicated Urinary Tract Infections or Acute Uncomplicated Pyel [NCT05887908]	Phase 3	600 participants (Anticipated)	Interventional	2023-05-23	Recruiting
A Multicenter, Randomized, Double Blind, Comparative Trial of Intravenous MERREM (Meropenem, ICI 194,660) vs PRIMAXIN I.V. (Imipenem-cilastatin) in the Treatment of Hospitalised Subjects With Complicated Skin and Skin Structure Infections. [NCT00619710]	Phase 3	1,000 participants (Anticipated)	Interventional	2001-02-28	Completed
Pharmacokinetics of Imipenem/Cilastatin/Relebactam in Critically Ill Patients Receiving Extracorporeal Membrane Oxygenation (ECMO) [NCT04493151]	Phase 1	8 participants (Actual)	Interventional	2021-01-01	Completed
A Randomized, Open-Label, Multicenter Study to Assess the Safety and Tolerability of Doripenem Compared With Imipenem in the Treatment of Subjects With Complicated Intra-Abdominal Infections or Ventilator Associated Pneumonia [NCT00515034]	Phase 2	146 participants (Actual)	Interventional	2007-10-31	Completed
Prospective, Multicenter, Investigator-blinded, Randomized, Comparative Study Estimate Safety, Tolerability, Efficacy of NXL104/Ceftazidime vs. Comparator Followed Appropriate Oral Therapy Treatment Complicated UTI Hosp Adults [NCT00690378]	Phase 2	137 participants (Actual)	Interventional	2008-11-30	Completed
A Prospective, Randomized, Double-Blind, Double-Dummy, Multicenter Study to Assess the Safety and Efficacy of Doripenem Compared With Imipenem-Cilastatin in the Treatment of Subjects With Ventilator-Associated Pneumonia [NCT00589693]	Phase 3	274 participants (Actual)	Interventional	2008-04-30	Terminated(stopped due to Observed lower cure rates and higher mortality rates in one of the treatment groups.)
An Investigator Initiated, Phase IV Single-Center, Randomized, Open-Label, Prospective Study to Determine the Impact of Serial Procalcitonin on Improving Antimicrobial Stewardship and on the Efficacy, Safety, and Tolerability of Imipenem - Relebactam Plus [NCT04983901]	Phase 2	100 participants (Actual)	Interventional	2021-09-14	Active, not recruiting
Imipenem Prophylaxis of Infectious Complications in Patients With Acute Pancreatitis [NCT02897206]	Phase 4	98 participants (Actual)	Interventional	2014-10-31	Completed
A De-Escalating Strategy for Antibiotic Treatment of Pneumonia in The Medical Intensive Care Unit [NCT00445094]	Phase 4	120 participants (Actual)	Interventional	2006-11-30	Completed
Impact of Obesity on the Pharmacokinetics of Imipenem-Relebactam in ICU Patients [NCT05146154]	Phase 4	12 participants (Anticipated)	Interventional	2023-01-01	Enrolling by invitation
A Phase I, Double-blind, Randomized, Placebo-controlled Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Intravenous ETX2514 Administered in Healthy Subjects [NCT02971423]	Phase 1	124 participants (Actual)	Interventional	2016-10-31	Completed
A Double-blind, Randomized, Placebo-controlled Study to Evaluate the Safety and Efficacy of Intravenous Sulbactam-ETX2514 in the Treatment of Hospitalized Adults With Complicated Urinary Tract Infections, Including Acute Pyelonephritis [NCT03445195]	Phase 2	80 participants (Actual)	Interventional	2018-01-17	Completed
A Phase 3, Multicenter, Randomized, Double-Blind, Comparative Study Of The Efficacy And Safety Of Tigecycline Vs Imipenem/Cilastatin For The Treatment Of Subjects With Nosocomial Pneumonia [NCT00080496]	Phase 3	430 participants	Interventional	2003-07-31	Completed
A PHASE 1, OPEN-LABEL STUDY TO EVALUATE THE PHARMACOKINETICS AND SAFETY OF XNW4107, IMIPENEM AND CILASTATIN ADMINISTERED CONCURRENTLY AS INTRAVENOUS INFUSION TO SUBJECTS WITH VARIOUS DEGREES OF RENAL FUNCTION [NCT04787562]	Phase 1	39 participants (Actual)	Interventional	2021-02-25	Completed
A Phase III, Randomized, Double-Blind, Active Comparator-Controlled Clinical Trial to Estimate the Efficacy and Safety of Imipenem/Cilastatin/Relebactam (MK-7655A) Versus Colistimethate Sodium + Imipenem/Cilastatin in Subjects With Imipenem-Resistant Bact [NCT02452047]	Phase 3	50 participants (Actual)	Interventional	2015-08-21	Completed
A Phase 1, Single-Dose, Randomized, Double Blind, Placebo-Controlled Study to Evaluate Pharmacokinetics, Safety and Tolerability of XNW4107 for Injection in Healthy Adult Young Females and in Healthy Adult Elderly Males and Females. [NCT04801043]	Phase 1	24 participants (Actual)	Interventional	2021-03-02	Completed
A Phase 1, Open-label Study to Evaluate the Safety and Intrapulmonary Pharmacokinetics of XNW4107, Imipenem and Cilastatin in Healthy Subjects [NCT04802863]	Phase 1	21 participants (Actual)	Interventional	2021-03-25	Completed
A Phase II, Randomized, Active Comparator-Controlled Clinical Trial to Study the Safety, Tolerability, and Efficacy of MK-7655 + Imipenem/Cilastatin Versus Imipenem/Cilastatin Alone in Patients With Complicated Intra-Abdominal Infection [cIAI] [NCT01506271]	Phase 2	351 participants (Actual)	Interventional	2012-06-01	Completed
A Randomised, Double-blind, Dose-finding, Multicenter Study of the Safety, Tolerability, and Efficacy of GSK2251052 Therapy Compared to Imipenem-cilastatin in the Treatment of Adult Subjects With Febrile Complicated Lower Urinary Tract Infections and Acut [NCT01381549]	Phase 2	20 participants (Actual)	Interventional	2011-06-28	Terminated(stopped due to Microbiological findings of resistance on therapy in patients with complicated urinary tract infection)
A Multicenter, Double-blind, Randomized, Comparison Study Of The Efficacy And Safety Of Tigecycline To Imipenem/Cilastatin To Treat Complicated Intra-abdominal Infections In Hospitalized Subjects. [NCT01721408]	Phase 4	470 participants (Actual)	Interventional	2012-11-30	Completed
A Phase 3, Randomized, Double-blind, Double-dummy, Multicenter, Multinational Study to Assess the Efficacy and Safety of Orally Administered Tebipenem Pivoxil Hydrobromide (TBP-PI-HBr) Compared to Intravenously Administered Imipenem-cilastatin in Patients [NCT06059846]	Phase 3	2,648 participants (Anticipated)	Interventional	2023-11-30	Not yet recruiting
A Multicenter, Randomized, Double-Blind, Double-Dummy, Comparative, Phase 3 Study to Evaluate the Efficacy and Safety of Intravenous Imipenem/Cilastatin/XNW4107 in Comparison With Meropenem in Hospitalized Adults With Complicated Urinary Tract Infections, [NCT05204368]	Phase 3	780 participants (Anticipated)	Interventional	2023-03-30	Not yet recruiting
A Single-Dose Study to Investigate the Pharmacokinetics of MK-7655 in Subjects With Impaired Renal Function [NCT01275170]	Phase 1	49 participants (Actual)	Interventional	2011-01-28	Completed
A Phase III, Randomized, Double-Blind, Active Comparator-Controlled Clinical Trial to Study the Safety, Tolerability, and Efficacy of Imipenem/Cilastatin/Relebactam (MK-7655A) Versus Piperacillin/Tazobactam in Subjects With Hospital-Acquired Bacterial Pne [NCT02493764]	Phase 3	537 participants (Actual)	Interventional	2015-11-24	Completed
A Multicenter, Open-label Study to Determine the Pharmacokinetics, Safety, and Outcomes of Imipenem/Cilastatin/Relebactam During Treatment of Acute Pulmonary Exacerbations in Adolescent and Adult Patients With Cystic Fibrosis [NCT05561764]	Phase 4	16 participants (Anticipated)	Interventional	2023-01-03	Recruiting
A Phase II, Randomized, Active Comparator-Controlled Clinical Trial to Study the Safety, Tolerability, and Efficacy of MK-7655 + Imipenem/Cilastatin Versus Imipenem/Cilastatin Alone in Patients With Complicated Urinary Tract Infection (cUTI) [NCT01505634]	Phase 2	302 participants (Actual)	Interventional	2012-05-16	Completed
A Multicenter, Double-blind, Randomized, Clinical Study to Assess the Efficacy and Safety of Intravenous S-649266 in Complicated Urinary Tract Infections With or Without Pyelonephritis or Acute Uncomplicated Pyelonephritis Caused by Gram-Negative Pathogen [NCT02321800]	Phase 2	452 participants (Actual)	Interventional	2015-02-05	Completed
Dose Escalating Study to Evaluate the Safety, Tolerability and Pharmacokinetic Profile of an Infusion of Cilastatin in Healthy Volunteers. [NCT03595189]	Phase 1	23 participants (Actual)	Interventional	2018-06-19	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00515034 (3) [back to overview]	Patients With VAP Who Were Clinically Cured
NCT00515034 (3) [back to overview]	Patients With cIAI Who Were Clinically Cured
NCT00515034 (3) [back to overview]	Patients With Incidence of Treatment-emergent Adverse Events (TEAEs).
NCT00589693 (5) [back to overview]	28-day All-cause Mortality Rate
NCT00589693 (5) [back to overview]	Clinical Cure Rate at the End-of-treatment (EOT) Visit
NCT00589693 (5) [back to overview]	Clinical Cure Rate at the End-of-treatment (EOT) Visit in Patients From Whom a Qualifying P. Aeruginosa Was Isolated at Baseline
NCT00589693 (5) [back to overview]	Clinical Cure Rate at the End-of-treatment (EOT) Visit in Patients From Whom at Least 1 of the Gram-negative Qualifying Pneumonia Pathogens (Enterobacteriaceae, P. Aeruginosa, and Acinetobacter Spp) Was Isolated at Baseline
NCT00589693 (5) [back to overview]	Number of Patients Who Had Emergence of P. Aeruginosa Resistance
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the LFU Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the LFU Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the LFU Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the LFU Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen E. Cloacae in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen E. Cloacae in ME Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome in ME Patients at the End of IV Therapy Visit
NCT00690378 (20) [back to overview]	Clinical Outcome in CE Patients at the Late Follow-up (LFU) Visit
NCT00690378 (20) [back to overview]	Clinical Outcome in CE Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Clinical Outcome in Clinically Evaluable (CE) Patients at the End of Intravenous (IV) Therapy Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the TOC Visit
NCT00690378 (20) [back to overview]	Microbiological Outcome in ME Patients at the LFU Visit
NCT00690378 (20) [back to overview]	Number of Participants With Microbiological Outcome at the Test of Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Duration of Intravenous Antibiotic Treatment, Hospital and Intensive Care Unit (ICU) Stay
NCT00707239 (17) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Tigecycline
NCT00707239 (17) [back to overview]	Number of Participants Who Experienced Nausea or Vomiting
NCT00707239 (17) [back to overview]	Percentage of Participants With Clinical Response in Clinical Modified Intent-to-treat (c-mITT) Population at Test-of-Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Percentage of Participants With Clinical Response in Clinically Evaluable (CE) Population at Test-of-Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Percentage of Participants With Clinical Response in Ventilator Associated Pneumonia (VAP) and Non-VAP Participants at Test-of-Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Percentage of Participants With Microbiological Response at the Participant Level Population at Test-of-Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Percentage of Participants With Microbiological Response at the Pathogen Level Population at Test-of-Cure (TOC) Visit
NCT00707239 (17) [back to overview]	Maximum Observed Plasma Concentration of Procalcitonin (Cmaxpd) and Predicted Procalcitonin Plasma Concentration at 24 Hours (Cpd,24) and 48 Hours (Cpd,48)
NCT00707239 (17) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-12)] of Tigecycline
NCT00707239 (17) [back to overview]	Clearance (CL) of Tigecycline
NCT00707239 (17) [back to overview]	Maximum Observed Serum Concentration (Cmax) of Tigecycline
NCT00707239 (17) [back to overview]	Number of Participants With Abnormal Electrocardiogram (ECG)
NCT00707239 (17) [back to overview]	Number of Participants With Abnormal Laboratory Examinations
NCT00707239 (17) [back to overview]	Time to Reach Maximum Observed Serum Concentration (Tmax) of Tigecycline
NCT00707239 (17) [back to overview]	Correlation of AUC (0-24) of Tigecycline With Nausea and Vomiting
NCT00707239 (17) [back to overview]	Correlation of AUC(0-24) to Minimum Inhibitory Concentration (MIC) Ratio (AUC [0-24]/MIC) of Tigecycline With Clinical Outcome
NCT01275170 (27) [back to overview]	Parts 1 and 2: Percentage of Participants With ≥1 Adverse Events (AEs)
NCT01275170 (27) [back to overview]	Part 1: Apparent t½ of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Apparent t½ of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Area Under the Plasma Concentration-time Curve From Dosing to Infinity (AUC0-inf) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: AUC0-inf of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: CLpred of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Ceoi of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Apparent Plasma Half-life (t½) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: CLpred of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: AUC0-inf of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Ceoi of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: CLR of Cilastin in Urine
NCT01275170 (27) [back to overview]	Part 1: CLR of Imipenem in Urine
NCT01275170 (27) [back to overview]	Part 1: Concentration at End of Infusion (Ceoi) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: Predicted Clearance (CLpred) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: Predicted Volume of Distribution During the Terminal Phase (VZpred) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: Renal Clearance (CLR) of MK-7655 in Urine
NCT01275170 (27) [back to overview]	Part 1: Time of Maximum Plasma Concentration (Tmax) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]	Part 1: Tmax of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: Tmax of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: VZpred of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 1: VZpred of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]	Part 2: Plasma AUC0-∞ of Caffeine as a Probe Substrate of Cytochrome P450 Enzyme (CYP)1A2
NCT01275170 (27) [back to overview]	Part 2: Plasma AUC0-∞ of Midazolam as a Probe Substrate of Cytochrome P450 Enzyme (CYP)3A4
NCT01275170 (27) [back to overview]	Part 2: Plasma AUC0-∞ of Omeprazole as a Probe Substrate of Cytochrome P450 Enzyme (CYP)2C19
NCT01275170 (27) [back to overview]	Dialysis Clearance (CLD) of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)
NCT01275170 (27) [back to overview]	Extraction Coefficient of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Red Blood Cell (RBC) Count and Reticulocytes
NCT01381549 (34) [back to overview]	Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Alanine Amino Transferase (ALT), Alkaline Phosphatase (ALP), Aspartate Amino Transferase (AST), Creatine Kinase and Gamma Glutamyl Transferase (GGT)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Alanine Amino Transferase (ALT), Alkaline Phosphatase (ALP), Aspartate Amino Transferase (AST), Creatine Kinase and Gamma Glutamyl Transferase (GGT)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Albumin and Total Protein
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Albumin and Total Protein
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Calcium, Carbon-dioxide (C02) Content/Bicarbonate, Chloride, Glucose, Potassium, Sodium and Urea/Blood Urea Nitrogen (BUN)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Calcium, Carbon-dioxide (C02) Content/Bicarbonate, Chloride, Glucose, Potassium, Sodium and Urea/Blood Urea Nitrogen (BUN)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Creatinine Clearance, Estimated (CCE)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Creatinine Clearance, Estimated (CCE)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Creatinine Clearance, Estimated (CCE)
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Creatinine, Direct Bilirubin and Total Bilirubin
NCT01381549 (34) [back to overview]	Change From Baseline in Clinical Laboratory Parameters- Creatinine, Direct Bilirubin and Total Bilirubin
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Basophils, Eosinophils, Lymphocytes, Monocytes, Platelet Count, Total Neutrophils and White Blood Cell Count (WBC)
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Hematocrit
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Hemoglobin and Mean Corpuscle Hemoglobin Concentration (MCHC)
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Mean Corpuscle Hemoglobin (MCH)
NCT01381549 (34) [back to overview]	Change From Baseline in Hematology Parameters- Mean Corpuscle Volume (MCV)
NCT01381549 (34) [back to overview]	Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Heart Rate
NCT01381549 (34) [back to overview]	Therapeutic Response (Combined Clinical and Microbiological Response) at the End of IV Visit and Late Follow-Up Visit
NCT01381549 (34) [back to overview]	Microbiological Response at the End of IV Therapy Visit, Test of Cure Visit and Late Follow-Up Visit
NCT01381549 (34) [back to overview]	Clinical Response at the End of IV Therapy Visit, Test of Cure Visit and Late Follow-Up Visit
NCT01381549 (34) [back to overview]	Summary of Vital Signs: Mean Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT01381549 (34) [back to overview]	Summary of Vital Signs: Mean Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT01381549 (34) [back to overview]	Summary of Vital Signs: Mean Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Temperature
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Temperature
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Temperature
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Respiration Rate
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Respiration Rate
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Respiration Rate
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Heart Rate
NCT01381549 (34) [back to overview]	Summary of Vital Signs- Mean Heart Rate
NCT01505634 (16) [back to overview]	Percentage of Participants With Specific AEs With Incidence of >= 4 Participants in One Treatment Group
NCT01505634 (16) [back to overview]	Percentage of Participants Who Discontinued IV Study Therapy Due to a Drug-related AE
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Completion of IV Study Therapy
NCT01505634 (16) [back to overview]	Percentage of Participants With a Drug-related SAE
NCT01505634 (16) [back to overview]	Percentage of Participants Who Discontinued IV Study Therapy Due to an AE
NCT01505634 (16) [back to overview]	Percentage of Participants With Any Drug-related AE
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Early Follow-up
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Late Follow-up
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Completion of IV Study Therapy
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Completion of IV Study Therapy Who Had Imipenem-resistant, Gram-negative cUTI Infections.
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Early Follow-up
NCT01505634 (16) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Late Follow-up
NCT01505634 (16) [back to overview]	Percentage of Participants With an Elevated Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) Laboratory Value That Was Greater Than or Equal to 5 Times the Upper Limit of Normal (ULN)
NCT01505634 (16) [back to overview]	Percentage of Participants With Any Serious Adverse Event (SAE)
NCT01505634 (16) [back to overview]	Percentage of Participants With at Least 1 Adverse Event (AE)
NCT01505634 (16) [back to overview]	Percentage of Participants With Elevated AST or ALT Laboratory Values ≥ 3 Times the ULN, as Well as Elevated Total Bilirubin ≥ 2 Times the ULN, and Alkaline Phosphatase Values That Were < 2 Times the ULN
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Early Follow-up
NCT01506271 (18) [back to overview]	Percentage of Participants With an Elevated Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) Laboratory Values That Are Greater Than or Equal to 5X the Upper Limit of Normal (ULN)
NCT01506271 (18) [back to overview]	Percentage of Participants With Any Adverse Event (AE)
NCT01506271 (18) [back to overview]	Percentage of Participants With Elevated AST or ALT Laboratory Values >= 3X the ULN, Total Bilirubin >= 2X the ULN, and Alkaline Phosphatase Values < 2X the ULN
NCT01506271 (18) [back to overview]	Percentage of Participants With Specific AEs With Incidence of >= 4 Participants in One Treatment Group
NCT01506271 (18) [back to overview]	Percentage of Participants With Any Drug-related SAE
NCT01506271 (18) [back to overview]	Percentage of Participants With Any Serious Adverse Event (SAE)
NCT01506271 (18) [back to overview]	Percentage of Participants With Predefined Limit of Change (PDLC) With Incidence of >= 4 Participants in One Treatment Group
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Late Follow-up
NCT01506271 (18) [back to overview]	Percentage of Participants With System Organ Class (SOC) With AEs With Incidence of >= 4 Participants in One Treatment Group
NCT01506271 (18) [back to overview]	Percentage of Participants Who Discontinued IV Study Therapy Due to a Drug-related AE
NCT01506271 (18) [back to overview]	Percentage of Participants Who Discontinued IV Study Therapy Due to an AE
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Completion of IV Study Therapy
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Completion of IV Study Therapy in Participants Who Have Imipenem-resistant, Gram-negative cIAI Infections.
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Early Follow-up
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Clinical Response at Late Follow-up
NCT01506271 (18) [back to overview]	Percentage of Participants With a Favorable Microbiological Response at Completion of IV Study Therapy
NCT01506271 (18) [back to overview]	Percentage of Participants With Any Drug-related AE
NCT01721408 (5) [back to overview]	Microbiological Response at the Subject Level in the ME Population at the TOC Assessment
NCT01721408 (5) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (AEs) by Relationship and Seriousness
NCT01721408 (5) [back to overview]	Clinical Response at the TOC Assessment Within the Modified Intent-to-Treat (mITT) Population
NCT01721408 (5) [back to overview]	Clinical Response at the TOC Assessment Within the Microbiologically Evaluable (ME) Population
NCT01721408 (5) [back to overview]	Clinical Response at the Test-of-Cure (TOC) Assessment Within the Clinically Evaluable (CE) Population
NCT02321800 (23) [back to overview]	Urine Concentration of Cefiderocol
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Early Assessment
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at End of Treatment
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Follow-up
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Test of Cure
NCT02321800 (23) [back to overview]	Percentage of Participants With Composite Response of Microbiological Eradication and Clinical Response at Early Assessment
NCT02321800 (23) [back to overview]	Percentage of Participants With Composite Response of Microbiological Eradication and Clinical Response at End of Treatment
NCT02321800 (23) [back to overview]	Percentage of Participants With Composite Response of Microbiological Eradication and Clinical Response at Follow-up
NCT02321800 (23) [back to overview]	Percentage of Participants With Composite Response of Microbiological Eradication and Clinical Response at Test of Cure
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Early Assessment
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at End of Treatment
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Follow-up
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Test of Cure
NCT02321800 (23) [back to overview]	Number of Participants With Adverse Events
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Early Assessment Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at End of Treatment Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Follow-up Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Clinical Response at Test of Cure Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Early Assessment Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at End of Treatment Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Follow-up Per Uropathogen
NCT02321800 (23) [back to overview]	Percentage of Participants With Microbiological Eradication at Test of Cure Per Uropathogen
NCT02321800 (23) [back to overview]	Plasma Concentration of Cefiderocol
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Drug-Related AEs
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Drug-Related SAEs
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Events of Treatment-Emergent Nephrotoxicity
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Serious Adverse Events (SAEs)
NCT02452047 (18) [back to overview]	Percentage of Participants With All-cause Mortality Up to Day 28
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Events of Clinical Interest (ECI)
NCT02452047 (18) [back to overview]	Percentage of Participants With Favorable Overall Response (FOR)
NCT02452047 (18) [back to overview]	Analysis of Specific AEs With an Incidence of ≥4 Participants in a Treatment Group
NCT02452047 (18) [back to overview]	Percentage of Participants With FCR on Therapy (OTX)
NCT02452047 (18) [back to overview]	Percentage of Participants With FCR at End of Therapy (EOT)
NCT02452047 (18) [back to overview]	Percentage of Participants With Favorable Clinical Response (FCR) at Day 28
NCT02452047 (18) [back to overview]	Percentage of Participants With FCR at EFU
NCT02452047 (18) [back to overview]	Percentage of Participants Discontinuing From Study Therapy Due to ≥1 Drug-Related AEs
NCT02452047 (18) [back to overview]	Percentage of Participants With ≥1 Adverse Events (AEs)
NCT02452047 (18) [back to overview]	Percentage of Participants Discontinuing From Study Therapy Due to ≥1 AEs
NCT02452047 (18) [back to overview]	Percentage of cUTI Participants With FMR at EOT
NCT02452047 (18) [back to overview]	Percentage of cUTI Participants With FMR at EFU
NCT02452047 (18) [back to overview]	Percentage of cUTI Participants With Favorable Microbiological Response (FMR) at OTX
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a FCR at OTX3 (Day 10)
NCT02493764 (22) [back to overview]	Percentage of Participants in the mMITT Population With a Favorable Microbiological Response (FMR) at End of Treatment (EOT) Visit
NCT02493764 (22) [back to overview]	Percentage of Participants With ≥1 Adverse Event (AE)
NCT02493764 (22) [back to overview]	Percentage of Participants With ACM at EFU in the MITT Population
NCT02493764 (22) [back to overview]	Percentage of Participants With ACM at EFU in the mMITT Population
NCT02493764 (22) [back to overview]	Percentage of Participants With ACM in the Microbiological Modified Intention-to-treat (mMITT) Population
NCT02493764 (22) [back to overview]	Percentage of Participants With All-cause Mortality (ACM) Through Day 28 in the Modified Intention-to-treat (MITT) Population
NCT02493764 (22) [back to overview]	Percentage of Participants in the mMITT Population With a FMR at EFU Visit
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a FCR at Day 28
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a FCR at EOT
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a FCR at OTX1 (Day 3)
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a FCR at OTX2 (Day 6)
NCT02493764 (22) [back to overview]	Percentage of Participants in the CE Population With a FCR at OTX2 (Day 6)
NCT02493764 (22) [back to overview]	Percentage of Participants Discontinuing Study Therapy Due to an AE
NCT02493764 (22) [back to overview]	Percentage of Participants in the CE Population With a FCR at Day 28
NCT02493764 (22) [back to overview]	Percentage of Participants in the CE Population With a FCR at EFU Visit
NCT02493764 (22) [back to overview]	Percentage of Participants in the CE Population With a FCR at EOT Visit
NCT02493764 (22) [back to overview]	Percentage of Participants in the Clinically Evaluable (CE) Population With a FCR at On-therapy Visit 1 (OTX1) [Day 3]
NCT02493764 (22) [back to overview]	Percentage of Participants in the CE Population With a FCR at OTX3 (Day 10)
NCT02493764 (22) [back to overview]	Percentage of Participants in the ME Population With a FMR at EFU Visit
NCT02493764 (22) [back to overview]	Percentage of Participants in the Microbiologically Evaluable (ME) Population With a FMR at EOT Visit
NCT02493764 (22) [back to overview]	Percentage of Participants in the MITT Population With a Favorable Clinical Response (FCR) at Early Follow-up (EFU) Visit
NCT03293485 (6) [back to overview]	Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event (AE)
NCT03293485 (6) [back to overview]	Percentage of Complicated Intra-Abdominal Infection (cIAI) Participants With Favorable Clinical Response at End of Therapy Visit
NCT03293485 (6) [back to overview]	Percentage of Complicated Intra-Abdominal Infection (cIAI) Participants With Favorable Clinical Response at Test of Cure Visit
NCT03293485 (6) [back to overview]	Percentage of Complicated Urinary Tract Infection (cUTI) Participants With Favorable Overall Microbiological Response at End of Therapy Visit
NCT03293485 (6) [back to overview]	Percentage of Complicated Urinary Tract Infection (cUTI) Participants With Favorable Overall Microbiological Response at Test of Cure Visit
NCT03293485 (6) [back to overview]	Percentage of Participants Experiencing ≥1 Adverse Events (AE)
NCT03445195 (3) [back to overview]	Number of Participants With Overall Success
NCT03445195 (3) [back to overview]	Clinical Cure
NCT03445195 (3) [back to overview]	Microbiologic Eradication
NCT03894046 (2) [back to overview]	Proportion of Patients With All-Cause Mortality in CRABC m-MITT Population
NCT03894046 (2) [back to overview]	Proportion of Patients With Nephrotoxicity

Patients With VAP Who Were Clinically Cured

clinical cure is the complete resolution of signs and symptoms of pneumonia or lack of progression of chest x-ray abnormalities to such an extent that no further antimicrobial therapy was necessary. (NCT00515034)
Timeframe: 7 to 14 days after the end of IV therapy

Intervention	participants (Number)
VAP Treated With Doripenem	16
VAP Treated With Imipenem/Cilastatin	7

Intervention	participants (Number)
cIAI Treated With Doripenem	39
cIAI Treated With Imipenem/Cilastatin	9

Intervention	days (Median)
	Intravenous antibiotic treatment (n = 36, 35, 34)	Hospital stay (n = 36, 35, 34)	ICU stay (n = 25, 25, 29)
Imipenem/Cilastatin 1 Gram	8.50	15.50	10.00
Tigecycline 100 mg	9.00	13.00	9.00
Tigecycline 75 mg	8.00	13.00	8.00

Intervention	participants (Number)
	Nausea	Vomiting
Imipenem/Cilastatin 1 Gram	1	4
Tigecycline 100 mg	3	1
Tigecycline 75 mg	1	3

Intervention	percentage of participants (Number)
	Cure	Failure	Indeterminate
Imipenem/Cilastatin 1 Gram	52.9	17.6	29.4
Tigecycline 100 mg	71.4	14.3	14.3
Tigecycline 75 mg	52.8	27.8	19.4

Intervention	percentage of participants (Number)
	VAP: Cure (n = 7, 7, 9)	VAP: Failure (n = 7, 7, 9)	Non-VAP: Cure (n = 16, 13, 15)	Non-VAP: Failure (n = 16, 13, 15)
Imipenem/Cilastatin 1 Gram	77.8	22.2	73.3	26.7
Tigecycline 100 mg	85.7	14.3	84.6	15.4
Tigecycline 75 mg	71.4	28.6	68.8	31.3

Intervention	percentage of participants (Number)
	Eradication	Persistence	Superinfection
Imipenem/Cilastatin 1 Gram	80.0	13.3	6.7
Tigecycline 100 mg	80.0	20.0	0.0
Tigecycline 75 mg	61.5	38.5	0.0

Intervention	percentage of participants (Number)
	Acinetobacter calcoaceticus: Eradication (n=3,2,3)	Acinetobacter calcoaceticus: Persistence (n=3,2,3)	Enterobacter cloacae: Eradication (n=0,0,2)	Enterobacter cloacae: Persistence (n=0,0,2)	Escherichia coli: Eradication (n=1,1,2)	Escherichia coli: Persistence (n=1,1,2)	Haemophilus: Eradication (n=1,0,0)	Haemophilus influenzae: Eradication (n=0,1,1)	Haemophilus influenzae: Persistence (n=0,1,1)	Klebsiella oxytoca: Eradication (n=1,0,0)	Klebsiella pneumoniae: Eradication (n=2,2,5)	Klebsiella pneumoniae: Persistence (n=2,2,5)	Serratia marcescens: Eradication (n=0,2,0)	Staphylococcus aureus (SA): Eradication (n=8,6,9)	SA: Persistence (n=8,6,9)	MRSA:Eradication (n=4,2,4)	MRSA:Persistence (n=4,2,4)	Methicillin-suseptible SA: Eradication (n=4,4,5)	Methicillin-suseptible SA: Persistence (n=4,4,5)	Streptococcus anginosus: Eradication (n=1,0,0)	Streptococcus mitis: Eradication (n=1,0,0)	Streptococcus oralis: Eradication (n=0,0,1)	Streptococcus pneumonia: Eradication (n=1,1,0)
Imipenem/Cilastatin 1 Gram	66.7	33.3	50.0	50.0	50.0	50.0	NA	0	100.0	NA	80.0	20.0	NA	88.9	11.1	100.0	0	80.0	20.0	NA	NA	100.0	NA
Tigecycline 100 mg	50.0	50.0	NA	NA	0	100.0	NA	100.0	0	NA	50.0	50.0	100.0	83.3	16.7	100.0	0	75.0	25.0	NA	NA	NA	100.0
Tigecycline 75 mg	66.7	33.3	NA	NA	0	100.0	100.0	NA	NA	100.0	50.0	50.0	NA	62.5	37.5	50.0	50.0	75.0	25.0	100.0	100.0	NA	100.0

Intervention	ng/mL (Mean)
	Cmax	Cpd,24	Cpd,48
Tigecycline or Imipenem/Cilastatin	2.83	1.86	1.74

Intervention	mg*hr/mL (Mean)
	Experienced nausea (n = 4)	Did not experience nausea (n = 35)	Experienced vomiting (n = 4)	Did not experience vomiting (n = 35)
Tigecycline	8.668	8.206	6.863	8.412

Intervention	ratio (Mean)
	Cure (n = 17)	Failure/indeterminate (n = 8)
Tigecycline	24.3	22.8

Intervention	Percentage of Participants (Number)
Panel A: Mild Renal Impairment	28.6
Panel C: Moderate Renal Impairment	16.7
Panel E: Severe Renal Impairment	16.7
Panel G: ESRD/HD Participants	33.3
Healthy Matched Controls (Part 1)	0.0
Panel E: Severe Renal Impairment (Part 2)	33.3
Panel G: ESRD/HD (Part 2)	33.3
Healthy Matched Controls (Part 2)	0.0

Intervention	hours (Geometric Mean)
Panel A: Mild Renal Impairment	1.43
Panel B: Healthy Controls to Panel A	1.08
Panel C: Moderate Renal Impairment	2.11
Panel D: Healthy Controls to Panel C	1.19
Panel E: Severe Renal Impairment	5.08
Panel F: Healthy Controls to Panel E	1.09
Panel G: ESRD/HD Period 1 Postdialysis	12.2
Panel H: Healthy Controls to Panel G	1.14
Panel G: ESRD/HD Period 2 Predialysis	12.2

Intervention	hours (Geometric Mean)
Panel A: Mild Renal Impairment	1.54
Panel B: Healthy Controls to Panel A	1.24
Panel C: Moderate Renal Impairment	2.18
Panel D: Healthy Controls to Panel C	1.40
Panel E: Severe Renal Impairment	2.78
Panel F: Healthy Controls to Panel E	1.32
Panel G: ESRD/HD Period 1 Postdialysis	3.24
Panel H: Healthy Controls to Panel G	1.21
Panel G: ESRD/HD Period 2 Predialysis	3.20

Intervention	µM*hr (Geometric Mean)
Panel A: Mild Renal Impairment	73.5
Panel B: Healthy Controls to Panel A	45.0
Panel C: Moderate Renal Impairment	115
Panel D: Healthy Controls to Panel C	52.3
Panel E: Severe Renal Impairment	236
Panel F: Healthy Controls to Panel E	48.5
Panel G: ESRD/HD Period 1 Postdialysis	414
Panel H: Healthy Controls to Panel G	44.5
Panel G: ESRD/HD Period 2 Predialysis	78.0

Intervention	µM*hr (Geometric Mean)
Panel A: Mild Renal Impairment	71.7
Panel B: Healthy Controls to Panel A	44.8
Panel C: Moderate Renal Impairment	100.0
Panel D: Healthy Controls to Panel C	53.6
Panel E: Severe Renal Impairment	300
Panel F: Healthy Controls to Panel E	53.7
Panel G: ESRD/HD Period 1 Postdialysis	777
Panel H: Healthy Controls to Panel G	56.5
Panel G: ESRD/HD Period 2 Predialysis	205

Intervention	µM (Geometric Mean)
Panel A: Mild Renal Impairment	43.4
Panel B: Healthy Controls to Panel A	34.8
Panel C: Moderate Renal Impairment	48.7
Panel D: Healthy Controls to Panel C	42.9
Panel E: Severe Renal Impairment	53.3
Panel F: Healthy Controls to Panel E	35.8
Panel G: ESRD/HD Period 1 Postdialysis	111
Panel H: Healthy Controls to Panel G	44.5
Panel G: ESRD/HD Period 2 Predialysis	41.7

Intervention	hours (Geometric Mean)
Panel A: Mild Renal Impairment	2.63
Panel B: Healthy Controls to Panel A	1.75
Panel C: Moderate Renal Impairment	4.51
Panel D: Healthy Controls to Panel C	2.10
Panel E: Severe Renal Impairment	8.65
Panel F: Healthy Controls to Panel E	2.00
Panel G: ESRD/HD Period 1 Postdialysis	15.6
Panel H: Healthy Controls to Panel G	1.79
Panel G: ESRD/HD Period 2 Predialysis	10.5

Intervention	µM*hr (Geometric Mean)
Panel A: Mild Renal Impairment	77.3
Panel B: Healthy Controls to Panel A	55.0
Panel C: Moderate Renal Impairment	101
Panel D: Healthy Controls to Panel C	66.0
Panel E: Severe Renal Impairment	160
Panel F: Healthy Controls to Panel E	63.8
Panel G: ESRD/HD Period 1 Postdialysis	223
Panel H: Healthy Controls to Panel G	71.8
Panel G: ESRD/HD Period 2 Predialysis	71.2

Intervention	µM (Geometric Mean)
Panel A: Mild Renal Impairment	40.7
Panel B: Healthy Controls to Panel A	35.3
Panel C: Moderate Renal Impairment	45.6
Panel D: Healthy Controls to Panel C	42.6
Panel E: Severe Renal Impairment	46.9
Panel F: Healthy Controls to Panel E	35.5
Panel G: ESRD/HD Period 1 Postdialysis	103
Panel H: Healthy Controls to Panel G	41.8
Panel G: ESRD/HD Period 2 Predialysis	35.9

Intervention	mL/min (Geometric Mean)
Panel A: Mild Renal Impairment	99.4
Panel B: Healthy Controls to Panel A	144
Panel C: Moderate Renal Impairment	59.6
Panel D: Healthy Controls to Panel C	136
Panel E: Severe Renal Impairment	24.5
Panel F: Healthy Controls to Panel E	140
Panel H: Healthy Controls to Panel G	146

cilastatin

Cross-References

Synonyms (50)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (4)

Drug Classes (4)

Protein Targets (9)

Potency Measurements

Inhibition Measurements

Biological Processes (14)

Molecular Functions (11)

Ceullar Components (7)

Bioassays (20)

Research

Studies (914)

Study Types

Clinical Trials (37)

Trial Overview

Trial Outcomes

Patients With VAP Who Were Clinically Cured

Patients With cIAI Who Were Clinically Cured

Patients With Incidence of Treatment-emergent Adverse Events (TEAEs).

28-day All-cause Mortality Rate

Clinical Cure Rate at the End-of-treatment (EOT) Visit

Clinical Cure Rate at the End-of-treatment (EOT) Visit in Patients From Whom a Qualifying P. Aeruginosa Was Isolated at Baseline

Clinical Cure Rate at the End-of-treatment (EOT) Visit in Patients From Whom at Least 1 of the Gram-negative Qualifying Pneumonia Pathogens (Enterobacteriaceae, P. Aeruginosa, and Acinetobacter Spp) Was Isolated at Baseline

Number of Patients Who Had Emergence of P. Aeruginosa Resistance

Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the LFU Visit

Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the End of IV Therapy Visit

Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the TOC Visit

Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the LFU Visit

Microbiological Outcome for the Urine Pathogen P. Aeruginosa in ME Patients at the End of IV Therapy Visit

Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the TOC Visit

Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the LFU Visit

Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the End of IV Therapy Visit

Microbiological Outcome for the Urine Pathogen E. Coli in ME Patients at the End of IV Therapy Visit

Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the LFU Visit

Microbiological Outcome for the Urine Pathogen C. Koseri in ME Patients at the TOC Visit

Microbiological Outcome for the Urine Pathogen E. Cloacae in ME Patients at the End of IV Therapy Visit

Microbiological Outcome for the Urine Pathogen E. Cloacae in ME Patients at the TOC Visit

Microbiological Outcome in ME Patients at the End of IV Therapy Visit

Clinical Outcome in CE Patients at the Late Follow-up (LFU) Visit

Clinical Outcome in CE Patients at the TOC Visit

Clinical Outcome in Clinically Evaluable (CE) Patients at the End of Intravenous (IV) Therapy Visit

Microbiological Outcome for the Urine Pathogen P. Mirabilis in ME Patients at the TOC Visit

Microbiological Outcome in ME Patients at the LFU Visit

Number of Participants With Microbiological Outcome at the Test of Cure (TOC) Visit

Duration of Intravenous Antibiotic Treatment, Hospital and Intensive Care Unit (ICU) Stay

Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Tigecycline

Number of Participants Who Experienced Nausea or Vomiting

Percentage of Participants With Clinical Response in Clinical Modified Intent-to-treat (c-mITT) Population at Test-of-Cure (TOC) Visit

Percentage of Participants With Clinical Response in Clinically Evaluable (CE) Population at Test-of-Cure (TOC) Visit

Percentage of Participants With Clinical Response in Ventilator Associated Pneumonia (VAP) and Non-VAP Participants at Test-of-Cure (TOC) Visit

Percentage of Participants With Microbiological Response at the Participant Level Population at Test-of-Cure (TOC) Visit

Percentage of Participants With Microbiological Response at the Pathogen Level Population at Test-of-Cure (TOC) Visit

Maximum Observed Plasma Concentration of Procalcitonin (Cmaxpd) and Predicted Procalcitonin Plasma Concentration at 24 Hours (Cpd,24) and 48 Hours (Cpd,48)

Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-12)] of Tigecycline

Clearance (CL) of Tigecycline

Maximum Observed Serum Concentration (Cmax) of Tigecycline

Number of Participants With Abnormal Electrocardiogram (ECG)

Number of Participants With Abnormal Laboratory Examinations

Time to Reach Maximum Observed Serum Concentration (Tmax) of Tigecycline

Correlation of AUC (0-24) of Tigecycline With Nausea and Vomiting

Correlation of AUC(0-24) to Minimum Inhibitory Concentration (MIC) Ratio (AUC [0-24]/MIC) of Tigecycline With Clinical Outcome

Parts 1 and 2: Percentage of Participants With ≥1 Adverse Events (AEs)

Part 1: Apparent t½ of Cilastin in Combination With MK-7655

Part 1: Apparent t½ of Imipenem in Combination With MK-7655

Part 1: Area Under the Plasma Concentration-time Curve From Dosing to Infinity (AUC0-inf) of MK-7655 in Combination With PRIMAXIN®

Part 1: AUC0-inf of Cilastin in Combination With MK-7655

Part 1: CLpred of Imipenem in Combination With MK-7655

Part 1: Ceoi of Cilastin in Combination With MK-7655

Part 1: Apparent Plasma Half-life (t½) of MK-7655 in Combination With PRIMAXIN®

Part 1: CLpred of Cilastin in Combination With MK-7655

Part 1: AUC0-inf of Imipenem in Combination With MK-7655

Part 1: Ceoi of Imipenem in Combination With MK-7655

Intervention	µM (Geometric Mean)
Panel A: Mild Renal Impairment	22.4
Panel B: Healthy Controls to Panel A	20.4
Panel C: Moderate Renal Impairment	23.5
Panel D: Healthy Controls to Panel C	22.5
Panel E: Severe Renal Impairment	23.6
Panel F: Healthy Controls to Panel E	18.1
Panel G: ESRD/HD Period 1 Postdialysis	53.1
Panel H: Healthy Controls to Panel G	22.7
Panel G: ESRD/HD Period 2 Predialysis	19.3

Intervention	mL/min (Geometric Mean)
Panel A: Mild Renal Impairment	81.3
Panel B: Healthy Controls to Panel A	133
Panel C: Moderate Renal Impairment	52.1
Panel D: Healthy Controls to Panel C	114
Panel E: Severe Renal Impairment	25.3
Panel F: Healthy Controls to Panel E	123
Panel G: ESRD/HD Period 1 Postdialysis	14.4
Panel H: Healthy Controls to Panel G	135
Panel G: ESRD/HD Period 2 Predialysis	76.6

Intervention	liters (L) (Geometric Mean)
Panel A: Mild Renal Impairment	21.4
Panel B: Healthy Controls to Panel A	21.6
Panel C: Moderate Renal Impairment	22.2
Panel D: Healthy Controls to Panel C	21.9
Panel E: Severe Renal Impairment	20.1
Panel F: Healthy Controls to Panel E	22.4
Panel G: ESRD/HD Period 1 Postdialysis	16.2
Panel H: Healthy Controls to Panel G	17.0
Panel G: ESRD/HD Period 2 Predialysis	55.7

Intervention	mL/min (Geometric Mean)
Panel A: Mild Renal Impairment	69.8
Panel B: Healthy Controls to Panel A	118
Panel C: Moderate Renal Impairment	38.4
Panel D: Healthy Controls to Panel C	110
Panel E: Severe Renal Impairment	22.3
Panel F: Healthy Controls to Panel E	107
Panel H: Healthy Controls to Panel G	110

Intervention	hours (Median)
Panel A: Mild Renal Impairment	0.50
Panel B: Healthy Controls to Panel A	0.50
Panel C: Moderate Renal Impairment	0.50
Panel D: Healthy Controls to Panel C	0.49
Panel E: Severe Renal Impairment	0.48
Panel F: Healthy Controls to Panel E	0.48
Panel G: ESRD/HD Period 1 Postdialysis	0.48
Panel H: Healthy Controls to Panel G	0.48
Panel G: ESRD/HD Period 2 Predialysis	0.48

Intervention	liters (L) (Geometric Mean)
Panel A: Mild Renal Impairment	19.2
Panel B: Healthy Controls to Panel A	23.9
Panel C: Moderate Renal Impairment	19.4
Panel D: Healthy Controls to Panel C	21.4
Panel E: Severe Renal Impairment	16.9
Panel F: Healthy Controls to Panel E	21.2
Panel G: ESRD/HD Period 1 Postdialysis	15.9
Panel H: Healthy Controls to Panel G	21.0
Panel G: ESRD/HD Period 2 Predialysis	59.1

Intervention	liters (L) (Geometric Mean)
Panel A: Mild Renal Impairment	21.1
Panel B: Healthy Controls to Panel A	26.1
Panel C: Moderate Renal Impairment	22.3
Panel D: Healthy Controls to Panel C	23.4
Panel E: Severe Renal Impairment	20.0
Panel F: Healthy Controls to Panel E	24.8
Panel G: ESRD/HD Period 1 Postdialysis	20.5
Panel H: Healthy Controls to Panel G	24.9
Panel G: ESRD/HD Period 2 Predialysis	63.3

Intervention	µM*hr (Geometric Mean)
Panel E: Severe Renal Impairment	0.130
Panel F: Healthy Controls to Panel E	0.121
Panel G: ESRD/HD Period 1 Postdialysis	0.0681
Panel G: ESRD/HD Period 2 Predialysis	0.0700
Panel H: Healthy Controls to Panel G	0.114

Intervention	µM*hr (Geometric Mean)
Panel E: Severe Renal Impairment	9.10
Panel F: Healthy Controls to Panel E	6.20
Panel G: ESRD/HD Period 1 Postdialysis	4.56
Panel G: ESRD/HD Period 2 Predialysis	4.08
Panel H: Healthy Controls to Panel G	5.03

Intervention	mL/min (Geometric Mean)
	1 hour postdose	1.5 hours postdose	2 hours postdose	2.5 hours postdose	3.0 hours postdose	3.5 hours postdose	4 hours postdose	4.5 hours postdose
Panel G: ESRD/HD Period 2 Predialysis	172	158	170	166	171	177	204	198