| ID Source | ID |
|---|---|
| PubMed CID | 5282372 |
| CHEMBL ID | 43708 |
| CHEBI ID | 51799 |
| SCHEMBL ID | 5980 |
| MeSH ID | M0023689 |
| Synonym |
|---|
| AC-6815 |
| AC-15445 |
| imipenem (usp) |
| D00206 |
| imipenem hydrate (jp17) |
| 74431-23-5 |
| (5r,6s)-3-((2-(formimidoylamino)ethyl)thio)-6-((r)-1-hydroxyethyl)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid monohydrate |
| 1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid, 6-(1-hydroxyethyl)-3-((2-((iminomethyl)amino)ethyl)thio)-7-oxo-, monohydrate, (5r-(5alpha,6alpha(r*)))- |
| imipenem-1-wasser |
| n-formimidoyl thienamycin monohydrate |
| (5r,6s)-6-[(1r)-1-hydroxyethyl]-3-({2-[(iminomethyl)amino]ethyl}sulfanyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid--water (1/1) |
| CHEBI:51799 , |
| imipenem hydrate |
| SR-05000000294-3 |
| imipenem, monohydrate |
| imipenem monohydrate (h2o) |
| CHEMBL43708 |
| imipenem monohydrate |
| nsc-759901 |
| 71otz9ze0a , |
| imipenem [usan:usp:inn:ban:jan] |
| nsc 759901 |
| unii-71otz9ze0a |
| imipemide monohydrate |
| S3667 |
| AKOS015962000 |
| primaxin component imipenem |
| imipenem monohydrate [who-dd] |
| imipenem [usp monograph] |
| imipenem monohydrate [usp-rs] |
| imipenem component of primaxin |
| imipenem monohydrate [ep monograph] |
| imipenem [usan] |
| imipenem [orange book] |
| imipenem [vandf] |
| imipenem [mart.] |
| imipenem component of recarbrio |
| imipenem monohydrate [mi] |
| recarbrio component imipenem |
| imipenem hydrate [jan] |
| CCG-213597 |
| SCHEMBL5980 |
| (5r,6s)-3-((2-formimidamidoethyl)thio)-6-((r)-1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate |
| imipenem, antibiotic for culture media use only |
| Q-101423 |
| (6 r,7 r)-7-amimo-8-oxo-3-(1-propenyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate |
| mfcd09753321 |
| imipenem monohydrate, united states pharmacopeia (usp) reference standard |
| imipenem monohydrate, >=98% (hplc) |
| imipenem, pharmaceutical secondary standard; certified reference material |
| CS-W019618 |
| 74431-23-5 (hydrate) |
| DS-5383 |
| DTXSID00873392 |
| HY-B1369 |
| GSOSVVULSKVSLQ-JJVRHELESA-N |
| (5r,6s)-6-[(1r)-1-hydroxyethyl]-3-[(2-methanimidamidoethyl)sulfanyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate |
| imipenem,monohydrate |
| (5r,6s)-3-(2-formimidamidoethylthio)-6-((r)-1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate |
| Q27122763 |
| (5r,6s)-3-((2-((e)-(aminomethylene)amino)ethyl)thio)-6-((r)-1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate |
| imipenem hydrate; imipenem monohydrate; 74431-23-5; c12h19n3o5s |
| (5r,6s)-3-((2-formimidamidoethyl)thio)-6-((r)-1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylicacidhydrate |
| Class | Description |
|---|---|
| carbapenems | The class of beta-lactam antibiotics that whose members have a carbapenem skeleton which is variously substituted at positions 3, 4, and 6. |
| [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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.1100 | 7.1903 | 10.0000 | AID1473738 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein binding | Bile salt export pump | Homo sapiens (human) |
| ATP binding | Bile salt export pump | Homo sapiens (human) |
| ABC-type xenobiotic transporter activity | Bile salt export pump | Homo sapiens (human) |
| bile acid transmembrane transporter activity | Bile salt export pump | Homo sapiens (human) |
| canalicular bile acid transmembrane transporter activity | Bile salt export pump | Homo sapiens (human) |
| carbohydrate transmembrane transporter activity | Bile salt export pump | Homo sapiens (human) |
| ABC-type bile acid transporter activity | Bile salt export pump | Homo sapiens (human) |
| ATP hydrolysis activity | Bile salt export pump | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| basolateral plasma membrane | Bile salt export pump | Homo sapiens (human) |
| Golgi membrane | Bile salt export pump | Homo sapiens (human) |
| endosome | Bile salt export pump | Homo sapiens (human) |
| plasma membrane | Bile salt export pump | Homo sapiens (human) |
| cell surface | Bile salt export pump | Homo sapiens (human) |
| apical plasma membrane | Bile salt export pump | Homo sapiens (human) |
| intercellular canaliculus | Bile salt export pump | Homo sapiens (human) |
| intracellular canaliculus | Bile salt export pump | Homo sapiens (human) |
| recycling endosome | Bile salt export pump | Homo sapiens (human) |
| recycling endosome membrane | Bile salt export pump | Homo sapiens (human) |
| extracellular exosome | Bile salt export pump | Homo sapiens (human) |
| membrane | Bile salt export pump | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID209265 | Antibacterial activity against Streptococcus pyogenes 308A | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID220993 | In vitro antibacterial activity against klebsiella pneumoniae A | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID10756 | Clearance of compound after iv administration of 20 mg/kg dose in rat | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Synthesis and biological properties of new 1beta-methylcarbapenems containing heteroaromatic thioether moiety. |
| AID165216 | In vitro antimicrobial activity against ceftazidime resistant Pseudomonas aeruginosa AKR 17 | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID202125 | In vitro antibacterial activity against Streptococcus pyogenes 4 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID69787 | Antibacterial activity against Escherichia coli 1507E | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID163900 | In vitro antibacterial activity against Ps. aeruginosa 18SH (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID219703 | In vitro antibacterial activity against citrobacter freundii BS-16 (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID165211 | In vitro antimicrobial activity against Pseudomonas aeruginosa AK 109 | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID206935 | In vitro antimicrobial activity against methicillin resistant Staphylococcus aureus pMS520 | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID38484 | In vitro antibacterial activity against Bacteroides fragilis F117A | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID219704 | In vitro antibacterial activity against clostridium histolyticum 503-86 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID38472 | In vitro antibacterial activity against Bacteroides thetaiotaomicron 62B | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID163788 | In vitro antimicrobial activity against Pseudomonas aeruginosa 1101-75 was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID219758 | Minimum protective concentration against beta-lactamase of Xanthomonas maltophilia GN 12873 (CXase-II) | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID219756 | In vitro antimicrobial activity against Xanthomonas maltophilia GN 12873 was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID10440 | Half life of compound after iv administration of 20 mg/kg dose in rat | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Synthesis and biological properties of new 1beta-methylcarbapenems containing heteroaromatic thioether moiety. |
| AID165199 | In vitro antibacterial activity was determined against Pseudomonas aeruginosa AK109. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID220761 | In vitro antibacterial activity against bacteroides fragilis S2 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID71111 | In vitro antibacterial activity was determined against Escherichia coli NIHJ JC2. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID66230 | In vitro antibacterial activity against enterobacter cloacae P99 (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID207407 | In vitro antimicrobial activity against Staphylococcus aureus 95 (methicillin-resistant strain) was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID69786 | Antibacterial activity against Escherichia coli 078 | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID206751 | In vitro antibacterial activity was determined against methicillin-resistant Staphylococcus aureus pMS520/Smith. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID207180 | Antibacterial activity against Staphylococcus aureus 285 | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID163929 | Minimum protective concentration against beta-lactamase of Pseudomonas aeruginosa 18S-H | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID164579 | Antibacterial activity against Pseudomonas aeruginosa 1592E | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID227860 | In vitro antibacterial activity against streptococcus pneumoniae 6301 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID201252 | In vitro antibacterial activity against Staphylococcus aureus 67(methicillin resistant) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID207408 | Minimum protective concentration against beta-lactamase of Staphylococcus aureus 95 | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID70618 | In vitro antimicrobial activity against Escherichia coli ATCC 39188 was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID219757 | Minimum protective concentration against beta-lactamase of Xanthomonas maltophilia GN 12873 (CXase-I) | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID42680 | In vitro antibacterial activity against Clostridium difficile 651 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID164581 | Antibacterial activity against Pseudomonas aeruginosa 9027 | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID10449 | Half life was calculated at a single intravenous administration of 20 mg/kg in rat | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID201254 | In vitro antibacterial activity against Staphylococcus aureus 753 (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID95702 | Antibacterial activity against Klebsiella aerogenes 1522E | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID163928 | In vitro antimicrobial activity against Pseudomonas aeruginosa 18S-H was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID56138 | Porcine renal DHP-1 susceptibility. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID207700 | In vitro antimicrobial activity against Staphylococcus aureus FDA 209P was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID229010 | In vitro antibacterial activity against serratia marcescens SM (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID10999 | Plasma clearance for the compound was calculated at a single intravenous administration of 20 mg/kg in rat | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID68686 | In vitro antimicrobial activity against Escherichia coli NIHJ JC2 | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID42688 | In vitro antibacterial activity against Clostridium perfringens 13424 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID206917 | In vitro antimicrobial activity against Staphylococcus aureus 209P NIHJ JCI | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID164580 | Antibacterial activity against Pseudomonas aeruginosa 1771M | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID180210 | Epileptogenicity at 200 ug in rat intracerebroventricular assay. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID11762 | Stability to porcine renal DHP-I | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID12343 | Area under the curve was calculated for the compound at a single intravenous administration of 20 mg/kg in rat | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID205749 | In vitro antibacterial activity was determined against methicillin-resistant Staphylococcus epidermidis MB5181. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID94369 | In vitro antimicrobial activity against Klebsiella pneumoniae NCTC 418 was determined | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Design, synthesis, and SAR of novel carbapenem antibiotics with high stability to Xanthomonas maltophilia oxyiminocephalosporinase type II. |
| AID207312 | Antibacterial activity against Staphylococcus aureus SG 511 | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID207181 | Antibacterial activity against Staphylococcus aureus 503 | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID206741 | In vitro antibacterial activity was determined against Staphylococcus aureus 209P NIHJ JCI. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID65224 | In vitro antibacterial activity against Escherichia coli TEM-1 (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID227852 | In vitro antibacterial activity against staphylococcus aureus smith | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID223834 | In vitro antibacterial activity against Pseudomonas aeruginosa 8780 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID42681 | In vitro antibacterial activity against Clostridium difficile 701 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID64080 | In vitro antibacterial activity against Escherichia coli 257 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID223832 | In vitro antibacterial activity against proteus vulgaris ATCC 6380 (constitutive beta-lactamase producer) | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID200852 | Antibacterial activity against Salmonella Typhimurium | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID165200 | In vitro antibacterial activity was determined against ceftazidime- resistant Pseudomonas aeruginosa AKR17. | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID152306 | In vitro antibacterial activity against Proteus mirabilis 90 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| AID205875 | In vitro antimicrobial activity against methicillin resistant Staphylococcus epidermidis MB5181 | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2 | Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds. |
| AID12151 | Area under curve of compound after iv administration of 20 mg/kg dose in rat | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Synthesis and biological properties of new 1beta-methylcarbapenems containing heteroaromatic thioether moiety. |
| AID68022 | Antibacterial activity against Enterobacter cloacae 1321E | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains. |
| AID19573 | Stability against mammalian enzyme dehydropeptidase (calculated for 1 microL of enzyme solution and 100 uM substrate). | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Dual-action penems and carbapenems. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (14.29) | 18.2507 |
| 2000's | 5 (71.43) | 29.6817 |
| 2010's | 1 (14.29) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (90.81) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| 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 | ||
| An Open-label, Randomized Equivalence Trial and Cost-effectiveness Analysis of Ertapenem Versus Other Carbapenems for Treatment of Extended -Spectrum Beta-Lactamase (ESBL)-Producing Gram-negative Bacterial Infections [NCT01297842] | Phase 4 | 100 participants (Anticipated) | Interventional | 2011-05-31 | Recruiting | ||
| Antibacterial Prophylaxis With Imipenem vs no Prophylaxis for Hematological Malignancies Patients Before Allogenetic Hematopoietic Stem Cell Transplantation [NCT03733340] | Phase 2/Phase 3 | 250 participants (Anticipated) | Interventional | 2018-12-01 | Recruiting | ||
| DetectAB - Detecting Antibiotics - A Pilot Project [NCT03678142] | 17 participants (Actual) | Observational | 2018-10-01 | Completed | |||
| 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 | ||
| Population Pharmacokinetics of Anti-infective Drugs in Children in Anti-infectious Therapies [NCT03113344] | 800 participants (Anticipated) | Observational [Patient Registry] | 2017-06-21 | Recruiting | |||
| The Pharmacodynamics of Imipenem in Critically Ill Patients With Ventilator-associated Pneumonia Following Administration by 4 h or 0.5 h Infusion [NCT01379157] | Phase 4 | 8 participants (Actual) | Interventional | 2011-11-30 | 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 | ||
| Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739] | 800 participants (Anticipated) | Observational [Patient Registry] | 2018-07-01 | Recruiting | |||
| Efficacy and Safety of the Administration of Betalactam Antibiotics in Continuous or Extended Infusion Compared to Intermittent Infusion in Patients With Sepsis in Two Pediatric Third-level Care Hospitals [NCT03019965] | 426 participants (Actual) | Interventional | 2017-02-01 | Completed | |||
| Preventive Effect of Prophylactic Oral Antibiotics Against Cholangitis After Kasai Portoenterostomy in Biliary Atresia: a Randomized Controlled Trial [NCT05925309] | 356 participants (Anticipated) | Interventional | 2023-07-01 | Recruiting | |||
| Is Combination Antibiotic Therapy Superior to Monotherapy in the Treatment of Acute Exacerbations of Chronic Obstructive Pulmonary Disease [NCT04879030] | Phase 2/Phase 3 | 170 participants (Actual) | Interventional | 2020-01-01 | Completed | ||
| 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 | ||
| Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) [NCT04310930] | Phase 2/Phase 3 | 300 participants (Anticipated) | Interventional | 2020-03-02 | Recruiting | ||
| The Role of Second-generation Sequencing in the Treatment of Severe Pneumonia With Initial Treatment Failure [NCT03884881] | 400 participants (Actual) | Interventional | 2018-01-01 | Active, not recruiting | |||
| Pharmacokinetics of Imipenem in Critically Ill Patients With Life-threatening Severe Infections During Support With Extracorporeal Membrane Oxygenation [NCT03776305] | Phase 4 | 12 participants (Anticipated) | Interventional | 2015-12-01 | Active, not recruiting | ||
| Imipenem and Tigecycline Versus Imipenem and Tigecycline With GM-CSF for the Management of Spontaneous Bacterial Peritonitis Presenting With Septic Shock. [NCT04208763] | 90 participants (Anticipated) | Interventional | 2019-12-20 | Recruiting | |||
| 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.) | ||
| Impact of Imipenem With Amikacin Pharmacokinetic and Pharmacodynamic [NCT00950222] | 70 participants (Actual) | Interventional | 2009-06-30 | Completed | |||
| 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 | ||
| Temocillin Versus a Carbapenem as Initial Intravenous Treatment for Extended-spectrum Beta-lactamase Related Urinary Tract Infections, a Non-inferiority Study [NCT03543436] | Phase 3 | 29 participants (Actual) | Interventional | 2019-01-04 | Completed | ||
| The Population Pharmacokinetics of Imipenem in Patients With Ventilator-associated Pneumonia [NCT01489124] | Phase 4 | 9 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| Dose Optimization by PK/PD of Antibiotics to Improve Clinical Outcome of CRKP Bloodstream Infections in Critically Ill Patients and in Vitro Study of Monotherapy, Combination Therapy and Molecular Biology of Drug Resistance at Phramongkutklao Hospital: Pr [NCT05862402] | Phase 4 | 76 participants (Anticipated) | Interventional | 2023-05-07 | Recruiting | ||
| 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 | ||
| Randomized, Multicenter, Phase III, Controlled Clinical Trial, to Demonstrate the no Inferiority of Reduced Antibiotic Treatment vs a Broad Spectrum Betalactam Antipseudomonal Treatment in Patients With Bacteremia by Enterobacteriaceae [NCT02795949] | Phase 3 | 344 participants (Actual) | Interventional | 2016-10-31 | Completed | ||
| A Randomized, Comparative Open Label Study of Imipenem Versus Cefepime in Spontaneous Bacterial Peritonitis and to Evaluate the Risk Factors for Treatment Failure. [NCT01852630] | 175 participants (Actual) | Interventional | 2012-12-31 | Completed | |||
| Preliminary Research On Two-step Dosing Of Imipenem/Cilastatin [NCT02616354] | Phase 4 | 24 participants (Anticipated) | Interventional | 2015-01-31 | Recruiting | ||
| Evidence Based Management of Acute Biliary Pancreatitis [NCT04615702] | 30 participants (Actual) | Observational [Patient Registry] | 2017-05-15 | Completed | |||
| Comparison of the Pharmacodynamics of Imipenem in Patients With Febrile Neutropenia Following Administration by 4-hour Infusion and Bolus Injection. [NCT02213783] | Phase 4 | 12 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| Evaluation of the Efficacy and Safety of Fosfomycin Plus Imipenem for the Treatment of Methicillin-resistant Staphylococcus Aureus (MRSA) Infective Endocarditis. [NCT00871104] | Phase 4 | 50 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Efficacy and Toxicity of Aerosolised Colistin in Ventilator Associated Pneumonia: A Prospective, Randomized Trial [NCT02683603] | Phase 4 | 133 participants (Actual) | Interventional | 2013-04-30 | 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 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 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 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 Multicenter, Randomized, Open Label Study to Compare the Safety and Efficacy of Levofloxacin With That of Imipenem/Cilastatin in the Treatment of Nosocomial Pneumonia [NCT00236834] | Phase 3 | 438 participants (Actual) | Interventional | 1997-12-31 | Completed | ||
| A Prospective, Randomized, Open Label Study of Piperacillin/Tazobactam Versus Imipenem/Cilastin for Empirical Therapy of Febrile Patients With Neutropenia After Hematopoietic Stem Cell Transplantation [NCT01714570] | 123 participants (Actual) | Interventional | 2012-11-30 | 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 | ||
| Bacterial Infections Associated With Healthcare (Healthcare-Associated) in Hospitalized Cirrhotic Patients: Randomized Study of Use of Traditional Empirical Antibiotic Therapy and Second-line Targeted at Multi-resistant Bacteria [NCT01820026] | Phase 4 | 96 participants (Anticipated) | Interventional | 2012-12-31 | Recruiting | ||
| Polymyxin B Monotherapy Versus Polymyxin B-Carbapenem Combination Therapy in Critically Ill Patients With Multi-drug Resistant Gram-negative Infection: A Prospective, Parallel-Group, Double-Blind, Randomized Controlled Study [NCT03159078] | Phase 3 | 40 participants (Anticipated) | Interventional | 2017-05-25 | Recruiting | ||
| Evaluation of Directed Antimicrobial Prophylaxis for Transrectal Ultrasound Guided Prostate Biopsy (TRUSP) [NCT01659866] | Phase 4 | 563 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| Determination of Single-dose Intrapulmonary Pharmacokinetics of Ciprofloxacin and Imipenem in Healthy Subjects and Intubated Patients Suffering From Pneumonia Using Bronchoalveolar Lavage [NCT03177720] | Phase 1 | 10 participants (Actual) | Interventional | 2016-05-29 | Completed | ||
| A Study Comparing Prospective Use of Imipenem/Cilastatin/Relebactam (IMI/REL) to Retrospective Data Using Meropenem/ Vabobactam (MVB) and Ceftazidime/Avibactam (CZA) in Treatment of Klebsiella Producing Carbapenemase Enterobacteriaceae Infections [NCT04785924] | Phase 4 | 0 participants (Actual) | Interventional | 2021-06-07 | Withdrawn(stopped due to Lack of enrollment) | ||
| Antimicrobial Treatment in Patients With Ventilator-associated Tracheobronchitis: a Prospective Randomized Placebo-controlled Double-blind Multicenter Trial [NCT03012360] | Phase 4 | 154 participants (Anticipated) | Interventional | 2018-02-08 | Recruiting | ||
| 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 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 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 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 | ||
| In Vitro Activity of Ceftolozane/Tazobactam and Imipenem/Relebactam in Clinical Isolates of Pseudomonas Aeruginosa and Enterobacterales Collected From Hematology and Oncology Patients [NCT04196608] | 1,005 participants (Anticipated) | Observational | 2019-11-01 | Recruiting | |||
| 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 | ||
| Evaluation of the Non-inferiority of Cefoxitin Versus Imipenem/Cilastatin in the Treatment of Urinary Tract Infections Caused by ESBL-producing Escherichia Coli [NCT02474706] | Phase 4 | 6 participants (Actual) | Interventional | 2016-03-31 | Terminated(stopped due to Lack of recruitment) | ||
| 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 | ||
| The Analysis of Factors Influencing the Apparent Volume of Distribution of Imipenem in Septic Shock Patients [NCT03308214] | 25 participants (Actual) | Observational | 2018-03-18 | 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 Urinary Tract Infection (cUTI) [NCT01505634] | Phase 2 | 302 participants (Actual) | Interventional | 2012-05-16 | Completed | ||
| An Open-label Pharmacokinetic Study of Imipenem-Relebactam in Critically Ill Patients With Augmented Renal Clearance [NCT04147221] | Phase 1 | 9 participants (Actual) | Interventional | 2020-02-10 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
clinical cure is the complete resolution or significant improvement of signs or symptoms of cIAI, such that no additional antimicrobial therapy or surgical or percutaneous intervention is required for the treatment of the current infection. (NCT00515034)
Timeframe: 7 to 14 days after the end of IV therapy
| Intervention | participants (Number) |
|---|---|
| cIAI Treated With Doripenem | 39 |
| cIAI Treated With Imipenem/Cilastatin | 9 |
Treatment-emergent adverse events (TEAEs) are defined as AEs with onset dates on or after the date of the start of the infusion of first dose of study therapy and within 30 days after administration of the last dose of study therapy. (NCT00515034)
Timeframe: from the initiation of the first infusion of study drug therapy and up to 30 days after the completion of study drug therapy
| Intervention | participants (Number) |
|---|---|
| VAP Treated With Doripenem | 42 |
| VAP Treated With Imipenem/Cilastatin | 13 |
| cIAI Treated With Doripenem | 37 |
| cIAI Treated With Imipenem/Cilastatin | 15 |
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 |
The clinical cure rate at the EOT visit in patients whose BAL or mini-BAL culture results yielded at least 1 of the following Gram-negative qualifying pneumonia pathogens was isolated at baseline: any Enterobacteriaceae, P. aeruginosa, and Acinetobacter Spp. (NCT00589693)
Timeframe: End-of-treatment (Day 10 or Day 11)
| Intervention | Participants (Number) |
|---|---|
| Doripenem | 32 |
| Imipenem-cilastatin | 34 |
Number of deaths which occured up to 28 days of the study period due to all causes (NCT00589693)
Timeframe: Up to 28 days
| Intervention | Participants (Number) |
|---|---|
| Doripenem | 17 |
| Imipenem-cilastatin | 13 |
The number of patients who achieved clinical cure at the EOT visit on Day 10. The patient's were classified as clinical cure if they had resolution of signs and symptoms and objective findings of pneumonia to such an extent that no further antimicrobial therapy was necessary. (NCT00589693)
Timeframe: End-of-treatment (Day 10 or Day 11)
| Intervention | Participants (Number) |
|---|---|
| Doripenem | 36 |
| Imipenem-cilastatin | 50 |
The clinical cure rate at the EOT visit in patients, whose bronchoalveolar lavage (BAL) or mini-BAL culture results yielded qualifying pneumonia pathogen P. aeruginosa at baseline. (NCT00589693)
Timeframe: End-of-treatment (Day 10 or Day 11)
| Intervention | Participants (Number) |
|---|---|
| Doripenem | 7 |
| Imipenem-cilastatin | 6 |
Number of patients who had P. aeruginosa isolates with a 4 fold or greater increase in minimum inhibitory concentration (MIC) at anytime during the study (after the study medication is received) from baseline (NCT00589693)
Timeframe: Up to 6 weeks
| Intervention | Participants (Number) |
|---|---|
| Doripenem | 3 |
| Imipenem-cilastatin | 6 |
Cure: all or most pre-therapy signs and symptoms of the index infection showed no evidence of resurgence and no additional antibiotic was required (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 20 |
| Imipenem Cilastatin | 24 |
Cure: all or most pre-therapy signs and symptoms of the index infection had resolved and no additional antibiotic was required (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 24 |
| Imipenem Cilastatin | 29 |
Cure: all or most pre-therapy signs and symptoms of the index infection had resolved and no additional antibiotic was required (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 28 |
| Imipenem Cilastatin | 36 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 1 |
| Imipenem Cilastatin | 0 |
Sustained eradication: a uropathogen found at entry at >10^5 CFU/mL remained <10^4 CFU/mL (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 1 |
| Imipenem Cilastatin | 0 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 1 |
| Imipenem Cilastatin | 0 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 1 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 1 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 24 |
| Imipenem Cilastatin | 32 |
Sustained eradication: a uropathogen found at entry at >10^5 CFU/mL remained <10^4 CFU/mL (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 15 |
| Imipenem Cilastatin | 17 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 19 |
| Imipenem Cilastatin | 23 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 1 |
| Imipenem Cilastatin | 0 |
Sustained eradication: a uropathogen found at entry at >10^5 CFU/mL remained <10^4 CFU/mL (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 0 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 0 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 1 |
Sustained eradication: a uropathogen found at entry at >10^5 CFU/mL remained <10^4 CFU/mL (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 1 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 0 |
| Imipenem Cilastatin | 1 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: End of IV therapy (4 to 14 days)
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 25 |
| Imipenem Cilastatin | 34 |
Sustained eradication: a uropathogen found at entry at >10^5 CFU/mL remained <10^4 CFU/mL (NCT00690378)
Timeframe: 4 to 6 weeks post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 15 |
| Imipenem Cilastatin | 18 |
Eradication: a uropathogen found at entry at >10^5 CFU/mL was reduced to <10^4 CFU/mL (NCT00690378)
Timeframe: 5 to 9 days post-therapy
| Intervention | Participants (Number) |
|---|---|
| NXL104/CAZ | 19 |
| Imipenem Cilastatin | 25 |
(NCT00707239)
Timeframe: Baseline up to Day 44 (30 days after LDOT)
| 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 |
(NCT00707239)
Timeframe: Baseline up to Day 6
| Intervention | ng/mL (Mean) | ||
|---|---|---|---|
| Cmax | Cpd,24 | Cpd,48 | |
| Tigecycline or Imipenem/Cilastatin | 2.83 | 1.86 | 1.74 |
(NCT00707239)
Timeframe: Baseline up to Day 29 to Day 35 (15 to 21 days after LDOT)
| Intervention | participants (Number) | |
|---|---|---|
| Nausea | Vomiting | |
| Imipenem/Cilastatin 1 Gram | 1 | 4 |
| Tigecycline 100 mg | 3 | 1 |
| Tigecycline 75 mg | 1 | 3 |
Clinical response: Cure=All initial SSx improved; CXR improved/stable; no other antibiotics for pneumonia; no worsening or new SSx. Failure=Persistence or worsening SSx; no clinical improvement or initial improvement with clinically important worsening; other antimicrobials for pneumonia; CXR progression; death > study day 2 due to pneumonia. Indeterminate=unable to determine outcome for non-study drug/infection reasons (e.g., lost to follow-up); death in 2 days after 1st dose for any reason, or >2 days but before TOC visit for non-pneumonia reason. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after LDOT)
| 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 |
Clinical response: Cure=All initial signs/symptoms of pneumonia (SSx) improved; chest x-ray (CXR) improved/stable; no other antibiotics for pneumonia; no worsening or new SSx. Failure=Persistence or worsening SSx; no clinical improvement or initial improvement with clinically important worsening; other antimicrobials for pneumonia; CXR progression; death > study day 2 due to pneumonia. Indeterminate=unable to determine outcome for non-study drug/infection reasons (e.g., lost to follow-up); death in 2 days after 1st dose for any reason, or >2 days but before TOC visit for non-pneumonia reason. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after last day of therapy [LDOT])
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Cure | Failure | |
| Imipenem/Cilastatin 1 Gram | 75.0 | 25.0 |
| Tigecycline 100 mg | 85.0 | 15.0 |
| Tigecycline 75 mg | 69.6 | 30.4 |
Clinical response: Cure=All initial SSx improved; CXR improved/stable; no other antibiotics for pneumonia; no worsening or new SSx. Failure=Persistence or worsening SSx; no clinical improvement or initial improvement with clinically important worsening; other antimicrobials for pneumonia; CXR progression; death > study day 2 due to pneumonia. Indeterminate=unable to determine outcome for non-study drug/infection reasons (e.g., lost to follow-up); death in 2 days after 1st dose for any reason, or >2 days but before TOC visit for non-pneumonia reason. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after LDOT)
| 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 |
Microbiological response assessed at participant level. Eradication = baseline isolate not present in repeat culture from the original infection site; Presumed Eradication = clinical response of cure precluded the availability of a specimen for culture; Persistence = baseline isolate present in repeat culture from the original infection site; Presumed Persistence = culture data not available for participants with a clinical response of failure; Superinfection = culture from the primary infection site had new pathogen not identified as a baseline isolate and clinical response was failure. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after LDOT)
| 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 |
Eradication=baseline isolate not present in repeat culture from the original infection site; Presumed Eradication=clinical response of cure precluded the availability of a specimen for culture; Persistence=baseline isolate present in repeat culture from the original infection site; Presumed Persistence=culture data not available for participants with a clinical response of failure; Indeterminate=unable to determine outcome for non-study drug/infection reasons; no baseline isolate; death in 2 days after 1st dose for any reason, or >2 days but before TOC visit for non-pneumonia reason. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after LDOT)
| 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 |
(NCT00707239)
Timeframe: Day 3, 4 or 5
| Intervention | nanogram/milliliter (ng/mL) (Mean) |
|---|---|
| Tigecycline 75 mg | 479 |
| Tigecycline 100 mg | 1217 |
AUC (0-12) = Area under the serum concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-12). Area under the serum concentration-time curve was derived from the population pharmacokinetic (PK) analysis by using each participant's dose and the post-hoc individual estimated systemic CL, AUC (0-12) = Dose divided by CL. (NCT00707239)
Timeframe: Day 3, 4 or 5
| Intervention | ng*hr/mL (Mean) |
|---|---|
| Tigecycline 75 mg | 3.20 |
| Tigecycline 100 mg | 5.04 |
AUC (0-24) = Area under the serum concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-24). Area under the serum concentration-time curve was derived from the population pharmacokinetic (PK) analysis by using each participant's dose and the post-hoc individual estimated systemic CL, AUC (0-12) = Dose divided by CL. Model-predicted AUC (0-24) was calculated by multiplying AUC (0-12) by 2. (NCT00707239)
Timeframe: Day 3, 4 or 5
| Intervention | mg*hr/mL (Mean) |
|---|---|
| Tigecycline 75 mg | 6.40 |
| Tigecycline 100 mg | 10.07 |
Drug clearance (CL) is a quantitative measure of the rate at which a drug substance is removed from the blood. It is defined as the volume of serum from which drug can be completely removed per unit of time. (NCT00707239)
Timeframe: Day 3, 4 or 5
| Intervention | Liter/hr (Mean) |
|---|---|
| Tigecycline | 22.6 |
Potentially clinically significant ECG data: Non-first values greater than 240 millisecond (msec) with increase of greater than or equal to 10 percent (%) from baseline for PR interval; Non-first values greater than or equal to 120 msec for QRS interval; Non-first values greater than 460 msec with increase of greater than or equal to 5% from baseline for corrected QT (QTc) interval; Non-first values greater than 460 msec with increase of greater than or equal to 5% from baseline for QTc using Framingham formula (QTc F). (NCT00707239)
Timeframe: Baseline up to Day 14 or LDOT
| Intervention | participants (Number) |
|---|---|
| Tigecycline 75 mg | 14 |
| Tigecycline 100 mg | 14 |
| Imipenem/Cilastatin 1 Gram | 14 |
Participants were evaluated for following laboratory parameters: albumin, alkaline phosphatase, amylase, urea (blood urea nitrogen [BUN]), total bilirubin, calcium, magnesium, carbon dioxide, international normalized ratio (INR), chloride, creatinine, glucose, lipase, potassium, phosphorus, aspartate aminotransferase (AST), alanine aminotransferase (ALT), sodium, total protein, hemoglobin, hematocrit, white blood cells, eosinophils, neutrophils, lymphocytes, platelets, prothrombin time, prothrombin activity and partial thromboplastin time. (NCT00707239)
Timeframe: Baseline up to Day 24 to Day 35 (10 to 21 days after LDOT)
| Intervention | participants (Number) |
|---|---|
| Tigecycline 75 mg | 34 |
| Tigecycline 100 mg | 31 |
| Imipenem/Cilastatin 1 Gram | 31 |
(NCT00707239)
Timeframe: Day 3, 4 or 5
| Intervention | hrs (Median) |
|---|---|
| Tigecycline 75 mg | 0.5 |
| Tigecycline 100 mg | 0.5 |
AUC (0-24) = Area under the serum concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-24). Area under the serum concentration-time curve was derived from the population PK analysis by using each participant's dose and the post-hoc individual estimated systemic CL, AUC (0-12) = Dose divided by CL. Model-predicted AUC (0-24) was calculated by multiplying AUC (0-12) by 2. (NCT00707239)
Timeframe: Baseline up to Day 29 to 35 (15 to 21 days after LDOT)
| 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 |
Clinical response:Cure =Initial SSx improved;CXR improved/stable;no other antibiotic for pneumonia;no worsening/new SSx. Failure=Persistence/worsening SSx;no clinical improvement/initial improvement with worsening; other antibiotic;CXR progression;death >study day 2 due to pneumonia. Indeterminate=unable to determine outcome for non-study drug/infection reason;death in 2 days after dose 1 for any reason or >2 days but before TOC visit for non-pneumonia reason. MIC=lowest drug concentration with no visible growth of microorganism. AUC(0-24)/MIC:reported for cure and failure/indeterminate. (NCT00707239)
Timeframe: Up to Day 24 to 35 (10 to 21 days after LDOT)
| Intervention | ratio (Mean) | |
|---|---|---|
| Cure (n = 17) | Failure/indeterminate (n = 8) | |
| Tigecycline | 24.3 | 22.8 |
Cilastin is 1 of the 2 constituents of PRIMAXIN®. AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Imipenem is 1 of the 2 constituents of PRIMAXIN®. Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Cilastin is 1 of the 2 constituents of PRIMAXIN®. Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
The extraction coefficient of MK-7655 was determined in ESRD/HD participants for 4.5 hours during HD. The formula for calculating extraction coefficient was: Extraction Coefficient = ABS[100*(post-dialyzer concentration - pre-dialyzer concentration) / pre-dialyzer concentration]. (NCT01275170)
Timeframe: 1, 1.5, 2, 2.5, 3, 3.5, 4, and 4.5 hours postdose
| Intervention | Extraction coefficient (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 | 73 | 67 | 73 | 71 | 73 | 76 | 87 | 84 |
The CLD of MK-7655 was determined in ESRD/HD participants for 4.5 hours during HD. The formula for calculating CLD was: CLd = (1-Hct)*QB*[(pre-dialyzer concentration - post-dialyzer concentration) / (pre-dialyzer concentration)] where QB=350 mL/min and Hct=hematocrit. (NCT01275170)
Timeframe: 1, 1.5, 2, 2.5, 3, 3.5, 4, and 4.5 hours postdose
| 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 |
An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01275170)
Timeframe: Up to 14 days after the last dose of study drug in Part 2 (up to 11 weeks)
| 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 |
Omeprazole was selected as a substrate of CYP2C19. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose
| 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 |
Midazolam was selected as a substrate of CYP3A4. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose
| 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 |
Cilastin is 1 of the 2 constituents of PRIMAXIN®. CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| Intervention | mL/min (Geometric Mean) |
|---|---|
| Panel A: Mild Renal Impairment | 162 |
| Panel B: Healthy Controls to Panel A | 259 |
| Panel C: Moderate Renal Impairment | 116 |
| Panel D: Healthy Controls to Panel C | 217 |
| Panel E: Severe Renal Impairment | 38.7 |
| Panel F: Healthy Controls to Panel E | 217 |
| Panel G: ESRD/HD Period 1 Postdialysis | 15.0 |
| Panel H: Healthy Controls to Panel G | 206 |
| Panel G: ESRD/HD Period 2 Predialysis | 56.6 |
Imipenem is 1 of the 2 constituents of PRIMAXIN®. Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose
| 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 |
Cilastin is 1 of the 2 constituents of PRIMAXIN®. Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose
| 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 |
Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose
| 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 |
Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| Intervention | hours (Median) |
|---|---|
| Panel A: Mild Renal Impairment | 0.50 |
| Panel B: Healthy Controls to Panel A | 0.50 |
| Panel C: Moderate Renal Impairment | 0.49 |
| Panel D: Healthy Controls to Panel C | 0.48 |
| 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 |
Caffeine was selected as a substrate of CYP1A2. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose
| Intervention | µM*hr (Geometric Mean) |
|---|---|
| Panel E: Severe Renal Impairment | 336 |
| Panel F: Healthy Controls to Panel E | 221 |
| Panel G: ESRD/HD Period 1 Postdialysis | 190 |
| Panel G: ESRD/HD Period 2 Predialysis | 200 |
| Panel H: Healthy Controls to Panel G | 300 |
Imipenem is 1 of the 2 constituents of PRIMAXIN®. VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Cilastin is 1 of the 2 constituents of PRIMAXIN®. VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Imipenem is 1 of the 2 constituents of PRIMAXIN®. AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| Intervention | hours (Median) |
|---|---|
| Panel A: Mild Renal Impairment | 0.50 |
| Panel B: Healthy Controls to Panel A | 0.50 |
| Panel C: Moderate Renal Impairment | 0.49 |
| Panel D: Healthy Controls to Panel C | 0.48 |
| 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 |
Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose
| 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 |
VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| 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 |
CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose
| Intervention | mL/min (Geometric Mean) |
|---|---|
| Panel A: Mild Renal Impairment | 75.0 |
| Panel B: Healthy Controls to Panel A | 115 |
| Panel C: Moderate Renal Impairment | 41.1 |
| Panel D: Healthy Controls to Panel C | 109 |
| Panel E: Severe Renal Impairment | 17.4 |
| Panel F: Healthy Controls to Panel E | 104 |
| Panel H: Healthy Controls to Panel G | 99.1 |
CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose
| 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 |
Imipenem is 1 of the 2 constituents of PRIMAXIN®. CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose
| Intervention | mL/min (Geometric Mean) |
|---|---|
| Panel A: Mild Renal Impairment | 180 |
| Panel B: Healthy Controls to Panel A | 253 |
| Panel C: Moderate Renal Impairment | 138 |
| Panel D: Healthy Controls to Panel C | 211 |
| Panel E: Severe Renal Impairment | 87.0 |
| Panel F: Healthy Controls to Panel E | 218 |
| Panel G: ESRD/HD Period 1 Postdialysis | 62.5 |
| Panel H: Healthy Controls to Panel G | 194 |
| Panel G: ESRD/HD Period 2 Predialysis | 195 |
Clinical laboratory parameters included ALT, ALP, AST, Creatine kinase and GGT. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in ALT, ALP, AST, Creatine kinase and GGT are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | International units per Liter (Mean) | ||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ALT: On IV therapy (Day 3) | ALT: On IV therapy (Day 5) | ALT: On IV therapy (Day 8) | ALT: End of IV therapy | ALT: Test of Cure | ALT: Early Follow-up | ALT: Late Follow-up | ALP: On IV therapy (Day 3) | ALP: On IV therapy (Day 5) | ALP: On IV therapy (Day 8) | ALP: End of IV therapy | ALP: Test of Cure | ALP: Early Follow-up | ALP: Late Follow-up | AST: On IV therapy (Day 3) | AST: On IV therapy (Day 5) | AST: On IV therapy (Day 8) | AST: End of IV therapy | AST: Test of Cure | AST: Early Follow-up | AST: Late Follow-up | Creatine kinase : On IV therapy (Day 5) | Creatine kinase : End of IV therapy | Creatine kinase : Test of Cure | Creatine kinase : Early Follow-up | Creatine kinase : Late Follow-up | GGT : On IV therapy (Day 5) | GGT : End of IV therapy | GGT : Test of Cure | GGT : Early Follow-up | GGT : Late Follow-up | |
| GSK2251052 1500 mg | 10.4 | 4.8 | 1.5 | 18.6 | 7.3 | 1.0 | -0.3 | 14.3 | 4.0 | 21.5 | 16.3 | 6.9 | 1.2 | 2.3 | 4.1 | 6.3 | 2.0 | 13.1 | -2.3 | -4.8 | -3.3 | -37.8 | -165.6 | -156.4 | -218.2 | -168.8 | 6.5 | 28.9 | 23.3 | 8.3 | 1.3 |
| Imipenem-Cilastatin | 12.8 | 13.3 | -3.0 | 21.3 | 7.0 | 5.8 | 4.2 | 13.2 | 17.7 | -10.0 | 10.2 | 14.8 | 8.2 | 3.6 | 19.2 | 20.0 | 2.0 | 15.7 | -1.4 | 1.2 | 3.4 | -26.0 | -23.7 | 18.4 | -6.0 | 0.2 | 24.0 | 14.0 | 3.6 | -0.8 | -3.8 |
Clinical laboratory parameters included ALT, ALP, AST, Creatine kinase and GGT. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in ALT, ALP, AST, Creatine kinase and GGT are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | International units per Liter (Mean) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ALT: On IV therapy (Day 3) | ALT: On IV therapy (Day 5) | ALT: On IV therapy (Day 8) | ALT: On IV therapy (Day 11) | ALT: End of IV therapy | ALT: Test of Cure | ALT: Early Follow-up | ALT: Late Follow-up | ALP: On IV therapy (Day 3) | ALP: On IV therapy (Day 5) | ALP: On IV therapy (Day 8) | ALP: On IV therapy (Day 11) | ALP: End of IV therapy | ALP: Test of Cure | ALP: Early Follow-up | ALP: Late Follow-up | AST: On IV therapy (Day 3) | AST: On IV therapy (Day 5) | AST: On IV therapy (Day 8) | AST: On IV therapy (Day 11) | AST: End of IV therapy | AST: Test of Cure | AST: Early Follow-up | AST: Late Follow-up | Creatine kinase : On IV therapy (Day 5) | Creatine kinase : On IV therapy (Day 11) | Creatine kinase : End of IV therapy | Creatine kinase : Test of Cure | Creatine kinase : Early Follow-up | Creatine kinase : Late Follow-up | GGT : On IV therapy (Day 5) | GGT : On IV therapy (Day 11) | GGT : End of IV therapy | GGT : Test of Cure | GGT : Early Follow-up | GGT : Late Follow-up | |
| GSK2251052 750 mg | 5.7 | 33.2 | 4.0 | 2.0 | 35.4 | 17.5 | 4.8 | 3.3 | 10.8 | 11.2 | -10.0 | -11.0 | 7.4 | 10.8 | 7.4 | 5.7 | 5.0 | 31.5 | -2.0 | 2.0 | 22.0 | 1.5 | -1.2 | 3.3 | -76.0 | 4.0 | -36.0 | -65.3 | -41.4 | -37.8 | 41.7 | 22.0 | 35.8 | 16.5 | -1.4 | -16.7 |
Clinical laboratory parameters included albumin and total protein. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in albumin and total protein are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Gram per Liter (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Albumin: On IV therapy (Day 5) | Albumin: End of IV therapy | Albumin: Test of Cure | Albumin: Early Follow-up | Albumin: Late Follow-up | Total protein: On IV therapy (Day 5) | Total protein: End of IV therapy | Total protein: Test of Cure | Total protein: Early Follow-up | Total protein: Late Follow-up | |
| GSK2251052 1500 mg | -3.8 | -2.1 | 1.7 | 3.5 | 3.5 | -5.0 | -3.3 | 2.1 | 5.3 | 5.3 |
| Imipenem-Cilastatin | -0.3 | 0.8 | 2.6 | 3.4 | 3.2 | 1.0 | 3.0 | 6.4 | 6.4 | 4.8 |
Clinical laboratory parameters included albumin and total protein. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in albumin and total protein are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Gram per Liter (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Albumin: On IV therapy (Day 5) | Albumin: On IV therapy (Day 11) | Albumin: End of IV therapy | Albumin: Test of Cure | Albumin: Early Follow-up | Albumin: Late Follow-up | Total protein: On IV therapy (Day 5) | Total protein: On IV therapy (Day 11) | Total protein: End of IV therapy | Total protein: Test of Cure | Total protein: Early Follow-up | Total protein: Late Follow-up | |
| GSK2251052 750 mg | -0.5 | 2.0 | 1.0 | 5.7 | 8.2 | 7.3 | 0.0 | -5.0 | -0.4 | 5.8 | 9.4 | 8.2 |
Clinical laboratory parameters included C02 content/bicarbonate, chloride, glucose, potassium, sodium and urea/BUN. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in C02 content/bicarbonate, chloride, glucose, potassium, sodium and urea/BUN are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Millimole per Liter (Mean) | ||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Calcium: On IV therapy (Day 5) | Calcium: End of IV therapy | Calcium: Test of Cure | Calcium: Early Follow-up | Calcium: Late Follow-up | C02 content/Bicarbonate: On IV therapy (Day 5) | C02 content/Bicarbonate: End of IV therapy | C02 content/Bicarbonate: Test of Cure | C02 content/Bicarbonate: Early Follow-up | C02 content/Bicarbonate: Late Follow-up | Chloride: On IV therapy (Day 5) | Chloride: End of IV therapy | Chloride: Test of Cure | Chloride: Early Follow-up | Chloride: Late Follow-up | Glucose: On IV therapy (Day 5) | Glucose: End of IV therapy | Glucose: Test of Cure | Glucose: Early Follow-up | Glucose: Late Follow-up | Potassium: On IV therapy (Day 5) | Potassium: End of IV therapy | Potassium: Test of Cure | Potassium: Early Follow-up | Potassium: Late Follow-up | Sodium: On IV therapy (Day 5) | Sodium: End of IV therapy | Sodium: Test of Cure | Sodium: Early Follow-up | Sodium: Late Follow-up | Urea/BUN: On IV therapy (Day 5) | Urea/BUN: End of IV therapy | Urea/BUN: Test of Cure | Urea/BUN: Early Follow-up | Urea/BUN: Late Follow-up | |
| GSK2251052 1500 mg | -0.112 | 0.071 | 0.096 | 0.120 | 0.115 | 0.0 | 0.6 | 2.7 | 0.3 | 1.8 | 1.8 | 3.0 | 1.0 | 0.5 | -0.5 | 2.25 | 1.09 | -0.11 | 0.07 | 0.58 | -0.05 | 0.24 | 0.40 | 0.50 | 0.53 | 0.3 | 1.7 | 1.3 | -0.5 | -1.2 | -0.45 | -1.13 | -0.73 | 0.20 | -0.33 |
| Imipenem-Cilastatin | 0.060 | 0.078 | 0.128 | 0.142 | 0.110 | -2.0 | -0.3 | 1.4 | -0.4 | 1.2 | 3.7 | -0.2 | 0.2 | 0.0 | 2.2 | -2.00 | -0.68 | -0.24 | -0.78 | -0.56 | 0.37 | 0.48 | 0.44 | 0.42 | 0.40 | 2.3 | -0.8 | 1.0 | 1.0 | 2.0 | -0.97 | -0.57 | -0.38 | -0.34 | -0.12 |
Clinical laboratory parameters included C02 content/bicarbonate, chloride, glucose, potassium, sodium and urea/BUN. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in C02 content/bicarbonate, chloride, glucose, potassium, sodium and urea/BUN are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Millimole per Liter (Mean) | |||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Calcium: On IV therapy (Day 5) | Calcium: On IV therapy (Day 11) | Calcium: End of IV therapy | Calcium: Test of Cure | Calcium: Early Follow-up | Calcium: Late Follow-up | C02 content/Bicarbonate: On IV therapy (Day 5) | C02 content/Bicarbonate: On IV therapy (Day 11) | C02 content/Bicarbonate: End of IV therapy | C02 content/Bicarbonate: Test of Cure | C02 content/Bicarbonate: Early Follow-up | C02 content/Bicarbonate: Late Follow-up | Chloride: On IV therapy (Day 5) | Chloride: On IV therapy (Day 11) | Chloride: End of IV therapy | Chloride: Test of Cure | Chloride: Early Follow-up | Chloride: Late Follow-up | Glucose: On IV therapy (Day 5) | Glucose: On IV therapy (Day 11) | Glucose: End of IV therapy | Glucose: Test of Cure | Glucose: Early Follow-up | Glucose: Late Follow-up | Potassium: On IV therapy (Day 5) | Potassium: On IV therapy (Day 11) | Potassium: End of IV therapy | Potassium: Test of Cure | Potassium: Early Follow-up | Potassium: Late Follow-up | Sodium: On IV therapy (Day 5) | Sodium: On IV therapy (Day 11) | Sodium: End of IV therapy | Sodium: Test of Cure | Sodium: Early Follow-up | Sodium: Late Follow-up | Urea/BUN: On IV therapy (Day 5) | Urea/BUN: On IV therapy (Day 11) | Urea/BUN: End of IV therapy | Urea/BUN: Test of Cure | Urea/BUN: Early Follow-up | Urea/BUN: Late Follow-up | |
| GSK2251052 750 mg | 0.082 | 0.030 | -0.020 | 0.235 | 0.276 | 0.243 | -1.7 | -3.0 | -2.4 | -0.8 | 0.0 | 0.7 | 1.2 | 4.0 | 1.0 | 0.5 | 0.6 | 0.3 | 0.42 | 1.50 | -1.06 | -0.35 | -0.80 | -0.45 | 0.52 | 0.00 | 0.46 | 0.78 | 0.40 | 0.28 | 1.2 | 4.0 | 0.4 | 1.8 | 1.8 | 1.2 | -0.98 | -2.50 | -0.30 | -0.38 | -0.64 | -0.30 |
Clinical laboratory parameters included CCE. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in CCE are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Milliliter per minute (Mean) | |
|---|---|---|
| CCE: Test of Cure | CCE: Early Follow-up | |
| Imipenem-Cilastatin | 56.0 | 60.0 |
Clinical laboratory parameters included CCE. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in CCE are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Milliliter per minute (Mean) | ||
|---|---|---|---|
| CCE: Test of Cure | CCE: Early Follow-up | CCE: Late Follow-up | |
| GSK2251052 750 mg | 2.0 | 1.0 | 25.0 |
Clinical laboratory parameters included CCE. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in CCE are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Milliliter per minute (Mean) | |||
|---|---|---|---|---|
| CCE: On IV therapy (Day 5) | CCE: Test of Cure | CCE: Early Follow-up | CCE: Late Follow-up | |
| GSK2251052 1500 mg | 18.0 | 13.0 | 21.0 | 21.0 |
Clinical laboratory parameters included creatinine, direct bilirubin and total bilirubin. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in creatinine, direct bilirubin and total bilirubin are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Micromole per liter (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Creatinine: On IV therapy (Day 5) | Creatinine: End of IV therapy | Creatinine: Test of Cure | Creatinine: Early Follow-up | Creatinine: Late Follow-up | Total bilirubin: On IV therapy (Day 3) | Total bilirubin: On IV therapy (Day 5) | Total bilirubin: On IV therapy (Day 8) | Total bilirubin: End of IV therapy | Total bilirubin: Test of Cure | Total bilirubin: Early Follow-up | Total bilirubin: Late Follow-up | |
| GSK2251052 1500 mg | -5.78 | -11.26 | -9.66 | 2.88 | -5.22 | -4.9 | -3.5 | -4.5 | -5.6 | -4.7 | -4.5 | -4.8 |
| Imipenem-Cilastatin | -11.97 | -8.70 | -8.54 | -4.56 | -5.22 | -7.2 | -7.3 | -1.0 | -5.5 | -6.4 | -6.0 | -5.0 |
Clinical laboratory parameters included creatinine, direct bilirubin and total bilirubin. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in creatinine, direct bilirubin and total bilirubin are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Micromole per liter (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Creatinine: On IV therapy (Day 5) | Creatinine: On IV therapy (Day 11) | Creatinine: End of IV therapy | Creatinine: Test of Cure | Creatinine: Early Follow-up | Creatinine: Late Follow-up | Total bilirubin: On IV therapy (Day 3) | Total bilirubin: On IV therapy (Day 5) | Total bilirubin: On IV therapy (Day 8) | Total bilirubin: On IV therapy (Day 11) | Total bilirubin: End of IV therapy | Total bilirubin: Test of Cure | Total bilirubin: Early Follow-up | Total bilirubin: Late Follow-up | |
| GSK2251052 750 mg | -4.20 | -1.50 | -0.24 | -2.17 | -3.90 | 4.43 | -7.5 | -7.0 | -5.0 | -1.0 | -8.2 | -7.7 | -6.2 | -5.2 |
Hematology parameters included basophils, eosinophils, lymphocytes, monocytes, platelet count, total neutrophils and WBC. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in basophils, eosinophils, lymphocytes, monocytes, platelet count, total neutrophils and WBC are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Gigacells per Liter (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Basophils: End of IV therapy | Basophils: Late Follow-up | Eosinophils: End of IV therapy | Eosinophils: Late Follow-up | Lymphocytes: End of IV therapy | Lymphocytes: Late Follow-up | Monocytes: End of IV therapy | Monocytes: Late Follow-up | Platelet count: End of IV therapy | Platelet count: Late Follow-up | Total neutrophils: End of IV therapy | Total neutrophils: Late Follow-up | WBC count: End of IV therapy | WBC count: Late Follow-up | |
| GSK2251052 1500 mg | 0.018 | 0.020 | 0.096 | 0.067 | 0.514 | 0.774 | -0.256 | -0.230 | 83.2 | 45.4 | -6.695 | -7.737 | -6.30 | -7.11 |
| GSK2251052 750 mg | 0.028 | 0.022 | 0.274 | 0.093 | 0.580 | 0.687 | -0.188 | -0.380 | 141.0 | 48.8 | -8.178 | -6.765 | -7.48 | -6.33 |
| Imipenem-Cilastatin | 0.014 | 0.016 | 0.090 | 0.086 | 0.596 | 0.436 | -0.442 | -0.186 | 105.4 | 39.8 | -4.656 | -7.902 | -4.36 | -7.54 |
Hematology parameters included hematocrit. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in hematocrit are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Fraction (Mean) | |
|---|---|---|
| End of IV therapy | Late Follow-up | |
| GSK2251052 1500 mg | -0.0155 | -0.0007 |
| GSK2251052 750 mg | -0.0140 | 0.0373 |
| Imipenem-Cilastatin | -0.0120 | -0.0038 |
Hematology parameters included hemoglobin and MCHC. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in hemoglobin and MCHC are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Gram per Liter (Mean) | |||
|---|---|---|---|---|
| Hemoglobin: End of IV therapy | Hemoglobin: Late Follow-up | MCHC: End of IV therapy | MCHC: Late Follow-up | |
| GSK2251052 1500 mg | -5.5 | -2.1 | -1.8 | -5.0 |
| GSK2251052 750 mg | -3.0 | 11.0 | 4.0 | -3.0 |
| Imipenem-Cilastatin | -2.5 | -0.6 | 4.2 | 1.8 |
Hematology parameters included MCH. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in MCH are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Picograms (Mean) | |
|---|---|---|
| End of IV therapy | Late Follow-up | |
| GSK2251052 1500 mg | -0.60 | -0.89 |
| GSK2251052 750 mg | -0.60 | -0.85 |
| Imipenem-Cilastatin | -0.07 | -0.14 |
Hematology parameters included MCV. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in MCV are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Femtoliters (Mean) | |
|---|---|---|
| End of IV therapy | Late Follow-up | |
| GSK2251052 1500 mg | -1.3 | -1.3 |
| GSK2251052 750 mg | -3.0 | -2.2 |
| Imipenem-Cilastatin | -1.0 | -0.8 |
Hematology parameters included RBC count and reticulocytes. Baseline was Day 1. Change from Baseline was calculated by subtracting Baseline values from individual post-Baseline values. Mean change from Baseline up to Late follow-up visit in RBC count and reticulocytes are presented. (NCT01381549)
Timeframe: Baseline (Day 1) to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Trillion cells per liter (Mean) | |||
|---|---|---|---|---|
| RBC: End of IV therapy | RBC: Late Follow-up | Reticulocytes: End of IV therapy | Reticulocytes: Late Follow-up | |
| GSK2251052 1500 mg | -0.10 | 0.07 | -0.0312 | -0.0092 |
| GSK2251052 750 mg | -0.10 | 0.52 | -0.0331 | -0.0466 |
| Imipenem-Cilastatin | -0.08 | 0.02 | -0.0072 | 0.0080 |
Twelve lead ECGs were obtained during the study using an ECG machine that automatically measured PR, QRS, QT, and QT corrected by Bazett's formula (QTcB), QT corrected by Fridericia's formula (QTcF) intervals. Twelve lead ECGs were performed with the participant in a semi-supine position having rested in this position for at least 10 minutes beforehand. Measurements that deviated substantially from previous readings were repeated immediately. Three measurements were taken at pre-dose on Day 1 at least 5 min apart. One additional ECG measurement was taken after completion of the first infusion of study medication. Two ECG measurements (pre and post-1st infusion of the day) were taken on Day 4 while the participant was on IV therapy. When there was an abnormal finding, two more were taken and the mean PR interval, QRS duration, QT interval and QTcB were calculated from automated ECG readings. One ECG measurement was taken at the early safety follow-up visit. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| Day 1: Pre-dose 1 | Day 1: Pre-dose 2 | Day 1: Pre-dose 3 | Day 1: Post-dose | Day 4 (on IV treatment): Pre-dose | Day 4 (on IV treatment): Post-dose | Early Follow-up | Withdrawal | |
| GSK2251052 1500 mg | 4 | 4 | 2 | 5 | 4 | 3 | 3 | 0 |
| GSK2251052 750 mg | 0 | 2 | 1 | 1 | 2 | 3 | 0 | 0 |
| Imipenem-Cilastatin | 2 | 2 | 3 | 3 | 2 | 2 | 2 | 0 |
AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. For marketed medicinal products, this also includes failure to produce expected benefits (i.e., lack of efficacy), abuse or misuse. SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. (NCT01381549)
Timeframe: Up to 28 days post-therapy
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| AE | SAE | |
| GSK2251052 1500 mg | 6 | 2 |
| GSK2251052 750 mg | 5 | 1 |
| Imipenem-Cilastatin | 5 | 0 |
Vital sign measurements included heart rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean heart rate is presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Beats per minute (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 1500 mg | 99.3 | 83.0 | 80.6 | 81.0 | 80.3 | 92.0 | 88.5 | 87.5 | 80.0 | 82.8 | 73.6 | 74.0 | 71.8 |
Vital sign measurements included temperature (oral, tympanic or rectal). Measurements that deviated substantially from previous readings were repeated immediately. Temperature was assessed as normal hospital practice dictated and the maximum daily temperature was recorded in the electronic case report form (eCRF). (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Celsius (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 1500 mg | 38.41 | 37.30 | 36.79 | 36.71 | 36.59 | 36.90 | 36.95 | 36.80 | 36.80 | 36.75 | 35.98 | 35.99 | 36.08 |
Vital sign measurements included temperature (oral, tympanic or rectal). Measurements that deviated substantially from previous readings were repeated immediately. Temperature was assessed as normal hospital practice dictated and the maximum daily temperature was recorded in the electronic case report form (eCRF). (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Celsius (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| Imipenem-Cilastatin | 38.30 | 37.30 | 37.74 | 37.38 | 36.96 | 36.40 | 36.93 | 36.50 | 36.50 | 36.50 | 36.38 | 36.14 | 36.28 | 36.00 |
Vital sign measurements included temperature (oral, tympanic or rectal). Measurements that deviated substantially from previous readings were repeated immediately. Temperature was assessed as normal hospital practice dictated and the maximum daily temperature was recorded in the electronic case report form (eCRF). (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Celsius (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | On IV therapy (Day 11) | On IV therapy (Day 12) | On IV therapy (Day 13) | On IV therapy (Day 14) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 750 mg | 38.08 | 36.97 | 36.75 | 36.60 | 36.27 | 37.00 | 36.20 | 36.80 | 36.50 | 37.00 | 37.00 | 36.80 | 36.20 | 36.80 | 36.18 | 36.25 | 36.23 | 36.40 |
Vital sign measurements included SBP and DBP (supine or semi-supine). Measurements that deviated substantially from previous readings were repeated immediately. Mean SBP and DBP are presented. (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Millimeters of mercury (mmHg) (Mean) | |||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBP: Baseline (Day 1) | SBP: On IV therapy (Day 2) | SBP: On IV therapy (Day 3) | SBP: On IV therapy (Day 4) | SBP: On IV therapy (Day 5) | SBP: On IV therapy (Day 6) | SBP: On IV therapy (Day 7) | SBP: On IV therapy (Day 8) | SBP: On IV therapy (Day 9) | SBP: End of IV therapy | SBP: Test of Cure | SBP: Early Follow-up | SBP: Late Follow-up | DBP: Baseline (Day 1) | DBP: On IV therapy (Day 2) | DBP: On IV therapy (Day 3) | DBP: On IV therapy (Day 4) | DBP: On IV therapy (Day 5) | DBP: On IV therapy (Day 6) | DBP: On IV therapy (Day 7) | DBP: On IV therapy (Day 8) | DBP: On IV therapy (Day 9) | DBP: End of IV therapy | DBP: Test of Cure | DBP: Early Follow-up | DBP: Late Follow-up | |
| GSK2251052 1500 mg | 131.9 | 125.4 | 126.6 | 127.0 | 126.6 | 125.5 | 125.0 | 125.0 | 130.0 | 116.1 | 126.9 | 120.1 | 117.6 | 77.3 | 69.0 | 72.1 | 79.5 | 79.7 | 81.0 | 70.0 | 69.0 | 80.0 | 69.4 | 70.6 | 72.0 | 67.5 |
Vital sign measurements included SBP and DBP (supine or semi-supine). Measurements that deviated substantially from previous readings were repeated immediately. Mean SBP and DBP are presented. (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Millimeters of mercury (mmHg) (Mean) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBP: Baseline (Day 1) | SBP: On IV therapy (Day 2) | SBP: On IV therapy (Day 3) | SBP: On IV therapy (Day 4) | SBP: On IV therapy (Day 5) | SBP: On IV therapy (Day 6) | SBP: On IV therapy (Day 7) | SBP: On IV therapy (Day 8) | SBP: On IV therapy (Day 9) | SBP: On IV therapy (Day 10) | SBP: End of IV therapy | SBP: Test of Cure | SBP: Early Follow-up | SBP: Late Follow-up | DBP: Baseline (Day 1) | DBP: On IV therapy (Day 2) | DBP: On IV therapy (Day 3) | DBP: On IV therapy (Day 4) | DBP: On IV therapy (Day 5) | DBP: On IV therapy (Day 6) | DBP: On IV therapy (Day 7) | DBP: On IV therapy (Day 8) | DBP: On IV therapy (Day 9) | DBP: On IV therapy (Day 10) | DBP: End of IV therapy | DBP: Test of Cure | DBP: Early Follow-up | DBP: Late Follow-up | |
| Imipenem-Cilastatin | 120.0 | 120.0 | 123.8 | 124.2 | 116.8 | 115.0 | 116.7 | 110.0 | 105.0 | 110.0 | 117.5 | 126.4 | 123.8 | 116.6 | 66.5 | 70.3 | 71.2 | 69.6 | 67.0 | 72.5 | 67.7 | 70.0 | 65.0 | 70.0 | 71.5 | 71.8 | 68.8 | 65.0 |
Vital sign measurements included SBP and DBP (supine or semi-supine). Measurements that deviated substantially from previous readings were repeated immediately. Mean SBP and DBP are presented. (NCT01381549)
Timeframe: Up to Late Follow up Visit (21 to 28 days post-IV therapy)
| Intervention | Millimeters of mercury (mmHg) (Mean) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBP: Baseline (Day 1) | SBP: On IV therapy (Day 2) | SBP: On IV therapy (Day 3) | SBP: On IV therapy (Day 4) | SBP: On IV therapy (Day 5) | SBP: On IV therapy (Day 6) | SBP: On IV therapy (Day 7) | SBP: On IV therapy (Day 8) | SBP: On IV therapy (Day 9) | SBP: On IV therapy (Day 10) | SBP: On IV therapy (Day 11) | SBP: On IV therapy (Day 12) | SBP: On IV therapy (Day 13) | SBP: On IV therapy (Day 14) | SBP: End of IV therapy | SBP: Test of Cure | SBP: Early Follow-up | SBP: Late Follow-up | DBP: Baseline (Day 1) | DBP: On IV therapy (Day 2) | DBP: On IV therapy (Day 3) | DBP: On IV therapy (Day 4) | DBP: On IV therapy (Day 5) | DBP: On IV therapy (Day 6) | DBP: On IV therapy (Day 7) | DBP: On IV therapy (Day 8) | DBP: On IV therapy (Day 9) | DBP: On IV therapy (Day 10) | DBP: On IV therapy (Day 11) | DBP: On IV therapy (Day 12) | DBP: On IV therapy (Day 13) | DBP: On IV therapy (Day 14) | DBP: End of IV therapy | DBP: Test of Cure | DBP: Early Follow-up | DBP: Late Follow-up | |
| GSK2251052 750 mg | 129.7 | 131.2 | 123.8 | 137.8 | 135.2 | 150.0 | 165.0 | 170.0 | 161.0 | 140.0 | 155.0 | 140.0 | 130.0 | 152.0 | 130.0 | 131.3 | 128.0 | 148.0 | 68.0 | 78.3 | 77.2 | 85.5 | 83.8 | 90.0 | 85.0 | 90.0 | 95.0 | 69.0 | 69.0 | 75.0 | 80.0 | 69.0 | 74.0 | 82.2 | 73.8 | 87.7 |
Vital sign measurements included heart rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean heart rate is presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Beats per minute (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| Imipenem-Cilastatin | 87.7 | 81.5 | 81.4 | 73.6 | 68.2 | 74.8 | 78.3 | 82.0 | 85.0 | 86.0 | 71.0 | 74.6 | 65.8 | 78.2 |
Clinical response was a combination of clinical success and clinical failure. In clinical success, participants showed no signs and symptoms of pyelonephritis and lower complicated urinary tract infection and antibiotics are not used for the same. In clinical failure, there is reappearance of signs and symptoms of and lower complicated urinary tract infection and participant required antibiotics for the same. (NCT01381549)
Timeframe: End of IV therapy (0-24 hours post-therapy), Test of Cure Visit (5 to 9 days post-IV therapy) and Late Follow-up (21-28 days post-therapy)
| Intervention | Participants (Count of Participants) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| End of IV therapy72057612 | End of IV therapy72057610 | End of IV therapy72057611 | Test of Cure72057612 | Test of Cure72057611 | Test of Cure72057610 | Late Follow-up72057612 | Late Follow-up72057610 | Late Follow-up72057611 | ||||||||||
| Clinical Success | Clinical Failure | |||||||||||||||||
| GSK2251052 750 mg | 4 | |||||||||||||||||
| Imipenem-Cilastatin | 5 | |||||||||||||||||
| GSK2251052 750 mg | 2 | |||||||||||||||||
| Imipenem-Cilastatin | 0 | |||||||||||||||||
| GSK2251052 1500 mg | 6 | |||||||||||||||||
| Imipenem-Cilastatin | 4 | |||||||||||||||||
| GSK2251052 1500 mg | 2 | |||||||||||||||||
| Imipenem-Cilastatin | 1 | |||||||||||||||||
| GSK2251052 750 mg | 3 | |||||||||||||||||
| Imipenem-Cilastatin | 2 | |||||||||||||||||
| Imipenem-Cilastatin | 3 | |||||||||||||||||
Microbiological response involved both microbiological success and microbiological failure. A reduction in the uropathogens in the urine culture and no growth on blood culture was termed as microbiological success. Increase in the uropathogens in the urine culture and pathogens identified in the blood culture or use of antibacterials other than study treatments were classified as microbiological failures. (NCT01381549)
Timeframe: End of IV therapy (0-24 hours post-therapy), Test of Cure Visit (5 to 9 days post-IV therapy) and Late Follow-up (21-28 days post-therapy)
| Intervention | Participants (Count of Participants) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| End of IV therapy72057612 | End of IV therapy72057610 | End of IV therapy72057611 | Test of Cure72057612 | Test of Cure72057610 | Test of Cure72057611 | Late Folllow-up72057612 | Late Folllow-up72057610 | Late Folllow-up72057611 | ||||||||||
| Microbiological Success | Microbiological Failure | |||||||||||||||||
| Imipenem-Cilastatin | 5 | |||||||||||||||||
| GSK2251052 750 mg | 3 | |||||||||||||||||
| Imipenem-Cilastatin | 0 | |||||||||||||||||
| GSK2251052 750 mg | 1 | |||||||||||||||||
| GSK2251052 1500 mg | 5 | |||||||||||||||||
| Imipenem-Cilastatin | 1 | |||||||||||||||||
| GSK2251052 750 mg | 5 | |||||||||||||||||
| GSK2251052 1500 mg | 3 | |||||||||||||||||
| Imipenem-Cilastatin | 4 | |||||||||||||||||
| GSK2251052 750 mg | 2 | |||||||||||||||||
| GSK2251052 1500 mg | 6 | |||||||||||||||||
| GSK2251052 750 mg | 4 | |||||||||||||||||
| GSK2251052 1500 mg | 2 | |||||||||||||||||
The therapeutic response was the combination of a participant's clinical and microbiological response. It was assessed at the Test of Cure visit in participants who have a qualifying Gram-negative uropathogen at Baseline and have had a minimum of 5 days of IV therapy. Therapeutic response was a measure of the overall efficacy response, and a therapeutic success referred to participants who have been deemed both a 'clinical success' and a 'microbiological success'. All other combinations (other than 'clinical success' + 'microbiological success') were deemed failures for therapeutic response. (NCT01381549)
Timeframe: End of IV therapy (0-24 hours post-therapy) and Late Follow-up (21-28 days post-therapy)
| Intervention | Participants (Count of Participants) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| End of IV therapy72057612 | End of IV therapy72057611 | End of IV therapy72057610 | Late Follow-up72057612 | Late Follow-up72057610 | Late Follow-up72057611 | |||||||
| Therapeutic Failure | Therapeutic Success | |||||||||||
| GSK2251052 750 mg | 3 | |||||||||||
| GSK2251052 1500 mg | 5 | |||||||||||
| Imipenem-Cilastatin | 5 | |||||||||||
| GSK2251052 1500 mg | 3 | |||||||||||
| Imipenem-Cilastatin | 0 | |||||||||||
| GSK2251052 750 mg | 2 | |||||||||||
| GSK2251052 1500 mg | 6 | |||||||||||
| Imipenem-Cilastatin | 1 | |||||||||||
| GSK2251052 750 mg | 4 | |||||||||||
| GSK2251052 1500 mg | 2 | |||||||||||
| Imipenem-Cilastatin | 4 | |||||||||||
Vital sign measurements included respiratory rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean respiration rate are presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Breaths/minute (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 1500 mg | 19.6 | 18.1 | 16.6 | 17.3 | 16.6 | 17.0 | 16.5 | 15.0 | 16.0 | 15.8 | 15.5 | 15.9 | 16.0 |
Vital sign measurements included respiratory rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean respiration rate are presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Breaths/minute (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| Imipenem-Cilastatin | 17.3 | 16.8 | 16.8 | 17.8 | 18.8 | 16.0 | 17.3 | 20.0 | 22.0 | 20.0 | 16.4 | 18.2 | 16.4 | 16.6 |
Vital sign measurements included heart rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean heart rate is presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Beats per minute (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | On IV therapy (Day 11) | On IV therapy (Day 12) | On IV therapy (Day 13) | On IV therapy (Day 14) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 750 mg | 85.8 | 78.2 | 77.8 | 78.5 | 72.3 | 89.0 | 81.0 | 88.0 | 84.0 | 91.0 | 100.0 | 84.0 | 90.0 | 92.0 | 72.8 | 74.5 | 72.5 | 76.8 |
Vital sign measurements included respiratory rate. Measurements that deviated substantially from previous readings were repeated immediately. Mean respiration rate are presented. (NCT01381549)
Timeframe: Up to Late Follow-up Visit (21 to 28 days post-IV therapy)
| Intervention | Breaths/minute (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (Day 1) | On IV therapy (Day 2) | On IV therapy (Day 3) | On IV therapy (Day 4) | On IV therapy (Day 5) | On IV therapy (Day 6) | On IV therapy (Day 7) | On IV therapy (Day 8) | On IV therapy (Day 9) | On IV therapy (Day 10) | On IV therapy (Day 11) | On IV therapy (Day 12) | On IV therapy (Day 13) | On IV therapy (Day 14) | End of IV therapy | Test of Cure | Early Follow-up | Late Follow-up | |
| GSK2251052 750 mg | 17.3 | 15.0 | 14.2 | 15.5 | 14.5 | 16.0 | 16.0 | 16.0 | 14.0 | 17.0 | 15.0 | 16.0 | 14.0 | 14.0 | 16.0 | 14.0 | 15.3 | 13.4 |
All randomized participants who received ≥1 dose of study treatment had AST and ALT levels measured up to 14 days following completion of all study medication. Participants who had 2 confirmed elevations of either AST or ALT that were 5 times ULN or greater were recorded. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam Placebo With Imipenem/Cilastatin | 0 |
An AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. A drug-related (DR) AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product that the investigator determined to be possibly, probably, or definitely related to the treatment. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 10.1 |
| Relebactam 125 mg With Imipenem/Cilastatin | 9.1 |
| Relebactam Placebo With Imipenem/Cilastatin | 9.0 |
A SAE was an AE that resulted in death, was life threatening, resulted in persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was a cancer, was associated with an overdose, was another important medical event. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 3.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam Placebo With Imipenem/Cilastatin | 3.0 |
An AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 28.3 |
| Relebactam 125 mg With Imipenem/Cilastatin | 29.3 |
| Relebactam Placebo With Imipenem/Cilastatin | 30.0 |
All randomized participants who received ≥1 dose of study treatment had AST, ALT, total bilirubin, and Alkaline Phosphatase (ALP) levels measured up to 14 days following completion of all study medication. Participants who had elevations of AST or ALT that were ≥3 times ULN, total bilirubin measurements that were ≥2 times ULN and, at the same time, an ALP measurement of < 2X ULN were recorded. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0 |
| Relebactam Placebo With Imipenem/Cilastatin | 0 |
An AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. Analysis includes specific adverse events with an incidence of ≥4 participants in one treatment group or system organ class. (NCT01505634)
Timeframe: Up to 14 days following completion of all study therapy (up to 28 days)
| Intervention | Percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| Diarrhoea | Nausea | Bacteriuria | White blood cells urine positive | Headache | |
| Relebactam 125 mg With Imipenem/Cilastatin | 2.0 | 6.1 | 2.0 | 1.0 | 3.0 |
| Relebactam 250 mg With Imipenem/Cilastatin | 5.1 | 4.0 | 1.0 | 1.0 | 7.1 |
| Relebactam Placebo With Imipenem/Cilastatin | 4.0 | 4.0 | 4.0 | 4.0 | 4.0 |
An AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. A drug-related AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product that the investigator determined to be possibly, probably, or definitely related to the treatment. (NCT01505634)
Timeframe: Up to 14 days
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 2.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam Placebo With Imipenem/Cilastatin | 1.0 |
An AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol-specified procedure, whether or not considered related to the medicinal product/protocol-specified procedure. Any worsening of a pre-existing condition temporally associated with the use of the product was also an AE. (NCT01505634)
Timeframe: Up to 14 days
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 3.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam Placebo With Imipenem/Cilastatin | 2.0 |
A serious, drug-related (DR) AE was an AE that resulted in death, was life threatening, resulted in persistent or significant disability/incapacity, resulted in or prolonged an existing inpatient hospitalization, was a congenital anomaly/birth defect, was a cancer, was associated with an overdose, was another important medical event. The SAE was determined to be possibly, probably, or definitely related to the treatment by the investigator. (NCT01505634)
Timeframe: Up to 42 days following completion of all study therapy (up to 56 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 1.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0 |
| Relebactam Placebo With Imipenem/Cilastatin | 1.0 |
Clinical response was assessed as favorable (cured or improved) or unfavorable (failure) relative to baseline. Response determination was based on physical findings including fever (or history of fever), chills or rigors (accompanied by fever), flank pain, costovertebral angle tenderness, dysuria, urinary urgency, urinary frequency, suprapubic or pelvic pain, nausea, or vomiting. Clinical response was assessed in the ME population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. (NCT01505634)
Timeframe: At time of last IV dose of study drug (up to postrandomization day 14)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 97.1 |
| Relebactam 125 mg With Imipenem/Cilastatin | 98.7 |
| Relebactam Placebo With Imipenem/Cilastatin | 98.8 |
Clinical response was assessed as favorable (cured or improved) or unfavorable (failure) relative to baseline. Response determination was based on physical findings including fever (or history of fever), chills or rigors (accompanied by fever), flank pain, costovertebral angle tenderness, dysuria, urinary urgency, urinary frequency, suprapubic or pelvic pain, nausea, or vomiting. Clinical response was assessed in the ME population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. (NCT01505634)
Timeframe: Up to 9 days following completion of all study IV and oral therapy (up to Day 23)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 89.1 |
| Relebactam 125 mg With Imipenem/Cilastatin | 91.8 |
| Relebactam Placebo With Imipenem/Cilastatin | 93.4 |
Clinical response was assessed as favorable (cured or improved) or unfavorable (failure) relative to baseline. Response determination was based on physical findings including fever (or history of fever), chills or rigors (accompanied by fever), flank pain, costovertebral angle tenderness, dysuria, urinary urgency, urinary frequency, suprapubic or pelvic pain, nausea, or vomiting. Clinical response was assessed in the ME population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. (NCT01505634)
Timeframe: Up to 42 days following completion of all study IV and oral therapy (up to Day 56)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 88.7 |
| Relebactam 125 mg With Imipenem/Cilastatin | 87.3 |
| Relebactam Placebo With Imipenem/Cilastatin | 88.2 |
"Microbiological response (MR) was assessed based on results of bacterial cultures obtained at completion of IV study medication relative to cultures obtained at baseline. A favorable microbiological response was defined as eradication of all pathogens identified at baseline. Microbiological response was assessed separately for each participant and pathogen identified in the Microbiologically Evaluable (ME) population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. The overall microbiological response was determined as favorable if all pathogens isolated from a participant at baseline demonstrated a favorable response (eradication) at the time point evaluated." (NCT01505634)
Timeframe: At time of last IV dose of study drug (up to post-randomization day 14)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 95.5 |
| Relebactam 125 mg With Imipenem/Cilastatin | 98.6 |
| Relebactam Placebo With Imipenem/Cilastatin | 98.7 |
"Microbiological response was assessed based on results of bacterial cultures obtained at completion of IV study medication relative to cultures obtained at baseline. A favorable microbiological response was defined as eradication of all pathogens identified at baseline. Microbiological response was assessed separately for each participant and pathogen identified in the Microbiologically Evaluable (ME) population that included participants with a urine culture confirmed to be positive for imipenem-resistant gram-negative or anaerobic infections at baseline. The overall microbiological response was determined as favorable if all pathogens isolated from a participant at baseline demonstrated a favorable response (eradication) at the time point evaluated." (NCT01505634)
Timeframe: At time of last IV dose of study drug (up to post-randomization day 14)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 100.0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 100.0 |
| Relebactam Placebo With Imipenem/Cilastatin | 100.0 |
"Microbiological response was assessed based on results of bacterial cultures obtained up to 9 days following completion of all study medication (IV and oral) relative to cultures obtained at baseline. A favorable microbiological response was defined as eradication of all pathogens identified at baseline. Microbiological response was assessed separately for each participant and pathogen identified in the ME population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. The overall microbiological response was determined as favorable if all pathogens isolated from a participant at baseline demonstrated a favorable response (eradication) at the time point evaluated." (NCT01505634)
Timeframe: Up to 9 days following completion of all study IV and oral therapy (up to Day 23)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 61.5 |
| Relebactam 125 mg With Imipenem/Cilastatin | 68.1 |
| Relebactam Placebo With Imipenem/Cilastatin | 70.4 |
"Microbiological response was assessed based on results of bacterial cultures obtained up to 42 days following completion of all study medication (IV and oral) relative to cultures obtained at baseline. A favorable microbiological response was defined as eradication of all pathogens identified at baseline. Microbiological response was assessed separately for each participant and pathogen identified in the ME population that included participants with a urine culture confirmed to be positive for at least 1 gram-negative and/or anaerobic pathogen(s) commonly isolated in UTI. The overall microbiological response was determined as favorable if all pathogens isolated from a participant at baseline demonstrated a favorable response (eradication) at the time point evaluated." (NCT01505634)
Timeframe: Up to 42 days following completion of all study IV and oral therapy (up to Day 56)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 68.3 |
| Relebactam 125 mg With Imipenem/Cilastatin | 65.2 |
| Relebactam Placebo With Imipenem/Cilastatin | 62.5 |
An AE is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the medicinal product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the medicinal product, is also an AE. A drug-related AE is an AE determined by the investigator to be possibly, probably or definitely related to drug treatment. Drug-related AEs assessed by the investigator that caused discontinuation of participant treatment are presented. (NCT01506271)
Timeframe: Up to 14 days post initiation of IV study therapy (up to 14 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 0 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0.9 |
| Placebo to Relebactam With Imipenem/Cilastatin | 2.6 |
A favorable clinical response is assessed by the clinical investigator as a cure, and is defined as a situation where all or most pre-therapy signs and symptoms of the index infection have resolved, or returned to pre-infection status, and no additional antibiotic therapy is required. (NCT01506271)
Timeframe: Up to 9 days following completion of all study therapy (up to Day 23)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 94.9 |
| Relebactam 125 mg With Imipenem/Cilastatin | 94.2 |
| Placebo to Relebactam With Imipenem/Cilastatin | 96.3 |
A serious adverse event (SAE) is any AE occurring at any dose that is life threatening; results in a persistent or significant disability/incapacity; prolongs an existing inpatient hospitalization; is a congenital anomaly/birth defect; or results in death. (NCT01506271)
Timeframe: Up to 14 days following completion of all study therapy (up to Day 28)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 3.4 |
| Relebactam 125 mg With Imipenem/Cilastatin | 9.5 |
| Placebo to Relebactam With Imipenem/Cilastatin | 7 |
Pre-specified events of interest were a confirmed (i.e., verified by repeat testing) elevated AST or ALT laboratory value that is greater than or equal to 3X ULN, as well as elevated total bilirubin greater than or equal to 2X the ULN, and alkaline phosphatase values that are less than 2X the ULN, as a result of within-protocol-specific testing or unscheduled testing. (NCT01506271)
Timeframe: Up to 14 days following completion of all study therapy (up to Day 28)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 0.9 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0 |
| Placebo to Relebactam With Imipenem/Cilastatin | 0 |
Predefined limit of change (PDLC) are presented based on values from the following laboratory tests on serum: alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (Bil), and alkaline phosphatase (AP). Results are presented for PDLC from tests with reported incidence greater than or equal to 4 participants in one treatment group. Laboratory tests which did not achieve the PDLC threshold are not reported. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| ALT >2.5-5.0 X Baseline | ALT >5.0 X Baseline | AST >2.5-5.0 X Baseline | AP >2.5-5.0 X Baseline | |
| Placebo to Relebactam With Imipenem/Cilastatin | 9.1 | 3.6 | 9.2 | 5.5 |
| Relebactam 125 mg With Imipenem/Cilastatin | 2.6 | 6.1 | 14.0 | 2.6 |
| Relebactam 250 mg With Imipenem/Cilastatin | 3.6 | 4.5 | 14.5 | 6.3 |
An AE is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the medicinal product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the medicinal product, is also an AE. AE preferred terms, with incidence greater than or equal to 4 in one treatment group are presented. AEs preferred terms which did not achieve this threshold are not reported. AE preferred terms are based on MedDRA version 17.0. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Diarrhoea | Nausea | Vomiting | Post-operative wound infection | Seroma | ALT increased | AST increased | Lipase increased | Hypertension | |
| Placebo to Relebactam With Imipenem/Cilastatin | 4.4 | 7.0 | 2.6 | 4.4 | 0 | 3.5 | 2.6 | 3.5 | 3.5 |
| Relebactam 125 mg With Imipenem/Cilastatin | 6.0 | 7.8 | 7.8 | 1.7 | 4.3 | 4.3 | 4.3 | 1.7 | 2.6 |
| Relebactam 250 mg With Imipenem/Cilastatin | 6.0 | 6.8 | 6.0 | 2.6 | 0.9 | 4.3 | 4.3 | 2.6 | 0 |
A system organ class (SOC) is the highest level of terminology used to describe disorders of the human body, and distinguishes by either anatomical or physiological systems, disease origin or purpose. SOCs with AE incidence greater than or equal to 4 in one treatment group are presented. SOCs with AE incidence which did not achieve this threshold are not reported. SOCs are based on MedDRA version 17.0. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Blood and lymphatic system disorders | Cardiac disorders | Gastrointestinal disorders | General disorders admin. site conditions | Infections and infestations | Injury, poisoning, procedural complications | Investigations | Nervous system disorders | Psychiatric disorders | Renal and urinary disorders | Respiratory, thoracic, mediastinal disorders | Skin, subcutaneous tissue disorders | Vascular disorders | |
| Placebo to Relebactam With Imipenem/Cilastatin | 5.3 | 2.6 | 13.2 | 3.5 | 7.0 | 5.3 | 12.3 | 4.4 | 3.5 | 3.5 | 6.1 | 1.8 | 6.1 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0.9 | 3.4 | 17.2 | 5.2 | 7.8 | 6.9 | 10.3 | 3.4 | 3.4 | 1.7 | 4.3 | 1.7 | 6.0 |
| Relebactam 250 mg With Imipenem/Cilastatin | 4.3 | 2.6 | 18.8 | 7.7 | 11.1 | 4.3 | 11.1 | 1.7 | 3.4 | 1.7 | 1.7 | 4.3 | 2.6 |
A SAE is any AE occurring at any dose that is life threatening; results in a persistent or significant disability/incapacity; prolongs an existing inpatient hospitalization; is a congenital anomaly/birth defect; or results in death. A drug-related SAE is a SAE determined by the investigator to be possibly, probably or definitely related to drug treatment. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 0.9 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0 |
| Placebo to Relebactam With Imipenem/Cilastatin | 0.9 |
An AE is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the medicinal product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the medicinal product, is also an AE. AEs assessed by the investigator that caused discontinuation of participant treatment are presented. (NCT01506271)
Timeframe: Up to 14 days post initiation of IV study therapy (up to 14 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 0.9 |
| Relebactam 125 mg With Imipenem/Cilastatin | 4.3 |
| Placebo to Relebactam With Imipenem/Cilastatin | 2.6 |
A favorable clinical response was assessed by the clinical investigator as a cure, and was defined as a situation where all or most pre-therapy signs and symptoms of the index infection had resolved, or returned to pre-infection status, and no additional antibiotic therapy was required. (NCT01506271)
Timeframe: 4 to 14 days post initiation of intravenous (IV) study therapy (up to postrandomization Day 14)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 96.3 |
| Relebactam 125 mg With Imipenem/Cilastatin | 98.8 |
| Placebo to Relebactam With Imipenem/Cilastatin | 95.2 |
A favorable clinical response is assessed by the clinical investigator as a cure, and is defined as a situation where all or most pre-therapy signs and symptoms of the index infection have resolved, or returned to pre-infection status, and no additional antibiotic therapy is required. (NCT01506271)
Timeframe: 4 to 14 days post initiation of IV study therapy (up to postrandomization day 14).
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 100 |
| Relebactam 125 mg With Imipenem/Cilastatin | 100 |
| Placebo to Relebactam With Imipenem/Cilastatin | 100 |
A favorable clinical response is assessed by the clinical investigator as a cure, and is defined as a situation where all or most pre-therapy signs and symptoms of the index infection have resolved, or returned to pre-infection status, and no additional antibiotic therapy is required. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 93.7 |
| Relebactam 125 mg With Imipenem/Cilastatin | 95.3 |
| Placebo to Relebactam With Imipenem/Cilastatin | 94.9 |
A favorable microbiological response is assessed by the clinical investigator, and is defined as the eradication or presumptive eradication of all bacterial pathogens identified at baseline. (NCT01506271)
Timeframe: Up to 14 days post initiation of IV study therapy (up to postrandomization day 14)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 97.6 |
| Relebactam 125 mg With Imipenem/Cilastatin | 100 |
| Placebo to Relebactam With Imipenem/Cilastatin | 97.6 |
A favorable microbiological response is assessed by the clinical investigator, and is defined as the eradication or presumptive eradication of all bacterial pathogens identified at baseline. (NCT01506271)
Timeframe: Up to 9 days following completion of all study therapy (up to Day 23)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 97.4 |
| Relebactam 125 mg With Imipenem/Cilastatin | 97.6 |
| Placebo to Relebactam With Imipenem/Cilastatin | 97.5 |
A favorable microbiological response is assessed by the clinical investigator, and is defined as the eradication or presumptive eradication of all bacterial pathogens identified at baseline. (NCT01506271)
Timeframe: Up to 42 days following completion of all study therapy (up to Day 56)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 96.2 |
| Relebactam 125 mg With Imipenem/Cilastatin | 97.5 |
| Placebo to Relebactam With Imipenem/Cilastatin | 96.2 |
Pre-specified events of interest were confirmed (i.e., verified by repeat testing) elevated AST or ALT laboratory value that is greater than or equal to 5 X ULN as a result of within-protocol-specific testing or unscheduled testing. (NCT01506271)
Timeframe: Up to 14 days following completion of all study therapy (up to Day 28)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 1.7 |
| Relebactam 125 mg With Imipenem/Cilastatin | 0 |
| Placebo to Relebactam With Imipenem/Cilastatin | 1.8 |
An adverse event (AE) is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the medicinal product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the medicinal product, is also an AE. (NCT01506271)
Timeframe: Up to 14 days following completion of all study therapy (up to Day 28)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 48.7 |
| Relebactam 125 mg With Imipenem/Cilastatin | 47.4 |
| Placebo to Relebactam With Imipenem/Cilastatin | 41.2 |
An AE is any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the medicinal product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which is temporally associated with the use of the medicinal product, is also an AE. A drug-related AE is a AE determined by the investigator to be possibly, probably or definitely related to drug treatment. (NCT01506271)
Timeframe: Up to 14 days following completion of all study therapy (up to Day 28)
| Intervention | Percentage of participants (Number) |
|---|---|
| Relebactam 250 mg With Imipenem/Cilastatin | 13.7 |
| Relebactam 125 mg With Imipenem/Cilastatin | 13.8 |
| Placebo to Relebactam With Imipenem/Cilastatin | 9.6 |
To measure and compare the rates of infection following TRUSP in subjects with and without CR-GNB. This measure is number of participants with post-biopsy infection. (NCT01659866)
Timeframe: 30 days post-biopsy
| Intervention | participants (Number) |
|---|---|
| Cipro-susceptible | 6 |
| Cipro-resistant | 3 |
The clinical response was to be determined by the investigator and was classified as 1 of the following: cure (relevant clinical signs and symptoms of infection at baseline disappeared or recovered to normal and relevant non microbiological results of laboratory tests returned to normal level or the resolution of signs and symptoms so that at no further therapy was required), failure (participant required additional surgical or radiologic intervention and/or received additional anti-infection therapy to cure the infection since administration of study drug until TOC; or death after study Day 2 due to the infection or a treatment related AE or discontinuation due to a treatment related AE or received greater than 120% of the prescribed number of investigational product doses), or indeterminate (lost to follow-up; or died within 2 days after the first dose of study drug for any reason; or died after study Day 2 but prior to the TOC assessment because of non infection related reasons). (NCT01721408)
Timeframe: Day 3, Day 14 or last day of therapy (treatment duration was at least 5 days and up to 14 days), and TOC (14-21 days after the last dose of therapy)
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Cure | Failure | |
| Imipenem/Cilastatin | 96.6 | 3.4 |
| Tigecycline 50mg | 89.9 | 10.1 |
The clinical response was to be determined by the investigator and was classified as 1 of the following: cure (relevant clinical signs and symptoms of infection at baseline disappeared or recovered to normal and relevant non microbiological results of laboratory tests returned to normal level or the resolution of signs and symptoms so that at no further therapy was required), failure (participant required additional surgical or radiologic intervention and/or received additional anti-infection therapy to cure the infection since administration of study drug until TOC; or death after study Day 2 due to the infection or a treatment related AE or discontinuation due to a treatment related AE or received greater than 120% of the prescribed number of investigational product doses), or indeterminate (lost to follow-up; or died within 2 days after the first dose of study drug for any reason; or died after study Day 2 but prior to the TOC assessment because of non infection related reasons). (NCT01721408)
Timeframe: Day 3, Day 14 or last day of therapy (treatment duration was at least 5 days and up to 14 days), and TOC (14-21 days after the last dose of therapy)
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Cure | Failure | |
| Imipenem/Cilastatin | 95.3 | 4.7 |
| Tigecycline 50mg | 88.0 | 12.0 |
The clinical response was to be determined by the investigator and was classified as 1 of the following: cure (relevant clinical signs and symptoms of infection at baseline disappeared or recovered to normal and relevant non microbiological results of laboratory tests returned to normal level or the resolution of signs and symptoms so that at no further therapy was required), failure (participant required additional surgical or radiologic intervention and/or received additional anti-infection therapy to cure the infection since administration of study drug until TOC; or death after study Day 2 due to the infection or a treatment related AE or discontinuation due to a treatment related AE or received greater than 120% of the prescribed number of investigational product doses), or indeterminate (lost to follow-up; or died within 2 days after the first dose of study drug for any reason; or died after study Day 2 but prior to the TOC assessment because of non infection related reasons). (NCT01721408)
Timeframe: Day 3, Day 14 or last day of therapy (treatment duration was at least 5 days and up to 14 days), and TOC (14-21 days after the last dose of therapy)
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Cure | Failure | Indeterminate | |
| Imipenem/Cilastatin | 88.7 | 3.5 | 7.8 |
| Tigecycline 50mg | 82.8 | 10.3 | 6.9 |
The microbiological response at the subject level was described according to the following definitions of efficacy. Eradication (documented or presumed): none of the baseline pathogens were present in repeat intra-abdominal cultures from the original site of infection taken during the study or a clinical response of cure precluded the necessity of a repeat intra-abdominal culture. Persistence (documented or presumed): documented: any baseline intra-abdominal pathogen was present in the cultures obtained from the original site of the intra-abdominal abscess, peritonitis, or surgical wound infection during the study; Presumed: repeat microbiological data were not obtained for a participant with a clinical response of failure. Superinfection: Emergence of a new pathogen during therapy, at the site of infection with emergence or worsening of clinical signs and symptoms of infection. (NCT01721408)
Timeframe: Day 3, Day 14 or last day of therapy (treatment duration was at least 5 days and up to 14 days), and TOC (14-21 days after the last dose of therapy)
| Intervention | percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Eradication (N=125, 107) | Documented Eradication (N=110, 102) | Presumed Eradication (N=110, 102) | Persistence (N=125, 107) | Documented Persistence (N=13, 5) | Presumed Persistence (N=13, 5) | Superinfection (N=125, 107) | |
| Imipenem/Cilastatin | 95.3 | 0.0 | 100.0 | 4.7 | 20.0 | 80.0 | 0.0 |
| Tigecycline 50mg | 88.0 | 2.7 | 97.3 | 10.4 | 7.7 | 92.3 | 1.6 |
An AE was any untoward medical occurrence without regard to causality in a participant who received study drug. A SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. AEs included both AEs and Non-SAEs. (NCT01721408)
Timeframe: From the first dose of study treatment through post therapy follow-up (28 days after the last dose of therapy)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Number (#) of Participants with AEs | # of Participants with Treatment-Related AEs | # of Participants with SAEs | # of Participants with Treatment-Related SAEs | |
| Imipenem/Cilastatin | 108 | 29 | 15 | 7 |
| Tigecycline 50mg | 131 | 53 | 32 | 19 |
Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as all bacterial uropathogens found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less. (NCT02321800)
Timeframe: End of treatment, Day 7 to 14
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 96.8 |
| Imipenem/Cilastatin | 95.8 |
Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as all bacterial uropathogens found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less. (NCT02321800)
Timeframe: Early assessment, Day 4
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 92.1 |
| Imipenem/Cilastatin | 90.8 |
"The primary efficacy endpoint was the composite outcome of clinical response and microbiological response at the test of cure assessment, defined as 7 days (±2 days) after the end of antibiotic treatment.~Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms.~Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less." (NCT02321800)
Timeframe: Test of cure (TOC; 7 days after end of treatment [EOT], equivalent to Study Day 14 to 21)
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 72.6 |
| Imipenem/Cilastatin | 54.6 |
"A composite response of clinical response and microbiological response at the follow-up assessment, defined as 14 days after the end of treatment.~Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with sustained response defined as all pre-therapy signs and symptoms of cUTI show no evidence of recurrence after administration of the last dose of study drug.~Microbiological outcome was based on quantitative microbiological urine cultures, with sustained eradication defined as a urine culture obtained after documented eradication at the TOC, up to and including the FUP, showed that the bacterial uropathogen(s) identified at baseline at ≥ 10⁵ CFU/mL remained < 10⁴ CFU/mL." (NCT02321800)
Timeframe: Follow-up (FUP; 14 days after end of treatment, Day 21 to 28)
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 54.4 |
| Imipenem/Cilastatin | 39.5 |
"A composite outcome of clinical response and microbiological response at the end of treatment, defined as the end of the last infusion of antibiotic treatment.~Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms.~Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less." (NCT02321800)
Timeframe: End of treatment (EOT; Day 7 to 14)
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 96.4 |
| Imipenem/Cilastatin | 95.8 |
"A composite outcome of clinical response and microbiological response at the early assessment, defined as Day 4 of antibiotic treatment.~Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms.~Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less." (NCT02321800)
Timeframe: Early assessment (EA; Day 4)
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 88.1 |
| Imipenem/Cilastatin | 87.4 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. (NCT02321800)
Timeframe: Test of cure, 7 days after end of treatment, Day 14 to 21
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 89.7 |
| Imipenem/Cilastatin | 87.4 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with sustained response defined as all pre-therapy signs and symptoms of cUTI showing no evidence of recurrence after administration of the last dose of study drug. (NCT02321800)
Timeframe: Follow-up, 14 days after end of treatment, Day 21 to 28
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 81.3 |
| Imipenem/Cilastatin | 72.3 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. (NCT02321800)
Timeframe: End of treatment, Day 7 to 14
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 98.0 |
| Imipenem/Cilastatin | 99.2 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. (NCT02321800)
Timeframe: Early assessment, Day 4
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 90.5 |
| Imipenem/Cilastatin | 90.8 |
(NCT02321800)
Timeframe: Day 3, 2 hours and 6 hours after end of infusion
| Intervention | µg/mL (Mean) | |
|---|---|---|
| 2 hours after end of infusion | 6 hours after end of infusion | |
| Cefiderocol | 2710 | 1520 |
(NCT02321800)
Timeframe: On Day 3 of dosing prior to infusion, end of infusion, and at 1 hour post infusion
| Intervention | µg/mL (Mean) | ||
|---|---|---|---|
| Pre-infusion | End of infusion | 1 hour after end of infusion | |
| Cefiderocol | 18.0 | 141 | 70.2 |
"Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less.~Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis." (NCT02321800)
Timeframe: Test of cure; 7 days after end of treatment, Day 14 to 21
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 75.0 | 75.0 | 44.4 | 76.5 |
| Imipenem/Cilastatin | 58.2 | 52.0 | 60.0 | 50.0 |
"Microbiological outcome was based on quantitative microbiological urine cultures, with sustained eradication defined as a urine culture obtained after documented eradication at the TOC, up to and including the FUP, where the bacterial uropathogen identified at baseline at ≥ 10⁵ CFU/mL remained < 10⁴ CFU/mL.~Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis." (NCT02321800)
Timeframe: Follow-up, 14 days after the end of treatment, Day 21 to 28
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 59.9 | 58.3 | 27.8 | 64.7 |
| Imipenem/Cilastatin | 41.8 | 52.0 | 20.0 | 0 |
"Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less.~Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis." (NCT02321800)
Timeframe: End of treatment, Day 7 to 14
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 98.7 | 97.9 | 88.9 | 94.1 |
| Imipenem/Cilastatin | 97.5 | 92.0 | 100.0 | 100.0 |
"Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as the bacterial pathogen found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less.~Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis." (NCT02321800)
Timeframe: Early assessment, Day 4
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 92.8 | 89.6 | 94.4 | 88.2 |
| Imipenem/Cilastatin | 94.9 | 88.0 | 80.0 | 100.0 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis. (NCT02321800)
Timeframe: Test of cure, 7 days after end of treatment, Day 14 to 21
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 89.7 | 89.1 | 73.3 | 100.0 |
| Imipenem/Cilastatin | 88.3 | 84.0 | 75.0 | 100.0 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with sustained response defined as all pre-therapy signs and symptoms of cUTI show no evidence of recurrence after administration of the last dose of study drug. Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis. (NCT02321800)
Timeframe: Follow-up, 14 days after the end of treatment, Day 21 to 28
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 82.9 | 82.6 | 53.3 | 84.6 |
| Imipenem/Cilastatin | 72.7 | 68.0 | 75.0 | 100.0 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis. (NCT02321800)
Timeframe: End of treatment, Day 7 to 14
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 97.9 | 100.0 | 93.3 | 100.0 |
| Imipenem/Cilastatin | 98.7 | 100.0 | 100.0 | 100.0 |
Clinical response was based on the investigator's evaluation of the participant's clinical signs and symptoms, with response defined as resolution or improvement of complicated urinary tract infection symptoms present at study entry and the absence of new symptoms. Results are reported for the 4 most frequent uropathogens, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis. (NCT02321800)
Timeframe: Early assessment, Day 4
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Escherichia coli | Klebsiella pneumoniae | Pseudomonas aeruginosa | Proteus mirabilis | |
| Cefiderocol | 91.8 | 82.6 | 93.3 | 84.6 |
| Imipenem/Cilastatin | 96.1 | 88.0 | 75.0 | 100.0 |
"A serious adverse event was defined by regulation as any adverse event (AE) occurring at any dose that resulted in any of the following outcomes:~Death~Life-threatening condition~Hospitalization or prolongation of existing hospitalization~Persistent or significant disability/incapacity~Congenital anomaly/birth defect~Other medically important condition.~The relationship of an event to the study drug was determined by the investigator based on whether the AE could be reasonably explained as being caused by the study drug." (NCT02321800)
Timeframe: From first dose of study drug until 28 days after end of treatment; Day 35 to 42
| Intervention | Participants (Count of Participants) | ||||||
|---|---|---|---|---|---|---|---|
| All adverse events | Drug-related adverse events | Deaths | Serious adverse events | Drug-related serious adverse events | Discontinuation of study drug due to AE | Discontinuation due to drug-related AE | |
| Cefiderocol | 122 | 27 | 1 | 14 | 1 | 5 | 3 |
| Imipenem/Cilastatin | 76 | 17 | 0 | 12 | 1 | 3 | 0 |
Microbiological outcome was based on quantitative microbiological urine cultures, with eradication defined as all bacterial uropathogens found at study entry at > 1 × 10⁵ CFU/mL reduced to 1 × 10⁴ CFU/mL or less. (NCT02321800)
Timeframe: Test of cure (7 days after end of treatment, Day 14 to 21)
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 73.0 |
| Imipenem/Cilastatin | 56.3 |
Microbiological outcome was based on quantitative microbiological urine cultures, with sustained eradication defined as a urine culture obtained after documented eradication at the TOC, up to and including the FUP, where the bacterial uropathogen(s) identified at baseline at ≥ 10⁵ CFU/mL remained < 10⁴ CFU/mL. (NCT02321800)
Timeframe: Follow-up, 14 days after end of treatment, Day 21 to 28
| Intervention | percentage of participants (Number) |
|---|---|
| Cefiderocol | 57.1 |
| Imipenem/Cilastatin | 43.7 |
The percentage of participants experiencing AEs that occurred in ≥4 participants within either Group 1 or Group 2 was assessed. An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol; Group 3 had <4 participants and therefore no data are presented. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) | |
|---|---|---|
| Pyrexia | Blood creatinine increased | |
| Group 1: Imipenem+Cilastatin/Relebactam | 12.9 | 0.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 12.5 | 25.0 |
The percentage of participants with all-cause mortality up to Day 28 was determined for Groups 1 and 2. (NCT02452047)
Timeframe: Up to Day 28
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 9.5 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 30.0 |
The percentage of participants in Groups 1, 2, and 3 experiencing ≥1 SAEs during treatment and 14-day follow-up was determined. An SAE is any untoward medical occurrence that, at any dose, results in death; is life-threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant injury/incapacity; is a congenital anomaly/birth defect; or is an other important medical event. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 9.7 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 31.3 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 100.0 |
The percentage of participants in Groups 1, 2, and 3 experiencing ≥1 drug-related SAEs during treatment and 14-day follow-up was determined. A drug-related SAE is any untoward medical occurrence that, at any dose, results in death; is life-threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant injury/incapacity; is a congenital anomaly/birth defect; or is an other important medical event, that is considered by the investigator to be related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 0.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 0.0 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 33.3 |
"The percentage of participants with FCR at EOT was determined for Groups 1 and 2. FCR at EOT was defined as cure or improved. Cure was defined as all pretherapy signs and symptoms of index infection resolved or returned to preinfection status, and no additional IV antibiotic therapy required, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures performed. Improved was defined as all or most pretherapy signs and symptoms of index infection have improved or resolved, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures have been performed." (NCT02452047)
Timeframe: At EOT (up to Day 21)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 90.5 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 60.0 |
"The percentage of participants with a FCR at OTX was determined for Groups 1 and 2. FCR at OTX was defined as improved. Improved was defined as all or most pretherapy signs and symptoms of index infection have improved or resolved, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures have been performed." (NCT02452047)
Timeframe: OTX (Day 3)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 81.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 40.0 |
"The percentage of participants with FMR at EOT was determined for participants with cUTI in Groups 1 and 2. FMR was defined as urine culture results at EOT showing eradication (i.e., ≥10^5 CFU/mL at baseline was reduced to <10^4 CFU/mL at EOT) or sustained eradication (i.e., ≥10^5 CFU/mL at baseline that was reduced to <10^4 CFU/mL previously remained <10^4 CFU/mL at EOT) of the uropathogen." (NCT02452047)
Timeframe: At EOT (up to Day 21)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 100.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 100.0 |
The percentage of participants in Groups 1, 2, and 3 having ECIs within 2 categories was determined. Category 1 ECIs included post-baseline laboratory values of an elevated aspartate aminotransferase (AST) or alanine aminotransferase (ALT) value that is ≥3x upper limit of normal (ULN) and an elevated total bilirubin value that is ≥2x ULN and (at the same time) an alkaline phosphatase value that is ≤2x ULN. Category 2 ECIs included a confirmed elevated AST or ALT value that is ≥5x ULN. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) | |
|---|---|---|
| Category 1 ECI | Category 2 ECI | |
| Group 1: Imipenem+Cilastatin/Relebactam | 0.0 | 0.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 12.5 | 12.5 |
The percentage of participants in Groups 1, 2, and 3 experiencing ≥1 drug-related AEs during treatment and 14-day follow-up was determined. A drug-related AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, and considered by the investigator to be related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 16.1 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 31.3 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 33.3 |
The percentage of participants in Groups 1, 2, and 3 experiencing ≥1 AEs during treatment and 14-day follow-up was determined. An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 71.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 81.3 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 100.0 |
The percentage of participants in Groups 1, 2, and 3 discontinuing from study drug due to ≥1 drug-related AEs during the treatment period was determined. A drug-related AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, and considered by the investigator to be related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 21
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 0.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 12.5 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 33.3 |
The percentage of participants in Group 1, 2, and 3 discontinuing from study drug due to ≥1 AEs during the treatment period was determined. An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. Statistical analysis included only Groups 1 and 2 as indicated by the protocol. (NCT02452047)
Timeframe: Up to Day 21
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 0.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 18.8 |
| Group 3: Open-Label Imipenem+Cilastatin/Relebactam | 33.3 |
"Treatment-emergent nephrotoxity was assessed in Groups 1 and 2 as indicated by the protocol (Group 3 was not included). Nephrotoxicity for participants with normal baseline serum creatinine levels (<1.2 mg/dL) was defined as doubling of serum creatinine to >1.2 mg/dL or reduction in creatinine clearance (ClCR) of ≥50%. Nephrotoxicity for participants with pre-existing renal dysfunction (baseline serum creatinine level ≥1.2 mg/dL) was defined as increase in serum creatinine by ≥1 mg/dL or reduction from baseline ClCR of ≥20% or need for renal replacement therapy (RRT)." (NCT02452047)
Timeframe: Up to Day 35 (up to 14 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 10.3 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 56.3 |
"The percentage of participants with FMR at EFU was determined for participants with cUTI in Groups 1 and 2. FMR was defined as urine culture results at EFU showing sustained eradication (i.e., ≥10^5 CFU/mL at baseline that was reduced to <10^4 CFU/mL previously remained <10^4 CFU/mL at EFU) of the uropathogen." (NCT02452047)
Timeframe: EFU (Between Day 10 and Day 30 [5 to 9 Days after EOT])
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 72.7 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 100.0 |
"The percentage of participants with FMR at OTX was determined for participants with cUTI in Groups 1 and 2. FMR was defined as urine culture results at OTX showing eradication (i.e., ≥10^5 colony forming units [CFU]/mL at baseline was reduced to <10^4 CFU/mL at OTX) of the uropathogen." (NCT02452047)
Timeframe: OTX (Day 3)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 100.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 100.0 |
"The percentage of participants with FCR at Day 28 was determined for Groups 1 and 2. FCR at Day 28 was defined as sustained cure or cure. Sustained cure (for participants with cure response at the prior visit) was defined as all pretherapy signs and symptoms of index infection resolved with no evidence of resurgence and no additional antibiotic therapy required, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures have been performed. Cure (for participants with improved response at EOT visit) was defined as all pretherapy signs and symptoms of index infection resolved or returned to preinfection status, and no additional IV antibiotic therapy required, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures performed." (NCT02452047)
Timeframe: Day 28
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 71.4 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 40.0 |
The percentage of participants with FOR was determined for Groups 1 and 2. FOR was determined based on clinically relevant outcomes for the primary site of infection as follows: HABP/VABP: survival through Day 28; cIAI: favorable clinical response (all pretherapy symptoms of index infection resolved with no evidence of resurgence, no additional antibiotic therapy required, and no unplanned surgical or percutaneous drainage procedures) at Day 28; cUTI: favorable composite clinical response (all pretherapy symptoms of index infection resolved with no evidence of resurgence, no additional antibiotic therapy required) and microbiological response (urine culture shows sustained eradication of the baseline uropathogen [e.g., ≥10^5 CFU/mL at study entry is reduced to <10^4 CFU/mL]) at Early Follow-up (EFU). (NCT02452047)
Timeframe: Up to Day 30 (up to 9 days after completing study treatment)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 71.4 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 70.0 |
"The percentage of participants with FCR at EFU was determined for Groups 1 and 2. FCR at EFU was defined as sustained cure or cure. Sustained cure (for participants with cure response at the prior visit) was defined as all pretherapy signs and symptoms of index infection resolved with no evidence of resurgence and no additional antibiotic therapy required, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures have been performed. Cure (for participants with improved response at EOT visit) was defined as all pretherapy signs and symptoms of index infection resolved or returned to preinfection status, and no additional IV antibiotic therapy required, and (for cIAI participants) no unplanned surgical procedures or percutaneous drainage procedures performed." (NCT02452047)
Timeframe: EFU (Between Day 10 and Day 30 [5 to 9 Days after EOT])
| Intervention | Percentage of Participants (Number) |
|---|---|
| Group 1: Imipenem+Cilastatin/Relebactam | 81.0 |
| Group 2: Colistimethate Sodium + Imipenem+Cilastatin | 50.0 |
"The percentage of participants with a FCR at EFU was determined for each arm. Favorable clinical response at EFU was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 74.3 |
| PIP/TAZ | 79.4 |
"The percentage of participants with a FCR at EOT was determined for each arm. Favorable clinical response at EOT was defined as either cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required) or improved (the majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: From Day 7 to Day 14
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 84.7 |
| PIP/TAZ | 85.3 |
"The percentage of participants with a FCR at OTX2 was determined for each arm. Favorable clinical response at OTX2 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 6 (OTX2)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 85.5 |
| PIP/TAZ | 87.8 |
"The percentage of participants with a FCR at OTX3 was determined for each arm. Favorable clinical response at OTX3 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 10 (OTX3)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 89.6 |
| PIP/TAZ | 83.6 |
"The percentage of participants with a FCR at OTX1 was determined for each arm. Favorable clinical response at OTX1 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 3 (OTX1)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 70.8 |
| PIP/TAZ | 72.8 |
"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 89.9 |
| PIP/TAZ | 86.4 |
"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: From Day 7 to Day 14
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 87.1 |
| PIP/TAZ | 85.5 |
"The percentage of participants with a FCR at EFU was determined for each arm. Favorable clinical response at EFU was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 61.0 |
| PIP/TAZ | 55.8 |
"The percentage of participants with a FCR at OTX2 was determined for each arm. Favorable clinical response at OTX2 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 6 (OTX2)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 83.5 |
| PIP/TAZ | 83.1 |
"The percentage of participants with a FCR at OTX1 was determined for each arm. Favorable clinical response at OTX1 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 3 (OTX1)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 68.0 |
| PIP/TAZ | 64.7 |
"The percentage of participants with a FCR at OTX3 was determined for each arm. Favorable clinical response at OTX3 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 10 (OTX3)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 83.5 |
| PIP/TAZ | 80.4 |
"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: From Day 7 to Day 14
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 77.2 |
| PIP/TAZ | 67.9 |
"The percentage of participants with a FMR at EFU was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EFU showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 67.9 |
| PIP/TAZ | 61.9 |
An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02493764)
Timeframe: Up to 30 days
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 85.0 |
| PIP/TAZ | 86.6 |
The percentage of participants in the MITT population with mortality due to any cause from randomization through EFU was determined for each arm. (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 14.8 |
| PIP/TAZ | 19.5 |
The percentage of participants in the mMITT population with mortality due to any cause from randomization through EFU was determined for each arm. (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 15.3 |
| PIP/TAZ | 18.3 |
The percentage of participants in the mMITT population with mortality due to any cause from randomization through Day 28 was determined for each arm. (NCT02493764)
Timeframe: Up to 28 days
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 16.7 |
| PIP/TAZ | 20.2 |
The percentage of participants in the MITT population with mortality due to any cause from randomization through Day 28 was determined for each arm. (NCT02493764)
Timeframe: Up to 28 days
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 15.9 |
| PIP/TAZ | 21.3 |
"The percentage of participants with a FCR at EOT was determined for each arm. Favorable clinical response at EOT was defined as either cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required) or improved (the majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: From Day 7 to Day 14
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 74.2 |
| PIP/TAZ | 69.7 |
An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02493764)
Timeframe: Up to 14 days
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 5.6 |
| PIP/TAZ | 8.2 |
"The percentage of participants with a FCR at Day 28 was determined for each arm. Favorable clinical response at Day 28 was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Day 28
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 70.5 |
| PIP/TAZ | 75.6 |
"The percentage of participants with a FCR at Day 28 was determined for each arm. Favorable clinical response at Day 28 was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Day 28
| Intervention | Percentage of participants (Number) |
|---|---|
| IMI/REL | 51.9 |
| PIP/TAZ | 50.6 |
Any harmful, undesirable, potentially serious and life threatening effects occurring during or after administration of the antibiotics proposed in this study (piperacillin / tazobactam, imipenem or meropenem), was evaluated as: none or adverse event classified according to the intensity of the clinical manifestation (severity) as: mild, moderate or severe and for each antibiotic. (NCT03019965)
Timeframe: Number of participants with adverse events evaluated by an physician at the time of administration of antibiotics, up to an average to 24 hours after the study drug cessation.
| Intervention | Participants (Count of Participants) |
|---|---|
| Intermittent. Piperacillin/Tazobactam, Imipenem, Meropenem | 1 |
| Prolonged Infusion. Continuous Piperacillin/Tazobactam, Extended Imipenem, Extended Meropenem | 3 |
"Resolution. Disappearance of all signs and symptoms related to the infection.~Failure. Insufficient lessening of the signs and symptoms of infection to qualify as improvement, including death or indeterminate (no evaluation possible, for any reason)." (NCT03019965)
Timeframe: Number of participants with clinical response at 14 days after antibiotic cessation, up to an average of 28 days or the day of your discharge if this occurred before 14 days after antibiotic cessation.
| Intervention | Participants (Count of Participants) |
|---|---|
| Intermittent. Piperacillin/Tazobactam, Imipenem, Meropenem | 178 |
| Prolonged Infusion. Continuous Piperacillin/Tazobactam, Extended Imipenem, Extended Meropenem | 169 |
"The percentage of participants with cIAI who display a favorable clinical response at End of Therapy visit was presented. Per protocol, a subset of the cIAI/cUTI study arm was analyzed: only participants with cIAI were evaluated because clinical response is primarily relevant to cIAI. Favorable clinical response is a rating of cure or improved as determined by the investigator at the End of Therapy Visit. Cure is defined as: all pretherapy signs and symptoms of the index infection(s) have resolved (or returned to preinfection status) AND no additional intravenous antibiotic therapy is required AND no unplanned surgical or percutaneous drainage procedures have been performed. Improved is defined as: All or most pretherapy signs and symptoms of the index infection(s) have improved or resolved (or returned to preinfection status) AND no additional intravenous antibiotic therapy is required AND no unplanned surgical or percutaneous drainage procedures have been performed." (NCT03293485)
Timeframe: Between Day 5 and Day 14 (End of Therapy Visit)
| Intervention | Percentage of Participants (Number) |
|---|---|
| cIAI | 85.7 |
The percentage of participants who discontinued from study medication due to an adverse event was calculated. An AE was defined as any unfavorable and unintended sign, symptom, or disease (new or worsening) temporally associated with the use of study therapy, regardless of whether or not a causal relationship with the study therapy could be determined. (NCT03293485)
Timeframe: Up to 14 days (End of Therapy Visit)
| Intervention | Percentage of Participants (Number) |
|---|---|
| cIAI/cUTI | 4.9 |
The percentage of participants with cUTI who display a favorable Overall Microbiological Response at the End of Therapy visit was calculated. Per protocol, only a subset of the cIAI/cUTI study arm was analyzed: only participants with cUTI were evaluated because the microbiological response evaluation is primarily relevant to cUTI. A favorable Overall Microbiological Response is defined as a urine culture taken at the End of Therapy Visit showing eradication (e.g., ≥10^5 CFU/mL is reduced to <10^4 CFU/mL) of all uropathogens found at study entry. (NCT03293485)
Timeframe: Between Day 5 and Day 14 (End of Therapy Visit)
| Intervention | Percentage of Participants (Number) |
|---|---|
| cUTI | 100 |
The percentage of participants experiencing ≥1 AE was calculated. An AE was defined as any unfavorable and unintended sign, symptom, or disease (new or worsening) temporally associated with the use of study therapy, regardless of whether or not a causal relationship with the study therapy could be determined. (NCT03293485)
Timeframe: Up to 28 days
| Intervention | Percentage of Participants (Number) |
|---|---|
| cIAI/cUTI | 74.1 |
The percentage of participants with cUTI who display a favorable Overall Microbiological Response at the Test of Cure visit was calculated. Per protocol, only a subset of the cIAI/cUTI study arm was analyzed: only participants with cUTI were evaluated because the microbiological response evaluation is primarily relevant to cUTI. A favorable Overall Microbiological Response is defined as a urine culture taken at the Test of Cure visit still showing eradication (e.g., ≥10^5 CFU/mL is reduced to <10^4 CFU/mL) of all uropathogens found at study entry. (NCT03293485)
Timeframe: Between Day 10 and Day 23 (Test of Cure Visit)
| Intervention | Percentage of Participants (Number) |
|---|---|
| cUTI | 59.0 |
"The percentage of participants with cIAI who display a favorable Clinical Response at the Test of Cure visit was calculated. Per protocol, only a subset of the cIAI/cUTI study arm was analyzed: only participants with cIAI were evaluated because the clinical response evaluation is primarily relevant to cIAI. A favorable clinical response is a rating of cure as determined by the investigator at the Test of Cure Visit. Cure is defined as: all pretherapy signs and symptoms of the index infection(s) have resolved (or returned to preinfection status) AND no additional intravenous antibiotic therapy is required AND no unplanned surgical or percutaneous drainage procedures have been performed." (NCT03293485)
Timeframe: Between Day 10 and Day 23 (Test of Cure Visit)
| Intervention | Percentage of Participants (Number) |
|---|---|
| cIAI | 82.1 |
Proportion of patients with a response of clinical cure for the MITT(modified intent to treat), m-MITT (microbiologically modified intent to treat), CE(clinically evaluable), and ME(microbiologically evaluable) populations at the TOC(test of cure) visit. (NCT03445195)
Timeframe: Baseline to day 21
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| MITT population | m-MITT population | CE population | ME population | |
| Placebo + Imipenem/Cilastatin | 27 | 21 | 27 | 21 |
| Sulbactam-ETX2514 (ETX2514SUL) + Imipenem/Cilastatin | 52 | 46 | 52 | 45 |
The primary efficacy endpoint for this study was the proportion of patients with an overall success (clinical cure and micro-biologic eradication) for the m-MITT (Micro-biologically Modified Intent-to-Treat) Population at the TOC Visit. (NCT03445195)
Timeframe: From baseline through day 21
| Intervention | Participants (Count of Participants) |
|---|---|
| Sulbactam-ETX2514 (ETX2514SUL) + Imipenem/Cilastatin | 36 |
| Placebo + Imipenem/Cilastatin | 17 |
Proportion of patients with a response of microbiologic eradication for the m-MITT(microbiologically modified intent to treat) and ME(microbiologically evaluable) populations at the TOC visit (NCT03445195)
Timeframe: Baseline to day 21
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| m-MITT population | ME population | |
| Placebo + Imipenem/Cilastatin | 17 | 17 |
| Sulbactam-ETX2514 (ETX2514SUL) + Imipenem/Cilastatin | 37 | 36 |
The primary efficacy endpoint for the study is 28-day all-cause mortality in the CRABC m-MITT population in Part A. (NCT03894046)
Timeframe: 28 Days
| Intervention | Participants (Count of Participants) |
|---|---|
| Part A - Group 1 | 12 |
| Part A - Group 2 | 20 |
The primary safety endpoint for the study is nephrotoxicity, as measured by the Risk-Injury-Failure-Loss-End-stage renal disease (RIFLE) criteria, in the MITT population in Part A. (NCT03894046)
Timeframe: 28 days
| Intervention | Participants (Count of Participants) |
|---|---|
| Part A - Group 1 | 12 |
| Part A - Group 2 | 32 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| melatonin [no description available] | 2.08 | 1 | 0 | acetamides; tryptamines | anticonvulsant; central nervous system depressant; geroprotector; hormone; human metabolite; immunological adjuvant; mouse metabolite; radical scavenger |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 2.08 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| 1-(3-chlorophenyl)piperazine 1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone. | 2.08 | 1 | 0 | monochlorobenzenes; N-arylpiperazine | drug metabolite; environmental contaminant; serotonergic agonist; xenobiotic |
| tacrine Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease. | 2.08 | 1 | 0 | acridines; aromatic amine | EC 3.1.1.7 (acetylcholinesterase) inhibitor |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 2.08 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 2.08 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| albendazole [no description available] | 2.08 | 1 | 0 | aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester | anthelminthic drug; microtubule-destabilising agent; tubulin modulator |
| albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). | 2.08 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alprenolol Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent. | 2.08 | 1 | 0 | secondary alcohol; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 2.08 | 1 | 0 | acetamides; benzoic acids; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| aminoglutethimide Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position. | 2.08 | 1 | 0 | dicarboximide; piperidones; substituted aniline | adrenergic agent; anticonvulsant; antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| theophylline [no description available] | 2.08 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| amiodarone Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. | 2.08 | 1 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| dan 2163 [no description available] | 2.08 | 1 | 0 | aromatic amide; aromatic amine; benzamides; pyrrolidines; sulfone | environmental contaminant; second generation antipsychotic; xenobiotic |
| amitriptyline Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5. | 2.08 | 1 | 0 | carbotricyclic compound; tertiary amine | adrenergic uptake inhibitor; antidepressant; environmental contaminant; tropomyosin-related kinase B receptor agonist; xenobiotic |
| amlexanox amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position. | 2.08 | 1 | 0 | monocarboxylic acid; pyridochromene | anti-allergic agent; anti-ulcer drug; non-steroidal anti-inflammatory drug |
| amlodipine Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina. | 2.08 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amoxapine Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position. | 2.08 | 1 | 0 | dibenzooxazepine | adrenergic uptake inhibitor; antidepressant; dopaminergic antagonist; geroprotector; serotonin uptake inhibitor |
| amsacrine Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity. | 2.08 | 1 | 0 | acridines; aromatic ether; sulfonamide | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| anastrozole [no description available] | 2.08 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| anthralin Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9. | 2.08 | 1 | 0 | anthracenes | antipsoriatic |
| antipyrine Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2. | 2.08 | 1 | 0 | pyrazolone | antipyretic; cyclooxygenase 3 inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity. | 2.08 | 1 | 0 | benzoic acids; phenyl acetates; salicylates | anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent |
| astemizole Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position. | 2.08 | 1 | 0 | benzimidazoles; piperidines | anti-allergic agent; anticoronaviral agent; H1-receptor antagonist |
| atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent. | 2.08 | 1 | 0 | ethanolamines; monocarboxylic acid amide; propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic |
| azathioprine Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS. | 2.08 | 1 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| baclofen [no description available] | 2.08 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 2.08 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| benzocaine Benzocaine: A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.. dextran sulfate sodium : An organic sodium salt of dextran sulfate. It induces colitis in mice.. benzocaine : A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina. | 2.08 | 1 | 0 | benzoate ester; substituted aniline | allergen; antipruritic drug; sensitiser; topical anaesthetic |
| bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| bay h 4502 bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1. | 2.08 | 1 | 0 | biphenyls; imidazoles | |
| bisacodyl Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | 2.08 | 1 | 0 | diarylmethane | |
| bromopride bromopride: RN given refers to parent cpd; structure | 2.08 | 1 | 0 | benzamides | |
| bronopol [no description available] | 2.08 | 1 | 0 | nitro compound | |
| bumetanide [no description available] | 2.08 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| busulfan [no description available] | 2.08 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| caffeine [no description available] | 2.08 | 1 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. | 2.08 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 2.08 | 1 | 0 | dibenzoazepine; ureas | analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic |
| carmustine Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group. | 2.08 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| carprofen carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs. | 2.08 | 1 | 0 | carbazoles; organochlorine compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug; photosensitizing agent |
| carvedilol [no description available] | 2.08 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 2.08 | 1 | 0 | organofluorine compound; pyrazoles; sulfonamide; toluenes | cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 2.08 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 2.08 | 1 | 0 | benzodiazepine | |
| chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. | 2.08 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 2.08 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antidepressant; antipruritic drug; H1-receptor antagonist; histamine antagonist; serotonin uptake inhibitor |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 2.08 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| chlorpropamide Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification. | 2.08 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 2.08 | 1 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm. | 2.08 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cifenline [no description available] | 2.08 | 1 | 0 | diarylmethane | |
| ciclopirox [no description available] | 2.08 | 1 | 0 | cyclic hydroxamic acid; hydroxypyridone antifungal drug; pyridone | antibacterial agent; antiseborrheic |
| ciglitazone ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist. | 2.08 | 1 | 0 | aromatic ether; thiazolidinone | antineoplastic agent; insulin-sensitizing drug |
| cilostazol [no description available] | 2.08 | 1 | 0 | lactam; tetrazoles | anticoagulant; bronchodilator agent; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; fibrin modulating drug; neuroprotective agent; platelet aggregation inhibitor; vasodilator agent |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 2.08 | 1 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofibrate [no description available] | 2.08 | 1 | 0 | cyclopropanes; monocarboxylic acid; organochlorine compound | antilipemic drug |
| ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | 2.42 | 2 | 0 | aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion | antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 2.08 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clioquinol Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease. | 2.08 | 1 | 0 | monohydroxyquinoline; organochlorine compound; organoiodine compound | antibacterial agent; antifungal agent; antimicrobial agent; antineoplastic agent; antiprotozoal drug; chelator; copper chelator |
| clobazam Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics. | 2.08 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator |
| clofazimine Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients. | 2.08 | 1 | 0 | monochlorobenzenes; phenazines | dye; leprostatic drug; non-steroidal anti-inflammatory drug |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 2.08 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 2.08 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor modulator |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 2.08 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| 4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide [no description available] | 2.08 | 1 | 0 | sulfonamide | |
| dapsone [no description available] | 2.08 | 1 | 0 | substituted aniline; sulfone | anti-inflammatory drug; antiinfective agent; antimalarial; leprostatic drug |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 2.08 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 2.08 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| diazoxide Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies. | 2.08 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfone | antihypertensive agent; beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; diuretic; K-ATP channel agonist; sodium channel blocker; sympathomimetic agent; vasodilator agent |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 2.08 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug. | 2.08 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 2.08 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| domperidone Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations. | 2.08 | 1 | 0 | benzimidazoles; heteroarylpiperidine | antiemetic; dopaminergic antagonist |
| donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. | 2.08 | 1 | 0 | aromatic ether; indanones; piperidines; racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent |
| doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. | 2.08 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| ebastine [no description available] | 2.08 | 1 | 0 | organic molecular entity | |
| enoxacin Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea. | 2.08 | 1 | 0 | 1,8-naphthyridine derivative; amino acid; fluoroquinolone antibiotic; monocarboxylic acid; N-arylpiperazine; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor |
| ethacrynic acid Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor. | 2.08 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethosuximide Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures. | 2.08 | 1 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| brl 42810 [no description available] | 2.08 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| 4-biphenylylacetic acid biphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis. | 2.08 | 1 | 0 | biphenyls; monocarboxylic acid | non-steroidal anti-inflammatory drug |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 2.08 | 1 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE | 2.08 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fleroxacin Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria. | 2.42 | 2 | 0 | difluorobenzene; fluoroquinolone antibiotic; monocarboxylic acid; N-alkylpiperazine; quinolines | antibacterial drug; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis. | 2.08 | 1 | 0 | conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug | environmental contaminant; P450 inhibitor; xenobiotic |
| flucytosine Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections. | 2.08 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 2.08 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 2.08 | 1 | 0 | benzoic acids; cyclic ketone; hydroxy monocarboxylic acid; organic heterotricyclic compound; phenols; xanthene dye | fluorescent dye; radioopaque medium |
| fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth. | 2.08 | 1 | 0 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
| furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure. | 2.08 | 1 | 0 | chlorobenzoic acid; furans; sulfonamide | environmental contaminant; loop diuretic; xenobiotic |
| gemfibrozil [no description available] | 2.08 | 1 | 0 | aromatic ether | antilipemic drug |
| gliclazide Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion. | 2.08 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; insulin secretagogue; radical scavenger |
| glimepiride glimepiride: structure given in first source | 2.08 | 1 | 0 | sulfonamide | |
| glipizide Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus. | 2.08 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 2.08 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 2.08 | 1 | 0 | acetamides | |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 2.08 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure. | 2.08 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroflumethiazide Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide. | 2.08 | 1 | 0 | benzothiadiazine; thiazide | antihypertensive agent; diuretic |
| hydroxyurea [no description available] | 2.08 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| lidocaine Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. | 2.08 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 2.08 | 1 | 0 | ifosfamides | alkylating agent; antineoplastic agent; environmental contaminant; immunosuppressive agent; xenobiotic |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 2.08 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| amrinone Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. | 2.08 | 1 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine. | 2.08 | 1 | 0 | indoles; organochlorine compound; sulfonamide | antihypertensive agent; diuretic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 2.08 | 1 | 0 | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic |
| iohexol Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position. | 2.08 | 1 | 0 | benzenedicarboxamide; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| iproniazid [no description available] | 2.08 | 1 | 0 | carbohydrazide; pyridines | |
| avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. | 2.08 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 2.08 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| isradipine Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. | 2.08 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 2.08 | 1 | 0 | piperazines | |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 2.08 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| ketanserin Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group. | 2.08 | 1 | 0 | aromatic ketone; organofluorine compound; piperidines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; cardiovascular drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; serotonergic antagonist |
| ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. | 2.08 | 1 | 0 | dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine | |
| lamotrigine [no description available] | 2.08 | 1 | 0 | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic |
| lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. | 2.08 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; isoxazoles; monocarboxylic acid amide | antineoplastic agent; antiparasitic agent; EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; hepatotoxic agent; immunosuppressive agent; non-steroidal anti-inflammatory drug; prodrug; pyrimidine synthesis inhibitor; tyrosine kinase inhibitor |
| letrozole [no description available] | 2.08 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lofepramine Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE. | 2.08 | 1 | 0 | aromatic ketone; dibenzoazepine; monochlorobenzenes; tertiary amino compound | antidepressant |
| lomustine [no description available] | 2.08 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 2.08 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| maprotiline Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. | 2.08 | 1 | 0 | anthracenes | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 2.08 | 1 | 0 | aromatic ketone; benzimidazoles; carbamate ester | antinematodal drug; microtubule-destabilising agent; tubulin modulator |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 2.08 | 1 | 0 | aminobenzoic acid; secondary amino compound | analgesic; antipyretic; antirheumatic drug; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 2.08 | 1 | 0 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 2.08 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 2.08 | 1 | 0 | aromatic ether; propanolamine; secondary alcohol; secondary amino compound | antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic |
| metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death. | 2.08 | 1 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| mexiletine Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. | 2.08 | 1 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 2.08 | 1 | 0 | imidazobenzodiazepine; monofluorobenzenes; organochlorine compound | anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative |
| minoxidil Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. | 2.08 | 1 | 0 | dialkylarylamine; tertiary amino compound | |
| mirtazapine Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders. | 2.08 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| moclobemide Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression. | 2.08 | 1 | 0 | benzamides; monochlorobenzenes; morpholines | antidepressant; environmental contaminant; xenobiotic |
| acecainide Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine. | 2.08 | 1 | 0 | acetamides; benzamides | anti-arrhythmia drug |
| nadolol [no description available] | 2.08 | 1 | 0 | tetralins | |
| nalidixic acid [no description available] | 2.08 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| nefazodone nefazodone: may be useful as an opiate adjunct | 2.08 | 1 | 0 | aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles | alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor |
| nefopam Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26). nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain.. 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively. | 2.08 | 1 | 0 | benzoxazocine; tertiary amino compound | |
| neostigmine Neostigmine: A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.. neostigmine : A quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor. | 2.08 | 1 | 0 | quaternary ammonium ion | antidote to curare poisoning; EC 3.1.1.7 (acetylcholinesterase) inhibitor |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 2.08 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nicardipine Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. | 2.08 | 1 | 0 | benzenes; C-nitro compound; diester; dihydropyridine; methyl ester; tertiary amino compound | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 2.08 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 2.08 | 1 | 0 | aromatic ether; C-nitro compound; sulfonamide | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| nimodipine Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. | 2.08 | 1 | 0 | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| nisoldipine Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris. | 2.08 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitrazepam Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome). | 2.08 | 1 | 0 | 1,4-benzodiazepinone; C-nitro compound | anticonvulsant; antispasmodic drug; drug metabolite; GABA modulator; sedative |
| nitrendipine Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension. | 2.08 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; ethyl ester; methyl ester | antihypertensive agent; calcium channel blocker; geroprotector; vasodilator agent |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 2.08 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug; DNA synthesis inhibitor; environmental contaminant; xenobiotic |
| nortriptyline Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline. | 2.08 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. | 2.08 | 1 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 2.08 | 1 | 0 | aromatic ether; benzimidazoles; pyridines; sulfoxide | |
| ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | 2.08 | 1 | 0 | carbazoles | |
| oxaprozin Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis. | 2.08 | 1 | 0 | 1,3-oxazoles; monocarboxylic acid | analgesic; non-steroidal anti-inflammatory drug |
| oxybutynin oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder. | 2.08 | 1 | 0 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 2.08 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pemoline Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity. | 2.08 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentamidine Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | 2.08 | 1 | 0 | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
| pentoxifylline [no description available] | 2.08 | 1 | 0 | oxopurine | |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 2.08 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenacetin Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione | 2.08 | 1 | 0 | acetamides; aromatic ether | cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug |
| pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol. | 2.08 | 1 | 0 | indoles; secondary amine | antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent |
| pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. | 2.08 | 1 | 0 | aromatic ether; pyridines; thiazolidinediones | antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic |
| piracetam Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent. | 2.08 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| piribedil Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist. | 2.08 | 1 | 0 | N-arylpiperazine | |
| ono 1078 pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist | 2.08 | 1 | 0 | chromones | |
| pyranoprofen pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source | 2.08 | 1 | 0 | pyridochromene | |
| praziquantel azinox: Russian drug | 2.08 | 1 | 0 | isoquinolines | |
| prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. | 2.08 | 1 | 0 | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| primaquine Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia. | 2.08 | 1 | 0 | aminoquinoline; aromatic ether; N-substituted diamine | antimalarial |
| primidone Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures. | 2.08 | 1 | 0 | pyrimidone | anticonvulsant; environmental contaminant; xenobiotic |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 2.08 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 2.08 | 1 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 2.08 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines | alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic |
| procyclidine Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3. | 2.08 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 2.08 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propafenone Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. | 2.08 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 2.08 | 1 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| ranitidine [no description available] | 2.08 | 1 | 0 | aralkylamine | |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 2.08 | 1 | 0 | benzothiazoles | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 2.08 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine | alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist |
| rofecoxib [no description available] | 2.08 | 1 | 0 | butenolide; sulfone | analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| sulfadiazine Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines. | 2.08 | 1 | 0 | pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; antiprotozoal drug; coccidiostat; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 2.08 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 2.08 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 2.08 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| sulfamethoxazole Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position. | 2.08 | 1 | 0 | isoxazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial agent; antiinfective agent; antimicrobial agent; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; epitope; P450 inhibitor; xenobiotic |
| sulfanitran [no description available] | 2.08 | 1 | 0 | sulfonamide | |
| sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. | 2.08 | 1 | 0 | ||
| sulfisoxazole Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.. sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms. | 2.08 | 1 | 0 | isoxazoles; sulfonamide antibiotic; sulfonamide | antibacterial drug; drug allergen |
| sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults. | 2.08 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| gatifloxacin Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes. | 2.08 | 1 | 0 | N-arylpiperazine; organofluorine compound; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antiinfective agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| tazarotene tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin. | 2.08 | 1 | 0 | acetylenic compound; ethyl ester; pyridines; retinoid; thiochromane | keratolytic drug; prodrug; teratogenic agent |
| temozolomide [no description available] | 2.08 | 1 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia | 2.08 | 1 | 0 | furans; piperazines; primary amino compound; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 2.08 | 1 | 0 | phenylethanolamines; resorcinols | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hypoglycemic agent; sympathomimetic agent; tocolytic agent |
| terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. | 2.08 | 1 | 0 | diarylmethane | |
| thiotepa Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed). | 2.08 | 1 | 0 | aziridines | |
| tiapride [no description available] | 2.08 | 1 | 0 | benzamides | |
| tilorone Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.. tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug. | 2.08 | 1 | 0 | aromatic ether; diether; fluoren-9-ones; tertiary amino compound | anti-inflammatory agent; antineoplastic agent; antiviral agent; interferon inducer; nicotinic acetylcholine receptor agonist |
| tinidazole Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent. | 2.08 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tizanidine tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | 2.08 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| nikethamide Nikethamide: A central nervous system stimulant. It was formerly used in the treatment of barbiturate overdose but is now considered to be of no value for such purposes and may be dangerous. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1229) | 2.08 | 1 | 0 | pyridinecarboxamide | |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 2.08 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolnaftate [no description available] | 2.08 | 1 | 0 | monothiocarbamic ester | antifungal drug |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 2.08 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 2.08 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 2.08 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 2.08 | 1 | 0 | chromanes; thiazolidinone | anticoagulant; anticonvulsant; antineoplastic agent; antioxidant; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; hypoglycemic agent; platelet aggregation inhibitor; vasodilator agent |
| thenoyltrifluoroacetone Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration. | 2.08 | 1 | 0 | ||
| undecylenic acid undecylenic acid: a fatty acid with a terminal double bond. 10-undecenoic acid : An undecenoic acid having its double bond in the 10-position. It is derived from castor oil and is used for the treatment of skin problems.. undecenoic acid : A C11, straight-chain fatty acid carrying a C=C double bond at any position. | 2.08 | 1 | 0 | undecenoic acid | antifungal drug; plant metabolite |
| urapidil [no description available] | 2.08 | 1 | 0 | piperazines | |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 2.08 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 2.08 | 1 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| pirinixic acid pirinixic acid: structure | 2.08 | 1 | 0 | aryl sulfide; organochlorine compound; pyrimidines | |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 2.08 | 1 | 0 | carbamate ester; indoles; N-sulfonylcarboxamide | anti-asthmatic agent; leukotriene antagonist |
| zaleplon zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position. | 2.08 | 1 | 0 | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position. | 2.08 | 1 | 0 | 1,2-benzoxazoles; sulfonamide | anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker |
| zopiclone zopiclone: S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position. | 2.08 | 1 | 0 | monochloropyridine; pyrrolopyrazine | central nervous system depressant; sedative |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic |
| reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. | 2.08 | 1 | 0 | alkaloid ester; methyl ester; yohimban alkaloid | adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 2.08 | 1 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 2 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| carbon tetrachloride Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups. | 2.08 | 1 | 0 | chlorocarbon; chloromethanes | hepatotoxic agent; refrigerant |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 2.08 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration. | 2.08 | 1 | 0 | 17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound | xenoestrogen |
| tubocurarine Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.. tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.. isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine. | 2.08 | 1 | 0 | bisbenzylisoquinoline alkaloid | drug allergen; muscle relaxant; nicotinic antagonist |
| apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. | 2.08 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 2.08 | 1 | 0 | kanamycins | bacterial metabolite |
| levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease | 2.08 | 1 | 0 | amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 2.08 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| triamcinolone diacetate triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone | 2.08 | 1 | 0 | corticosteroid hormone | |
| cytarabine [no description available] | 2.08 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| medroxyprogesterone acetate [no description available] | 2.08 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester | adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive |
| triamcinolone acetonide Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections. | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; cyclic ketal; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone | anti-allergic agent; anti-inflammatory drug |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 2.08 | 1 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| rotenone Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds. | 2.08 | 1 | 0 | organic heteropentacyclic compound; rotenones | antineoplastic agent; metabolite; mitochondrial NADH:ubiquinone reductase inhibitor; phytogenic insecticide; piscicide; toxin |
| phenformin Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis. | 2.08 | 1 | 0 | biguanides | antineoplastic agent; geroprotector; hypoglycemic agent |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 2.08 | 1 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. | 2.08 | 1 | 0 | benzazepine alkaloid fundamental parent; benzazepine alkaloid; organic heterotetracyclic compound; tertiary amino compound | antidote to curare poisoning; cholinergic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant metabolite |
| procarbazine hydrochloride procarbazine hydrochloride : A hydrochloride obtained by combining procarbazine with one equivalent of hydrochloric acid. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands. | 2.08 | 1 | 0 | hydrochloride | antineoplastic agent |
| betamethasone Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724) | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | anti-asthmatic agent; anti-inflammatory drug; immunosuppressive agent |
| emetine Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties. | 2.08 | 1 | 0 | isoquinoline alkaloid; pyridoisoquinoline | antiamoebic agent; anticoronaviral agent; antiinfective agent; antimalarial; antineoplastic agent; antiprotozoal drug; antiviral agent; autophagy inhibitor; emetic; expectorant; plant metabolite; protein synthesis inhibitor |
| dimenhydrinate gravinol: has antioxidant and ant-inflammatory activities; structure in first source | 2.08 | 1 | 0 | diarylmethane | |
| 1-naphthylisothiocyanate 1-Naphthylisothiocyanate: A tool for the study of liver damage which causes bile stasis and hyperbilirubinemia acutely and bile duct hyperplasia and biliary cirrhosis chronically, with changes in hepatocyte function. It may cause skin and kidney damage. | 2.08 | 1 | 0 | isothiocyanate | insecticide |
| megestrol acetate [no description available] | 2.08 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively. | 2.08 | 1 | 0 | cyclic ketone; erythromycin | |
| hydroxychloroquine sulfate [no description available] | 2.08 | 1 | 0 | ||
| levonorgestrel Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. | 2.08 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| ethambutol hydrochloride ethambutol dihydrochloride : The dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone. | 2.08 | 1 | 0 | hydrochloride | antitubercular agent |
| antimycin a [no description available] | 2.08 | 1 | 0 | benzamides; formamides; macrodiolide; phenols | antifungal agent; mitochondrial respiratory-chain inhibitor; piscicide |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 2.41 | 2 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| pregnenolone carbonitrile Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage. | 2.08 | 1 | 0 | aliphatic nitrile | |
| metylperon metylperon: RN given refers to parent cpd | 2.08 | 1 | 0 | aromatic ketone | |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 2.08 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group. | 2.08 | 1 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| cladribine [no description available] | 2.08 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| metocurine metocurine: from Chinese herb Cyclea hainanensis Mrr | 2.08 | 1 | 0 | isoquinolines | |
| etidronate disodium etidronate disodium : An organic sodium salt resulting from the replacement of two protons from etidronic acid (one from from each of the phosphonic acid groups) by sodium ions. | 2.08 | 1 | 0 | organic sodium salt | antineoplastic agent; bone density conservation agent; chelator |
| zalcitabine Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase. | 2.08 | 1 | 0 | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source | 2.08 | 1 | 0 | delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite |
| mafenide acetate [no description available] | 2.08 | 1 | 0 | carboxylic acid | |
| diacerein diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase; | 2.08 | 1 | 0 | anthraquinone | |
| selegiline hydrochloride, (r)-isomer [no description available] | 2.08 | 1 | 0 | hydrochloride; terminal acetylenic compound | antiparkinson drug; dopaminergic agent; EC 1.4.3.4 (monoamine oxidase) inhibitor |
| thiamphenicol [no description available] | 2.08 | 1 | 0 | monocarboxylic acid amide; sulfone | antimicrobial agent; immunosuppressive agent |
| pancuronium bromide pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication. | 2.08 | 1 | 0 | bromide salt | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| ornidazole Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections. | 2.08 | 1 | 0 | C-nitro compound; imidazoles; organochlorine compound; secondary alcohol | antiamoebic agent; antibacterial drug; antiinfective agent; antiprotozoal drug; antitrichomonal drug; epitope |
| danazol Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders. | 2.08 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| fludarabine phosphate fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas. | 2.08 | 1 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| benzonidazole benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease. | 2.08 | 1 | 0 | C-nitro compound; imidazoles; monocarboxylic acid amide | antiprotozoal drug |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 2.08 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| timolol (S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine. | 2.08 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| indoramin Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent. | 2.08 | 1 | 0 | tryptamines | |
| oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. | 2.08 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| carbidopa carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa. | 2.08 | 1 | 0 | catechols; hydrazines; monocarboxylic acid | antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 2.08 | 1 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| feprazone Feprazone: A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15) | 2.08 | 1 | 0 | organic molecular entity | |
| tobramycin Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring. | 2.08 | 1 | 0 | amino cyclitol glycoside | antibacterial agent; antimicrobial agent; toxin |
| paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | 2.08 | 1 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 2.08 | 1 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| ribavirin Rebetron: Rebetron is tradename | 2.08 | 1 | 0 | 1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide | anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| amikacin Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group. | 2.08 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 2.08 | 1 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
| vecuronium bromide Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents. | 2.08 | 1 | 0 | organic bromide salt; quaternary ammonium salt | muscle relaxant; neuromuscular agent; nicotinic antagonist |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 2.08 | 1 | 0 | benzamides; carboxylic ester | |
| acarbose [no description available] | 2.08 | 1 | 0 | tetrasaccharide derivative | EC 3.2.1.1 (alpha-amylase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; geroprotector; hypoglycemic agent |
| lorcainide [no description available] | 2.08 | 1 | 0 | acetamides | |
| captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug. | 2.08 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| staurosporine [no description available] | 2.08 | 1 | 0 | indolocarbazole alkaloid; organic heterooctacyclic compound | apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector |
| foscarnet sodium trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 2.08 | 1 | 0 | one-carbon compound; organic sodium salt | antiviral drug |
| atracurium besylate atracurium besylate : The bisbenzenesulfonate salt of atracurium. | 2.08 | 1 | 0 | organosulfonate salt; quaternary ammonium salt | muscle relaxant; nicotinic antagonist |
| nicorandil Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris. | 2.08 | 1 | 0 | nitrate ester; pyridinecarboxamide | potassium channel opener; vasodilator agent |
| pergolide mesylate pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. | 2.08 | 1 | 0 | methanesulfonate salt | antiparkinson drug; dopamine agonist; geroprotector |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.08 | 1 | 0 | cephalosporin | antibacterial drug |
| talniflumate talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma | 2.08 | 1 | 0 | benzofurans | |
| fenoldopam mesylate [no description available] | 2.08 | 1 | 0 | benzazepine | |
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.08 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| pefloxacin Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively. | 2.08 | 1 | 0 | fluoroquinolone antibiotic; monocarboxylic acid; N-alkylpiperazine; N-arylpiperazine; quinolone antibiotic; quinolone | antibacterial drug; antiinfective agent; DNA synthesis inhibitor |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 2.08 | 1 | 0 | ||
| lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom). | 2.08 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| flupirtine flupirtine: RN given refers to parent cpd without isomeric designation | 2.08 | 1 | 0 | aminopyridine | |
| enoximone Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE. | 2.08 | 1 | 0 | aromatic ketone | |
| stepronin [no description available] | 2.08 | 1 | 0 | N-acyl-amino acid | |
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 2.08 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic) | EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug |
| idazoxan Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group. | 2.08 | 1 | 0 | benzodioxine; imidazolines | alpha-adrenergic antagonist |
| remoxipride Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. | 2.08 | 1 | 0 | dimethoxybenzene | |
| cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia. | 2.08 | 1 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| atomoxetine hydrochloride Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine. | 2.08 | 1 | 0 | hydrochloride | adrenergic uptake inhibitor; antidepressant |
| quinapril Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. | 2.08 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 2.08 | 1 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| salmeterol xinafoate Salmeterol Xinafoate: A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE. | 2.08 | 1 | 0 | naphthoic acid | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 2.08 | 1 | 0 | 3-oxo steroid; aza-steroid; delta-lactam | androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| imiquimod Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. | 2.08 | 1 | 0 | imidazoquinoline | antineoplastic agent; interferon inducer |
| sertindole sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group. | 2.08 | 1 | 0 | heteroarylpiperidine; imidazolidinone; organochlorine compound; organofluorine compound; phenylindole | alpha-adrenergic antagonist; H1-receptor antagonist; second generation antipsychotic; serotonergic antagonist |
| adapalene Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether. | 2.08 | 1 | 0 | adamantanes; monocarboxylic acid; naphthoic acid | dermatologic drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; non-steroidal anti-inflammatory drug |
| aromasil [no description available] | 2.08 | 1 | 0 | 17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic |
| sparfloxacin [no description available] | 2.08 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | |
| zileuton [no description available] | 2.08 | 1 | 0 | 1-benzothiophenes; ureas | anti-asthmatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor; leukotriene antagonist; non-steroidal anti-inflammatory drug |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 2.08 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| bromfenac bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure. | 2.08 | 1 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gemcitabine hydrochloride [no description available] | 2.08 | 1 | 0 | hydrochloride; organofluorine compound | anticoronaviral agent; antimetabolite; antineoplastic agent; antiviral drug; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; immunosuppressive agent; radiosensitizing agent |
| aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders. | 2.08 | 1 | 0 | aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone | drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist |
| atorvastatin calcium anhydrous [no description available] | 2.08 | 1 | 0 | organic calcium salt | |
| lamivudine [no description available] | 2.08 | 1 | 0 | monothioacetal; nucleoside analogue; oxacycle; primary alcohol | allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug |
| duloxetine hydrochloride Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration. | 2.08 | 1 | 0 | duloxetine hydrochloride | antidepressant |
| valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. | 2.08 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine. | 2.08 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| adefovir dipivoxil bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection. | 2.08 | 1 | 0 | 6-aminopurines; carbonate ester; ether; organic phosphonate | antiviral drug; DNA synthesis inhibitor; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent; prodrug |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 2.08 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| paroxetine hydrochloride paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug. | 2.08 | 1 | 0 | hydrochloride | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| bupropion hydrochloride [no description available] | 2.08 | 1 | 0 | aromatic ketone | |
| trazodone hydrochloride Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride. | 2.08 | 1 | 0 | hydrochloride | adrenergic antagonist; antidepressant; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| doxazosin mesylate Cardura: Trade name in United States. | 2.08 | 1 | 0 | methanesulfonate salt | geroprotector |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 2.08 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 2.08 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| mevastatin mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals. | 2.08 | 1 | 0 | 2-pyranones; carboxylic ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | antifungal agent; apoptosis inducer; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; fungal metabolite; Penicillium metabolite |
| bupivacaine hydrochloride bupivacaine hydrochloride (anhydrous) : A racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride : A hydrochloride obtained by combining 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide with one molar equivalent of hydrochloric acid. | 2.08 | 1 | 0 | hydrochloride; racemate | adrenergic antagonist; amphiphile; EC 3.1.1.8 (cholinesterase) inhibitor; EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor; local anaesthetic |
| plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. | 2.08 | 1 | 0 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| amprenavir [no description available] | 2.08 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| ticlopidine hydrochloride [no description available] | 2.08 | 1 | 0 | hydrochloride | |
| epirubicin hydrochloride [no description available] | 2.08 | 1 | 0 | ||
| pazufloxacin [no description available] | 2.08 | 1 | 0 | quinolines | |
| repaglinide [no description available] | 2.08 | 1 | 0 | piperidines | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 2.08 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| miconazole nitrate miconazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-miconazole nitrate. An antifungal used for the treatment of athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes. | 2.08 | 1 | 0 | ||
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 2.08 | 1 | 0 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| artemisinin (+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria. | 2.08 | 1 | 0 | organic peroxide; sesquiterpene lactone | antimalarial; plant metabolite |
| brinzolamide brinzolamide: an antiglaucoma agent | 2.08 | 1 | 0 | sulfonamide; thienothiazine | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| drospirenone drospirenone: a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source | 2.08 | 1 | 0 | 3-oxo-Delta(4) steroid; steroid lactone | aldosterone antagonist; contraceptive drug; progestin |
| artemether Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria. | 2.08 | 1 | 0 | artemisinin derivative; cyclic acetal; organic peroxide; semisynthetic derivative; sesquiterpenoid | antimalarial |
| uk 68798 [no description available] | 2.08 | 1 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| hp 873 iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia. | 2.08 | 1 | 0 | 1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound | dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist |
| loxapine succinate [no description available] | 2.08 | 1 | 0 | succinate salt | geroprotector |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 2.08 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| betamipron [no description available] | 2.08 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| uroxatral [no description available] | 2.08 | 1 | 0 | hydrochloride | |
| aceclofenac [no description available] | 2.08 | 1 | 0 | amino acid; carboxylic ester; dichlorobenzene; monocarboxylic acid; secondary amino compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| thiocolchicoside [no description available] | 2.08 | 1 | 0 | glycoside | |
| doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | 2.08 | 1 | 0 | carbapenems | |
| rosiglitazone [no description available] | 2.08 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| tamiflu [no description available] | 2.08 | 1 | 0 | phosphate salt | |
| bexarotene [no description available] | 2.08 | 1 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic agent |
| s20098 [no description available] | 2.08 | 1 | 0 | acetamides | |
| flunisolide flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic ketal; fluorinated steroid; primary alpha-hydroxy ketone | anti-asthmatic drug; anti-inflammatory drug; immunosuppressive agent |
| ketorolac tromethamine Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. | 2.08 | 1 | 0 | organoammonium salt | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor |
| clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis. | 2.08 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum. | 2.08 | 1 | 0 | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic |
| gliquidone gliquidone: structure; RN given refers to parent cpd | 2.08 | 1 | 0 | isoquinolines | |
| lopinavir [no description available] | 2.08 | 1 | 0 | amphetamines; dicarboxylic acid diamide | anticoronaviral agent; antiviral drug; HIV protease inhibitor |
| glycyl-l-phenylalanine glycylphenylalanine: RN given refers to (DL)-isomer. Gly-Phe : A dipeptide formed from glycine and L-phenylalanine residues. | 1.98 | 1 | 0 | dipeptide zwitterion; dipeptide | human metabolite; metabolite |
| moxifloxacin hydrochloride moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride. | 2.08 | 1 | 0 | hydrochloride | antibacterial drug |
| fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer. | 2.08 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| mizoribine [no description available] | 2.08 | 1 | 0 | imidazoles | anticoronaviral agent |
| sr141716 [no description available] | 2.08 | 1 | 0 | amidopiperidine; carbohydrazide; dichlorobenzene; monochlorobenzenes; pyrazoles | anti-obesity agent; appetite depressant; CB1 receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 2.08 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| racecadotril racecadotril: parenterally active enkephalinase inhibitor | 2.08 | 1 | 0 | N-acyl-amino acid | |
| tadalafil [no description available] | 2.08 | 1 | 0 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| plavix [no description available] | 2.08 | 1 | 0 | azaheterocycle sulfate salt; organoammonium sulfate salt | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| clofarabine [no description available] | 2.08 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| pramipexole Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively. | 2.08 | 1 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 2.08 | 1 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| mk 0663 [no description available] | 2.08 | 1 | 0 | bipyridines; organochlorine compound; sulfone | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| gefitinib [no description available] | 2.08 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| desloratadine desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | 2.08 | 1 | 0 | benzocycloheptapyridine | anti-allergic agent; cholinergic antagonist; drug metabolite; H1-receptor antagonist |
| methotrexate [no description available] | 2.08 | 1 | 0 | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent |
| sulbactam [no description available] | 2.08 | 1 | 0 | penicillanic acids | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 2.08 | 1 | 0 | biphenyls | |
| abiraterone [no description available] | 2.08 | 1 | 0 | 3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor |
| febuxostat Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout. | 2.08 | 1 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| lexapro Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram. | 2.08 | 1 | 0 | ||
| docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | 2.08 | 1 | 0 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | 2.08 | 1 | 0 | 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). | 2.08 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| cox 189 lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity. | 2.08 | 1 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| xamoterol Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist. | 2.08 | 1 | 0 | morpholines | |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 2.08 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| telbivudine [no description available] | 2.08 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 2.08 | 1 | 0 | ||
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 2.08 | 1 | 0 | indanes | |
| deferasirox Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. | 2.08 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| bms204352 BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source | 2.08 | 1 | 0 | ||
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 2.08 | 1 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 2.08 | 1 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| lenalidomide [no description available] | 2.08 | 1 | 0 | aromatic amine; dicarboximide; isoindoles; piperidones | angiogenesis inhibitor; antineoplastic agent; immunomodulator |
| lacosamide Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | 2.08 | 1 | 0 | N-acyl-amino acid | |
| vincaleukoblastine [no description available] | 2.08 | 1 | 0 | acetate ester; indole alkaloid fundamental parent; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; immunosuppressive agent; microtubule-destabilising agent; plant metabolite |
| vincristine sulfate [no description available] | 2.08 | 1 | 0 | organic sulfate salt | antineoplastic agent; geroprotector |
| wortmannin [no description available] | 2.08 | 1 | 0 | acetate ester; cyclic ketone; delta-lactone; organic heteropentacyclic compound | anticoronaviral agent; antineoplastic agent; autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector; Penicillium metabolite; radiosensitizing agent |
| bortezomib [no description available] | 2.08 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 2.08 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| pentostatin Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia. | 2.08 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 2.08 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively. | 2.72 | 3 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| digitoxin Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain. | 2.08 | 1 | 0 | cardenolide glycoside | EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 2.08 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| perindopril erbumine [no description available] | 2.08 | 1 | 0 | addition compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| miglitol [no description available] | 2.08 | 1 | 0 | piperidines | |
| rocuronium bromide rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents. | 2.08 | 1 | 0 | organic bromide salt; quaternary ammonium salt | muscle relaxant; neuromuscular agent |
| linezolid [no description available] | 2.08 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| pemirolast potassium salt [no description available] | 2.08 | 1 | 0 | ||
| eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 2.08 | 1 | 0 | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
| ao 128 AO 128: alpha-glucosidase inhibitor; structure given in first source | 2.08 | 1 | 0 | organic molecular entity | |
| loteprednol etabonate Loteprednol Etabonate: An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions. | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; etabonate ester; organochlorine compound; steroid acid ester; steroid ester | anti-inflammatory drug |
| fluticasone propionate fluticasone propionate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity. | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; corticosteroid; fluorinated steroid; propanoate ester; steroid ester; thioester | adrenergic agent; anti-allergic agent; anti-asthmatic drug; anti-inflammatory drug; bronchodilator agent; dermatologic drug |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 2.08 | 1 | 0 | retinoic acid; vitamin A | anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 2.08 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| mupirocin Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections. | 2.08 | 1 | 0 | alpha,beta-unsaturated carboxylic ester; epoxide; monocarboxylic acid; oxanes; secondary alcohol; triol | antibacterial drug; bacterial metabolite; protein synthesis inhibitor |
| zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections. | 2.08 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| decitabine [no description available] | 2.08 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 2.08 | 1 | 0 | aromatic ether; beta-D-glucoside; cyclic acetal; furonaphthodioxole; gamma-lactone; monosaccharide derivative; phenols; thiophenes | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| valrubicin [no description available] | 2.08 | 1 | 0 | anthracycline; trifluoroacetamide | |
| melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring. | 2.08 | 1 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| posaconazole [no description available] | 2.08 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| rubitecan rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin. | 2.08 | 1 | 0 | C-nitro compound; delta-lactone; pyranoindolizinoquinoline; semisynthetic derivative; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 2.08 | 1 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| trilostane trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions. | 2.08 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; androstanoid; epoxy steroid; nitrile | abortifacient; antineoplastic agent; EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor |
| leuprolide acetate leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty. | 2.08 | 1 | 0 | acetate salt | antineoplastic agent; gonadotropin releasing hormone agonist |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 2.08 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 2.08 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| levosulpiride (S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively). | 2.08 | 1 | 0 | sulpiride | antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist |
| eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. | 2.08 | 1 | 0 | zopiclone | central nervous system depressant; sedative |
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 2.08 | 1 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid drug |
| cinnarizine Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS. | 2.08 | 1 | 0 | diarylmethane; N-alkylpiperazine; olefinic compound | anti-allergic agent; antiemetic; calcium channel blocker; geroprotector; H1-receptor antagonist; histamine antagonist; muscarinic antagonist |
| sulindac Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions. | 2.08 | 1 | 0 | monocarboxylic acid; organofluorine compound; sulfoxide | analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent |
| epalrestat epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy. | 2.08 | 1 | 0 | monocarboxylic acid; thiazolidines | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| drotaverin drotaverin: Hungarian drug; RN given refers to parent cpd; structure | 2.08 | 1 | 0 | isoquinolines | |
| tamoxifen [no description available] | 2.08 | 1 | 0 | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator |
| fusidic acid Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum. | 2.08 | 1 | 0 | 11alpha-hydroxy steroid; 3alpha-hydroxy steroid; alpha,beta-unsaturated monocarboxylic acid; steroid acid; steroid antibiotic; sterol ester | EC 2.7.1.33 (pantothenate kinase) inhibitor; Escherichia coli metabolite; protein synthesis inhibitor |
| valinomycin Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains. | 2.08 | 1 | 0 | cyclodepsipeptide; macrocycle | antimicrobial agent; antiviral agent; bacterial metabolite; potassium ionophore |
| hmr 3647 [no description available] | 2.08 | 1 | 0 | ||
| latoconazole latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source | 2.08 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug | |
| maraviroc [no description available] | 2.08 | 1 | 0 | tropane alkaloid | |
| toremifene citrate [no description available] | 2.08 | 1 | 0 | stilbenoid | anticoronaviral agent |
| nelarabine nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). | 2.08 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| gestodene Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer | 2.08 | 1 | 0 | steroid | estrogen |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 2.08 | 1 | 0 | beta-lactone; carboxylic ester; formamides; L-leucine derivative | anti-obesity agent; bacterial metabolite; EC 2.3.1.85 (fatty acid synthase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor |
| quinine [no description available] | 2.08 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| azilect [no description available] | 2.08 | 1 | 0 | ||
| dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). | 2.08 | 1 | 0 | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 2.08 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 2.08 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| quercetin [no description available] | 2.08 | 1 | 0 | 7-hydroxyflavonol; pentahydroxyflavone | antibacterial agent; antineoplastic agent; antioxidant; Aurora kinase inhibitor; chelator; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; geroprotector; phytoestrogen; plant metabolite; protein kinase inhibitor; radical scavenger |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 2.08 | 1 | 0 | D3 vitamins; hydroxycalciol; triol | antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical |
| alprostadil [no description available] | 2.08 | 1 | 0 | prostaglandins E | anticoagulant; human metabolite; platelet aggregation inhibitor; vasodilator agent |
| vitamin d 2 Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa. | 2.08 | 1 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 2.08 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| oxymetholone Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects. | 2.08 | 1 | 0 | ||
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 2.08 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| brompheniramine maleate brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 2.08 | 1 | 0 | maleate salt | anti-allergic agent |
| dexchlorpheniramine maleate [no description available] | 2.08 | 1 | 0 | organic molecular entity | |
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 2.08 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 2.08 | 1 | 0 | 2-nitrophenols; catechols; monocarboxylic acid amide; nitrile | antidyskinesia agent; antiparkinson drug; central nervous system drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| l 660,711 [no description available] | 2.08 | 1 | 0 | quinolines | |
| travoprost Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; isopropyl ester; prostaglandins Falpha | antiglaucoma drug; antihypertensive agent; ophthalmology drug; prodrug; prostaglandin receptor agonist |
| tranilast tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group. | 2.08 | 1 | 0 | amidobenzoic acid; cinnamamides; dimethoxybenzene; secondary carboxamide | anti-allergic agent; anti-asthmatic drug; antineoplastic agent; aryl hydrocarbon receptor agonist; calcium channel blocker; hepatoprotective agent; nephroprotective agent |
| etretinate retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof. | 2.08 | 1 | 0 | enoate ester; ethyl ester; retinoid | keratolytic drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 2.08 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| ketotifen fumarate ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug. | 2.08 | 1 | 0 | organoammonium salt | anti-asthmatic drug; H1-receptor antagonist |
| dinoprost tromethamine [no description available] | 2.08 | 1 | 0 | organic molecular entity | |
| rosuvastatin calcium S 4522: structure in first source | 2.08 | 1 | 0 | N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine; organic calcium salt | anti-inflammatory agent; cardioprotective agent; CETP inhibitor |
| terbinafine hydrochloride terbinafine hydrochloride : A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride. | 2.08 | 1 | 0 | allylamine antifungal drug; hydrochloride | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor |
| cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | 2.08 | 1 | 0 | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite |
| natamycin [no description available] | 2.08 | 1 | 0 | antibiotic antifungal drug; dicarboxylic acid monoester; epoxide; macrolide antibiotic; monosaccharide derivative; polyene antibiotic | antifungal agrochemical; antimicrobial food preservative; apoptosis inducer; bacterial metabolite; ophthalmology drug |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 2.08 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| levetiracetam Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine. | 2.08 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| nalmefene nalmefene: RN given refers to 5-alpha isomer | 2.08 | 1 | 0 | morphinane alkaloid | |
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 2.08 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 2.08 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| demycarosylturimycin h [no description available] | 2.08 | 1 | 0 | ||
| acipimox acipimox: lipolysis inhibitor | 2.08 | 1 | 0 | pyrazinecarboxylic acid | |
| atosiban [no description available] | 2.08 | 1 | 0 | oligopeptide | |
| bimatoprost Bimatoprost: A cloprostenol-derived amide that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION. | 2.08 | 1 | 0 | monocarboxylic acid amide | antiglaucoma drug; antihypertensive agent |
| latanoprost Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension. | 2.08 | 1 | 0 | isopropyl ester; prostaglandins Falpha; triol | antiglaucoma drug; antihypertensive agent; EC 4.2.1.1 (carbonic anhydrase) inhibitor; prodrug |
| nateglinide Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus. | 2.08 | 1 | 0 | phenylalanine derivative | |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 2.08 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| molsidomine [no description available] | 2.08 | 1 | 0 | ethyl ester; morpholines; oxadiazole; zwitterion | antioxidant; apoptosis inhibitor; cardioprotective agent; nitric oxide donor; vasodilator agent |
| butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | 2.08 | 1 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 2.08 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| lisinopril Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. | 2.08 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 2.08 | 1 | 0 | azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester | bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug |
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 2.08 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| enalapril maleate enalapril maleate : The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. | 2.08 | 1 | 0 | maleate salt | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. | 2.08 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| trandolapril trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. | 2.08 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; organic heterobicyclic compound; secondary amino compound; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. | 2.08 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 2.08 | 1 | 0 | peptide | |
| famotidine [no description available] | 2.08 | 1 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cci 15641 [no description available] | 2.08 | 1 | 0 | cephalosporin | |
| tenofovir disoproxil fumarate tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection. | 2.08 | 1 | 0 | fumarate salt | antiviral drug; HIV-1 reverse transcriptase inhibitor; prodrug |
| dexbrompheniramine maleate dexbrompheniramine maleate : The maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 2.08 | 1 | 0 | brompheniramine maleate | anti-allergic agent; H1-receptor antagonist |
| rifaximin [no description available] | 2.08 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 2.08 | 1 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| cefpodoxime proxetil cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis. | 2.08 | 1 | 0 | carboxylic acid; carboxylic ester; cephalosporin | antibacterial drug; prodrug |
| fluphenazine [no description available] | 2.08 | 1 | 0 | ||
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 2.08 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| roxithromycin (E)-roxithromycin : A major geometrical isomer of roxithromycin. | 2.08 | 1 | 0 | roxithromycin | environmental contaminant; xenobiotic |
| cefdinir [no description available] | 2.08 | 1 | 0 | cephalosporin; ketoxime | antibacterial drug |
| bisoprolol, fumarate (1:1) salt [no description available] | 2.08 | 1 | 0 | ||
| artesunate artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether | 2.08 | 1 | 0 | artemisinin derivative; cyclic acetal; dicarboxylic acid monoester; hemisuccinate; semisynthetic derivative; sesquiterpenoid | antimalarial; antineoplastic agent; ferroptosis inducer |
| etoposide phosphate [no description available] | 2.08 | 1 | 0 | furonaphthodioxole | |
| ciclesonide ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis | 2.08 | 1 | 0 | organic molecular entity | |
| temsirolimus [no description available] | 2.08 | 1 | 0 | macrolide lactam | |
| dutasteride Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| tekturna [no description available] | 2.08 | 1 | 0 | fumarate salt | antihypertensive agent |
| vildagliptin [no description available] | 2.08 | 1 | 0 | amino acid amide | |
| sgd 301-76 [no description available] | 2.08 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; organic nitrate salt | antiinfective agent |
| fluvoxamine maleate [no description available] | 2.08 | 1 | 0 | (trifluoromethyl)benzenes | |
| thioacetazone Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives. | 2.08 | 1 | 0 | ||
| dexlansoprazole Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | 2.08 | 1 | 0 | benzimidazoles; sulfoxide | |
| gemifloxacin mesylate gemifloxacin mesylate : The mesylate salt of gemifloxacin. | 2.08 | 1 | 0 | methanesulfonate salt | antimicrobial agent; topoisomerase IV inhibitor |
| rivaroxaban Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery. | 2.08 | 1 | 0 | aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| hki 272 [no description available] | 2.08 | 1 | 0 | nitrile; quinolines | antineoplastic agent; tyrosine kinase inhibitor |
| tofacitinib tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis. | 2.08 | 1 | 0 | N-acylpiperidine; nitrile; pyrrolopyrimidine; tertiary amino compound | antirheumatic drug; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor |
| pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. | 2.08 | 1 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| amg 009 AMG 009: an anti-inflammatory agent; structure in first source | 2.08 | 1 | 0 | ||
| cefotaxime sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| losartan potassium Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation. | 2.08 | 1 | 0 | ||
| dactolisib dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. | 2.08 | 1 | 0 | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
| rabeprazole sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| bivalirudin bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | 2.08 | 1 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| somatostatin [no description available] | 2.08 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | |
| ly-146032 [no description available] | 2.08 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| warfarin sodium warfarin sodium : A racemate comprising equal amounts of (R)- and (S)-warfarin sodium. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice. | 2.08 | 1 | 0 | ||
| pravastatin sodium pravastatin sodium : An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 2.08 | 1 | 0 | organic sodium salt; statin (semi-synthetic) | anticholesteremic drug |
| alendronate sodium [no description available] | 2.08 | 1 | 0 | ||
| sl 80.0750 [no description available] | 2.08 | 1 | 0 | ||
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 2.08 | 1 | 0 | organosulfonic acid | |
| clavulanate potassium potassium clavulanate : A potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases. | 2.08 | 1 | 0 | potassium salt | antibacterial drug; antimicrobial agent; EC 3.5.2.6 (beta-lactamase) inhibitor |
| piperacillin sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| oxacillin sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| cefazolin sodium cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups. | 2.08 | 1 | 0 | organic sodium salt | |
| azlocillin sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 2.08 | 1 | 0 | ||
| piroxicam [no description available] | 2.08 | 1 | 0 | benzothiazine; monocarboxylic acid amide; pyridines | analgesic; antirheumatic drug; cyclooxygenase 1 inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| roquinimex roquinimex: structure in first source | 2.08 | 1 | 0 | aromatic amide | |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 2.08 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| mobiflex tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries. | 2.08 | 1 | 0 | heteroaryl hydroxy compound; monocarboxylic acid amide; pyridines; thienothiazine | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| isoxicam isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome. | 2.08 | 1 | 0 | benzothiazine; isoxazoles; monocarboxylic acid amide | antirheumatic drug; non-steroidal anti-inflammatory drug |
| minocycline hydrochloride [no description available] | 2.08 | 1 | 0 | ||
| tigecycline [no description available] | 2.08 | 1 | 0 | ||
| lornoxicam lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations. | 2.08 | 1 | 0 | heteroaryl hydroxy compound; monocarboxylic acid amide; organochlorine compound; pyridines; thienothiazine | antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 2.08 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 2.08 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 2.08 | 1 | 0 | cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion | angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor |
| clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. | 2.08 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound | adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic |
| dacarbazine (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | 2.08 | 1 | 0 | dacarbazine | |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 2.08 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 2.08 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valtrex [no description available] | 2.08 | 1 | 0 | organic molecular entity | |
| olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. | 2.08 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| raltitrexed [no description available] | 2.08 | 1 | 0 | N-acyl-amino acid | |
| allopurinol Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. | 2.08 | 1 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 2.08 | 1 | 0 | tetrahydrofolic acid | |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 2.08 | 1 | 0 | N-alkylpiperazine; N-iminopiperazine; rifamycins | antitubercular agent; leprostatic drug |
| sildenafil citrate Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil. | 2.08 | 1 | 0 | citrate salt | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. | 2.08 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| tegaserod maleate [no description available] | 2.08 | 1 | 0 | maleate salt | serotonergic agonist |
| rifabutin [no description available] | 2.08 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 2.08 | 1 | 0 |
| Adverse Drug Event [description not available] | 0 | 2.08 | 1 | 0 |
| Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment. | 0 | 2.08 | 1 | 0 |
| Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals. | 0 | 2.08 | 1 | 0 |