eravacycline: has antibacterial activity
ID Source | ID |
---|---|
PubMed CID | 54726192 |
CHEMBL ID | 1951095 |
CHEMBL ID | 4597183 |
CHEBI ID | 177804 |
SCHEMBL ID | 10040430 |
MeSH ID | M000606732 |
Synonym |
---|
CHEBI:177804 |
(4s,4as,5ar,12ar)-4-(dimethylamino)-7-luoro-1,10,11,12a-tetrahydroxy-3,12-dioxo-9-[(2-pyrrolidin-1-ylacetyl)amino]-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide |
eravacycline |
tp-434 , |
1-pyrrolidineacetamide, n-((5ar,6as,7s,10as)-9-(aminocarbonyl)-7-(dimethylamino)-4-fluoro-5,5a,6,6a,7,10,10a,12-octahydro-1,8,10a,11-tetrahydroxy-10,12-dioxo-2-naphthacenyl)- |
eravacycline [usan:inn] |
(4s,4as,5ar,12as)-4-(dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-((pyrrolidin-1-ylacetyl)amino)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide |
07896928zc , |
7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline |
xerava |
unii-07896928zc |
1207283-85-9 |
(4s,4as,5ar,12as)-4-(dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-[(2-pyrrolidin-1-ylacetyl)amino]-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide |
CHEMBL1951095 |
eravacycline (usan) |
D10369 |
eravacycline [who-dd] |
eravacycline [usan] |
eravacycline [inn] |
eravacycline [mi] |
(4s,4as,5ar,12as)-4-(dimethylamino)-7-fluoro-3,10,12,12atetrahydroxy-1,11-dioxo-9-(2-(pyrrolidin-1-yl)acetamido)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide |
4s,4as,5ar,12as)-4-(dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-((pyrrolidin-1-ylacetyl)amino)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide |
SCHEMBL10040430 |
CS-7564 |
tp434 |
(4s,4as,5ar,12ar)-4-(dimethylamino)-7-fluoro-1,10,11,12a-tetrahydroxy-3,12-dioxo-9-[(2-pyrrolidin-1-ylacetyl)amino]-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide |
J-690064 |
7-[6-(2-hydroxy-2-propanyl)-3-pyridinyl]-1-(4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
EX-A751 |
tp434;eravacycline |
n-[(5ar,6as,7s,10as)-9-(aminocarbonyl)-7-(dimethylamino)-4-fluoro-5,5a,6,6a,7,10,10a,12-octahydro-1,8,10a,11-tetrahydroxy-10,12-dioxo-2-naphthacenyl]-1-pyrrolidineacetamide |
DB12329 |
HY-16980 |
Q15410941 |
compound 17j [pmid: 2148514] |
gtpl10805 |
yqm , |
(4s,4as,5ar,12ar)-4-(dimethylamino)-7-fluoro-1,10,11,12a-tetrahydroxy-3,12-dioxo-9-[2-(pyrrolidin-1-yl)acetamido]-3,4,4a,5,5a,6,12,12a-octahydrotetracene-2-carboxamide |
CHEMBL4597183 |
DTXSID401026285 |
EN300-37158604 |
(4s,4as,5ar,12as)-4-(dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-[2-(pyrrolidin-1-yl)acetamido]-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide |
Eravacycline is a potent new therapy option to treat organisms that exhibit extended-spectrum -lactamases and carbapenem-resistant Enterobacteriaceae. Eravacy Cline is an intravenous fluorocycline antibiotic approved for the treatment of complicated intra-abdominal infections.
Excerpt | Reference | Relevance |
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"Eravacycline is a novel, fully-synthetic tetracycline approved by the FDA for treatment of complicated intra-abdominal infections in August 2018. " | ( A retrospective, multicentre evaluation of eravacycline utilisation in community and academic hospitals. Cleveland, KO; Gelfand, MS; Hobbs, ALV; Saddler, K; Sierra-Hoffman, MA, 2022) | 2.43 |
"Eravacycline is a potent new therapy option to treat organisms that exhibit extended-spectrum -lactamases and carbapenem-resistant Enterobacteriaceae." | ( Eravacycline -Synergistic activity with other antimicrobials in carbapenem resistant isolates of Escherichia coli and Acinetobacter baumannii. Damodaran, N; Leela, KV; Maheswary, D; Rahul, R, 2023) | 3.07 |
"Eravacycline is a broad-spectrum, intravenous fluorocycline antibiotic approved for the treatment of complicated intra-abdominal infections in adults. " | ( Assessment of the Physical Compatibility of Eravacycline and Common Parenteral Drugs During Simulated Y-site Administration. Avery, LM; Chen, IH; Kuti, JL; Nicolau, DP; Reyes, S, 2019) | 2.22 |
"Eravacycline is a novel synthetic fluorocycline antibacterial approved for complicated intra-abdominal infections." | ( In vitro activity of eravacycline against common ribotypes of Clostridioides difficile. Alam, MJ; Bassères, E; Begum, K; Carlson, TJ; Eyre, DW; Garey, KW; Gonzales-Luna, AJ; Lancaster, C; Miranda, J; Rashid, T; Wilcox, MH, 2020) | 2.32 |
"Eravacycline is a new antibiotic for the treatment of complicated intra-abdominal infections." | ( Eravacycline, a novel tetracycline derivative, does not induce Clostridioides difficile infection in an in vitro human gut model. Altringham, J; Bently, K; Buckley, AM; Clark, E; Davis, G; Ewin, D; Moura, IB; Spittal, W; Wilcox, MH; Wilkinson, V, 2021) | 2.79 |
"Eravacycline is a novel synthetic halogenated tetracycline derivative with a broad antibacterial spectrum. " | ( In vitro activity of eravacycline, a novel synthetic halogenated tetracycline, against the malaria parasite Plasmodium falciparum. Adegbite, BR; Adegnika, AA; Agnandji, ST; Held, J; Koehne, E; Kreidenweiss, A; Manego, RZ; McCall, MBB; Mombo-Ngoma, G; Mordmüller, B, 2021) | 2.38 |
"Eravacycline is a novel, broad-spectrum, synthetic fluorocycline antibiotic for the treatment of complicated urinary tract infection (cUTI) and complicated intra-abdominal infection (cIAI) due to multidrug-resistant Gram-positive, Gram-negative and anaerobic bacteria that has demonstrated superior potency to that of currently marketed antibiotics. " | ( Eravacycline for the treatment of patients with bacterial infections. Chopra, S; Dasgupta, A; Thakare, R, 2018) | 3.37 |
"Eravacycline is a newly developed, fully synthetic tetracycline derivative that has shown potent broad-spectrum activity against a wide variety of microorganisms, including those such as extended spectrum β-lactamase producing Enterobacteriaceae and Acinetobacter." | ( Eravacycline, a newly approved fluorocycline. Burton, CE; Lee, YR, 2019) | 2.68 |
"Eravacycline is a novel, broad-spectrum synthetic tetracycline indicated for the treatment of severe infections caused by Gram-positive and Gram-negative bacteria." | ( Eravacycline for the treatment of intra-abdominal infections. Bassetti, M; Righi, E, 2014) | 2.57 |
"Eravacycline is a fluorocycline antibiotic in phase 3 clinical development for complicated intra-abdominal and urinary tract infections. " | ( In vitro susceptibility testing of eravacycline is unaffected by medium age and nonstandard assay parameters. Grossman, TH; Pillar, CM; Sahm, DF; Sutcliffe, JA, 2015) | 2.14 |
"Eravacycline is a novel broad-spectrum fluorocycline antibiotic being developed for a wide range of serious infections. " | ( Eravacycline (TP-434) is efficacious in animal models of infection. Grossman, TH; Lofland, D; Murphy, TM; Slee, AM; Sutcliffe, JA, 2015) | 3.3 |
"Eravacycline is a novel broad-spectrum fluorocycline with potent Gram-negative activity, including for multidrug-resistant strains. " | ( Activity of Eravacycline against Escherichia coli Clinical Isolates Collected from U.S. Veterans in 2011 in Relation to Coresistance Phenotype and Sequence Type 131 Genotype. Johnson, JR; Johnston, BD; Porter, SB; Thuras, P, 2015) | 2.24 |
"Eravacycline is an investigational, synthetic fluorocycline antibacterial agent that is structurally similar to tigecycline with two modifications to the D-ring of its tetracycline core: a fluorine atom replaces the dimethylamine moiety at C-7 and a pyrrolidinoacetamido group replaces the 2-tertiary-butyl glycylamido at C-9. " | ( Review of Eravacycline, a Novel Fluorocycline Antibacterial Agent. Adam, H; Cheung, D; Gin, AS; Golden, A; Gorityala, B; Hoban, DJ; Karlowsky, JA; Lagacé-Wiens, PR; Schweizer, F; Walkty, A; Zelenitsky, S; Zhanel, GG, 2016) | 2.28 |
"Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class being developed for the treatment of complicated urinary tract infections and complicated intra-abdominal infections. " | ( In vitro susceptibility of β-lactamase-producing carbapenem-resistant Enterobacteriaceae (CRE) to eravacycline. Bush, K; Lin, X; Zhang, Y, 2016) | 2.09 |
"Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class with in vitro activity against clinically important gram-negative, gram-positive aerobic, and facultative bacteria including most of those resistant to cephalosporins, fluoroquinolones, β-lactam/β-lactamase inhibitors, multidrug resistant strains and carbapenem-resistant Enterobacteriaceae, and most anaerobic pathogens." | ( Assessing the Efficacy and Safety of Eravacycline vs Ertapenem in Complicated Intra-abdominal Infections in the Investigating Gram-Negative Infections Treated With Eravacycline (IGNITE 1) Trial: A Randomized Clinical Trial. Evans, D; Horn, P; Lee, P; Marsh, A; Slepavicius, A; Solomkin, J; Sutcliffe, JA; Tsai, L, 2017) | 2.17 |
Eravacycline has shown potent antibacterial activity against common and clinically important antibiotic-resistant pathogens.
Excerpt | Reference | Relevance |
---|---|---|
"Eravacycline has shown activity against many gram-positive organisms such as methicillin-resistant S." | ( Eravacycline, a newly approved fluorocycline. Burton, CE; Lee, YR, 2019) | 2.68 |
"Eravacycline has shown potent antibacterial activity against common and clinically important antibiotic-resistant pathogens. " | ( In vitro activities of Eravacycline against 336 isolates collected from 2012 to 2016 from 11 teaching hospitals in China. Li, H; Wang, H; Wang, Q; Wang, R; Wang, X; Zhang, Y; Zhao, C, 2019) | 2.27 |
Excerpt | Reference | Relevance |
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"Treatment with eravacycline was noninferior to meropenem in adult patients with cIAI, including infections caused by resistant pathogens." | ( IGNITE4: Results of a Phase 3, Randomized, Multicenter, Prospective Trial of Eravacycline vs Meropenem in the Treatment of Complicated Intraabdominal Infections. Evans, D; Gardovskis, J; Lawrence, K; Montravers, P; Solomkin, JS; Sway, A; Tsai, L, 2019) | 1.1 |
Excerpt | Reference | Relevance |
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" The study outcomes included clinical response, all-cause mortality and adverse events (AEs)." | ( Efficacy and safety of eravacycline: A meta-analysis. Almangour, TA; Bassetti, M; Eljaaly, K; Ortwine, JK; Shaikhomer, M, 2021) | 0.93 |
" Statistically significant trends were observed favoring cefotaxime plus metronidazole, which exhibited fewer discontinuations because of adverse events (AEs) when compared with eravacycline, meropenem and ceftolozane/tazobactam plus metronidazole (OR = 0." | ( Efficacy, safety, and tolerability of antimicrobial agents for complicated intra-abdominal infection: a systematic review and network meta-analysis. Deng, T; Kong, W; Li, S; Shu, Y; Wu, Y, 2023) | 1.1 |
Excerpt | Reference | Relevance |
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"We assessed the pharmacokinetic profile of eravacycline, a novel antibiotic of the tetracycline class, and determined the dose in an immunocompetent murine thigh infection model that would provide free-drug exposure similar to that observed in humans after the administration of 1 mg/kg intravenously (i." | ( Eravacycline Pharmacokinetics and Challenges in Defining Humanized Exposure In Vivo. Monogue, ML; Nicolau, DP; Thabit, AK, 2016) | 2.14 |
" This decision was based on substantial clinical and pre-clinical data, including rigorous pharmacokinetic and pharmacodynamic work." | ( Clinical Pharmacokinetics and Pharmacodynamics of Eravacycline. McCarthy, MW, 2019) | 0.77 |
Eravacycline combined with β-lactams or polymyxin B can lead to synergistic effects against clinically common carbapenem-resistant Gram-negative bacteria.
Excerpt | Reference | Relevance |
---|---|---|
"This study aimed to investigate the synergistic activity of eravacycline combined with other antimicrobial agents against carbapenem-resistant Enterobacteriaceae and Acinetobacter baumannii collected from China." | ( Synergism of eravacycline combined with other antimicrobial agents against carbapenem-resistant Enterobacteriaceae and Acinetobacter baumannii. Cui, L; Li, Y; Wang, Q; Xue, F; Zheng, B, 2022) | 1.33 |
" Imipenem, ceftazidime, cefoperazone-sulbactam, ciprofloxacin, amikacin, and polymyxin B were selected to investigate their efficacy in combination with eravacycline against 60 carbapenem-resistant strains." | ( Synergism of eravacycline combined with other antimicrobial agents against carbapenem-resistant Enterobacteriaceae and Acinetobacter baumannii. Cui, L; Li, Y; Wang, Q; Xue, F; Zheng, B, 2022) | 1.29 |
"Eravacycline combined with β-lactams or polymyxin B can lead to synergistic effects against clinically common carbapenem-resistant Gram-negative bacteria." | ( Synergism of eravacycline combined with other antimicrobial agents against carbapenem-resistant Enterobacteriaceae and Acinetobacter baumannii. Cui, L; Li, Y; Wang, Q; Xue, F; Zheng, B, 2022) | 2.53 |
Excerpt | Reference | Relevance |
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" Two compounds were identified that exhibit both oral bioavailability in rat and clinically relevant bacterial susceptibility profiles against major respiratory pathogens." | ( Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. Achorn, C; Chen, CL; Clark, RB; Deng, Y; Fyfe, C; Grossman, TH; He, M; Hogan, PC; Hunt, DK; O'Brien, WJ; Plamondon, L; Rönn, M; Sutcliffe, JA; Xiao, XY; Zhu, Z, 2012) | 0.38 |
Excerpt | Relevance | Reference |
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" Omadacycline offers once daily oral and IV dosing and a clinical tolerability and safety profile that compares favorably with contemporary antibiotics used across serious community-acquired infections where resistance has rendered many less effective." | ( Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. Steenbergen, J; Tanaka, SK; Villano, S, 2016) | 0.43 |
"0 g every 24 hours, for a minimum of four 24-hour dosing cycles." | ( Assessing the Efficacy and Safety of Eravacycline vs Ertapenem in Complicated Intra-abdominal Infections in the Investigating Gram-Negative Infections Treated With Eravacycline (IGNITE 1) Trial: A Randomized Clinical Trial. Evans, D; Horn, P; Lee, P; Marsh, A; Slepavicius, A; Solomkin, J; Sutcliffe, JA; Tsai, L, 2017) | 0.73 |
" A lack of pediatric-specific comparative effectiveness data, uncertain pediatric dosing regimens for several agents, and a relative lack of new antibiotics with pediatric indications approved by the US Food and Drug Administration (FDA) collectively present unique challenges for children." | ( Treatment of Carbapenem-Resistant Enterobacteriaceae Infections in Children. Chiotos, K; Gerber, JS; Hayes, M; Tamma, PD, 2020) | 0.56 |
"Effective bacterial infection eradication requires not only potent antibacterial agents but also proper dosing strategies." | ( Semimechanistic Modeling of Eravacycline Pharmacodynamics Using Bensman, TJ; Moore, JN; Nguyen, K; Wei, XT, 2020) | 0.85 |
" Hence, a green highly sensitive, cost-effective, fast, and selective fluorimetric approach was developed for the estimation of ERV in milk, dosage form, content uniformity, and human plasma." | ( A Novel Design Eco-friendly Microwave-assisted Cu-N@CQDs Sensor for the Quantification of Eravacycline via Spectrofluorimetric Method; Application to Greenness Assessments, Dosage Form and Biological Samples. Salman, BI, 2023) | 1.13 |
Class | Description |
---|---|
tetracyclines | A subclass of polyketides having an octahydrotetracene-2-carboxamide skeleton, substituted with many hydroxy and other groups. |
[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) |
---|---|---|---|---|---|---|---|
30S ribosomal protein S6 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S7 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L15 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L10 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L11 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L7/L12 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L19 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L1 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L20 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L27 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L28 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L29 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L31 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L31 type B | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L32 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L33 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L34 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L35 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L36 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S10 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S11 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S12 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S13 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S16 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S18 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S19 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S20 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S2 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S3 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S4 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S5 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S8 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S9 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L13 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L14 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L16 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L23 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S15 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L17 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L21 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L30 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L6 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S14 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S17 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S1 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L18 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L2 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L3 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L24 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L4 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L22 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L5 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
30S ribosomal protein S21 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L25 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
50S ribosomal protein L36 2 | Escherichia coli K-12 | IC50 (µMol) | 0.6200 | 0.0089 | 1.2035 | 5.0000 | AID646205 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID646225 | Ratio of tigecycline MIC to compound MIC for Escherichia coli ATCC 107 25922 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID671548 | Antibacterial activity against tetracycline-susceptible Staphylococcus aureus ATCC 13709 Smith isolate SA100 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID1525376 | Antibacterial activity against Klebsiella pneumoniae | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID1525371 | Antibacterial activity against methicillin-resistant Staphylococcus aureus | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID1329030 | Cmax in human at 100 mg, po q12h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID646218 | Antibacterial activity against Klebsiella pneumoniae ATCC 109 13883 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1525372 | Antibacterial activity against Staphylococcus epidermidis | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID646204 | Ratio of tetracycline IC50 to compound IC50 for Escherichia coli ribosome-mediated translation | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1525375 | Antibacterial activity against Escherichia coli | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID1329029 | Cmax in human at 1.5 mg/kg, iv q24h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID1525377 | Antibacterial activity against Pseudomonas aeruginosa | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID646213 | Antibacterial activity against Escherichia coli ATCC 107 25922 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646219 | Antibacterial activity against tetracycline-resistant Klebsiella pneumoniae 153 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646232 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646208 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus 158 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646210 | Antibacterial activity against tetracycline-resistant Enterococcus faecalis 159 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID671552 | Antibacterial activity against tetracycline-resistant Streptococcus pneumoniae isolate 160 expressing tetM gene | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID671553 | Antibacterial activity against Escherichia coli ATCC 25922 isolate 107 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID646355 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646211 | Antibacterial activity against Streptococcus pneumoniae ATCC 106 49619 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646227 | Antibacterial activity against tetracycline-resistant Escherichia coli 133 infected in iv dosed CD-1 mouse assessed as protection from infection administered 1 hr post infection measured after 24 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646229 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus 191 infected in iv dosed CD-1 mouse assessed as dose required for 1 log bacterial burden reduction administered 1.5 hr post infection measured after 24 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1329033 | Systemic clearance in human at 1.5 mg/kg, iv q24h or 100 mg, po q12h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID1329031 | AUC(0 to 24 hrs) in human at 1.5 mg/kg, iv q24h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID646228 | Antibacterial activity against tetracycline-resistant Escherichia coli 133 infected in iv dosed CD-1 mouse assessed as reduction in bacterial burden administered 1 hr post infection measured after 24 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646226 | Ratio of tigecycline MIC to compound MIC for Acinetobacter baumannii ATCC 19606 110 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1329035 | Oral bioavailability in human at 100 mg administered q12h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID646235 | Elimination half life in Sprague-Dawley rat at 10 mg/kg, po by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646224 | Ratio of tigecycline MIC to compound MIC for tetracycline-resistant Enterococcus faecalis 159 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646230 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus 191 infected in iv dosed CD-1 mouse assessed as dose required for 3 log bacterial burden reduction administered 1.5 hr post infection measured after 24 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646215 | Antibacterial activity against Acinetobacter baumannii ATCC 19606 110 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646220 | Ratio of tigecycline MIC to compound MIC for Staphylococcus aureus ATCC 101 29213 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646233 | Apparent volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646214 | Antibacterial activity against tetracycline-resistant Escherichia coli 155 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID671550 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus isolate SA158 expressing TetK gene | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID646231 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus 191 infected in iv dosed CD-1 mouse assessed as reduction in bacterial burden administered 1.5 hr post infection measured after 24 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1329034 | Terminal half life in human at 1.5 mg/kg, iv q24h or 100 mg, po q12h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID671554 | Antibacterial activity against Escherichia coli isolate EC155 expressing tetA gene | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID1525373 | Antibacterial activity against Enterococcus faecium | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID646236 | AUClast in Sprague-Dawley rat at 1 mg/kg, iv by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646207 | Antibacterial activity against tetracycline- and methicillin-resistant Staphylococcus aureus 161 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1329041 | Protein binding in human plasma | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID671549 | Antibacterial activity against tetracycline-resistant Staphylococcus aureus isolate SA161 expressing TetM gene | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID646223 | Ratio of tigecycline MIC to compound MIC for Enterococcus faecalis ATCC 103 29212 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1329032 | AUC(0 to 24 hrs) in human at 100 mg, po q12h | 2016 | Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24 | Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic. |
AID646212 | Antibacterial activity against tetracycline-resistant Streptococcus pneumoniae 160 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646221 | Ratio of tigecycline MIC to compound MIC for tetracycline- and methicillin-resistant Staphylococcus aureus 161 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646216 | Antibacterial activity against Pseudomonas aeruginosa ATCC 111 27853 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646234 | Elimination half life in Sprague-Dawley rat at 1 mg/kg, iv by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID671551 | Antibacterial activity against Streptococcus pneumoniae ATCC 49619 isolate 106 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
AID646354 | AUClast in Sprague-Dawley rat at 10 mg/kg, po by LC/MS-MS analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646206 | Antibacterial activity against Staphylococcus aureus ATCC 101 29213 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646222 | Ratio of tigecycline MIC to compound MIC for tetracycline-resistant Staphylococcus aureus 158 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID1525374 | Antibacterial activity against Streptococcus pneumoniae | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance. |
AID646217 | Antibacterial activity against Enterobacter cloacae ATCC 108 13047 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646209 | Antibacterial activity against Enterococcus faecalis ATCC 103 29212 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID646205 | Inhibition of Escherichia coli ribosome-mediated translation after 60 mins by transcription/translation-coupled luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent. |
AID671555 | Antibacterial activity against Klebsiella pneumoniae ATCC 13883 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy. |
[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 | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 40 (43.01) | 24.3611 |
2020's | 53 (56.99) | 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 (57.31) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (3.16%) | 5.53% |
Reviews | 22 (23.16%) | 6.00% |
Case Studies | 2 (2.11%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 68 (71.58%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |