Pipeline of Known Chemical Classes of Antibiotics
Abstract
:1. Introduction
2. Experimental
- Identification of companies doing research and development into new antibiotics around the world;
- Mapping of the antibiotic development pipelines of the companies identified.
2.1. Identification of Companies Doing R&D into New Antibiotics
2.2. Mapping the Companies’ New Antibiotics Pipeline
3. Pipeline of New Antibiotics in Chemical Classes Known on the Market
Class | Compound (Subclass) | Company (Country) | Development Phase | Bacteria | Chemical structure | Source |
---|---|---|---|---|---|---|
Quinolones | ||||||
Nemonoxacin | TaiGen Biotechnology (Taiwan) | Phase III | Broad-spectrum | | [13,14,15,16,17,18] | |
Ozenoxacin (topical use) | Ferrer Internacional (Spain) | Phase III | Gram-positive | | [19,20,21] | |
Zabofloxacin (fluoroquinolone) | Dong Wha Pharmaceutical (South Korea) | Phase III | Broad-spectrum | | [22,23,24,25] | |
Delafloxacin (fluoroquinolone) | Rib-X Pharmaceuticals (USA) | Phase III | Broad-spectrum | | [26,27,28] | |
Avarofloxacin (fluoroquinolone) | Furiex Pharmaceuticals (USA) | Phase II completed | Broad-spectrum | | [29,30,31,32,33,34,35] | |
Finafloxacin (fluoroquinolone) | MerLion Pharmaceuticals (Singapore) | Phase II | H. pylori, Broad-Spectrum | | [36,37,38,39] | |
WCK 2349 a prodrug of WCK 771 a,b (fluoroquinolone) | Wockhardt ( India) | Phase II | Gram-positive | S-(−)-nadifloxacin b | [40,41,42,43] | |
KRP-AM1977X (oral) | Kyorin (Japan) | Phase I | Respiratory infections | ND | [44,45] | |
KRP-AM1977Y | Kyorin | Phase I | MRSA | ND | [44,45] | |
DS-8587 (fluoroquinolone) | Daiichi Sankyo (Japan) | Phase I | Broad-spectrum | | [46,47] | |
ACH-702 (Isothiazoloquinolone) | Achillion Pharmaceuticals (USA) | Pre-Clinical | Broad-spectrum | | [48,49] | |
Aminoglycosides | ||||||
Plazomicin | Achaogen (USA) | Phase II completed | Broad-spectrum | | [50,51,52,53,54,55,56] | |
Neomycin analogs c | Achaogen (USA) | Discovery | Broad-spectrum | | [57,58,59,60,61,62,63] | |
FY-901 | Changzhou Fangyuan Pharmaceutical (China) | Pre-Clinical | S. Aureus | ND | [64] | |
FY-902 | Changzhou Fangyuan Pharmaceutical | Pre-Clinical | M. tuberculosis | ND | [64] | |
New compounds | Changzhou Fangyuan Pharmaceutical | Discovery | ND | ND | [65] | |
Macrolides | ||||||
Solithromycin (2-fluoroketolide) | Cempra Pharmaceuticals (USA) | Phase III | S. pneumoniae; N. gonorrhoeae | | [66,67,68,69,70,71,72] | |
New Macrolides d | Cempra Pharmaceuticals | Discovery | ND | | [73,74] | |
EDP-788 (bicyclolide-bridged bicyclic macrolide) | Enanta Pharmaceuticals (USA) | Pre-Clinical | Gram-positive | ND | [75,76] | |
new bicyclolides c | Enanta Pharmaceuticals | Discovery | Gram-positive | | [77,78,79,80] | |
WCK 4873 (Ketolide) | Wockhardt | Pre-Clinical | MDR pneumoccocus, Strep, H. influenzae | ND | [81,82] | |
RX-02 program | Rib-X Pharmaceuticals | Discovery | Gram-positive | ND | [83] | |
Oxazolidinones | ||||||
Tedizolid | Cubist Pharmaceuticals (USA) | Phase III | Gram-positive | | [84,85,86,87,88] | |
Cadazolid | Actelion (Switzerland) | Phase II completed | Clostridium difficile | | [89,90,91,92] | |
Radezolid | Rib-X Pharmaceuticals | Phase II completed | Gram-positive | | [93,94,95,96,97,98] | |
AZD5847 | AstraZeneca (UK) | Phase II | M. tuberculosis | | [99,100,101,102] | |
LCB01-0371 | LegoChem Biosciences (South Korea) | Phase I | Gram-positive | | [103,104] | |
MRX-I | MicuRx Pharmaceuticals (USA) | Phase I | Gram-positive | | [105,106] | |
MRX-II | MicuRx Pharmaceuticals | Pre-Clinical | Gram-positive | ND | [106] | |
2nd Generation Oxazolidinones | Wockhardt | Pre-Clinical | Gram-positive | ND | [81] | |
Tetracyclines | ||||||
Omadacycline (aminomethylcycline) | Paratek (USA) | Phase III | Broad-spectrum | | [93,107,108] | |
Aminomethylcyclines | Paratek | Discovery | Clostridium difficile | ND | [107] | |
Eravacycline (fluorocycline) | Tetraphase Pharmaceuticals (USA) | Phase II (cIAI) | Gram-negative | | [109,110,111,112] | |
TP-271 | Tetraphase Pharmaceuticals | Pre-Clinical | bacterial biothreats, CABP pathogens | | [109,113,114] | |
TP-834 | Tetraphase Pharmaceuticals | Pre-Clinical | CABP pathogens | ND | [109] | |
New tetracycline derivatives c | Tetraphase Pharmaceuticals | Discovery | Gram-negative | | [115,116,117,118] | |
Pleuromutilins | ||||||
BC-3781 | Nabriva (Austria) | Phase II Completed | Gram-positive, including MRSA | | [119,120,121,122,123,124] | |
BC-7013 (topical) | Nabriva | Phase I | Gram-positive | | [119,124] | |
Discovery/development of pleuromutilins | Nabriva | Discovery | Broad spectrum | | [119,125,126,127] | |
Beta-lactams | ||||||
Ceftolozane + tazobactam (CXA-201) | Cubist Pharmaceuticals | Phase III | Gram-negative | (ceftolozane) | [6,128,129,130,131,132] | |
BAL30072 (sulfactam) | Basilea Pharmaceutica (Switzerland) | Phase I | Gram-negative | | [133,134,135] | |
S-649266 (GSK2696266) (Cephalosporin) | Shionogi (Japan)/ GlaxoSmithKline (UK) | Phase I | Gram-negative | ND | [136,137,138] | |
CB-027 (Cephalosporin) | Cubist Pharmaceuticals | Pre-Clinical | Broad-spectrum | ND | [139] | |
FSI-1671 (Carbapenem) | FOB Synthesis, Inc. (USA) | Pre-Clinical | Gram-negative | | [140,141] | |
Beta-lactamase inhibitors—Diazabicyclooctanes (DBOs) | ||||||
Ceftazidime/Avibactam (CAZ AVI) e | Forest Laboratories (USA)/Astrazeneca | Phase III | Gram-negative | (avibactam) | [142,143,144,145,146,147,148] | |
Ceftaroline/Avibactam (CXL) e | Forest Laboratories/ Astrazeneca | Phase II | Gram-negative | (avibactam) | [120,143,147,148,149,150,151] | |
MK-7655 + Imipenem/Cilastatin | Merck & Co., Inc. (USA) | Phase II | Gram-negative | (MK-7655) | [6,147,148,152,153,154,155] | |
FPI-1465 | Fedora Pharmaceuticals Inc. (USA) | Pre-Clinical | Gram-negative | | [156,157] | |
Beta-lactamase inhibitors—Boronate β-lactamase inhibitor | ||||||
Carbavance (biapenem + RPX7009) | Rempex Pharmaceuticals (Sweden) | Phase I | Gram-negative | (RPX7009) | [158,159,160,161] | |
Beta-lactamase inhibitors—phosphonate-based beta-lactamase inhibitor (BLI) | ||||||
MG96077 | Mirati Therapeutics (USA) | Pre-Clinical | Gram-negative | | [162,163] | |
Lipoglycopeptides | ||||||
Dalbavancin | Durata Therapeutics (USA) | Phase III completed | Gram-positive | | [164,165,166,167,168,169,170,171,172,173] | |
Oritavancin Diphosphate | The Medicines Company (USA) | Phase III completed | Gram-positive | | [7,169,170,173,174] | |
Polymyxins | ||||||
NAB739 | Northern Antibiotics (Finland) | Pre-Clinical | Gram-negative | | [89,175,176,177,178,179] | |
NAB7061 | Northern Antibiotics | Pre-Clinical | Gram-negative | | [176,177,178,179] | |
NAB741 | Northern Antibiotics | Pre-Clinical | Gram-negative | | [176,177,178,179] | |
Cyclic lipopeptides | ||||||
Surotomycin | Cubist Pharmaceuticals | Phase III | C. difficile | | [180,181,182,183] | |
WAP-8294A2 (lotilibcin) | Green Cross (South Korea) | Phase I | S. aureus | ND | [184,185,186] |
4. Quinolones
5. Aminoglycosides
6. Macrolides
7. Oxazolidinones
8. Tetracyclines
9. Pleuromutilins
10. Beta-Lactams
11. Beta-Lactamase Inhibitors—Diazabicyclooctanes (DBOs)
12. Beta-Lactamase Inhibitors—Boronate β-Lactamase Inhibitor
13. Beta-Lactamase Inhibitors—Non-beta-Lactam Phosphonate-Based
14. Glycopeptides (Lipoglycopeptides)
15. Polymyxins
16. Cyclic Lipopeptides
17. Final Remarks
Conflicts of Interest
References
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De Souza Mendes, C.D.; De Souza Antunes, A.M. Pipeline of Known Chemical Classes of Antibiotics. Antibiotics 2013, 2, 500-534. https://doi.org/10.3390/antibiotics2040500
De Souza Mendes CD, De Souza Antunes AM. Pipeline of Known Chemical Classes of Antibiotics. Antibiotics. 2013; 2(4):500-534. https://doi.org/10.3390/antibiotics2040500
Chicago/Turabian StyleDe Souza Mendes, Cristina D'Urso, and Adelaide Maria De Souza Antunes. 2013. "Pipeline of Known Chemical Classes of Antibiotics" Antibiotics 2, no. 4: 500-534. https://doi.org/10.3390/antibiotics2040500