Doripenem (Hydrate) is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens similar to imipenem and, especially, meropenem. Doripenem has a broad spectrum of activity against many common hospital pathogens, including P. aeruginosa and Burkholderia cepacia[3]. Doripenem has been approved for use in treatment of complicated intra-abdominal infection and complicated urinary tract infection. In vitro, doripenem lacks the propensity to cause seizures, and a low risk of seizures has been demonstrated in clinical studies[4]. In addition, the synergistic use of doripenem and cefotaxime plays a significant role in inhibiting the efficiency of CTX-M-15 type β-lactamase[5].
Doripenem Monohydrate/多尼培南 一水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Caco-2 cells
50 mM
24 h
To investigate the effect of Doripenem on gut microbiota composition, results showed Doripenem had similar effects on microbiota as meropenem trihydrate but differed from tobramycin.
Arch Toxicol. 2022 Dec;96(12):3291-3303.
mutM mutant
8 mg/L
48 h
Evaluate the bactericidal activity of polymyxin B alone, showing initial rapid killing followed by regrowth
To evaluate the bactericidal activity of doripenem, polymyxin B, and rifampin in combination. Results showed that the triple combination was bactericidal against 5/5 E. coli isolates.
To evaluate the bactericidal activity of doripenem, polymyxin B, and rifampin in combination. Results showed that the triple combination was bactericidal against 5/5 P. aeruginosa isolates.
To evaluate the bactericidal activity of doripenem, polymyxin B, and rifampin in combination. Results showed that the triple combination was bactericidal against 3/5 A. baumannii isolates.
To evaluate the bactericidal activity of doripenem, polymyxin B, and rifampin in combination. Results showed that the triple combination was bactericidal against 4/5 K. pneumoniae isolates.
Evaluate the inhibitory effect of Doripenem on PBP3, IC50 was 0.0042 μg/ml.
Antimicrob Agents Chemother. 2015;59(6):3548-55.
Streptococcus pneumoniae IU1945
0.0082±0.0009 μg/ml
30 min
Evaluate the inhibitory effect of Doripenem on PBP2x, IC50 was 0.0082 μg/ml.
Antimicrob Agents Chemother. 2015;59(6):3548-55.
Streptococcus pneumoniae IU1945
0.0085 ± 0.0013 μg/ml
30 min
Evaluate the inhibitory effect of Doripenem on PBP1a, IC50 was 0.0085 μg/ml.
Antimicrob Agents Chemother. 2015;59(6):3548-55.
Multidrug-resistant A. baumannii (MDR A. baumannii)
8 µg/mL
24 h
Evaluate the synergistic effect and bactericidal activity of Doripenem in combination with Colistin or Tigecycline. Results showed a high synergy rate (53.6%) with Colistin-Doripenem combination, while a lower synergy rate (14.3%) was observed with Doripenem-Tigecycline combination.
Ann Lab Med. 2016 Mar;36(2):124-30.
Extensively drug-resistant A. baumannii (XDR A. baumannii)
8 µg/mL
24 h
Evaluate the synergistic effect and bactericidal activity of Doripenem in combination with Colistin or Tigecycline. Results showed the highest synergy rate (53.6%) and bactericidal activity (75.4%) with Colistin-Doripenem combination, while the lowest synergy rate (14.5%) was observed with Doripenem-Tigecycline combination.
Ann Lab Med. 2016 Mar;36(2):124-30.
Pseudomonas aeruginosa FADDI PA070
2.0 mg/L
240 h
To evaluate the antibacterial activity of Doripenem against Pseudomonas aeruginosa FADDI PA070, results showed that Doripenem monotherapy achieved 1.94-4.06 log10 killing at 6 h, but extensive regrowth was observed at 48 h.
J Antimicrob Chemother. 2015 May;70(5):1434-42.
Pseudomonas aeruginosa FADDI PA033
1.0 mg/L
240 h
To evaluate the antibacterial activity of Doripenem against Pseudomonas aeruginosa FADDI PA033, results showed that Doripenem monotherapy achieved 1.94-4.06 log10 killing at 6 h, but extensive regrowth was observed at 48 h.
J Antimicrob Chemother. 2015 May;70(5):1434-42.
Pseudomonas aeruginosa ATCC 27853
0.5 mg/L
240 h
To evaluate the antibacterial activity of Doripenem against Pseudomonas aeruginosa ATCC 27853, results showed that Doripenem monotherapy achieved 1.94-4.06 log10 killing at 6 h, but extensive regrowth was observed at 48 h.
J Antimicrob Chemother. 2015 May;70(5):1434-42.
Acinetobacter baumannii ATCC 19606
25 mg/L
1 h
45 differentially expressed genes were detected, involved in biofilm formation and carbohydrate degradation
J Antimicrob Chemother. 2015 May;70(5):1303-13.
Acinetobacter baumannii ATCC 19606
25 mg/L
15 min
No differentially expressed genes were detected
J Antimicrob Chemother. 2015 May;70(5):1303-13.
Acinetobacter baumannii N16870
5.25, 10.5, 21, 31.5, 42 mg/L
48 h
To evaluate the bactericidal effect of Doripenem in combination with polymyxin B (PMB) against carbapenem-resistant Acinetobacter baumannii. Results showed that Doripenem combined with PMB achieved reductions at the limit of detection (100 CFU/mL) at an inoculum of 106 CFU/mL, while the maximum reduction at 108 CFU/mL was 1.6 log10 CFU/mL.
Int J Antimicrob Agents. 2016 Dec;48(6):719-724.
Acinetobacter baumannii 03-149-1
5.25, 10.5, 21, 31.5, 42 mg/L
48 h
To evaluate the bactericidal effect of Doripenem in combination with polymyxin B (PMB) against carbapenem-resistant Acinetobacter baumannii. Results showed that Doripenem combined with PMB achieved a ≥3 log10 CFU/mL reduction within 4 h at an inoculum of 106 CFU/mL, while the maximum reduction at 108 CFU/mL was 3.2 log10 CFU/mL.
Int J Antimicrob Agents. 2016 Dec;48(6):719-724.
Klebsiella pneumoniae
0.06 μg/ml
16 to 20 h
Determine the MIC of Doripenem against Klebsiella pneumoniae
Immunocompetent and neutropenic mouse thigh infection models
Intravenous
500 mg/8 h and 2 g/8 h
Every 8 h for 24 h
To evaluate the in vivo efficacy of Doripenem against NDM-1-producing Enterobacteriaceae. Results showed that despite in vitro resistance, high-dose, prolonged infusion of Doripenem achieved >1-log10 CFU reductions in six of eight clinical strains.
Antimicrob Agents Chemother. 2014;58(3):1671-7
C3H/HeJ mice
Klebsiella pneumoniae pneumonia model
Subcutaneous injection
50 mg/kg
Multiple doses over 57 hours
To study the antibacterial effect of Doripenem on Klebsiella pneumoniae-infected mice. The results showed that Doripenem significantly reduced the Klebsiella burden in the lungs of mice by 2 log10 CFU/g lung tissue over the first 48 h of the infection
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