| Name | Durlobactam sodium salt |
| Description | Durlobactam sodium salt (ETX2514) is a beta-lactamase inhibitor with IC50 values of 4 nM, 14 nM and 190 nM against class A KPC-2, class C AmpC and class D OXA-24. |
| In vitro | Method: After pre-incubation of Durlobactam sodium salt (ETX2514) with enzyme for 5 minutes, the IC50 value of Durlobactam for representative class A, C and D β-lactamases was measured.
RESULTS The IC50 values of Durlobactam against Class A KPC-2, Class C AmpC, and Class D OXA-24 are 0.004μM, 0.014μM and 0.19μM respectively. [1]
METHODS: Antimicrobial susceptibility testing of BCC and B. gladioli clinical isolates was performed with Durlobactam (2-64 μg/ml).
RESULTS Durlobactam showed moderate activity (MIC90= 16 μg/ml). [2] |
| In vivo | METHODS: Subjects were randomly assigned to 1 of 6 sequences, including a single 3-hour intravenous infusion of Durlobactam sodium salt (ETX2514) 4 g, a single 3-hour intravenous infusion of placebo, and a single 3-hour intravenous infusion of placebo plus a single dose. The second oral dose of moxifloxacin 400 mg was given open label at the end of the intravenous infusion. During each treatment period, ambulatory electrocardiogram (ECG) measurements were obtained from before dosing to 24 hours after the start of infusion.
RESULTS Durlobactam had no significant effect on electrocardiographic parameters, including QT interval prolongation. Durlobactam carries a low risk of prolonging the QT interval and is unlikely to produce any proarrhythmic effects. [3] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (167.1 mM), Sonication is recommended.
H2O : 2.5 mg/mL (8.35 mM), Sonication is recommended.
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| Keywords | β-Lactamase | ETX-2514 | ETX 2514 | Durlobactam sodium | Class D OXA-24 | Class C AmpC | Class A KPC-2 |
| Inhibitors Related | Neomycin sulfate | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate | BES |
United States
