杜洛巴坦三乙胺盐 T25355L

Product Introduction
Bioactivity


英文名: Durlobactam Triethylamine

描述: Durlobactam Triethylamine (ETX2514 Triethylamine) 是一种二氮杂双环辛烷β-内酰胺酶抑制剂，可抑制 A、C 和 D 类β-内酰胺。Durlobactam Triethylamine 具有抗真菌感染活性。

体内活性: This was a phase 1 study to evaluate the effects of various degrees of renal impairment, including subjects with end-stage renal disease (ESRD) on hemodialysis (HD), on the pharmacokinetics and safety profile of Durlobactam (also known as ETX2514) and sulbactam after single intravenous (i.v.) dose administration. For healthy subjects and those with mild or moderate renal impairment (RI), single 1,000-mg doses each of Durlobactam and sulbactam via a 3-h i.v. infusion was administered, and for severe renal impairment, 500mg doses were administered. For subjects with ESRD and HD, 500 mg i.v. doses of Durlobactam and sulbactam were administered post-HD and pre-HD, with a 1-week washout between doses. Among 34 subjects, decreasing renal function increased systemic exposure (peak plasma concentration [Cmax] and area under the concentration-time curve [AUC]) to Durlobactam and sulbactam in a generally linear manner. In healthy subjects and in those with mild or moderate renal impairment, the majority of Durlobactam and sulbactam was excreted in the urine, while approximately 40% or less was excreted in the urine in subjects with severe renal impairment or ESRD. In subjects with ESRD, hemodialysis was effective at removing both Durlobactam and sulbactam from plasma. Renal impairment had no effect on the safety/tolerability profile of Durlobactam and sulbactam. In summary, RI and ESRD had a predictable effect on the pharmacokinetic (PK) profile of Durlobactam and sulbactam with no adverse effects on the safety/tolerability profile. Durlobactam and sulbactam are cleared to a similar extent by renal elimination and are impacted similarly by renal impairment. The results from this study have been used with population PK modeling and non-clinically derived PK/PD (pharmacodynamic) exposure targets to establish dosage recommendations for Durlobactam and sulbactam in patients with various degrees of RI. The dosing regimen of Durlobactam-sulbactam will require adjustment in patients with severe renal insufficiency and in those with ESRD.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Durlobactam Triethylamine

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