化合物AAI101 T14081

Product Introduction
Bioactivity


英文名: Enmetazobactam

描述: Enmetazobactam (AAI101) 是一种广谱β-lactamase 抑制剂，有抗耐药革兰氏阴性细菌。

体外活性: Enmetazobactam是一种新型的扩展谱β-内酰胺酶抑制剂。在223个对头孢吡肟不敏感的分离株中，95%对头孢他啶不敏感，49%对依他培南不敏感，57%对哌拉西林/他唑巴坦不敏感，90%属于多重耐药（对3类药物耐药），22%产生碳青霉烯酶，67%产生ESBLs。添加Enmetazobactam后，能显著降低头孢吡肟的最小抑菌浓度（MIC50），从>64 mg/L降至头孢吡肟/Enmetazobactam的0.13 mg/L，支持其在治疗这些微生物引起的感染中继续开发使用。Enmetazobactam对特定耐药表型表现出强大的活性，其MIC50和MIC90分别为0.125 mg/L和64 mg/L[1]。对于大多数菌株，随着Enmetazobactam浓度的增加（在1至16 mg/L范围内），头孢吡肟-Enmetazobactam的MICs显示出降低趋势，这表明Enmetazobactam在恢复头孢菌素类抗菌活性方面呈现浓度依赖性[1]。

体内活性: Against a panel of 20 mostly carbapenemase-producing cefepime-nonsusceptible strains of the family Enterobacteriaceae, we evaluated the MICs of cefepime in the presence of various fixed AAI101 concentrations (1, 2, 4, 8, and 16 mg/liter) and the in vivo efficacy of simulated human doses of cefepime and cefepime-AAI101 in a neutropenic murine thigh infection model.?At 2 h after inoculation, mice were dosed with regimens that provided a profile mimicking the free drug concentration-time profile observed in humans given cefepime at 2 g every 8 h (q8h;?as a 30-min infusion) or cefepime-AAI101 at 2 g/0.5 g q8h (as a 30-min infusion).?Efficacy was determined by calculation of the change in thigh bacterial density (log10 number of CFU) after 24 h relative to the starting inoculum (0 h). After 24 h, bacterial growth of 2.7 0.1 log10 CFU (mean standard error) was observed in control animals.?Efficacy for cefepime monotherapy was observed against only 3 isolates, whereas increases in bacterial density similar to that in the control animals were noted for the remaining 17 strains (all with cefepime MICs of 64 mg/liter).?The humanized cefepime-AAI101 dosing regimen resulted in bacterial reductions of 0.5 log10 CFU for 12 of the 20 strains[2].

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

溶解度: DMSO : 113.3 mg/mL (360.46 mM)


关键字: Enmetazobactam | Bacterial | inhibit | AAI-101 | AAI 101 | Inhibitor

相关产品: Daptomycin | Nifursol | Sulfacetamide sodium monohydrate | WCK-5153 | Sinapaldehyde | Leucomycin | Sorbic acid | Lutein | Gliotoxin | Neomycin sulfate

相关库: Drug Repurposing Compound Library | Antibiotics Library | ReFRAME Related Library | Drug-induced Liver Injury (DILI) Compound Library | Beta-Lactam Compound Library | Inhibitor Library | Anti-Bacterial Compound Library | Covalent Inhibitor Library | NO PAINS Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途