Eravacycline dihydrochloride (TP-434 dihydrochloride) is a novel tetracycline (TET) antibiotic. It exhibits in vitro activity against various gram-positive, gram-negative aerobic and anaerobic pathogens, including those exhibiting TET-specific acquired resistance mechanisms[1]. It inhibits protein synthesis through binding to the 30S ribosomal subunit[2]. Eravacycline dihydrochloride (TP-434 dihydrochloride) was approved for the treatment of complicated intraabdominal infections (cIAIs) in adults[3-4].
Eravacycline dihydrochloride (TP-434 dihydrochloride) (0.03 to 4 μg/ml; 24h) showed obvious bacteriostatic effect on pre-established biofilms formed by a uropathogenic Escherichia coli strain in vitro[5]. Eravacycline (0-8 μg/ml) has antibacterial activity against a large panel of clinical M. abscessus isolates in vitro[6].
Eravacycline (3-12mg/kg) was injected intravenically through the tail vein 2 and 12 h after infection with tetracycline resistant Streptococcus pneumoniae and MRSA isolates. Eravacycline has obvious therapeutic effect on infected mice, for lung infections with MRSA SA191, eravacycline given at 10 mg/kg i.v. produced a 2.4 log10 CFU reduction versus the values for the 24-hour untreated controls.[7].
References:
[1]. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Eravacycline. 2019 Apr 10. PMID: 31643186.
[2]. Chopra I, Roberts M. Tetracycline antibiotics: mode of action, applications, molecular biology, and epidemiology of bacterial resistance. Microbiol Mol Biol Rev. 2001 Jun;65(2):232-60 ; second page, table of contents. doi: 10.1128/MMBR.65.2.232-260.2001. PMID: 11381101; PMCID: PMC99026.
[3]. Alosaimy S, Abdul-Mutakabbir JC, et,al. Evaluation of Eravacycline: A Novel Fluorocycline. Pharmacotherapy. 2020 Mar;40(3):221-238. doi: 10.1002/phar.2366. Epub 2020 Feb 21. PMID: 31944332.
[4]. Sutcliffe JA, O'Brien W, et,al. Antibacterial activity of Eravacycline dihydrochloride (TP-434 dihydrochloride), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58. doi: 10.1128/AAC.01288-13. Epub 2013 Aug 26. PMID: 23979750; PMCID: PMC3811277.[5]. Grossman TH, O'Brien W, et,al. Eravacycline dihydrochloride (TP-434 dihydrochloride) is active in vitro against biofilms formed by uropathogenic Escherichia coli. Antimicrob Agents Chemother. 2015 Apr;59(4):2446-9. doi: 10.1128/AAC.04967-14. Epub 2015 Jan 26. PMID: 25624334; PMCID: PMC4356792.
[6]. Li A, He S, et,al. Omadacycline, Eravacycline, and Tigecycline Express Anti-Mycobacterium abscessus Activity In Vitro. Microbiol Spectr. 2023 Jun 15;11(3):e0071823. doi: 10.1128/spectrum.00718-23. Epub 2023 May 4. PMID: 37140428; PMCID: PMC10269442.
[7]. Grossman TH, Murphy TM, et,al. Eravacycline dihydrochloride (TP-434 dihydrochloride) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71. doi: 10.1128/AAC.04354-14. Epub 2015 Feb 17. PMID: 25691636; PMCID: PMC4394802.
Eravacycline dihydrochloride (TP-434 dihydrochloride)是一种新型四环素(TET)抗生素。TP-434在体外对各种革兰氏阳性、革兰氏阴性的好氧和厌氧病原体具有活性，包括那些表现出TET特异性获得性耐药机制的病原体[1]。Eravacycline通过与30S核糖体亚基结合抑制蛋白质合成[2]。Eravacycline可用于治疗成人并发腹腔内感染(cIAIs)[3-4]。
Eravacycline dihydrochloride (TP-434 dihydrochloride) (0.03 to 4 μg/ml; 24h)对尿路致病性大肠杆菌菌株形成的生物膜有明显的抑菌作用[5]。Eravacycline (0-8 μg/ml)在体外对临床脓肿分枝杆菌分离株具有抗菌活性[6]。
Eravacycline dihydrochloride (TP-434 dihydrochloride) (3-12mg/kg)在感染四环素耐药肺炎链球菌和MRSA分离株后2和12 h经尾静脉注射小鼠后对感染小鼠有明显的治疗作用, 对于MRSA SA191肺部感染，与未治疗组相比，10mg /kg静脉滴注Eravacycline可使CFU降低2.4 log10[7]。