Etravirine

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Chemical Structure| 269055-15-4 同义名 : 依曲韦林 (TMC125) ;R165335;TMC125;Etravirine. Intelence.
CAS号 : 269055-15-4
货号 : A403297
分子式 : C20H15BrN6O
纯度 : 98%
分子量 : 435.277
MDL号 : MFCD09837879
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(114.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Etravirine (TMC 125) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that demonstrates potent in vitro activity against wild-type strains of HIV type 1 (HIV-1), as well as against numerous strains resistant to available NNRTIs. Furthermore, the potential for resistance to etravirine developing appears to be lower than for first-generation NNRTIs[3]. Etravirine is used in combination with other agents in the therapy of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS)[4]. TMC125, was highly active against wild-type HIV-1 (EC50 = 1.4 to 4.8 nM) and showed some activity against HIV-2 (EC50 = 3.5 mM). TMC125 also inhibited a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus[5]. Etravirine 5.2 mg/kg twice daily in treatment-experienced, HIV-1-infected children and adolescents provides comparable exposure to that in adults receiving etravirine 200 mg twice daily and is the recommended dose for children and adolescents[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02616783 HIV-1 Infection Phase 3 Completed - Belgium ... 展开 >> CHU Saint-Pierre University Hospital Brussels, Belgium University Hospital Gent Ghent, Belgium France CHU - Groupe Saint-Andre Bordeaux, France CHU de Dijon Dijon, France Hopital Europeen Marseille Marseille, France C.H.U. de Nantes Nantes, France C.H.U. de NICE Nice, France Hopital Saint Louis Paris cedex 10, France Hopital Saint Antoine Paris cedex 12, France CHU Hotel Dieu Paris, France Hopital Necker les Enfants Malades Paris, France Hopital Haut-Leveque Pessac, Cedex, France Service des Maladies Infectieuses et du Voyageur Tourcoing, France Italy Azienda Ospedaliera Papa Giovanni XXIII Bergamo, Italy Busto Arsizio Hospital Busto Arsizio, Italy IRCCS A.O.U. San Martino Genova, Italy Azienda Ospedaliera Luigi Sacco Milano, Italy Azienda Ospedaliero Universitaria Policlinico di Modena Modena, Italy U.O. Malattie Infettive Pescara, Italy Istituto Nazionale Malattie Infettive Lazzaro Spallanzani I.R.C.C.S. Roma, Italy Azienda Ospedaliero Universitaria di Sassari Sassari, Italy Dipartimento di Malattie Infettive e Tropicali Torino, Italy Spain Hospital Clinic de Barcelona Barcelona, Spain Hospital de la Santa Creu i Sant Pau Barcelona, Spain Hospital Universitari Germans Trias i Pujol Barcelona, Spain Hospital Vall d'Hebron Barcelona, Spain Hospital 12 de Octubre Madrid, Spain Hospital General Universitario Gregorio Maranon Madrid, Spain Hospital Universitario La Paz Madrid, Spain Ramon Y Cajal University Hospital Madrid, Spain Hospital Costa Del Sol Marbella, Spain Hospital General Universitario de Valencia Valencia, Spain United Kingdom Royal Victoria Hospital Belfast, United Kingdom Mortimer Market Centre London, United Kingdom Newcastle Royal Victoria Infirmary Newcastle Upon Tyne, United Kingdom 收起 <<
NCT00708162 HIV Infection Phase 3 Completed - -
NCT00708162 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.49mL

2.30mL

1.15mL

22.97mL

4.59mL

2.30mL
参考文献

[1]Das K, Clark AD Jr, et al. Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants. J Med Chem. 2004 May 6;47(10):2550-60.

[2]Andries K, Azijn H, et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6.

[3]Deeks ED, Keating GM. Etravirine. Drugs. 2008;68(16):2357-72

[4]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Etravirine. 2018 Feb 20

[5]Andries K, Azijn H, Thielemans T, Ludovici D, Kukla M, Heeres J, Janssen P, De Corte B, Vingerhoets J, Pauwels R, de Béthune MP. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6

[6]Kakuda TN, Brochot A, Green B, Nijs S, Vis P, Opsomer M, Tomaka FL, Hoetelmans RM. Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Relationships of Etravirine in HIV-1-Infected, Treatment-Experienced Children and Adolescents in PIANO. J Clin Pharmacol. 2016 Nov;56(11):1395-1405