| Description | Etravirine (R165335) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT. |
| In vitro | Etravirine (TMC125) 对野生型HIV-1具有高度活性，EC50为1.4 nM至4.8 nM，对HIV-2也显示出一定的活性，EC50为3.5 μM。TMC125还能抑制多种HIV-1群M亚型、循环重组形式以及O群病毒。[1] [2] |
| In vivo | Etravirine（TMC125）对于当前可用的NNRTIs具有较高的遗传抗性发展阻碍。在对经治疗患者，包括那些感染了对NNRTIs和蛋白酶抑制剂（PIs）有抗性的病毒者进行的IIb期试验中，TMC125对抗HIV的活性表现出与对照组相似的耐受性。 |
| Synonyms | TMC125, 依曲韦林, R165335 |
| molecular weight | 435.28 |
| Molecular formula | C20H15BrN6O |
| CAS | 269055-15-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (114.87 mM) |
| References | 1. Das K, et al. J Med Chem, 2004, 47(10), 2550-2560. 2. Andries K, et al. Antimicrob Agents Chemother, 2004, 48(12), 4680-4686. 3. Lazzarin A, et al. Lancet, 2007, 370(9581), 39-48. 4. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 |
| Citations | 1. Ly T T G, Yun J, Ha J S, et al. Inhibitory Effect of Etravirine, a Non-Nucleoside Reverse Transcriptase Inhibitor, via Anterior Gradient Protein 2 Homolog Degradation against Ovarian Cancer Metastasis. International Journal of Molecular Sciences. 2022, 23(2): 944. 2. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 3. Ekiciler A, Chen W L K, Bo Y, et al.Quantitative Cytochrome P450 3A4 Induction Risk Assessment Using Human Hepatocytes Complemented with Pregnane X Receptor-Activating Profiles.Drug Metabolism and Disposition.2023, 51(3): 276-284. |