For research use only. Not for therapeutic Use.
Lersivirine (Cat.No:I003643) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV-1 infection. It works by binding to and inhibiting the reverse transcriptase enzyme, thereby preventing the replication of the virus. Lersivirine has demonstrated potent antiviral activity and a high barrier to resistance. It is being studied for its efficacy and safety in HIV treatment regimens.
| Catalog Number | I003643 |
| CAS Number | 473921-12-9 |
| Synonyms | 5-[3,5-diethyl-1-(2-hydroxyethyl)pyrazol-4-yl]oxybenzene-1,3-dicarbonitrile |
| Molecular Formula | C17H18N4O2 |
| Purity | ≥95% |
| Target | Reverse Transcriptase |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 0.119 uM [1] |
| InChI | InChI=1S/C17H18N4O2/c1-3-15-17(16(4-2)21(20-15)5-6-22)23-14-8-12(10-18)7-13(9-14)11-19/h7-9,22H,3-6H2,1-2H3 |
| InChIKey | MCPUZZJBAHRIPO-UHFFFAOYSA-N |
| SMILES | N#CC1=CC(OC2=C(CC)N(CCO)N=C2CC)=CC(C#N)=C1 |
| Reference | </br>1:Single-dose pharmacokinetics, safety, and tolerability of modified-release formulations of lersivirine in healthy subjects. Vourvahis M, Wang R, Mendes da Costa L, Wang C, Weatherley B, Mukwaya G, Tawadrous M, Heera J.Clin Pharmacol Drug Dev. 2014 Nov;3(6):472-6. doi: 10.1002/cpdd.117. Epub 2014 May 26. No abstract available. PMID: 27129121 </br>2:Efficacy and safety of lersivirine versus etravirine for the treatment of HIV-1 infection in patients with prior non-nucleoside reverse transcriptase inhibitor (NNRTI) use and evidence of NNRTI resistance: a randomized phase 2B trial. DeJesus E, Fätkenheuer G, Orrell C, Wang C, Jones J, Craig C, Tawadrous M, Heera J.HIV Clin Trials. 2014 Sep-Oct;15(5):209-17. doi: 10.1310/hct1505-209. PMID: 25350959 </br>3:Effects of lersivirine on canine and rodent thyroid function. Houle CD, Finch GL, Mauthe RJ, Potter DM, Walisser JA, Gardner IB, DeWit RH.Toxicol Pathol. 2014 Jul;42(5):897-912. doi: 10.1177/0192623313503516. Epub 2013 Oct 16. PMID: 24135463 </br>4:Lersivirine – a new drug for HIV infection therapy. Platten M, Fätkenheuer G.Expert Opin Investig Drugs. 2013 Dec;22(12):1687-94. doi: 10.1517/13543784.2013.846325. Epub 2013 Oct 16. Review. PMID: 24128277 </br>5:Pharmacokinetic interactions between lersivirine and zidovudine, tenofovir disoproxil fumarate/emtricitabine and abacavir/lamivudine. Vourvahis M, Davis J, Langdon G, Layton G, Fang J, Choo HW, Hansson AG, Tawadrous M.Antivir Ther. 2013;18(6):745-54. doi: 10.3851/IMP2566. Epub 2013 Apr 4. PMID: 23558061 </br>6:Efficacy and safety of lersivirine (UK-453,061) versus efavirenz in antiretroviral treatment-naive HIV-1-infected patients: week 48 primary analysis results from an ongoing, multicenter, randomized, double-blind, phase IIb trial. Vernazza P, Wang C, Pozniak A, Weil E, Pulik P, Cooper DA, Kaplan R, Lazzarin A, Valdez H, Goodrich J, Mori J, Craig C, Tawadrous M.J Acquir Immune Defic Syndr. 2013 Feb 1;62(2):171-9. doi: 10.1097/QAI.0b013e31827a2ba2.. PMID: 23328090 </br>7:Effect of lersivirine co-administration on pharmacokinetics of methadone in healthy volunteers. Vourvahis M, Wang R, Gruener DM, Bruce RD, Haider S, Tawadrous M.Drug Alcohol Depend. 2012 Nov 1;126(1-2):183-8. doi: 10.1016/j.drugalcdep.2012.05.009. Epub 2012 Jun 8. PMID: 22682979 </br>8:Effect of rifampin and rifabutin on the pharmacokinetics of lersivirine and effect of lersivirine on the pharmacokinetics of rifabutin and 25-O-desacetyl-rifabutin in healthy subjects. Vourvahis M, Davis J, Wang R, Layton G, Choo HW, Chong CL, Tawadrous M.Antimicrob Agents Chemother. 2012 Aug;56(8):4303-9. doi: 10.1128/AAC.06282-11. Epub 2012 May 29. PMID: 22644026 Free PMC Article</br>9:Energetics of mutation-induced changes in potency of lersivirine against HIV-1 reverse transcriptase. Kar P, Knecht V.J Phys Chem B. 2012 Jun 7;116(22):6269-78. doi: 10.1021/jp300818c. Epub 2012 May 22. PMID: 22574920 </br>10:The effect of lersivirine, a next-generation NNRTI, on the pharmacokinetics of midazolam and oral contraceptives in healthy subjects. Davis J, Langdon G, Layton G, Chong CL, Ndongo MN, Vourvahis M.Eur J Clin Pharmacol. 2012 Nov;68(11):1567-72. doi: 10.1007/s00228-012-1287-5. Epub 2012 Apr 22. PMID: 22527351 |
