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Raltegravir, better known as Isentress, (3l2v)

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Retroviral Integrase Inhibitor Pharmacokinetics
Parameter Raltegravir Elvitegravir MK-2048
Tmax (hr) 1.8 2-4 N/A
Cmax (ng/ml) 4253 2070 N/A
Bioavailability (%) 32 ~30 N/A
Protein Binding (%) 83 N/A N/A
T1/2 (hr) 10.8 7.6 N/A
AUC (ng/ml/hr) 10168 21200 N/A
Dosage (mg) 400 150 N/A
Metabolism Hepatic - (UGT1A1) Hepatic - (CYP3A4) N/A

For Pharmacokinetic Data References, See: References


  1. Steigbigel RT, Cooper DA, Kumar PN, Eron JE, Schechter M, Markowitz M, Loutfy MR, Lennox JL, Gatell JM, Rockstroh JK, Katlama C, Yeni P, Lazzarin A, Clotet B, Zhao J, Chen J, Ryan DM, Rhodes RR, Killar JA, Gilde LR, Strohmaier KM, Meibohm AR, Miller MD, Hazuda DJ, Nessly ML, DiNubile MJ, Isaacs RD, Nguyen BY, Teppler H. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med. 2008 Jul 24;359(4):339-54. PMID:18650512 doi:10.1056/NEJMoa0708975
  2. Savarino A. A historical sketch of the discovery and development of HIV-1 integrase inhibitors. Expert Opin Investig Drugs. 2006 Dec;15(12):1507-22. PMID:17107277 doi:10.1517/13543784.15.12.1507
  3. Hare S, Gupta SS, Valkov E, Engelman A, Cherepanov P. Retroviral intasome assembly and inhibition of DNA strand transfer. Nature. 2010 Mar 11;464(7286):232-6. Epub 2010 Jan 31. PMID:20118915 doi:10.1038/nature08784
  4. Hare S, Vos AM, Clayton RF, Thuring JW, Cummings MD, Cherepanov P. Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A. 2010 Oct 28. PMID:21030679 doi:10.1073/pnas.1010246107

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