Raltegravir

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Raltegravir, better known as Isentress, (3l2v)

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Better Known as: Isentress

  • Marketed By: Merck & Co.
  • Major Indication: Human Immunodeficiency Virus Infection
  • Drug Class: Retroviral Integrase Inhibitor
  • FDA Approval (Patent Expiration): 2007 (2022)
  • 2009 Sales: ~$1.1 Billion
  • Importance: It was the first drug of the Integrase Inhibitor class to be approved by the FDA. It offers a powerful new tool to be utilized in combination therapies against HIV infections.[1]
  • The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

Retroviral Integrase is produced by the HIV retrovirus, enabling HIV to integrate its genetic material into the DNA of the infected cell. This integration step effectively transforms the infected cell into a permanent carrier of the viral genome, allowing the virus to persist and proliferate extensively.[2] Raltegravir

Pharmacokinetics

Retroviral Integrase Inhibitor Pharmacokinetics [3][4]
Parameter Raltegravir Elvitegravir
Tmax (hr) 1.8 2-4
Cmax (ng/ml) 4253 2070
Bioavailability (%) 32 ~30
Protein Binding (%) 83 N/A
T1/2 (hr) 10.8 7.6
AUC (ng/ml/hr) 10168 21200
Dosage (mg) 400 150
Metabolism Hepatic - (UGT1A1) Hepatic - (CYP3A4)

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. ↑ A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.
  4. ↑ Iwamoto M, Wenning LA, Petry AS, Laethem M, De Smet M, Kost JT, Breidinger SA, Mangin EC, Azrolan N, Greenberg HE, Haazen W, Stone JA, Gottesdiener KM, Wagner JA. Minimal effects of ritonavir and efavirenz on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother. 2008 Dec;52(12):4338-43. Epub 2008 Oct 6. PMID:18838589 doi:10.1128/AAC.01543-07


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