Skip to main content
Log in

Atazanavir

  • Adis Drug Profile
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

  • ▴ Atazanavir is a novel azapeptide protease inhibitor with high specificity for, and activity against, HIV-1 protease.

  • ▴ The resistance profile of atazanavir is distinct, with an I50L protease substitution appearing to be the signature mutation.

  • ▴ Atazanavir was not associated with increases in total cholesterol, low density lipoprotein-cholesterol or triglyceride levels after 108 weeks.

  • ▴ Atazanavir has a pharmacokinetic profile that allows for once-daily oral administration. It is a moderate inhibitor of hepatic cytochrome P450 enzymes and interacts with several drugs.

  • ▴ In combination with stavudine plus didanosine, atazanavir 200, 400 or 500mg once daily produced a rapid and sustained reduction from baseline in viral load of 2.57, 2.42 and 2.53 log10 copies/mL, respectively, in treatment-naive patients after 48 weeks, compared with a decrease of 2.33 log10 copies/mL with nelfinavir 750mg three times daily.

  • ▴ Nausea was the most clinically relevant adverse event reported in patients receiving atazanavir-based regimens.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig

Similar content being viewed by others

Notes

  1. Use of tradename is for product identification purposes only and does not imply endorsement.

References

  1. Yeni PG, Hammer SM, Carpenter CC, et al. Antiretroviral treatment for adult HIV infection in 2002: updated recommendations of the International AIDS Society — USA panel. JAMA 2002 Jul 10; 288(2): 222–35

    Article  PubMed  CAS  Google Scholar 

  2. Panel on Clinical Practices for Treatment of HIV Infection convened by the Department of Health and Human Services (DHHS) and the Henry J. Kaiser Family Foundation. Guidelines for the use of antiretroviral agents in HIV-infected adults and adolescents [online]. Available from URL: http://www.aidsinfo.nih.gov/guidelines/default_db2.asp?id=50 [Accessed 2003 Jun 19]

  3. BHIVA Writing Committee on behalf of the BHIVA Executive Committee. British HIV Association (BHIVA) guidelines for the treatment of HIV-infected adults with antiretroviral therapy. HIV Med 2001 Oct; 2: 276–313

    Article  Google Scholar 

  4. Sanne I, Piliero P, Squires K, et al. Results of a phase 2 clinical trial at 48 weeks (AI424-007): a dose-ranging, safety, and efficacy comparative trial of atazanavir at three doses in combination with didanosine and stavudine in antiretroviral-naive subjects. J Acquir Immune Defic Syndr 2003 Jan 1; 32(1): 18–29

    Article  PubMed  CAS  Google Scholar 

  5. Piliero PJ. Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs 2002 Sep; 11(9): 1295–301

    Article  PubMed  CAS  Google Scholar 

  6. O’Mara E, Randall D, Uderman L, et al. Steady-state pharmacokinetic interaction study between BMS-232632 and ketoconazole in healthy subjects [poster no. 1646]. 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2000 Sep 17–20; Toronto (ON)

  7. Witherell G. BMS-232632 (Novartis/Bristol-Myers Squibb). Curr Opin Investig Drugs 2001 Mar; 2(3): 340–7

    PubMed  CAS  Google Scholar 

  8. Robinson BS, Riccardi KA, Gong Y, et al. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother 2000 Aug; 44(8): 2093–9

    Article  PubMed  CAS  Google Scholar 

  9. Gong Y, Robinson BS, Rose RE, et al. Invitroresistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632. Antimicrob Agents Chemother 2000 Sep; 44(9): 2319–26

    Article  PubMed  CAS  Google Scholar 

  10. Colonno RJ, Hertogs K, Larder BA, et al. BMS-232632 sensitivity of a panel of HIV-1 clinical isolates resistant to one or more approved protease inhibitors [poster no. 8]. 4th International Workshop on HIV Drug Resistance and Treatment Strategies; 2000 Jun 12–16; Sitges

  11. Drusano GL, Bilello JA, Preston SL, et al. Hollow-fibre unit evaluation of a new human immunodeficiency virus type 1 protease inhibitor, BMS-232632, for determination of the linked pharmacodynamic variable. J Infect Dis 2001; 183: 1126–9

    Article  PubMed  CAS  Google Scholar 

  12. Colonno R, Rose R, Cianci C, et al. Emergence of atazanavir resistance and maintenance of susceptibility to other PIs is associated with an I50L substitution in HIV protease [abstract no. 597 plus poster]. 10th Conference on Retroviruses and Opportunistic Infections; 2003 Feb 10–14; Boston (MA) [online]. Available from URL: http://www.retroconference.org/ 2003/Abstract/Abstract.aspx?AbstractID=1925 [Accessed 2003 Jun 19]

  13. Colonno RJ, Friborg J, Rose RE, et al. Identification of amino acid substitutions correlated with reduced atazanavir susceptibility in patients treated with atazanavir containing regimens [abstract no. 004 with poster]. 11th International HIV Drug Resistance Workshop; 2002 Jul 2–5; Seville

  14. Colonno RJ, Hertogs K, Larder BA, et al. Efficacy of BMS-232632 against a panel of HIV-1 clinical isolates resistant to currently used protease inhibitors [abstract no. 2114]. 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2000 Sep 17–20; Toronto (ON), 349

  15. Colonno RJ, Thiry A, Parkin NT. Amino acid substitutions that correlate with decreased susceptibility to atazanavir and other HIV-1 protease inhibitors [abstract no. H-2049 plus poster]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego (CA), 291

  16. Colonno RJ, Thiry A, Limoli K, et al. Activities of atazanavir (BMS-232632) against a large panel of human immunodeficiency virus type 1 clinical isolates resistant to one or more approved protease inhibitors. Antimicrob Agents Chemother 2003 Apr; 47(4): 1324–33

    Article  PubMed  CAS  Google Scholar 

  17. Squires KE, Thiry A, Giordano M, et al. Atazanavir (ATV) qd vs efavirenz (EFV) qd with fixed-dose zidovudine (ZDV) and lamivudine (3TC) bid: comparison of antiviral efficacy and safety: 48-week results from BMS AI424-034 phase III pivotal study [poster]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego (CA)

  18. Haas DW, Zala C, Schrader S, et al. Therapy with atazanavir plus saquinavir in patients failing highly active antiretroviral therapy: a randomized comparative pilot trial. AIDS 2003 Jun 17; 17(9): 1339–49

    Article  PubMed  CAS  Google Scholar 

  19. Murphy R, Pokrovskiy V, Rozenbaum W, et al. Long-term efficacy and safety of atazanavir with stavudine and lamivudine in patients previously treated with nelfinavir or ATV: 108-week results of BMS Study 008/044 [abstract no. 555 plus poster G1-36]. 10th Conference on Retroviruses and Opportunistic Infections; 2003 Feb 10–14; Boston (MA) [online]. Available from URL: http://www.retroconference.org/2003/ Abstract/Abstract.aspx?AbstractID=2075 [Accessed 2003 Jun 20]

  20. Bristol-Myers Squibb Company. BMS-232632: Atazanavir Briefing Document May-2003 [online]. Available from URL:http://www.fda.gov/ohrms/dockets/ac/03/briefing/3950Bl_01_BristolMyersSquibb-Atazanavir.pdf [Accessed 2003 May 15]

  21. Piliero PJ, Cahn P, Pantaleo G, et al. Atazanavir: a once-daily protease inhibitor with a superior lipid profile-results of clinical trials beyond week 48 [abstract 706-T plus poster]. 9th Conference on Retroviruses and Opportunistic Infections; 2002 Feb 24–28; Seattle (WA) [online]. Available from URL: http://www.retroconference.org/2002/Abstract/13827.htm [Accessed 2003 Jan 30]

  22. Haas DW, Zala C, Schrader S, et al. Atazanavir (ATV) plus saquinavir (SQV) once daily: favorable effects on lipid profiles in patients failing prior therapy (Trial AI424-009) [poster]. 51st Annual Scientific Session of the American College of Cardiology; 2002 Mar 17–20; Atlanta (GA)

  23. Bristol-Myers Squibb. Data show HIV patients switched to Bristol-Myers Squibb investigational protease inhibitor may have significant reductions in cholesterol and triglyceride levels [media release]. Bristol-Myers Squibb: 2002 Jul 11

  24. O’Mara E, Randall D, Stoltz R, et al. BMS-232632: a prospective study of age and gender effects on the single-dose pharmacokinetics in healthy volunteers [abstract]. 1st International Aids Society Conference; 2001 Jul 8; Buenos Aires, 180

  25. O’Mara E, Mummaneni V, Bifano M, et al. Steady-state pharmacokinetic interaction study between BMS-232632 and ritonavir in healthy subjects [abstract no. 740]. 8th Conference on Retroviruses and Opportunistic Infections; 2001 Feb 4; Chicago (IL)

  26. Agarwala S, Russo R, Mummaneni V, et al. Steady-state pharmacokinetic (PK) interaction study of atazanavir (ATV) with ritonavir (RTV) in healthy subjects. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27; San Diego (CA), 274

  27. Tackett D, Child M, Argarwala S, et al. Atazanavir (ATV): a summary of two pharmacokinetic (PK) drug interaction studies in healthy subjects [poster no. 543]. 10th Conference on Retroviruses and Opportunistic Infections; 2003 Feb 10–14; Boston (MA) [online]. Available from URL: http://www.retroconference.org/2003/Abstract/Abstract.aspx?AbstractID=649 [Accessed 2003 Jun 20]

  28. Preston S, Piliero P, O’Mara E, et al. Evaluation of the steady state interaction between atazanavir (ATV) and efavirenz (EFV) [abstract no. 443-W]. 9th Conference on Retroviruses and Opportunistic Infections; 2002 Feb 24–28; Seattle (WA) [online]. Available from URL: http://www.retroconference.org/2003/Abstract/Abstract.aspx?AbstractID=649 [Accessed 2003 Jan 30]

  29. Mummaneni D, Randall D, Chabuel M, et al. Steady-state pharmacokinetic (PK) interaction study of atazanavir (ATV) with clarithromycin (CLR) in healthy subjects. 42nd Inter-science Conference on Antimicrobial Agents and Chemotherapy;2002 Sep 27–30; San Diego (CA), 275

  30. Agarwala S, Mummaneni V, Randall D, et al. Pharmacokinetic (PK) effect of rifabutin (RIF) on atazanavir (ATV) with and without ritonavir (RTV) in healthy subjects [abstract no. 445-W]. 9th Conference on Retroviruses and Opportunistic Infections; 2002 Feb 24–28; Seattle (WA) [online]. Available from URL: http://www.retroconference.org/2002/Abstract/13619.htm [Accessed 2003 Jan 30]

  31. O’Mara E, Agarwala S, Randall M, et al. Steady-state pharmacokineticinteraction study of atazanavir (ATV) with efavirenz (EFV) and ritonavir (RTV) in healthy subjects [abstract no. 444-W]. 9th Conference on Retroviruses and Opportunistic Infections; 2002 Feb 24–28; Seattle (WA) [online]. Available from URL: http://www.retroconference.org/2002/Abstract/13653.htm [Accessed 2003 Jan 30]

  32. O’Mara E, Piliero P, Drusano G, et al. BMS-232632: a preliminary pharmacokinetic and pharmacodynamic evaluation of BMS-232632 in a protease inhibitor-naive HIV+ population [abstract no. P9]. AIDS 2000 Oct 4; 14 Suppl. 4: S19

    Google Scholar 

  33. O’Mara EM, Smith J, Olsen SJ, et al. BMS-232632: single-oral dose-safety and pharmacokinetic study in healthy volunteers [abstract no. I-242]. 38th Interscience Conference on AntimicrobialAgents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 440

  34. O’Mara E, Mummaneni V, Randall D, et al. BMS-232632: a summary of multiple dose pharmacokinetic, food effect and drug interaction studies in healthy subjects [abstract no. 504].7th Conference on Retroviruses and Opportunistic Infections; 2000 Jan 30–Feb 4; San Francisco (CA) [online]. Available from URL: http://www.retroconference.org/2000/abstracts/504.htm [Accessed 2003 Mar 7]

  35. Randall D, Agarwala S, Mummaneni V, et al. Tissue compartment concentrations of atazanavir (ATV) in cerebrospinal fluid, seminal fluid and plasma in HIV + subjects [abstract no. H-1711]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego (CA), 273

  36. O’Mara E, Cirincione B, Mummaneni V, et al. Population pharmacodynamic (PD) assessment of the safety and antiretroviralactivity of B-MS 232632 [abstract plus poster]. 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; 2001 Sep 22; Chicago (IL), 18

  37. Taburet AM, Piketty C, Gerard L, et al. Pharmacokinetic parameters of atazanavir/ritonavir when combined to tenofovirin HIV infected patients with multiple treatment failures: a sub-study of Puzzle2-ANRS 107 Trial [abstract no. 537 plus poster]. 10th Conference on Retroviruses and Opportunistic Infections; 2003 Feb 10–14; Boston (MA) [online]. Available from URL: http://www.retroconference.org/2003/Abstract/Abstract.aspx?AbstractID=1515 [Accessed 2003 Jun 23]

  38. Mummaneni V, Randall D, Geraldes M, et al. Steady-state pharmacokinetic interaction study of atazanavir with lamivudine(3-TC) and zidovudine in healthy subjects [abstract no. H-1713]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego (CA), 274

  39. Pantaleo G, Gatell J, Cahn P, et al. Additional evidence for the absence of serum lipid elevations after 48-week treatment with atazanavir (BMS-232632) in treatment-naive HIV-positive subjects (Trial AI424-008) [abstract plus poster]. 8th European Conference on Clinical Aspects and Treatment of HIV-Infection; 2001 Oct 28–31; Athens, 149

  40. Cahn P, Piliero P, Giordano M, et al. Atazanavir (ATV): antiretroviral efficacy in HIV-infected patients co-infected with hepatitis B and/or C viruses (HBV, HCV) [abstract no. H-1730]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 2002 Sep 27–30; San Diego (CA), 278

  41. Data on file, Bristol-Myers Squibb Company, 2003.

  42. Prescribing Information. Reyataz™ (atazanavir sulfate) capsules [online]. Available from URL: http://www.reyataz.com [Accessed 2003 Jun 23]

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to David R. Goldsmith.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Goldsmith, D.R., Perry, C.M. Atazanavir. Drugs 63, 1679–1693 (2003). https://doi.org/10.2165/00003495-200363160-00003

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-200363160-00003

Keywords

Navigation