Skip to main content
Log in

Efavirenz

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

Abstract

  • ▴ Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) which shows good inhibitory activity against HIV-1.

  • ▴ Reduced susceptibility to efavirenz has been reported with HIV-1 variants containing single and multiple mutations to the reverse transcriptase enzyme. In vitro and in vivo data suggest that the resistance profile of efavirenz overlaps with that of the NNRTIs nevirapine and delavirdine.

  • ▴ Clinically significant drug interactions have been reported with efavirenz and indinavir and saquinavir. An increase in dosage of indinavir from 800 to 1000mg 3 times daily is recommended during coadministration with efavirenz. Use of efavirenz in combination with saquinavir as the sole protease inhibitor is not recommended.

  • ▴ Once-daily efavirenz in combination with zidovudine plus lamivudine or indinavir or nelfinavir increased CD4+ cell counts and reduced HIV RNA plasma levels to below quantifiable levels (<400 copies/m1) in HIV-infected patients. A sustained reduction in viral load was maintained for at least 72 weeks in 1 study.

  • ▴ Nervous system symptoms (including headache, dizziness, insomnia and fatigue) and dermatological effects (including maculopapular rash) appear to be the most common adverse events reported with efavirenz-containing antiretroviral 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

Similar content being viewed by others

References

  1. Carpenter CCJ, Fischl MA, Hammer SM, et al. Antiretroviral therapy for HIV infection in 1998: updated recommendations of the International AIDS Society -USA Panel. JAMA 1998 Jul 1; 280: 78–86

    Article  PubMed  CAS  Google Scholar 

  2. Gazzard B, Moyle G, on behalf of the BfflVA Guidelines Writing Committee. 1998 revision to the British HIV association guidelines for antiretroviral treatment of HIV seropositive individuals. Lancet 1998 Jul 25; 352: 314–6

    Article  PubMed  CAS  Google Scholar 

  3. Young SD, Britcher SF, Tran LO, et al. L-743,726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother 1995 Dec; 39(12): 2602–5

    Article  PubMed  CAS  Google Scholar 

  4. DuPont Pharmaceuticals Company. Sustiva™ (efavirenz capsules). Prescribing information; 1998 Sep 17; http://www.sustiva.com

  5. Winslow DL, Garber S, Reid C, et al. Selection conditions affect the evolution of specific mutations in the reverse transcriptase gene associated with resistance to DMP 266. AIDS 1996 Sep; 10: 1205–9

    Article  PubMed  CAS  Google Scholar 

  6. Bacheler L, Weislow O, Snyder S, et al. Virologic resistance to efavirenz [abstract]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva, 784

  7. Jeffrey S, Baker D, Tritch R, et al. A resistance and cross resistance profile for Sustiva™ (efavirenz, DMP 266) [poster presentation 702]. 5th Conference on Retroviruses and Opportunistic Infections; 1998 Feb 1–5; Chicago (IL)

  8. Benedek IH, Joshi A, Fiske WD, et al. Pharmacokinetic (PK) interaction studies in healthy volunteers with efavirenz (EFV) and the macrolide antibiotics, azithromycin (AZM) and clarithromycin (CLR) [poster presentation 347]. 5th Conference on Retroviruses and Opportunistic Infections; 1998 Feb 1–5; Chicago (IL)

  9. Benedek I, Joshi A, Fiske WD, et al. Pharmacokinetic interaction between efavirenz (EFV) and rifampin (RIF) in healthy volunteers [abstract]. 12th WorldAIDS Conference; 1998 Jun 28–Jul 3; Geneva, 829

  10. Joshi AS, Fiske WD, Benedek IH, et al. Lack of pharmacokinetic interaction between efavirenz (DMP 266) and ethinyl estradiol in healthy female volunteers [poster presentation 348]. 5th Conference on Retroviruses and Opportunistic Infections; 1998 Feb 1–5; Chicago (IL)

  11. Benedek IH, Fiske WD, White SJ, et al. Plasma levels of fluconazole (FL) are not altered by coadministration of DMP 266 in healthy volunteers [abstract]. 37th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1997 Sep 28–Oct 1; Toronto (ON), 1

  12. Fiske WD, Benedek IH, White SJ, et al. Pharmacokinetic interaction between DMP 266 and nelfinavir mesylate (NFV) in healthy volunteers [abstract]. 37th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1997 Sep 28–Oct 1; Toronto (ON), 275

  13. Fiske WD, Benedek IH, White SJ, et al. Pharmacokinetic interaction between efavirenz (EFV) and nelfinavir mesylate (NFV) in healthy volunteers [poster presentation 349]. 5th Conference on Retroviruses and Opportunistic Infections; 1998 Feb 1–5; Chicago (IL)

  14. Benedek IH, Fiske WD, White SJ, et al. Lack of a pharmacokinetic interaction between single doses of DMP 266, an HIV-1 reverse transcriptase inhibitor, and famotidine or Mylanta® [poster presentation 3270]. American Association of Pharmaceutical Scientists; 1997 Nov 5; Boston (MA)

  15. Fiske W, Benedek IH, Joseph JL, et al. Pharmacokinetics of efavirenz (EFV) and ritonavir (RIT) after multiple oral doses in healthy volunteers [abstract]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva, 827

  16. Mayers D, Jemsek J, Eyster E, et al. A double-blind, placebo-controlled study to assess the safety, tolerability and antiretroviral activity of efavirenz (EFV, Sustiva™ DMP 266) in combination with open-label zidovudine (ZDV) and lamivudine (3TC) in HIV-l infected patients [DMP 266-004] [abstract]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva, 331

  17. Mayers D, Jemesk J, Eyster E, et al. A double-blind, placebocontrolled study to assess the safety, tolerability and antiretroviral activity of efavirenz (EFV, Sustiva™, DMP 266) in combination with open-label zidovudine (ZDV) and lamivudine (3TC) in HIV-l infected patients [DMP 266-004] [poster presentation 22340]. 12th World AIDS Conference; 1998 Jun 28—Jul 3; Geneva

  18. Gallant J, Seekins D, Hicks C, et al. A phase II, double-blind, placebo-control, dose-ranging study to assess the antiretroviral activity and safety of efavirenz (EFV, Sustiva, DMP266) in combination with open-label zidovudine (ZDV) w/ lamivudine (3TC) at >48 weeks PMP 266-005] [abstract]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 441

  19. Gallant J, Seekins D, Hicks C, et al. A phase II, double-blind, placebo-controlled, dose ranging study to assess the antiretroviral activity and safety of efavirenz (EFV, Sustiva™, DMP 266) in combination with open-label zidovudine (ZDV) with lamivudine (3TC) at 48 weeks PMP 266-005] [poster presentation 1-245]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA)

  20. Morales-Ramirez J, Tashima K, Hardy D, et al. A phase II, multi-center randomized, open-label study to compare the antiretroviral activity and tolerability of efavirenz (EFV) + indinavir (IDV), versus EFV + zidovudine (ZDV) + lamivudine (3TC), versus IDV + 3TC at >36 weeks [DMP 266-006] [abstract]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 394

  21. Morales-Ramirez J, Tashima K, Hardy D, et al. A phase III, multicenter, randomized, open-label study to compare the antiretroviral activity and tolerability of efavirenz (EFV) + indinavir (IDV), versus EFV + zidovudine (ZDV) + lamivudine (3TC), versus IDV + ZDV + 3TC at 36 weeks (DMP 266-006) [poster presentation I-103]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA)

  22. Tashima KT, Caliendo AMC, Ahmad MA, et al. Cerebrospinal fluid HIV-1 RNA levels and efavirenz concentrations in patients enrolled in clinical trials [abstract]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva, 561

  23. Havlir D, Hicks C, Kahn J, et al. Durability of antiviral activity of efavirenz (EFV, DMP 266) in combination with indinavir (IDV) [abstract]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 395

  24. Riddler S, Kahn J, Hicks C, et al. Durable clinical anti-HIV-1 activity (72 weeks) and tolerability for efavirenz (DMP 266) in combination with indinavir (IDV) [DMP 266-003, cohortTV] [poster presentation 12359]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva

  25. Haas DW, Fessel WJ, Delapenha RA, et al. A phase II, double-blind, placebo-controlled, multi-center study to determine the effectiveness and tolerability of the combination of efavirenz (EFV, Sustiva, DMP 266) and indinavir (IDV) versus IDV in HJV-1 infected patients receiving nucleoside analogue (NRTI) therapy at >36 weeks [Study DMP 266-020] [abstract]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 441

  26. Haas DW, Fessel WJ, Delaphena RA, et al. A phase III, double-blind, placebo-controlled, multicenter study to determine the effectiveness and tolerability of the combination of efavirenz (EFV, Sustiva™, DMP 266) and indinavir (IDV) versus indinavir in HIV-1 infected patients receiving nucleoside analogue (NRTI) therapy at 36 weeks PMP 266-020] [poster presentation I-244]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA)

  27. Kagan S, Jemsek J, Martin DG, et al. Initial effectiveness and tolerability of nelfinavir (NFV) in combination with efavirenz (EFV, Sustiva, DMP 266) in antiretroviral therapy naive or nucleoside analogue experienced HIV-1 infected patients: characterization in a phase II, open-label, multi-center study at >36 weeks [study DMP 266-024] [abstract]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA), 394

  28. Jemsek J, Kagan S, Martin G, et al. Combination with DMP 266 in antiretroviral therapy naive or nucleoside analogue experienced HTV-infected patients [DMP 266-024] [poster presentation 1–102]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA)

  29. DuPont Pharmaceuticals Company. Internal report: study protocol ACTG 364. Data on file

  30. Albrecht M, Katzenstein D, Bosch RJ, et al. ACTG 364: virologic efficacy of nelfinavir (NFV) and/or efavirenz (EFV) in combination with new nucleoside analogs in nucleoside experienced subjects [abstract]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva, 52

  31. Starr SE, Fletcher CV, Spector SA, et al. Efavirenz in combination with nelfinavir and nucleoside reverse transcriptase inhibitors (NRTIs) is safe and virologically effective in HIV-infected children [poster presentation LB-6]. 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24–27; San Diego (CA)

  32. Study shows efavirenz promising in treating pediatric HIV infection; leads to approval of new drug profile for treating HIV-infected children (media release). Today’s News 1998 Sep 29; http://www.prnewswire.com/cgi-bin

  33. Mayers D, Riddler S, Stein D, et al. A double-blind pilot study to evaluate the antiviral activity, tolerability and pharmacokinetics of DMP 266 alone and in combination with indinavir [abstract]. 36th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1996 Sep 15–18; New Orleans, (LO), 8

  34. Staszewski S, Morales-Ramirez J, Tashima K, et al. Aphase III, multicenter, randomized, open-label study to compare the antiretroviral activity and tolerability of efavirenz (EFV) + indinavir (IDV), versus EFV + zidovudine (ZDV) + lamivudine (3TC), versus IDV + ZDV + 3TC at 24 weeks [DMP 266-006] [poster presentation 22336]. 12th World AIDS Conference; 1998 Jun 28–Jul 3; Geneva

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Julie C. Adkins.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Adkins, J.C., Noble, S. Efavirenz. Drugs 56, 1055–1064 (1998). https://doi.org/10.2165/00003495-199856060-00014

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-199856060-00014

Keywords

Navigation