Mechanism of Action
RUKOBIA, with its novel mechanism of action, was developed for heavily treatment-experienced (HTE) adults with HIV-1 and failing therapy.1 It is the first approved oral treatment option in this ARV class.2,3 See what makes RUKOBIA a first-in-class HIV-1 attachment inhibitor.
A first-in-class attachment inhibitor with a novel mechanism of action1,2
RUKOBIA prevents HIV-1 from interacting with host immune cells by binding to the viral envelope protein gp120, leaving CD4+ T-cells untouched.2,4
- Temsavir, the active moiety of RUKOBIA, attaches directly to gp120 on the surface of HIV-1 virions, near the CD4 attachment site.5 The attachment of temsavir locks gp120 into a closed formation that prevents the initial interaction between the virus and host immune cells
- This action prevents the first step of viral entry4
- No observed cross-resistance
ARV=antiretroviral; gp120=glycoprotein 120.
- Data on file, ViiV Healthcare.
- Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in adults and adolescents with HIV. US Department of Health and Human Services. Updated June 3, 2021. Accessed June 7, 2021. https://clinicalinfo.hiv.gov/sites/default/files/guidelines/documents/AdultandAdolescentGL.pdf
- FDA-approved HIV medicines. HIVinfo.NIH.gov website. Accessed June 10, 2021. https://hivinfo.nih.gov/understanding-hiv/fact-sheets/fda-approved-hiv-medicines
- Cahn P, Fink V, Patterson P. Fostemsavir: a new CD4 attachment inhibitor. Curr Opin HIV AIDS. 2018;13(4):341-345.
- Thompson M, Lalezari JP, Kaplan R, et al. Safety and efficacy of the HIV-1 attachment inhibitor prodrug fostemsavir in antiretroviral-experienced subjects: week 48 analysis of AI438011, a Phase IIb, randomized controlled trial. Antivir Ther. 2017;22(3):215-223.