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. Department of Health and Human Services. https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf. Updated December 18, 2019. Accessed March 3, 2020.
- FDA approval of HIV medicines. AIDSinfo website. https://aidsinfo.nih.gov/understanding-hiv-aids/infographics/25/fda-approval-of-hiv-medicines. Updated April 30, 2019. Accessed March 3, 2020.
- 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.