Which mutations cause the resistance to fusion inhibitors (FIs) in antiretroviral therapy of HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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Resistance to enfuvirtide has been well described and occurs in the HR1 domain of gp41. Amino acid substitutions occur in the 36-45 regions and result in significant loss of enfuvirtide activity. [93]

The risk of resistance can be minimized by combining enfuvirtide with other antiretroviral agents that display genotypic or phenotypic activity, which is now more easily achieved with the availability of second-generation nonnucleoside reverse transcriptase inhibitors and protease inhibitors and new antiretroviral classes (e.g., integrase strand-transfer inhibitors and CCR5 inhibitors). [94, 95] Cross-resistance with other antiretroviral agents has not been demonstrated to date.

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