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Entry Entry and attachment inhibitors

Mechanism of action

Maraviroc blocks the CCR5 co-receptor (R5-tropic virus only); fostemsavir's active moiety temsavir binds gp120 and prevents attachment to CD4.

Genetic barrier to resistance

Reserved for multiclass resistance.

Class effects to know

  • Maraviroc: hepatotoxicity, postural hypotension
  • Fostemsavir: QT prolongation at high exposure
HIV-1 replication cycle and antiretroviral targets Seven steps from attachment to maturation, each labelled with the antiretroviral class that blocks it. CD4⁺ T cell Nucleus — host DNA provirus HIV virion new infectious virion Attachment & fusion gp120 binds CD4 then CCR5/CXCR4 Capsid transport & uncoating capsid docks at the nuclear pore Reverse transcription RNA → double-stranded DNA Integration integrase inserts provirus Transcription & translation host machinery makes viral RNA/protein Assembly & budding Gag/Gag-Pol at the membrane Maturation protease cleaves Gag-Pol Entry Capsid NRTI NNRTI INSTI Capsid PI

This class acts at the step labelled Entry (entry).

Drugs in this class