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Booster Pharmacokinetic enhancers

Mechanism of action

Strong mechanism-based CYP3A inhibitors with no useful antiviral activity at booster doses; they raise and prolong exposure to the co-administered protease inhibitor.

Genetic barrier to resistance

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Class effects to know

  • Extensive drug–drug interactions
  • Cobicistat inhibits tubular creatinine secretion (MATE1) — creatinine rises without a true fall in GFR
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 Booster (maturation).

Drugs in this class

Ritonavir (RTV) SmPC not downloaded Cobicistat (COBI) SmPC not downloaded