Learn: antiretroviral pharmacology

Start from the viral life cycle, then go into each class, drug and UK product. Product pages reproduce the UK SmPC and add visual summaries of appearance, adverse reactions and pharmacology.

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

Drug classes

NRTI

Nucleoside/nucleotide reverse transcriptase inhibitors

Prodrugs phosphorylated by host-cell kinases to the active triphosphate (diphosphate for tenofovir). The active anabolite competes with the natural deoxynucleotide for HIV reverse transcriptase and, lacking a...

Tenofovir alafenamideTenofovir disoproxilEmtricitabineLamivudineAbacavirZidovudine
NNRTI

Non-nucleoside reverse transcriptase inhibitors

Bind a hydrophobic pocket close to (not in) the reverse transcriptase active site, causing an allosteric change that blocks DNA polymerisation. No intracellular activation is needed. Active against HIV-1 only (not...

EfavirenzRilpivirineDoravirineEtravirine
INSTI

Integrase strand-transfer inhibitors

Chelate the two Mg²⁺ ions in the integrase active site, blocking the strand-transfer step that inserts proviral DNA into the host genome.

DolutegravirBictegravirRaltegravirCabotegravir
PI

Protease inhibitors

Peptidomimetic inhibitors of the viral aspartyl protease, preventing cleavage of the Gag and Gag-Pol polyproteins so that new virions are immature and non-infectious. Given with a pharmacokinetic booster (ritonavir...

DarunavirAtazanavir
Booster

Pharmacokinetic enhancers

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

RitonavirCobicistat
Entry

Entry and attachment inhibitors

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

MaravirocFostemsavir
Capsid

Capsid inhibitors

Lenacapavir binds the interface between capsid protein subunits, disrupting capsid-mediated nuclear import, assembly and capsid formation — it acts at several stages of the life cycle.

Lenacapavir

Explore

UK formularyEvery product drawn from its SmPC description — identify tablets at a glance. Regimens & BHIVA tiersPreferred, alternative and other regimens by scenario. Interaction matrixCo-medications × antiretrovirals, each cell from SmPC 4.3/4.5. Resistance primerKey mutations, what they do and how they are scored. Resistance explorerBuild a genotype and watch drug activity change. Concentration–time curvesAccumulation, trough cover and the long tail of the injectables. QuizCase-based questions with cited feedback.