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. Author manuscript; available in PMC: 2020 May 13.
Published in final edited form as: Curr Pharm Des. 2016;22(35):5477–5486. doi: 10.2174/1381612822666160726113001

Table 1:

CNS penetrating efficiency (CPE) of anti-retroviral drugs used in HIV treatment.

CNS penetrating efficiency (CPE)
Drug Class 4 3 2 1 Non-classified
Nucleoside Reverse Transcriptase Inhibitors Zidovudine Abacavir Didanosine Tenofovir
Emtricitabine Stavudine Zalcitabine
Lamivudine
Nonnucleoside Reverse Transcriptase Inhibitors Nevirapine Delavirdine Etravirine Rilpivirine: CSF/Plasma ratio 1.2–1.6% but above IC50
Efavirenz
Protease Indinavir/r Darunavir/r Atazanavir Nelfinavir
Inhibitors Fosamprenavir/r Atazanavir/r Ritonavir
Indinavir Fosamprenavir/r Saquinavir
Lopinavir/r Saquinavir/r
Tipranavir/r
Entry/Fusion Vicriviroc Maraviroc Enfuvirtide
Inhibitors
Integrase Raltegravir Dolutrgravir: CSF/Plasma ratio 0.467–0.546% but above IC50
Inhibitors
Elvitegravir:
No data (clinical study underway UCSD, Letendre S.)