Drug intelligence / Profile preview

CNS-targeted highly active antiretroviral therapy

Development stage
Unknown
Lead developer
University of California, San Diego
Modality
Peptides, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

CNS-targeted highly active antiretroviral therapy (CNS-T HAART) is a therapeutic strategy developed and evaluated by researchers at the University of California, San Diego (notably through the CIT2 clinical trial) to treat HIV-associated neurocognitive impairment (HNCI). This approach involves selecting a combination of antiretroviral drugs—such as reverse transcriptase inhibitors, protease inhibitors, and integrase inhibitors—that demonstrate high central nervous system (CNS) penetration, often quantified by a CNS Penetration Effectiveness (CPE) score. By optimizing drug delivery across the blood-brain barrier, the strategy aims to suppress HIV replication within the brain, reduce neuroinflammation, and improve cognitive function in patients with HIV-associated neurocognitive disorders (HAND).

Other names
CNS-targeted HAARTCNS-T HAARTCNS-penetrating antiretroviral therapy
02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePOLG (Mitochondrial DNA polymerase gamma)gp41 (Human immunodeficiency virus type 1 glycoprotein 41)CCR5 (C-C chemokine receptor type 5)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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