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Introduction Principles Management NRTI Info NNRTI Info
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CCR5 and CXCR4 Coreceptor Blockers

Key Management Information

 

Direct Links to CCR5 Receptor Blocker Info
Key Points
Generic Brand
Maraviroc Selzentry

 

Key Principles of CCR5 Coreceptor Inhibitor Administration

 

The CCR5 receptor inhibitors represent a new class of antiretroviral therapy which became available as of late 2007 and is indicated only for treatment experienced individuals at this time.  This drug class is only effective against pure CCR5 tropic virus; if there is CXCR4 virus present whether mixed or unmixed with CCR5 virus, CCR5 receptor blockade will not be effective virologically.

Therefore an assay to detect the receptor tropism for the patient's HIV-1 strain will be necessary prior to beginning therapy.  This assay, the Monogram Trofile, became commercially available at the time that the first of this class of drugs was approved. 

CCR5 tropic virus is found in early and later stage disease, but there is a shift in tropism in populations of HIV individuals toward more mixed (CCR5 and CXCR4) and pure CXCR4 tropic HIV as disease progresses.  Overall approximately 50% of all HIV-infected individuals who undergo a tropism assay (Trofile) harbor only CCR5-tropic HIV.  The test is priced at approximately $1500.

Like any other class of antiretroviral drugs, the CCR5 receptor inhibitors must be administered with at least 2 other active antiretroviral agents.

Maraviroc is the first co-receptor inhibitor available.  Vicriviroc, another pure CCR5-receptor inhibitor, is under development.  There are also pure CXCR4-receptor inhibitors under investigation.

 

 

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Click HERE for a summary of antiretroviral drug therapy

 

 

Links to Antiretroviral Sections (click on anything)
Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI)
AZT  |  ddC  |  ddI  |  d4T  |  3TC  |  ABC  |  FTC  |  TDF  |  Combivir  |  Trizivir  |  Epzicom  |  Truvada  |  Atripla
Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI)
efavirenz  |  nevirapine  |  delavirdine  |  etravirine
Protease Inhibitors (PI)  Boosted Protease Inhibitors
saquinavir  indinavir  |  ritonavir  |  nelfinavir  |  amprenavir  |  lopinavir + ritonavir  |  atazanavir  |  fosamprenavir  | tipranavir
Fusion Inhibitors
enfuvirtide
Co-Receptor Inhibitors
maraviroc
Integrase inhibitors
raltegravir
 
 
Quick Menu / Table of Contents
Introduction Principles Management NRTI Info NNRTI Info
PI Info Fusion Inhibitors Coreceptor Inhibitors Integrase Inhibitors Drug Summary
Investigational Adherence Lab Evaluation Resistance Tests PEP
Antiretroviral Tables OI Prevention Vaccinations TB Therapy Hepatitis Therapy
OI Diagnosis OI Therapy Bibliography Links Palliative Therapy

 

Updated 10.31.2007