|
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. The Trofile DNA is now available to perform tropism testing in persons with undetectable HIV RNA. 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 and only co-receptor inhibitor available. |
| Click HERE for a summary of antiretroviral drug therapy |
| Links to Antiretroviral Sections |
| Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI) |
| AZT | ddI | d4T | 3TC | ABC | FTC | TDF ||| Coformulation NRTI: Combivir | Trizivir | Epzicom | Truvada |
| Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI) |
| efavirenz | nevirapine | delavirdine | etravirine | rilpivirine |
| Protease Inhibitors (PI) | Boosted Protease Inhibitors |
| saquinavir | indinavir | ritonavir | nelfinavir | lopinavir + ritonavir | atazanavir | fosamprenavir | tipranavir |
| Co-receptor Inhibitors |
| maraviroc |
| Fusion Inhibitors |
| enfuvirtide |
| Integrase Inhibitors |
| raltegravir | elvitegravir |
| Antiretroviral Metabolic Inhibitors |
| cobicistat | ritonavir |
| Coformulations |
| Atripla (efavirenz/tenofovir/emtricitabine) | Complera (rilpivirine/tenofovir/emtricitabine) | Stribild (elvitegravir/cobicistat/tenofovir/emtricitabine) |
Updated 1/27/2013