CCR5, Fusion, Integrase Inhibitors - Anti - HIV

HIV-Related Drug Classes Navigation
  Anti-HIV Drug Classes (Home)  

Enfuvirtide (Fuzeon ®) maraviroc (Selzentry™)
raltegravir (Isentress ®)  

Enfuvirtide (Fuzeon ®)  top of page icon
Fusion protein inhibitor.
Dosing (Adults): 90 mg SQ twice daily. (Administer subcutaneously into upper arm, abdomen, or anterior thigh.)

Supplied: Injection (powder for reconstitution): 108 mg (90 mg/ml following reconstitution).

maraviroc (Selzentry™) top of page icon
Mechanism of Action
Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc

INDICATIONS AND USAGE
SELZENTRY, in combination with other antiretroviral agents, is indicated for treatment-experienced adult patients infected with only CCR5-tropic HIV-1, who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.

This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of SELZENTRY of 48 weeks duration. Both studies were conducted in clinically advanced, 3-class antiretroviral (NRTI, NNRTI, PI, or enfuvirtide) treatment-experienced adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy.

The following points should be considered when initiating therapy with SELZENTRY:

Tropism testing is required for the appropriate use of SELZENTRY.
Use of SELZENTRY is not recommended in patients with dual/mixed or CXCR4-tropic HIV-1 as efficacy was not demonstrated in a phase 2 study of this patient group.
The safety and efficacy of SELZENTRY have not been established in treatment-naïve adult patients or pediatric patients.


Recommended Dosing Regimen
Concomitant Medications SELZENTRY Dose
CYP3A inhibitors (with or without a CYP3A inducer)including:
  • protease inhibitors (except tipranavir/ritonavir)
  • delavirdine
  • ketoconazole, itraconazole, clarithromycin,
  • other strong CYP3A inhibitors (e.g., nefazadone, telithromycin)
 150 mg twice daily
Other concomitant medications, including tipranavir/ritonavir, nevirapine, all NRTIs and enfuvirtide 300 mg twice daily
CYP3A inducers (without a strong CYP3A inhibitor) including:
  • efavirenz
  • rifampin
  • carbamazepine, phenobarbital, and phenytoin
 600 mg twice daily

Supplied: 
Tablets: 150 mg and 300 mg

raltegravir (Isentress ®) top of page icon
INDICATIONS AND USAGE: 
ISENTRESS™ is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated:
• In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents
.
The safety and efficacy of ISENTRESS have not been established in treatment-naïve adult patients or pediatric patients

Dosing (Adults): 
400 mg administered orally, twice daily with or without food

Supplied: 
Tablets: 400 mg

Disclaimer   top of page icon
Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.

Popular Tools brain image

IV Dilution Protocols Renal Dosing Protocols Calculator Categories