Oral CCR5 inhibitors: Will they make it through?

Priscilla Biswas, Silvia Nozza, Gabriella Scarlatti, Adriano Lazzarin, Giuseppe Tambussi

Research output: Contribution to journalArticlepeer-review


The therapeutic armamentarium against HIV has recently gained a drug belonging to a novel class of antiretrovirals, the entry inhibitors. The last decade has driven an in-depth knowledge of the HIV entry process, unravelling the multiple engagements of the HIV envelope proteins with the cellular receptorial complex that is composed of a primary receptor (CD4) and a co-receptor (CCR5 or CXCR4). The vast majority of HIV-infected subjects exhibit biological viral variants that use CCR5 as a co-receptor. Individuals with a mutated CCR5 gene, both homo- and heterozygotes, appear to be healthy. For these and other reasons, CCR5 represents an appealing target for treatment intervention, although certain challenges can not be ignored. Promising small-molecule, orally bioavailable CCR5 antagonists are under development for the treatment of HIV-1 infection.

Original languageEnglish
Pages (from-to)451-464
Number of pages14
JournalExpert Opinion on Investigational Drugs
Issue number5
Publication statusPublished - May 2006


  • Antiretroviral therapy CCR5
  • CCR5 inhibitors
  • HIV-1
  • Viral entry

ASJC Scopus subject areas

  • Pharmacology


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