ABSTRAC
Introduction: Despite the unquestionable success of antiretroviral therapy achieved in recent years, there are still cases of heavily treated patients who do not achieve or struggle to maintain undetectable HIV-RNA due to drug resistance. New antiretroviral options are needed to address this issue.
Area covered: The authors first provide an overview of fostemsavir and its role in the treatment of HTE PLWH. Data from pre-clinical and clinical studies are reviewed and the pharmacokinetic and farmacodynamic properties are highlited. Drug-drug interactions and safety data from available clinical studies are also discussed.
Expert opinion: Fostemsavir is a promising antiretroviral belonging to the class of entry inhibitors; its novel mechanism of action represents a very important innovation. Its use will be limited to the heavy-treatment-experienced patient population. This use will have to be monitored to avoid abuse and waste of a molecule that for some patients may represent a life-saving drug.
Article highlights
Heavily treated patients (HTE) are a minority of people living with HIV, but an important population with limited treatment options.
Fostemsavir is a novel, oral, entry inhibitor, acting directly on the HIV-1 surface.
Its innovative mechanism of action overcomes the drug resistances selected by older antiretroviral agents.
Fostemsavir allows the achievement of HIV RNA < 40 copies/mL in up to 60% of HTE patients failing their previous antiretroviral regimen.
As gp–120 is highly conserved, the fostemsavir is unlikely to promote resistance.
This box summarizes key points contained in the article.
Reviewer disclosures
Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.
Declaration of interest
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.