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Objective of the present study was then to assess the antiviral activity of the protease inhibitor amprenavir in macrophages (M/M), and to compare it with its efficacy in peripheral blood lymphocytes (PBL). M/M were obtained from blood of sero-negative healthy donors and infected with M-tropic HIV-1 strain (HIV-1(Ba-L)). The stabilized infection was assessed by monitoring the HIV-1 p24 gag antigen production in the supernatants of M/M cultures. In the setting of acute infection (treatment before HIV-1 challenge), amprenavir showed substantial activity both in M/M and PBL at similar concentrations (EC50: 0.011 and 0.031 muM, respectively); complete inhibition of HIV-1 replication was achieved in both cell types at concentration of about 2 muM. In the setting of chronical infection (i.e. antiviral treatment several days after established infection), an antiviral effect of amprenavir was achieved in M/M, but at concentrations higher than those active in acutely infected M/M (EC50: 0.72 muM, EC90: 18.2 muM). The antiviral effect in chronically infected M/M was sustained for at least 2 weeks of continuous treatment. These findings suggest that amprenavir (at relatively high concentrations) has a clinically relevant antiviral effect in persistently infected reservoirs of HIV. (C) 2003 Elsevier B.V. All rights reserved.

Aquaro, S., Guenci, T., Di Santo, F., Francesconi, M., Calio, R., & Perno, C.F. (2004). Potent antiviral activity of amprenavir in primary macrophages infected by human immunodeficiency virus. ANTIVIRAL RESEARCH, 61(2), 133-137.

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