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Monitoring Abacavir Bioactivation in Humans: Screening for an Aldehyde Metabolite

Grilo, N; Antunes, A; Caixas, U; Marinho, A; Charneira, C; Oliveira, MC; Monteiro, E; Marques, MM; Pereira, S

The anti-HIV drug abacavir is associated with idiosyncratic hypersensitivity reactions and cardiotoxicity. Although the mechanism underlying abacavir-toxicity is not fully understood, drug bioactivation to reactive metabolites may be involved. This work was aimed at identifying abacavir-protein adducts in the hemoglobin of HIV patients as biomarkers of abacavir bioactivation and protein modification. The protoc...


Evidence for nevirapine bioactivation in man: Searching for the first step in t...

Caixas, U; Antunes, A; Marinho, A; Godinho, A; Grilo, N; Marques, M; Oliveira, M; Branco, T; Monteiro, E; Pereira, S

Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used against human immunodeficiency virus type-1 (HIV-1), mostly to prevent mother-to-child HIV-1 transmission in developing countries. Despite its clinical efficacy, NVP administration is associated with a variety of toxic responses that include hepatotoxicity and skin rash. Although the reasons for the adverse effects of NVP administration a...


Evidence for Nevirapine Bioactivation in Man: Searching for the First Step in t...

Caixas, U; Antunes, A; Marinho, A; Godinho, A; Grilo, N; Marques, M; Oliveira, MC; Branco, T; Monteiro, E; Pereira, S

Despite its efficacy, including in the prevention of vertical transmission, the antiretroviral nevirapine is associated with severe idiosyncratic hepatotoxicity and skin rash. The mechanisms underlying nevirapine toxicity are not fully understood, but drug bioactivation to reactive metabolites capable of forming stable protein adducts is thought to be involved. This hypothesis is based on the paradigm that drug...


Long-Term Maraviroc Use As Salvage Therapy in HIV-2 Infection

Caixas, U; Ferreira, J; Marinho, A; Faustino, I; Grilo, N; Lampreia, F; Germano, I; Monteiro, E; Pereira, S


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