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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, SThe 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, MC; Branco, T; Monteiro, E; Pereira, SDespite 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...
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