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High resolution mass spectrometry-based methodologies for identification of Etr...

Godinho, A; Martins, I; Nunes, J; Charneira, C; Grilo, J; Silva, D; Pereira, S; Soto, K, et al.

Drug bioactivation to reactive metabolites capable of covalent adduct formation with bionucleophiles is a major cause of drug-induced adverse reactions. Therefore, elucidation of reactive metabolites is essential to unravel the toxicity mechanisms induced by drugs and thereby identify patient subgroups at higher risk. Etravirine (ETR) was the first second-generation Non-Nucleoside Reverse Transcriptase Inhibito...


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...


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