Bioanalysis Zone

Development and validation of an LC–MS/MS assay for the quantification of efavirenz in different biological matrices

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Drug penetration into the CNS is an important factor influencing therapy efficacy and side effects in numerous diseases areas. This is a particularly relevant for the treatment of HIV, where the CNS represents a sanctuary site for the viral replication, as well as a potential site for toxicity [1–3]. Efavirenz is a key antiretroviral and displays many desirable PK properties, such as a long half-life allowing once daily dosing and potency against HIV [4]. Despite these favorable properties, efavirenz-containing therapy is associated with the development of CNS toxicities. There is a paucity of information describing the distribution and characterization of drugs in the CNS [3]. We have validated a rapid, versatile and sensitive LC–MS/MS for the detection of efavirenz in different matrices to investigate efavirenz distribution in to the CNS.

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