Original Publication Date: 9 September, 2016
Publication / Source: Bioanalysis 8(20)
Authors: Curley P, Siccardi M, Moss DM, Owen A
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 . 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 . 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.