Intracellular accumulation of efavirenz and nevirapine is independent of P-glycoprotein activity in cultured CD4 T cells and primary human lymphocytes | Zendy

Omar Janneh | Zendy; Becky Chandler | Zendy; Ruben C. Hartkoorn | Zendy; Wai San Kwan | Zendy; C Jenkinson | Zendy; S. Evans | Zendy; David Back | Zendy; Andrew Owen | Zendy; SH Khoo | Zendy

Open Access

Intracellular accumulation of efavirenz and nevirapine is independent of P-glycoprotein activity in cultured CD4 T cells and primary human lymphocytes

Author(s) -

Omar Janneh,

Becky Chandler,

Ruben C. Hartkoorn,

Wai San Kwan,

C Jenkinson,

S. Evans,

David Back,

Andrew Owen,

SH Khoo

Publication year - 2009

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkp335

Subject(s) - efavirenz , multidrug resistance associated protein 2 , pharmacology , p glycoprotein , abcg2 , nevirapine , organic anion transporting polypeptide , chemistry , efflux , multidrug resistance associated proteins , peripheral blood mononuclear cell , transporter , atp binding cassette transporter , biology , multiple drug resistance , biochemistry , immunology , in vitro , antibiotics , viral load , human immunodeficiency virus (hiv) , antiretroviral therapy , gene

Interaction of antiretrovirals with drug transporters such as P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP), breast cancer resistance protein (BCRP) and solute carrier organic anion transporter (SLCO) may influence the emergence of viral mutants by altering intracellular drug concentrations. Here we characterize the effect of transporter expression in a variety of cell types such as control CEM, CEM(VBL) (P-gp-overexpressing), CEM(E1000) (MRP1-overexpressing), MT4, control MDCKII, MDCKII(MDR1) (P-gp-overexpressing) and peripheral blood mononuclear cells (PBMCs) on the uptake of [(14)C]efavirenz and [(3)H]nevirapine. We also investigated the lipophilicity of [(14)C]efavirenz and [(3)H]nevirapine.

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