38
Views
0
CrossRef citations to date
0
Altmetric
Original Research

Induction effect of antiretroviral bictegravir on the expression of Abcb1, Abcg2 and Abcc1 genes associated with P-gp, BCRP and MRP1 transporters present in rat peripheral blood mononuclear cells

, , , & ORCID Icon
Received 15 Jan 2024, Accepted 29 Apr 2024, Published online: 13 May 2024

References

  • Siraj J, Feyissa D, Mamo Y, et al. Antiretroviral treatment failure and associated factors among HIV patients on the first-line antiretroviral therapy at Mizan-Tepi University teaching hospital, Southwest Ethiopia: a cross-sectional study. Medicine. 2021;100(51):e28357. doi: 10.1097/MD.0000000000028357
  • Pennings P. HIV drug resistance: problems and perspectives. Infect Dis Rep. 2013;5(Suppl 11):e5. doi: 10.4081/idr.2013.s1.e5
  • Schlaeppi C, Vanobberghen F, Sikalengo G, et al. Prevalence and management of drug–drug interactions with antiretroviral treatment in 2069 people living with HIV in rural Tanzania: a prospective cohort study. HIV Med. 2020;21(1):53–63. doi: 10.1111/hiv.12801
  • Bertagnolio S, De Luca A, Vitoria M, et al. Determinants of HIV drug resistance and public health implications in low-and middle-income countries. Antivir Ther. 2012;17(6):941–953. doi: 10.3851/IMP2320
  • Cianfriglia M, Dupuis ML, Molinari A, et al. HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein. Retrovirology. 2007;4(1):1–10. doi: 10.1186/1742-4690-4-17
  • Chan GN, Patel R, Cummins CL, et al. Induction of P-glycoprotein by antiretroviral drugs in human brain microvessel endothelial cells. Antimicrob Agents Chemother. 2013;57(9):4481–4488. doi: 10.1128/AAC.00486-13
  • Burhenne J, Matthée A-K, Pasáková I, et al. No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. Antimicrob Agents Chemother. 2010;54(10):4185–4191. doi: 10.1128/AAC.00283-10
  • Svärd J, Blanco F, Nevin D, et al. Differential interactions of antiretroviral agents with LXR, ER and GR nuclear receptors: potential contributing factors to adverse events. Br J Pharmacol. 2014;171(2):480–497. doi: 10.1111/bph.12480
  • Rastinejad F, Huang P, Chandra V, et al. Understanding nuclear receptor form and function using structural biology. J Mol Endocrinol. 2013;51(3):T1–T21. doi: 10.1530/JME-13-0173
  • Timsit YE, Negishi MJS. CAR and PXR: the xenobiotic-sensing receptors. Steroids. 2007;72(3):231–246. doi: 10.1016/j.steroids.2006.12.006
  • Chai SC, Cherian MT, Wang Y-M, et al. Small-molecule modulators of PXR and CAR. Biochim Biophys Acta Gene Regul Mech. 2016;1859(9):1141–1154. doi: 10.1016/j.bbagrm.2016.02.013
  • Gwag T, Meng Z, Sui Y, et al. Non-nucleoside reverse transcriptase inhibitor efavirenz activates PXR to induce hypercholesterolemia and hepatic steatosis. J Hepatol. 2019;70(5):930–940. doi: 10.1016/j.jhep.2018.12.038
  • Sharma D, Lau AJ, Sherman MA, et al. Differential activation of human constitutive androstane receptor and its SV23 and SV24 splice variants by rilpivirine and etravirine. Br J Pharmacol. 2015;172(5):1263–1276. doi: 10.1111/bph.12997
  • Ekiciler A, Chen WLK, Bo Y, et al. Quantitative cytochrome P450 3A4 induction risk assessment using human hepatocytes complemented with pregnane X receptor-activating profiles. Drug Metab Dispos. 2023;51(3):276–284. doi: 10.1124/dmd.122.001132
  • Tsiang M, Jones GS, Goldsmith J, et al. Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved resistance profile. Antimicrob Agents Chemother. 2016;60(12):7086–7097. doi: 10.1128/AAC.01474-16
  • Chen T. Overcoming drug resistance by regulating nuclear receptors. 2010;62(13):1257–1264. doi: 10.1016/j.addr.2010.07.008
  • Center for drug evaluation and Research. Multi-discipline review of BIKTARVY. [cited 2023 Sep 20]. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210251Orig1s000MultidisciplineR.pdf
  • Nair AB, Jacob S. Jacob SJJob, pharmacy c. A simple practice guide for dose conversion between animals and human. J Basic Clin Pharm. 2016;7(2):27. doi: 10.4103/0976-0105.177703
  • Jadav T, Rajput N, Sahu AK, et al. LC-QQQ-MS based intracellular quantification of bictegravir in peripheral blood mononuclear cells and plasma. Anal Biochem. 2023;667:115084. doi: 10.1016/j.ab.2023.115084.
  • Wacker MJ, Godard MPJJobt J. Analysis of one-step and two-step real-time RT-PCR using SuperScript III. J Biomol Tech. 2005;16(3):266.
  • Wang Y-M, Ong SS, Chai SC, et al. Role of CAR and PXR in xenobiotic sensing and metabolism. Expert Opin Drug Metab Toxicol. 2012;8(7):803–817. doi: 10.1517/17425255.2012.685237
  • Shizu R, Nishiguchi H, Tashiro S, et al. Helix 12 stabilization contributes to basal transcriptional activity of PXR. J Biol Chem. 2021;297(3):100978. doi: 10.1016/j.jbc.2021.100978
  • Narayanan B, Lade JM, Heck CJ, et al. Probing ligand structure–activity relationships in pregnane X receptor (PXR): efavirenz and 8‐Hydroxyefavirenz exhibit divergence in activation. ChemMedchem. 2018;13(7):736–747. doi: 10.1002/cmdc.201700730
  • Windshügel B, Poso AJJo MR. Constitutive activity and ligand‐dependent activation of the nuclear receptor CAR—insights from molecular dynamics simulations. J Mol Recog. 2011;24(5):875–882. doi: 10.1002/jmr.1132
  • Soldin OP, Elin RJ, SJJAop S, et al. Therapeutic drug monitoring in human immunodeficiency virus/acquired immunodeficiency syndrome: quo vadis? Arch Pathol Lab Med. 2003;127(1):102–105. doi: 10.5858/2003-127-102-TDMIHI
  • Subramanian R, Wang J, Murray B, et al. Human pharmacokinetics prediction with an in vitro-in vivo correction factor approach and in vitro drug-drug interaction profile of bictegravir, a potent integrase-strand transfer inhibitor component in approved biktarvy® for the treatment of HIV-1 infection. Xenobiotica. 2022;52(12):1020–1030. doi: 10.1080/00498254.2023.2169207
  • Deeks EDJD. Bictegravir/Emtricitabine/Tenofovir alafenamide: a review in HIV-1 infection. 2018;78(17):1817–1828. doi: 10.1007/s40265-018-1010-7
  • Bousquet L, Pruvost A, Didier N, et al. Emtricitabine: inhibitor and substrate of multidrug resistance associated protein. Eur J Pharmaceut Sci. 2008;35(4):247–256. doi: 10.1016/j.ejps.2008.06.017
  • Albermann N, Schmitz-Winnenthal FH, Z’graggen K, et al. Expression of the drug transporters MDR1/ABCB1, MRP1/ABCC1, MRP2/ABCC2, BCRP/ABCG2, and PXR in peripheral blood mononuclear cells and their relationship with the expression in intestine and liver. Biochem Pharmacol. 2005;70(6):949–958. doi: 10.1016/j.bcp.2005.06.018
  • Chen Y, Tang Y, Guo C, et al. Nuclear receptors in the multidrug resistance through the regulation of drug-metabolizing enzymes and drug transporters. Biochem Pharmacol. 2012;83(8):1112–1126. doi: 10.1016/j.bcp.2012.01.030

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.