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Xenobiotica
the fate of foreign compounds in biological systems
Volume 52, 2022 - Issue 9-11
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Clinical Pharmacokinetics and Metabolism

Human and nonclinical disposition of [14C]bictegravir, a potent integrase strand-transfer inhibitor for the treatment of HIV-1 infection

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Pages 973-985 | Received 19 Oct 2022, Accepted 13 Dec 2022, Published online: 06 Jan 2023

References

  • Birkus G, Bam RA, Willkom M, Frey CR, Tsai L, Stray KM, Yant SR, Cihlar T. 2016. Intracellular activation of tenofovir alafenamide and the effect of viral and host protease inhibitors. Antimicrob Agents Chemother. 60(1):316–322.
  • CDER (Center for Drug Evaluation and Research). 2016. Guidance for industry: safety testing of drug metabolites. Silver Spring, MD: U.S. Department of Health and Human Services, Food and Drug Administration. [accessed 2022 Dec 7]. https://www.fda.gov/media/72279/download.
  • Cockcroft DW, Gault MH. 1976. Prediction of creatinine clearance from serum creatinine. Nephron. 16(1):31–41.
  • EMA (European Medicines Agency). 2018. Public assessment report Biktarvy®. [accessed 2022 Dec 7]. https://www.ema.europa.eu/documents/assessment-report/biktarvy-epar-public-assessment-report_en.pdf. Last.
  • FDA (Food and Drug Administration). 2018. Biktarvy® (bictegravir, emtricitabine, and tenofovir alafenamide) tablets, for oral use. [accessed 2022 Dec 10]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf.
  • Hop CE, Wang Z, Chen Q, Kwei G. 1998. Plasma-pooling methods to increase throughput for in vivo pharmacokinetic screening. J Pharm Sci. 87(7):901–903.
  • Jin H, Pyun H, Smith BJ, Subramanian R, Wang J, inventors; Gilead Sciences, Inc., assignee. 2019 Jan 18. Metabolites of bictegravir. International Patent WO/2019/144015 Al.
  • Santoro MM, Fornabaio C, Malena M, Galli L, Poli A, Menozzi M, Zazzi M, White KL, Castagna A, for the PRESTIGIO Study Group. 2020. Susceptibility to HIV-1 integrase strand transfer inhibitors (INSTIs) in highly treatment-experienced patients who failed an INSTI-based regimen. Int J Antimicrob Agents. 56(1):106027.
  • Tiraboschi J, Imaz A, Khoo S, Niubo J, Prieto P, Saumoy M, Penchala SD, Garcia B, Padilla C, Videla S, et al. 2020. Total and unbound bictegravir concentrations and viral suppression in cerebrospinal fluid of human immunodeficiency virus-infected patients (Spanish HIV/AIDS Research Network, PreEC/RIS 56). J Infect Dis. 221(9):1425–1428.
  • Tsiang M, Jones GS, Goldsmith J, Mulato A, Hansen D, Kan E, Tsai L, Bam RA, Stepan G, Stray KM, et al. 2016. Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved resistance profile. Antimicrob Agents Chemother. 60(12):7086–7097.
  • Wang J, Lazerwith S, Morganelli P, Pyun H, Jin H, Tang J, Matles M, Mwangi J, Wang K, Eisenberg G, et al. 2017. P16. Prediction of bictegravir human pharmacokinetics from protein binding and in vitro-in vivo correlation. Poster Session Presented at: 21st North American ISSX Meeting; Sep 24 − 28; Providence, RI.
  • Zhang H, Custodio J, Wei X, Wang H, Wu A, Ling J, Martin H, Quirk E, Elliot C, Kearney B. 2017. Clinical pharmacology of the HIV integrase strand transfer inhibitor bictegravir. Sex Transm Infect. 93(Suppl 1):A74.