Advanced search
Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 46, 2016 - Issue 2
Submit an article Journal homepage
1,752
Views
40
CrossRef citations to date
0
Altmetric
Clinical Pharmacokinetics and Metabolism

Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans

Gary David BowersDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA, Correspondence[email protected]
,
Amanda CulpDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Melinda J. ReeseDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Glenn TaboltDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Lee MossDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Stephen PiscitelliInfectious Diseases Medicines Discovery and Development, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Phuong HuynhDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
David WagnerDepartment of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC, USA,
,
Susan L. FordProject Clinical Platforms & Sciences, GlaxoSmithKline, Research Triangle Park, NC, USA, and
,
Elizabeth P. GouldProject Clinical Platforms & Sciences, GlaxoSmithKline, Research Triangle Park, NC, USA, and
,
Rennan PanProduct Development, GlaxoSmithKline, Upper Providence, PA, USA
,
Yu LouProject Clinical Platforms & Sciences, GlaxoSmithKline, Research Triangle Park, NC, USA, and
,
David A. MargolisInfectious Diseases Medicines Discovery and Development, GlaxoSmithKline, Research Triangle Park, NC, USA,
&
William R. SpreenInfectious Diseases Medicines Discovery and Development, GlaxoSmithKline, Research Triangle Park, NC, USA,
show all
Pages 147-162 | Received 12 May 2015, Accepted 05 Jun 2015, Published online: 01 Jul 2015

References

  • Anderson MS, Kakuda TN, Hanley W, et al. (2008). Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects. Antimicrob Agents Chemother 52:4228–32
  • Andrews CD, Spreen WR, Mohri H, et al. (2014). Long-acting integrase inhibitor protects macaques from interrectal simian/human immunodeficiency virus. Science 343:1151–14
  • Castellino S, Moss L, Wagner D, et al. (2013). Metabolism, excretion and mass balance of the HIV-1 integrase inhibitor dolutegravir in humans. Antimicrob Agents Chemother 57:3536–46
  • Chmela Z, Vesely J, Lemr K, et al. (2001). In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route. Drug Metab Dispos 29:326–34
  • Curie L. (1968). Limits for qualitative detection and quantitative determination – application to radioactivity. Anal Chem 40:586–93
  • European Medicines Agency. (2012). Guideline on the investigation of drug interactions. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2012/07/WC500129606.pdf [last accessed 5 May 2015]
  • Ford SL, Gould E, Chen S, et al. (2013). Effects of etravirine on the pharmacokinetics of the integrase inhibitor S/GSK1265744. Antimicrob Agents Chemother 57:277–80
  • Gautam N, Roy U, Balkundi S, et al. (2013). Preclinical pharmacokinetics and tissue distribution of long-acting nanoformulated antiretroviral therapy. Antimicrob Agents Chemother 57:3110–20
  • Gill KL, Houston JB, Galetin A. (2012). Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. Drug Metab Dispos 40:825–35
  • Guiney WJ, Beaumont C, Thomas SR, et al. (2011). Use of Entero-Test, a simple approach for non-invasive clinical evaluation of the biliary disposition of drugs. Br J Clin Pharmacol 72:133–42
  • Hop CECA, Wang Z, Qing C, Kwei G. (1998). Plasma-pooling methods to increase throughput for in vivo pharmacokinetic screening. J Pharm Sci 87:901–3
  • Jackson AGA, Else JJ, Mesquita PMM, et al. (2014). A compartmental pharmacokietic evaluation of long-acting rilpivirine in HIV-negative volunteers for pre-exposure prophylaxis. Clin Pharmacol Ther 96:314–23
  • Kassahun K, McIntosh I, Cui D, et al. (2007). Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme. Drug Metab Dispos 35:1657–63
  • Loevinger RL, Budinger TF, Watson EE. (1991). MIRD primer for absorbed dose calculations. Revised ed. New York (NY): Society of Nuclear Medicine
  • Moss L, Wagner D, Kanaoka E, et al. (2015). The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica 45:60–70
  • Reese MJ, Savina PM, Generaux GT, et al. (2013). In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. Drug Metab Dispos 41:353–61
  • Roffey SJ, Obach RS, Gedge JI, Smith DA. (2007). What is the objective of the mass balance study? A retrospective analysis of data in animal and human excretion studies employing radiolabeled drugs. Drug Metab Rev 39:17–43
  • Shipkova M, Strassburg CP, Braun F, et al. (2001). Glucuronide and glucoside conjugation of mycophenolic acid by human liver, kidney and intestinal microsomes. Br J Pharmacol 132:1027–34
  • Song I, Borland J, Min S, et al. (2011). Effects of etravirine alone and with ritonavir-boosted protease inhibitors on the pharmacokinetics of dolutegravir. Antimicrob Agents Chemother 55:3517–21
  • Spreen W, Min S, Ford SL, et al. (2013a). Pharmacokinetics, safety and monotherapy antiviral activity of GSK1265744, an HIV integrase strand transfer inhibitor. HIV Clin Trials 14:192–203
  • Spreen WR, Margolis DA, Pottage JC. (2013b). Long-acting injectable antiretrovirals for HIV treatment and prevention. Curr Opin HIV AIDS 8:565–71
  • Spreen W, Ford SL, Chen S, et al. (2014). GSK1265744 pharmacokinetics in plasma and tissue after single-dose long-acting (LA) injectable administration in healthy subjects. J Acquir Immune Defic Syndr 67:481–6
  • Tang B-K. (1990). Drug glucosidation. Pharmacol Ther 46:53–6

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:

Order Reprints Request Corporate Permissions

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:

Request Academic Permissions

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.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.