Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 50, 2020 - Issue 9
442
Views
3
CrossRef citations to date
0
Altmetric
Animal Pharmacokinetics and Metabolism

Metabolic disposition of H3B-8800, an orally available small-molecule splicing modulator, in rats, monkeys, and humans

, , , , , , , & show all
Pages 1101-1114 | Received 03 Dec 2019, Accepted 21 Dec 2019, Published online: 06 Jan 2020

References

  • Bohnert T, Gan LS. (2013). Plasma protein binding: from discovery to development. J Phar Sci 102:2953–94.
  • Buonamici S, Yoshimi A, Thomas M, et al. (2016). H3B-8800, an orally bioavailable modulator of the SF3b complex, shows efficacy in spliceosome-mutant myeloid malignancies. Blood 128:966.
  • Cashman JR. (2012). Flavin-containing monooxygenases in Encyclopedia of drug metabolism and interactions. In Lyubimov A, ed. Encyclopedia of Drug Metabolism and Interactions. New York: Wiley.
  • Davies B, Morris T. (1993). Physiological parameters in laboratory animals and humans. Pharm Res 10:1093–95.
  • Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers. Available from: https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/DrugInteractionsLabeling/ucm093664.html [last accessed 18 Jun 2019].
  • European Medicines Agency. 2012. Guideline on the investigation of drug interactions. Committee for Human Medicinal Products (CHMP). Available from: https://www.ema.europa.eu/en/documents/scientific-guideline/guideline-investigation-drug-interactions_en.pdf [last accessed 18 Jun 2019].
  • Hamilton RA, Garnett WR, Kline BJ. (1981). Determination of mean valproic acid serum level by assay of a single pooled sample. Clin Pharmacol Ther 29:408–13.
  • Harrell AW, Sychterz C, Ho MY, et al. (2015). Interrogating the relationship between rat in vivo tissue distribution and drug property data for >200 structurally unrelated molecules. Pharmacol Res Perspect 3:e00173.
  • Leblanc B, Jezequel S, Davies G, et al. (1998). Binding of drugs to eye melanin is not predictive of ocular toxicity. Regul Toxicol Pharmacol 28:124–32.
  • Partridge WM. (2012). Drug transport across the blood-brain barrier. J Cereb Blood Flow Metab 32:1959–72.
  • 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.
  • Seiler M, Yoshimi A, Darman R, et al. (2018). H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers. Nat Med 24:497–504.
  • Steensma D, Klimek V, Yang J, et al. 2019. Phase 1 dose escalation clinical trial of H3B-8800, a splicing modulator, in patients with advances myeloid malignancies. EHA 266651:PS1034.
  • Umehara KI, Iwatsubo T, Noguchi K, Kamimura H. (2007). Functional involvement of organic cation transporter1 (OCT1/Oct1) in the hepatic uptake of organic cations in humans and rats. Xenobiotica 37:818–31.
  • U.S Food and Drug Administration. 2017. Guidance for Industry: In vitro metabolism- and transporter- mediated drug-drug interaction studies guidance for industry (Draft guidance). Silver Spring, US: U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research. Available from: https://www.fda.gov/media/108130/download.
  • Yoshida K, Sanada M, Shiraishi Y, et al. (2011). Frequent pathway mutations of splicing machinery in myelodysplasia. Nature 478:64–9.
  • Zientek MA, Youdim K. (2015). Reaction phenotyping: advances in the experimental strategies used to characterize the contribution of drug-metabolizing enzymes. Drug Metab Dispos 43:163–81.

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.