Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 47, 2017 - Issue 12
511
Views
21
CrossRef citations to date
0
Altmetric
Clinical Pharmacokinetics and Metabolism

Metabolism, excretion and pharmacokinetics of [14C]glasdegib (PF-04449913) in healthy volunteers following oral administration

, , , , &
Pages 1064-1076 | Received 13 Sep 2016, Accepted 12 Nov 2016, Published online: 03 Jan 2017

References

  • Dierks C, Grbic J, Zirlik K, et al. (2007). Essential role of stromally induced hedgehog signaling in B-cell malignancies. Nat Med 13:944–51
  • 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
  • Ingham PW, McMahon AP. (2001). Hedgehog signaling in animal development: paradigms and principles. Genes Dev 15:3059–87
  • Irvine DA, Copland M. (2012). Targeting hedgehog in hematologic malignancy. Blood 119:2196–204
  • Martinelli G, Oehler VG, Papayannidis C, et al. (2015). Treatment with PF-04449913, an oral smoothened antagonist, in patients with myeloid malignancies: a phase 1 safety and pharmacokinetics study. Lancet Haematol 2:e339–46
  • McMillan R, Matsui W. (2012). Molecular pathways: the hedgehog signaling pathway in cancer. Clin Cancer Res 18:4883–8
  • Munchhof MJ, Li Q, Shavnya A, et al. (2012). Discovery of PF-04449913, a potent and orally bioavailable inhibitor of Smoothened. ACS Med Chem Lett 3:106–11
  • Peacock CD, Wang Q, Gesell GS, et al. (2007). Hedgehog signaling maintains a tumor stem cell compartment in multiple myeloma. Proc Natl Acad Sci USA 104:4048–53
  • Robison TW, Jacobs A. (2009). Metabolites in safety testing. Bioanalysis 1:1193–200
  • Shaik MN, Labadie RR, Rudin D, Levin WJ. (2014). Evaluation of the effect of food and ketoconazole on the pharmacokinetics of the smoothened inhibitor PF-04449913 in healthy volunteers. Cancer Chemother Pharmacol 74:411–8
  • Wagner AJ, Messersmith WA, Shaik MN, et al. (2015). A phase I study of PF-04449913, an oral hedgehog inhibitor, in patients with advanced solid tumors. Clin Cancer Res 21:1044–51
  • Yang X, Atkinson K, Di L. (2016). Novel cytochrome P450 reaction phenotyping for low-clearance compounds using the hepatocyte relay method. Drug Metab Dispos 44:460–5
  • Zhao C, Chen A, Jamieson CH, et al. (2009). Hedgehog signalling is essential for maintenance of cancer stem cells in myeloid leukaemia. Nature 458:776–9

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.