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Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene-related peptide receptor antagonist, in adults

Tae H Han, Rebecca L Blanchard, John Palcza, Jacqueline B McCrea, Tine Laethem, Kenneth Willson, Yang Xu, Susan Ermlich, Janet Boyle, Christopher Lines, et al. (2010) JOURNAL OF CLINICAL PHARMACOLOGY. 50(12). p.1367-1376
abstract
Telcagepant is a novel, orally active, and selective calcitonin gene-related peptide receptor antagonist being developed for acute treatment of migraine with and without aura. Three separate clinical studies were conducted to evaluate the pharmacokinetics and tolerability of telcagepant following single oral doses in healthy young and elderly men and women and multiple oral doses in men. Telcagepant was rapidly absorbed with a time to maximum concentration of approximately 1.5 hours. The terminal half-life was approximately 6 hours. A greater than dose-proportional increase was observed in the area under the plasma concentration versus time curve from zero to infinity. Following twice-daily dosing, with each dose separated by 2 hours, steady state was achieved in approximately 3 to 4 days with an accumulation ratio of approximately 2. There were no clinically meaningful pharmacokinetic differences when compared across age and gender. Telcagepant was generally well tolerated up to single doses of 1200 mg and multiple doses of 400 mg twice daily.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (proceedingsPaper)
publication status
published
subject
keyword
POTENT
journal title
JOURNAL OF CLINICAL PHARMACOLOGY
J. Clin. Pharmacol.
volume
50
issue
12
pages
1367 - 1376
conference name
Annual Meeting of the American-Society-for-Clinical-Pharmacology-and-Therapeutics
conference location
Washington, DC, USA
conference start
2009-03-18
conference end
2009-03-21
Web of Science type
Proceedings Paper
Web of Science id
000283854600002
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
3.59 (2010)
JCR rank
59/249 (2010)
JCR quartile
1 (2010)
ISSN
0091-2700
DOI
10.1177/0091270010361741
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
1165613
handle
http://hdl.handle.net/1854/LU-1165613
date created
2011-02-23 10:22:43
date last changed
2016-12-19 15:46:40
@article{1165613,
  abstract     = {Telcagepant is a novel, orally active, and selective calcitonin gene-related peptide receptor antagonist being developed for acute treatment of migraine with and without aura. Three separate clinical studies were conducted to evaluate the pharmacokinetics and tolerability of telcagepant following single oral doses in healthy young and elderly men and women and multiple oral doses in men. Telcagepant was rapidly absorbed with a time to maximum concentration of approximately 1.5 hours. The terminal half-life was approximately 6 hours. A greater than dose-proportional increase was observed in the area under the plasma concentration versus time curve from zero to infinity. Following twice-daily dosing, with each dose separated by 2 hours, steady state was achieved in approximately 3 to 4 days with an accumulation ratio of approximately 2. There were no clinically meaningful pharmacokinetic differences when compared across age and gender. Telcagepant was generally well tolerated up to single doses of 1200 mg and multiple doses of 400 mg twice daily.},
  author       = {Han, Tae H and Blanchard, Rebecca L and Palcza, John and McCrea, Jacqueline B and Laethem, Tine and Willson, Kenneth and Xu, Yang and Ermlich, Susan and Boyle, Janet and Lines, Christopher and Gutierrez, Maria and Van Bortel, Lucas and Xiao, Alan J and Sinclair, Simon and Hickey, Lisa and Panebianco, Deborah and Murphy, M Gail},
  issn         = {0091-2700},
  journal      = {JOURNAL OF CLINICAL PHARMACOLOGY},
  keyword      = {POTENT},
  language     = {eng},
  location     = {Washington, DC, USA},
  number       = {12},
  pages        = {1367--1376},
  title        = {Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene-related peptide receptor antagonist, in adults},
  url          = {http://dx.doi.org/10.1177/0091270010361741},
  volume       = {50},
  year         = {2010},
}

Chicago
Han, Tae H, Rebecca L Blanchard, John Palcza, Jacqueline B McCrea, Tine Laethem, Kenneth Willson, Yang Xu, et al. 2010. “Single- and Multiple-dose Pharmacokinetics and Tolerability of Telcagepant, an Oral Calcitonin Gene-related Peptide Receptor Antagonist, in Adults.” Journal of Clinical Pharmacology 50 (12): 1367–1376.
APA
Han, Tae H, Blanchard, R. L., Palcza, J., McCrea, J. B., Laethem, T., Willson, K., Xu, Y., et al. (2010). Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene-related peptide receptor antagonist, in adults. JOURNAL OF CLINICAL PHARMACOLOGY, 50(12), 1367–1376. Presented at the Annual Meeting of the American-Society-for-Clinical-Pharmacology-and-Therapeutics.
Vancouver
1.
Han TH, Blanchard RL, Palcza J, McCrea JB, Laethem T, Willson K, et al. Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene-related peptide receptor antagonist, in adults. JOURNAL OF CLINICAL PHARMACOLOGY. 2010;50(12):1367–76.
MLA
Han, Tae H, Rebecca L Blanchard, John Palcza, et al. “Single- and Multiple-dose Pharmacokinetics and Tolerability of Telcagepant, an Oral Calcitonin Gene-related Peptide Receptor Antagonist, in Adults.” JOURNAL OF CLINICAL PHARMACOLOGY 50.12 (2010): 1367–1376. Print.