Advanced search
1 file | 368.57 KB

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

(2010) JOURNAL OF CLINICAL PHARMACOLOGY. 50(12). p.1367-1376
Author
Organization
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.
Keywords
POTENT

Downloads

  • (...).pdf
    • full text
    • |
    • UGent only
    • |
    • PDF
    • |
    • 368.57 KB

Citation

Please use this url to cite or link to this publication:

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.
@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},
}

Altmetric
View in Altmetric
Web of Science
Times cited: