Pharmacokinetics of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors: The role of alpha-1-acid glycoprotein binding Academic Article uri icon

Overview

MeSH Major

  • Anilides
  • Hedgehog Proteins
  • Neoplasms
  • Pyridines
  • Signal Transduction

abstract

  • GDC-0449 levels strongly correlated with AAG levels, showing parallel fluctuations of AAG and total drug over time and consistently low, unbound drug levels, different from previously reported AAG-binding drugs. This PK profile is due to high-affinity, reversible binding to AAG and binding to albumin, in addition to solubility-limited absorption and slow metabolic elimination properties.

publication date

  • April 15, 2011

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3703823

Digital Object Identifier (DOI)

  • 10.1158/1078-0432.CCR-10-2736

PubMed ID

  • 21300760

Additional Document Info

start page

  • 2512

end page

  • 20

volume

  • 17

number

  • 8