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Simcyp Simulator aids in preclinical ADME assessment of Genentech compound
Date: 11 Nov 2009
A recent paper, by researchers at Genentech, describes the preclinical evaluation of the pharmacokinetic properties of GDC-0449, a potent selective Hedgehog signalling pathway inhibitor which is being developed for the treatment of various cancers. The study has been published in the journal Xenobiotica.
As part of the investigation, the Simcyp Simulator was used to predict the in vivo drug-drug interaction potential of GDC-0449 following in vitro studies with human liver microsomes. Using rosiglitazone and S-warfarin as probe substrates, simulations were performed to predict inhibition of CYP2C8 and CYP2C9 respectively. The simulation results indicate that GDC-0449 has a low potential for inhibition of these enzymes in vivo.
The paper, by H. Wong et al., is entitled ‘Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.’
Please click here for a link to the abstract and full text options.