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Dear all,
in addition to the microsomal stability discussion I would like to ask
if anyone is using the microsomal instability as an exclusive no-go
criterium in further development of drugs ( in the lead Opt stage)?
Or would you rather validate further with a hepatozyte read out? Is
there any data available where microsomal stability is correlated with
the outcome in in vivo data?
Many thanks for your help
Matthias
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Dear Matthias
You may find the following papers useful.
Howgate EM, Rowland Yeo K, Proctor NJ, Tucker GT and Rostami-
Hodjegan A (2006) Prediction of in vivo drug clearance from in vitro
data. I: impact of inter-individual variability. Xenobiotica 36:473-497.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16769646
Inoue S, Howgate EM, Rowland-Yeo K, Shimada T, Yamazaki H, Tucker GT
and Rostami-Hodjegan A (2006) Prediction of in vivo drug clearance
from in vitro data. II: potential inter-ethnic differences.
Xenobiotica 36:499-513.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16865818
Shiran MR, Proctor NJ, Howgate EM, Rowland-Yeo K, Tucker GT and
Rostami-Hodjegan A (2006) Prediction of metabolic drug clearance in
humans: in vitro-in vivo extrapolation vs allometric scaling.
Xenobiotica 36:567-580.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16864504
Regards
Masoud
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