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Der Pharmacia Sinica
ISSN: 0976-8688
Eurosc i con Conference on
Medicinal Chemistry
and Biosimilars
M a r c h 2 5 - 2 6 , 2 0 1 9
B u d a p e s t , H u n g a r y
Medicinal Chemistry & Biosimilars 2019
Biomimetic HPLC stationary phases such as immobilized artificial
membrane (IAM), human serum albumin (Chiral-HSA) and α-1-glycoprotein
(Chiral-AgP) are able to mimic the in vivo interactions of the drug molecules to
lipids and proteins. The calibrated retention times obtained on the biomimetic
HPLC stationary phases can be used to build models for in vivo tissue-
plasma partition, unbound volume of distribution, drug efficiency, and cellular
concentration without using animal experiments. The measurements can be
fully automated and large number of compounds can be ranked for further
studies for the fraction of the cost of in vivo experiments. The methodology can
be applied for new modalities in drug discovery such as peptides that would
be difficult to characterize by traditional methods such as equilibrium dialysis
to estimate their tissue binding and volume of distribution. Comparison of IAM
partition and membrane disruption of antibiotic peptides has been investigated
in order to predict their interactions with lipids. The chromatographic retention
of potential drug molecules on biomimetic stationary phases can mimic their
in vivo binding to lipids and proteins that was validated using human clinical
data of over 150 known drug molecules.
Biography
KlaraValkohascompletedhisPhDfromSemmelweisUniversity
and Postdoctoral studies from Yale University, CT, USA. After
working at GSK for 22 years, currenty, she is the Director of
Bio-Mimetic Chromatography Ltd, providing consultations and
measurement services for biotech companies involved in drug
discovery. She is also an Honorary Professor at UCL School of
Pharmacy where she teaches the Physchem/ADMEmodule for
Drug Discovery and Pharma Management master course. She
has published more than 100 papers in reputed journals and
has been serving as an Editorial Board Member of ADMET &
DMPK journal. She is a Fellow of the Royal Society of Chemistry.
Biomimetic HPLC property measurements to estimate human
in vivodistribution and tissue binding of drug discovery
compounds
Klara Valko1,2
1Bio-Mimetic Chromatography Ltd, UK
2UCL School of Pharmacy, UK
Klara Valko, Der Pharmacia Sinica 2019, Volume:10
DOI: 10.21767/0976-8688-C1-002