Cost-efficient high throughput screen for in vitro prediction of phospholipidosis and comprehensive, real physicochemical profiling
Kibron PLDscreen - outperforming cell based assays
Poor ADME/Tox properties are the major reason for the failure of NCEs in pharmaceutical R&D. This can be extremely costly, in particular, if adverse effects such as induction of phospholipidosis or serious CNS side effects manifest just in clinical trials. Accordingly, there is an increasing pressure to screen compound libraries and NCEs for their ADME/Tox properties in vitro, preferably already before lead optimization.
Kibron PLDscreen is a biophysical screen for the prediction of the ability of compounds to induce phospholipidosis. PLDscreen yields an accuracy corresponding to in vivo data, a high throughput with minimal compound volumes, providing a fast, reliable and cost-efficient screening of drug-phospholipid complex formation. The Kibron PLDscreen enables recognition of potentially problematic compounds in the lead optimization and diminishes the need for animal tests.
Understanding QSAR for BBB permeation and FA: taking your research beyond PAMPA, logP and PSA
One of the key tasks in ADME research is to identify compounds that will pass passively through the plasma membrane surrounding cells, such as functioning in the Blood-Brain-Barrier (BBB) and in the intestinal mucosa. In addition to revealing potential PLD causing compounds, Kibron PLDscreen delivers comprehensive physicochemical profiles of compounds, by providing the parameters Kaw (lipophilicity), TSA (true surface area), CMC (critical micelle concentration) and pKa (surface ionization constant), further correlating with ADME properties such as Blood-Brain-Barrier (BBB) permeation. Importantly, the siginificance of these parameters to QSAR far outperforms the data obtained by artificial membranes (PAMPA), logP and PSA in predicting BBB permeation, for instance. Further, unlike PAMPA, the data are reproducible and comprehensive, definitely taking your compound design to a whole new level. Importantly, PLDscreen improves and speeds up your R&D, while also bringing significant savings in cost. Please contact us for further details and literature.
