Assessing the risk of drug crystallization in vivo

Assessing the risk of drug crystallization in vivo

Low intrinsic solubility leading to poor oral bioavailability is a common challenge in drug discovery that can often be overcome by formulation strategies, however, it remains a potential limitation that can pose challenges for early risk assessment and represent a significant obstacle to drug devel...

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Veröffentlicht in:Journal of pharmacological and toxicological methods 2019-03, Vol.96, p.1-8
Hauptverfasser: Ruepp, Stefan, Janovitz, Evan, Brodie, Thomas, White, Randy, Santella, Joseph, Hynes, John, Carman, Julie, Pan, Duohai, Wu, Yang, Hanumegowda, Umesh, Gemzik, Brian, Megill, John, DiPiero, Janet, Drexler, Dieter, Su, Ching-Chiang, Hageman, Michael
Format: Artikel
Sprache:eng
Schlagworte:
Birefringent crystal
Granulomatous inflammation
IRAK4
Methods
Microscopy
Raman spectroscopy
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Zusammenfassung:Low intrinsic solubility leading to poor oral bioavailability is a common challenge in drug discovery that can often be overcome by formulation strategies, however, it remains a potential limitation that can pose challenges for early risk assessment and represent a significant obstacle to drug development. We identified a selective inhibitor (BMS-986126) of the IL-1 receptor–associated kinase 4 (IRAK4) with favorable properties as a lead candidate, but with unusually low intrinsic solubility of
ISSN:1056-8719
1873-488X
DOI:10.1016/j.vascn.2018.12.003