[HTML][HTML] Fundamental aspects of DMPK optimization of targeted protein degraders
C Cantrill, P Chaturvedi, C Rynn, JP Schaffland… - Drug discovery today, 2020 - Elsevier
Highlights•Degraders are an emerging modality which fall into the 'beyond rule of
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …
Targeted protein degradation: advances, challenges, and prospects for computational methods
The therapeutic approach of targeted protein degradation (TPD) is gaining momentum due
to its potentially superior effects compared with protein inhibition. Recent advancements in …
to its potentially superior effects compared with protein inhibition. Recent advancements in …
Formulation of 3D printed tablet for rapid drug release by fused deposition modeling: screening polymers for drug release, drug-polymer miscibility and printability
The primary aim of this study was to identify pharmaceutically acceptable amorphous
polymers for producing 3D printed tablets of a model drug, haloperidol, for rapid release by …
polymers for producing 3D printed tablets of a model drug, haloperidol, for rapid release by …
[HTML][HTML] Discovery solubility measurement and assessment of small molecules with drug development in mind
JA Barrett, W Yang, SM Skolnik, LM Belliveau… - Drug discovery today, 2022 - Elsevier
Highlights•Seamless solubility understanding requires discovery-development
collaboration.•Gold standard methods in drug development map solubility of drug …
collaboration.•Gold standard methods in drug development map solubility of drug …
A review of methods for solubility determination in biopharmaceutical drug characterization
A Veseli, S Žakelj, A Kristl - Drug development and industrial …, 2019 - Taylor & Francis
The significance of thermodynamic solubility in biopharmaceutical compound or drug
characterization as well as the importance of having methods that accurately establish it …
characterization as well as the importance of having methods that accurately establish it …
Findings of the second challenge to predict aqueous solubility
Ten years ago, we issued an open prediction challenge to the cheminformatics community:
would participants be able to predict the equilibrium intrinsic solubilities of 32 druglike …
would participants be able to predict the equilibrium intrinsic solubilities of 32 druglike …
[HTML][HTML] Challenges and strategies for solubility measurements and dissolution method development for amorphous solid dispersion formulations
A Hermans, J Milsmann, H Li, C Jede, A Moir, B Hens… - The AAPS Journal, 2022 - Springer
This manuscript represents the view of the Dissolution Working Group of the IQ Consortium
on the challenges of and recommendations on solubility measurements and development of …
on the challenges of and recommendations on solubility measurements and development of …
[HTML][HTML] An integrated high-throughput robotic platform and active learning approach for accelerated discovery of optimal electrolyte formulations
Solubility of redox-active molecules is an important determining factor of the energy density
in redox flow batteries. However, the advancement of electrolyte materials discovery has …
in redox flow batteries. However, the advancement of electrolyte materials discovery has …
Novel hydrate and anhydrate cocrystals/salts of norfloxacin and their physicochemical properties
The low solubility and low permeability of Biopharmaceutics Classification System BCS
class IV antibiotic drug norfloxacin (NORF) were studied for improvement of …
class IV antibiotic drug norfloxacin (NORF) were studied for improvement of …
Solubility challenge revisited after ten years, with multilab shake-flask data, using tight (SD∼ 0.17 log) and loose (SD∼ 0.62 log) test sets
Ten years ago we issued, in conjunction with the Journal of Chemical Information and
Modeling, an open prediction challenge to the cheminformatics community. Would they be …
Modeling, an open prediction challenge to the cheminformatics community. Would they be …