Abstract:
:A new methodology based on Nuclear Magnetic Resonance (NMR) was developed to determine plasma protein binding (PPB) of drug candidates in drug discovery programs. A strong correlation was found between the attenuation of NMR signals of diverse drugs in the presence of different plasma concentrations and their fraction bound (fb) reported in the literature. Based on these results, a protocol for a rapid calculation of fb of small molecules was established. The advantage of using plasma instead of purified recombinant proteins and the possibility of pool analysis to increase throughput were also evaluated. This novel methodology proved to be very versatile, cost-effective, fast and suitable for automation. As a plus, it contemporarily provides a quality check and solubility of the compound.
journal_name
J Pharm Biomed Analjournal_title
Journal of pharmaceutical and biomedical analysisauthors
Gallo M,Matteucci S,Alaimo N,Pitti E,Orsale MV,Summa V,Cicero DO,Monteagudo Edoi
10.1016/j.jpba.2019.01.049subject
Has Abstractpub_date
2019-04-15 00:00:00pages
21-29eissn
0731-7085issn
1873-264Xpii
S0731-7085(18)32370-7journal_volume
167pub_type
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