Chemical Biology and Drug Design

SEPTEMBER 20, 2023

Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. CaCO-2 cell transwell assay was employed for transport evaluation, and the metabolic stability of luteolin and CYP3A activity were assessed in rat liver microsomes.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Regulations Research 100

Chemical Biology and Drug Design

JUNE 8, 2023

The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. The Caco-2 cells were employed to evaluate the transport of cryptotanshinone, and the metabolic stability was studied in the rat liver microsomes.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Research 100

Chemical Biology and Drug Design

OCTOBER 5, 2023

However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.

Metabolic Stability 100

Metabolic Stability Treatment Disease Research 100

DrugBank

OCTOBER 17, 2024

By utilizing high-resolution protein structures obtained through X-ray crystallography, researchers could design small molecules that potently inhibit the SARS-CoV-2 main protease, a key enzyme essential for viral replication.   Moreover, data science designs novel drugs, such as antibody-drug conjugates (ADC) and bispecific antibodies.

Drug Development 98

Drug Development Metabolic Stability Clinical Trials Drugs 98

Drug Target Review

JUNE 12, 2023

Leveraging AI-guided structure-based drug design, Insilico’s research and development team generated an impressive portfolio of over 6,000 molecules and identified three highly promising hit series. He is an adjunct professor of artificial intelligence at the Buck Institute for Research on Aging.

Metabolic Stability 92

Metabolic Stability Clinical Trials Small Molecule Pharmacokinetics 92

Drug Target Review

SEPTEMBER 20, 2023

Complex challenges such as metabolic stability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. Research and Development in the Pharmaceutical Industry | Congressional Budget Office [Internet].

Drugs 105

Drugs Metabolic Stability Computational Chemistry Pharmaceuticals 105

Metabolite Tales Blog

DECEMBER 13, 2023

To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolic stability, but also resulted in increased potency of the final lead compound. Figure 4: Optimisation of an IDO1 inhibitor incorporating installation of a gem-dimethyl group to control glucuronidation of a key hydroxyl group.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Drugs 59