Metabolite Tales Blog

JULY 5, 2023

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. 20 (March 20, 2014).

Drugs 52

Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. 20 (March 20, 2014).

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Metabolic Stability Drugs FDA Approval Treatment 52

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. Paine and Aleksandra Galetin (2014). Drug Metabolism and Disposition 42 (4) 650-664; [link]. [2] Polli, Mary F.

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Small Molecule Metabolic Stability Treatment Drugs 59

Molecular Design

MAY 11, 2019

Design decisions in lead optimization are typically supported by assays for a range of properties such as solubility, permeability, metabolic stability and off-target activity as well as pharmacokinetic studies.

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Metabolic Stability Pharmacokinetics Pharmaceuticals Drugs 52

Drug Target Review

JANUARY 16, 2025

Nature Chemical Biology , 10(9):696698, 2014. Cyclic Peptide Design, Chapter 2: Strategies to Enhance Metabolic Stabilities. Macrocycles as protein-protein interaction inhibitors. Biochemical Journal , 474(7):11091125, 2017. Tools and rules for macrocycles. Jain AN, Brueckner AC, Jorge C, et al. Springer, 2019.

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Drug Development Small Molecule Drugs FDA Approval 52