Drug Target Review

JUNE 12, 2023

The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more. 2021 – and a robust pipeline that includes 3 AI-designed drugs (for IPF, COVID-19 and cancer) currently in clinical trials.

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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. Drug discovery today , 26(1), 80–93 (2021). Congressional Budget Office. Available from: [link] Schneider G.

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Drugs Metabolic Stability Computational Chemistry Pharmaceuticals 105

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]. Gangl et al.,

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]. Gangl et al.,

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

MAY 12, 2023

In 2021, almost one third of FDA approved drugs contained at least one fluorine. This was surprising given that replacement of a phenyl with a pyrimidine and fluorination of aryl or heteroaryl rings are techniques often used to increase metabolic stability. Molecules 2021, 26, 1160. Angew Chem Int Ed Engl. Soloshonok.

Drugs 52

Drugs Small Molecule FDA Approval Metabolic Stability 52

Metabolite Tales Blog

APRIL 4, 2023

Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolic stability. 2021 Apr;84(4):1059-1067. Xenobiotica, 49:6, 718-733, [link] [7] FDA Prescribing information for CAMZYOS® (mavacamten) [link] [8] Bissonnette et al., J Am Acad Dermatol.

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Small Molecule FDA Approval FDA Drugs 52

Drug Target Review

JANUARY 16, 2025

Angewandte Chemie , 133(15):84668471, 2021. Cyclic Peptide Design, Chapter 2: Strategies to Enhance Metabolic Stabilities. Accounts of Chemical Research , 54(18):36043617, 2021. Journal of Medicinal Chemistry , 64(6):32823298, 2021. Costa L, Sousa E, Fernandes C. Pharmaceuticals , 16(7):996, 2023. Springer, 2019.

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Drug Development Small Molecule Drugs FDA Approval 52