2022 FDA Approval Metabolic Stability 
Metabolite Tales Blog
JULY 5, 2023
Metabolism of de novo-designed macrocyclic drugs approved by the FDA By Julia Shanu-Wilson To date, only 4% (67) of FDA approved drugs are macrocycles [1]. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Chen et al.,
Metabolite Tales Blog
JULY 5, 2023
Metabolism of de novo-designed macrocyclic drugs approved by the FDA By Julia Shanu-Wilson To date, only 4% (67) of FDA approved drugs are macrocycles [1]. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Chen et al.,
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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. 2022), JBMR Plus, 6: e10557. ACS Med Chem Lett.
Metabolite Tales Blog
APRIL 4, 2023
Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Drug metabolism in drug discovery and development.
Practical Cheminformatics
AUGUST 3, 2023
In a 2022 review by Haddad of the CNS penetration of antibiotics, the percentage of Ceftriaxone in CSF relative to plasma varied between 0.5 Clintox – This dataset consists of 1483 SMILES strings and two binary labels indicating whether a molecule is an FDA-approved drug and whether a toxicity outcome has been reported.
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