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Metabolism of macrocyclic drugs

Metabolite Tales Blog

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]. Gangl et al.,

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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

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]. Gangl et al.,

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Breaking C-F bonds in drugs

Metabolite Tales Blog

In 2021, almost one third of FDA approved drugs contained at least one fluorine. Even newer from the pharma benches are 12 small molecule drugs highlighted by Chris de Savi [4], whose structures were first disclosed at the ACS and AACR meetings in Q1 2023. Of these 12 drugs, 9 contain at least one fluorine!

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