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Metabolism of macrocyclic drugs

Metabolite Tales Blog

With metabolic stability in mind, we take a look at the metabolism of some FDA approved synthetic macrocyclic drugs, and a few of those that were/are in clinical development where metabolism data was available. A combination therapy of glecaprevir and pibrentasvir has recently been implicated in a case of liver injury.

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

With metabolic stability in mind, we take a look at the metabolism of some FDA approved synthetic macrocyclic drugs, and a few of those that were/are in clinical development where metabolism data was available. A combination therapy of glecaprevir and pibrentasvir has recently been implicated in a case of liver injury.

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ATICAPRANT

New Drug Approvals

2] As of July 2022, it is in phase 3 clinical trials for major depressive disorder. [2] 2] Like other kappa opioid antagonists currently under clinical investigation for the treatment of major depression, its efficacy may be compromised by the countervailing activation of pro-inflammatory cytokines in microglia within the CNS. [7]

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Acoramidis

New Drug Approvals

2013 Jun 11;110(24):9992-7. Epub 2013 May 28 PATENT [link] Chemical Synthesis Methyl 3-(3-bromopropoxy)-4-fluorobenzoate (Compound 2) To a solution of methyl 4-fluoro-3-hydroxybenzoate 1 (3.0 June 2013). New Drug Therapy Approvals 2024 (PDF). June 2013). It is taken by mouth. [1] Proc Natl Acad Sci U S A.