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Metabolism of macrocyclic drugs

Metabolite Tales Blog

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]. Balazs et al.,

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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

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]. Balazs et al.,

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolic stability. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer. Journal of Medicinal Chemistry 63 (13), 6679-6693.