Remove 2022 Remove Clinical Development Remove Metabolic Stability Remove Trials
article thumbnail

Metabolism of macrocyclic drugs

Metabolite Tales Blog

Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. CYP3A4 is involved in clearance to two major metabolites M1 and M2, representing 9.6% Chen et al.,

article thumbnail

Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Still, of the 34 macrocycles currently in clinical trials, only 18% are de novo designed. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Several metabolites were observed with an S -oxide and an acyl glucuronide being major human metabolites.