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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

With 13 preclinical candidates and three AI-designed drugs currently undergoing clinical trials, Insilico is spearheading a revolution in cancer treatment and beyond. The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more.

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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]. Several metabolites were observed with an S -oxide and an acyl glucuronide being major human metabolites.

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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.