Metabolite Tales Blog

JULY 5, 2023

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].

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

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]. Previously natural products have provided the source of 80-90% of macrocyclic drugs, not surprising given that 20% of natural product derived ring systems are macrocyclic.

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

DECEMBER 13, 2023

N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Glucuronidation is the most common phase II reaction observed in the metabolism of drugs in humans.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59

Molecular Design

MAY 11, 2019

While the Ro5 article highlighted molecular size and lipophilicity as pharmaceutical risk factors, the rule itself is actually of limited utility as a drug design tool. back in 2015 and you may find this review of that seminal contribution to the drug design literature to be informative.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Pharmaceuticals Drugs 52