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Targeted modification of furan?2?carboxaldehydes into Michael acceptor analogs yielded long?acting hemoglobin modulators with dual antisickling activities

Chemical Biology and Drug Design

Abstract Sickle cell disease (SCD) is the most common genetic disorder, affecting millions of people worldwide. However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.

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The Data-Driven Future of Drug Development

DrugBank

For instance, Insilico Medicine , an AI-driven drug discovery company, has leveraged generative models to design novel molecules with desired properties, such as improved solubility and metabolic stability.    Moreover, data science designs novel drugs, such as antibody-drug conjugates (ADC) and bispecific antibodies.

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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. Can you provide a summary of the key findings and implications of the preclinical studies on ISM6331 for the treatment of advanced solid tumours?

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

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]. However, in the quest to tackle challenging disease targets with difficult drug binding sites, there is revived interest in developing this compound type to offer unique solutions.

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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

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]. However, in the quest to tackle challenging disease targets with difficult drug binding sites, there is revived interest in developing this compound type to offer unique solutions.

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N-glucuronidation: the human element

Metabolite Tales Blog

The pyrazole in a drug compound developed by LEO as an oral IL-17A protein-protein interaction modulator for the treatment of psoriasis and other inflammatory disorders is susceptible to N -glucuronidation. 22(5):803-11; [link] [10] Glucuronidation and UGT isozymes in bladder: new targets for the treatment of uroepithelial carcinomas?