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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

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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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?

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Metabolism of five membered nitrogen containing heterocycles

Metabolite Tales Blog

9 The evidence here is that treatment with P450 inhibitors removed the toxic effects seen in the compounds of interest. 2013, 41, 508-517 [link] 21 J. 44, 797–814 [link] Take a look at our other blogs The post Metabolism of five membered nitrogen containing heterocycles appeared first on Hypha Discovery.