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Analyzing Oxygen Atom Distribution in FDA‐Approved Drugs to Enhance Drug Discovery Strategies

Chemical Biology and Drug Design

The study examines the frequency, distribution, prevalence, and diversity of oxygen atoms in a dataset of 2049 small molecules approved by the FDA and other agencies. The analysis focuses on various types of oxygen atoms, including sp 3 , sp 2 -hybridized, ring, and nonring.

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Shifting the ADC focus from antibody to payload

Drug Target Review

With an extensive background in small molecule chemistry, bioconjugation and protein science, these expert teams are leading efforts to place payload development at the centre of ADC innovation. The ADC itself is not necessarily a large molecule – it’s a small molecule with aspects of a large molecule, and vice versa.

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The future of CNS drug development: signs of real progress

Drug Target Review

2 A raft of emerging therapeutic modalities sits at the centre of this boom, spanning advanced biologics, engineered platforms and next-generation small molecules. This protective barrier prevents more than 98 percent of small-molecule drugs and all macromolecular therapeutics 3 from accessing the brain.

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PALAZESTRANT

New Drug Approvals

It is a small molecule with a dual mechanism of action, acting as both a complete estrogen receptor antagonist and a selective estrogen receptor degrader (SERD). Promising Results: Preliminary results from clinical trials have shown promising antitumor efficacy and favorable pharmacokinetic properties for palazestrant.

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The rising impact of biomarkers in early clinical development

Drug Target Review

Novel mechanisms of action associated with CGTs naturally create dosing effects that apply in very different ways than with traditional small molecule pharmacotherapies. Trial design and statistical methods are also key to determining the utility and validity of biomarkers.

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How GPCR agonists, including antibodies, are shaping the future of metabolic care

Drug Target Review

In addition to generating agonistic antibodies, Confo is also successfully applying the ConfoBody/ConfoChimer technology to drugging GPCR with small molecules. A suitable pharmacokinetics profile can be achieved with the addition of half-life extending moieties to the molecule.

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A spatial approach to understanding drug dynamics using mass spectrometry imaging

Drug Target Review

Unlike traditional pharmacokinetic (PK) studies that rely on plasma measurements alone, MSI, when combined with traditional histology, enables spatial mapping of drug distribution, metabolism and target engagement. For instance, Cheng et al.