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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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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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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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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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Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolite Tales Blog

Table 1: Small molecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.

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Metabolism of 2023 FDA Approved Small Molecules – PART 1

Metabolite Tales Blog

Metabolism of 2023 FDA Approved Small Molecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 small molecules out of a total of 55 new drugs [1]. References [1] 2023 Novel Small Molecule FDA Drug Approvals. Health Sci Rep. 6(10):e1610.

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. We hope it was a useful two-parter! We’re looking forward to the next crop! Br J Pharmacol.