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

Drug Target Review

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. A suitable pharmacokinetics profile can be achieved with the addition of half-life extending moieties to the molecule.

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The rising impact of biomarkers in early clinical development

Drug Target Review

For example, transcriptomic processes are showing the potential to identify and track failures in gene expression and gene regulation of amyloid and tau-related biomarkers, understood as precursors to the onset of Alzheimers disease (AD). Trial design and statistical methods are also key to determining the utility and validity of biomarkers.

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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. Dermavant’s tapinarof is one such friend. 8 This is not the only point of interest.

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Looking beyond traditional oncogenic pathways to break cancer resistance

Drug Target Review

BRAF and downstream mitogen-activated extracellular signal-regulated kinase (MEK) inhibitors are combined to treat BRAF-mutated melanoma, for example. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner.

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Aptorum Group Receives Clearance from Health Canada to Initiate a Phase 1 Clinical Trial for ALS-4, a Small Molecule Drug for Infections Caused by Staphylococcus aureus including Methicillin-resistant Staphylococcus aureus (MRSA)

The Pharma Data

The secondary objective is to assess the pharmacokinetic profile of SAD and MAD of ALS-4 administered orally to healthy subjects. This announcement is not a prospectus within the meaning of the Regulation (EU) n°2017/1129 of 14 June 2017 as amended by Regulations Delegated (EU) n°2019/980 of 14 March 2019 and n°2019/979 of 14 March 2019.

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Deconstructing the Diligence Process: An Approach to Vetting New Product Theses

LifeSciVC

For KLK5 and KLK7 as well as their endogenous regulator (LEKTI, encoded by SPINK5 ) and one of their substrates (filaggrin, FLG ) there is evidence that KLK5 and 7 up-regulation is pathogenic and down-regulation protective in epidermal barrier dysfunction (especially for Atopic Dermatitis). in liver, in CNS)?

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Aptorum Group Announces Submission of Clinical Trial Application for ALS-4, an Orally Administered Small Molecule Drug for the Treatment of Infections caused by Staphylococcus aureus including Methicillin-resistant Staphylococcus aureus (MRSA)

The Pharma Data

Pending Health Canada’s approval, the Phase 1 trial is designed to test the safety, tolerability and pharmacokinetics of ALS-4 in healthy volunteers. ALS-4 is a novel small molecule adopting an anti-virulence (non-antibiotic) approach to address the growing unmet medical needs of infections caused by Staphylococcus aureus.