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Open Targets Platform 25.06 has been released!

The Open Targets Blog

ESR1 is a known target for osteoporosis, with approved drugs such as Estradiol. Directionality annotations for pharmacogenetics data Pharmacogenetics widgets on the variant, target, and drug profile pages now have an additional Directionality column. Pharmacogenetics widget on the VKORC1 profile page.

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Inside The Altascientist: Understanding Drug Interaction Factors for Safer, More Effective Therapies

Alta Sciences

One of the most important factors to consider during the course of your early-phase clinical research is drug-drug interactions (DDIs), which occurs when one drug alters the effect of another, either by reducing its effectiveness or elevating systemic concentrations to potentially dangerous levelsultimately causing side effects.

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Challenges and Solutions to Drug-Drug Interactions for Clinical Development

DrugBank

Drug-drug interactions (DDI) are a significant concern in clinical trials, where the safe and effective administration of drugs to patients is crucial. These interactions can alter the pharmacological activity of one or more drugs, potentially leading to diminished therapeutic effects or unexpected toxic reactions.

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Integrating pharmacogenetics data: a new lens for target prioritisation

The Open Targets Blog

In December 2023, we introduced the pharmacogenetics widget in the Open Targets Platform, which brings in data from PharmGKB on the influence of genetic variation on drug responses. Different predicted functional consequences of pharmacogenetics variants from the PharmGKB data. What's new?

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Dysregulation of Human Hepatic Drug Transporters by Proinflammatory Cytokines [Metabolism, Transport, and Pharmacogenetics]

ASPET

Proinflammatory cytokines, elevated during inflammation caused by infection and/or autoimmune disorders, result in reduced clearance of drugs eliminated primarily by cytochrome P450 enzymes (CYPs). However, the effect of cytokines on hepatic drug transporter expression or activity has not been well-studied. or 1 ng/mL).

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Gene polymorphisms and drug-drug interactions determine the metabolic profile of blonanserin [Metabolism, Transport, and Pharmacogenetics]

ASPET

This study aimed to evaluate the effects of cytochrome P450 3A4 (CYP3A4) gene polymorphism and drug interaction on the metabolism of blonanserin. A microsomal enzyme reaction system was established, and drug-drug interactions were evaluated using Sprague-Dawley rats. Clearance of blonanserin by CYP3A4.4,

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Central Nervous System Distributional Kinetics of Selected Histone Deacetylase Inhibitors [Metabolism, Transport, and Pharmacogenetics]

ASPET

This lack of activity could be due to insufficient CNS exposure to the unbound drug. Although many HDACIs have shown potential in in vitro studies, they have had modest efficacy in vivo. Both compounds undergo in vitro degradation in mouse plasma, requiring precautions during sample processing.