This site uses cookies to improve your experience. To help us insure we adhere to various privacy regulations, please select your country/region of residence. If you do not select a country, we will assume you are from the United States. Select your Cookie Settings or view our Privacy Policy and Terms of Use.
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Used for the proper function of the website
Used for monitoring website traffic and interactions
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Strictly Necessary: Used for the proper function of the website
Performance/Analytics: Used for monitoring website traffic and interactions
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.
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.
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.
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?
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).
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,
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.
This lack of translation between in vitro metabolism assays and in vivo disposition can confound drug development. This suggests that the inter-strain difference in enzymatic activity did not affect the in vivo pharmacokinetic behavior of panobinostat and its CNS distribution in mice.
The team identified 370 priority drug targets for 27 cancer types in a truly data-driven approach, leveraging clinical-relevant transcriptional signatures, metabolic and proteomics data, protein-protein interaction networks and more. In addition, we now indicate whether a target is a direct target of the drug. DOI: 10.1016/j.ccell.2023.12.016
Organic anions (OA) are compounds including drugs or toxicants that are negatively charged at physiological pH and are typically transported by Organic Anion Transporters (OATs). For the profile of OTA inhibition by OAs, IC 50 values were determined for several clinically important drugs and toxicants. pmol/cm 2 , respectively.
Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few FDA-approved drugs that exhibit atropisomerism. The volume of distribution was moderate in nonclinical species and consistent with the tissue distribution observed by whole body autoradiography in rats.
GBM has a poor prognosis despite aggressive treatment, in part due to lack of adequate drug permeability at the BBB. CNS distribution of elimusertib is partially limited by P-gp efflux at the BBB, and high binding to CNS tissues leads to low levels of pharmacologically active (unbound) drug in the brain.
A first pharmacological phenotyping with the OATP2B1 substrate-drug atorvastatin revealed reduced hepatic content and increased expression of rCYP3A1 in the humanized animals. In order to assess the in vivo relevance of the transporter, we applied SLCO2B1 +/+ knock-in and Slco2b1 -/- knock-out rats.
First, we assessed the substrate potential of riboflavin towards other major drug transporters using established transfected cell systems. Overall, these data indicate that plasma riboflavin is a promising biomarker of BCRP that may offer a possibility to assess drug candidate as a BCRP modulator in early drug development.
Target prioritisation A major new feature of this release is the Target Prioritisation view, which provides an assessment of target-specific properties of interest when evaluating the suitability of a target for a drug discovery programme. It is presented here with an additional layer of analysis with a drug discovery focus.
Results highlight the potential interplay between time-dependent and reversible inhibition of intestinal CYP3A as the mechanism underlying natural product-drug interactions, even after acute exposure to the precipitant.
Quantitative pharmacokinetic models should therefore focus on OCT2/MATE when describing serum creatinine and creatinine clearance modulation by inhibitor drugs and genotype- or disease-related activity changes.
Food and Drug Administration (FDA). SAN DIEGO , Oct. Clinical laboratories can process thousands of samples each day for less than $10 per sample running the assay on a single MassARRAY instrument, making it one of the highest throughput SARS-CoV-2 tests available under the Emergency Use Authorization program. SOURCE Agena Bioscience.
Efficacy of radiosensitizers for brain tumors may be influenced by a lack of effective drug delivery across the blood-brain barrier (BBB). Ataxia telangiectasia mutated (ATM) kinase is a key regulator of DSB repair, and ATM inhibitors are being explored as radiosensitizers for various tumors, including primary and metastatic brain tumors.
Over the last 10 years, Open Targets has shared foundational data and resources to enhance our collective ability to identify and prioritise therapeutic drug targets. One of our strategic themes has been to democratise access to the scattered human genetics evidence in a way that can inform the selection of safe and effective drug targets.
The Platform now has 6 entities: Target, Disease, Drug, Credible set, Variant, and Study. Credible sets, drugs, and other data sources contribute evidence of target-disease associations. This includes L2G, rare disease clinical annotations, and pharmacogenetics annotations. The Open Targets data model.
We organize all of the trending information in your field so you don't have to. Join 15,000+ users and stay up to date on the latest articles your peers are reading.
You know about us, now we want to get to know you!
Let's personalize your content
Let's get even more personalized
We recognize your account from another site in our network, please click 'Send Email' below to continue with verifying your account and setting a password.
Let's personalize your content