Articles tagged with Pharmacokinetics
A recent NIH-funded study reveals that oral small-molecule GLP-1 drugs can suppress eating for pleasure and reduce cravings by targeting a deeper brain region, potentially treating other dysfunctions in reward processing. The findings provide insight into the neural mechanisms underlying the effects of these medications.
The Phase I MYTHIC trial demonstrated a strong synergy between zedoresertib and lunresertib, showing durable regressions and consistent tumor shrinkage in patients with ovarian cancer. The combination achieved an overall disease control rate of 68.5% and a molecular response rate of 47%.
Scientists at the University of Virginia Health System have developed a suite of AI-powered tools, called YuelDesign, YuelPocket and YuelBond, to transform how new drugs are created. These tools can design drug molecules tailored to fit their protein targets exactly, even accounting for protein flexibility.
Acute sepsis alters fluid kinetics and creates a 'third space' resistant to adrenergic modulation, leading to maldistribution of crystalloid fluid. Vasoactive drugs have limited effect on fluid distribution in septic sheep compared to healthy animals.
Astrocytic glutamine synthetase plays a key role in regulating glutamate signaling, contributing to nicotine-induced brain changes and locomotor sensitization. A custom-designed peptide inhibits this process, demonstrating the importance of astrocyte communication in nicotine addiction.
A team at the University of Pennsylvania has solved the mechanism of action of hydralazine, revealing its potential to halt the growth of brain cancer cells. By blocking an oxygen-sensing enzyme, hydralazine can reduce intracellular calcium levels, causing blood vessels to relax and tumor cells to enter a dormant state.
Researchers developed nanomachines that can function stably within living organisms, enabling starvation therapy to treat refractory pancreatic cancer. This approach improved treatment outcomes by depleting essential nutrients for cancer cell growth.
A large international clinical trial found that elinzanetant significantly reduces hot flashes and night sweats in postmenopausal women by over 73%. The drug also shows secondary benefits such as improved quality of life and reduced sleep disturbances, with no harmful effects on the liver or bone density.
Ibezapolstat, a new antibiotic, has been shown to be effective in treating Clostridioides difficile (C. diff) infections with high rates of sustained clinical cures. The study found that ibezapolstat killed harmful bacteria without harming the good bacteria in the gut, which helps prevent recurrent C. diff infections.
A new U-M study found that xylazine does not amplify the decrease in breathing rate caused by fentanyl use, but reduces heart rate more than fentanyl. This reduction in heart rate may be a more important driver of increased overdose risk, highlighting the need for further research into polysubstance use involving opioids.
Researchers found that certain antibodies can reduce antitumor immune cells, highlighting the need to consider ADCC activity when designing or selecting ICI therapeutics. This study could help improve cancer treatment by engineering antibodies that avoid damaging essential immune cells.
A new study found that new psychoactive substances (NPS) are a significant concern in roadway crashes in California. NPS, also known as ‘designer drugs’, were detected in the blood of 17 patients, with most frequent being designer benzodiazepines and fentanyl analogs.
Researchers at the University of Zurich have developed a technology to test 25 antibodies simultaneously in a single mouse, greatly reducing the number of laboratory animals required. The method uses protein fragments as barcodes for analysis, allowing for high-quality preclinical data on multiple antibody candidates.
The article discusses the need for bioanalytical assays to measure immune responses to oligonucleotide therapeutic drugs, especially when they include carriers or conjugates. Highly specific antibodies may enhance the development and production of ONTs, expanding studies on their safety and efficacy.
The study identified 105 compounds in Shenqi Fuzheng extract, with organic acids and amino acids showing higher concentrations in the bloodstream. Compounds such as Astragalosides promptly enter the bloodstream within 5 minutes after administration.
This study compares the pharmacokinetics of aumolertinib, osimertinib, and gefitinib in mouse models and NSCLC patients. Aumolertinib exhibits better pharmacokinetic profiles, with higher concentrations in plasma and tissues, making it a promising candidate for EGFR mutation-positive NSCLC treatment.
A new study provides first-of-its-kind data on the pharmacokinetics and safety of intravenous remdesivir in treating SARS-CoV-2 coronavirus in pregnant women. The research reveals that no dose adjustments are necessary for remdesivir when used in pregnant women, with no safety concerns or adverse pregnancy outcomes identified.
Researchers have developed a novel solubilizer for olaparib, a selective PARP inhibitor, using π-π-stacked poly (ɛ-caprolactone)-based micelles. The studies found that these micelles improved the solubility of olaparib and exhibited sustained release behavior in vitro.
Researchers at Xi'an Jiaotong-Liverpool University developed a new method that enables the efficient production of cysteine-rich peptides and microproteins in their naturally folded 3D structure. The approach uses organic solvents to mimic nature's oxidative folding process, resulting in speeds of over 100,000 times faster than aqueous...
A study of 104 patients found that 83.5% had divergent phenotypes, with a significant increase in CYP2D6 poor metabolizers due to phenoconversion. The results highlight the importance of pharmacogenetic testing and personalized treatment approaches in psychiatric care.
A multidisciplinary team created a new algorithm to provide optimal personalized treatment options for individuals with esophageal cancer. The framework uses various heterogeneous factors that facilitate the progression of the disease and demonstrated high accuracy in controlling esophageal cancer.
Researchers at IISc have developed a novel method to improve pharmacokinetic properties of macrocyclic peptides, which are used in pharmaceutical industries worldwide. By substituting oxygen with sulphur in the backbone of these peptides, they increase resistance to digestive enzymes and lipophilicity, thereby boosting bioavailability.
A team of Chinese and UK researchers has identified superoxide dismutase 1 (SOD1) as a potential target for reversing drug resistance in ovarian cancer. By using nanoparticles to deliver siRNA that reduces SOD1 levels, the study showed reduced growth and decreased resistance to cisplatin in female mice.
Scientists have developed a new method to deliver genetic information to stem cells using nanoparticles coated with a specific polymer, enabling more efficient control over cellular differentiation. This innovation has the potential to improve the efficiency and effectiveness of regenerative medicine treatments.
Research finds diclofenac's high variability in metabolism due to UGT2B17, a little-studied enzyme. The study suggests genetic testing and dose adjustments for specific populations can help minimize side effects.
Researchers found a partial response in a patient with pancreatic acinar cell carcinoma, as well as stable disease in 11 patients, when combining riluzole with sorafenib in a phase I trial. The combination was safe and tolerable, and further exploration of its potential is warranted.
Researchers at Rice University have created a new technology called PULSED that can deliver time-released drugs and vaccines for extended periods. The technology uses high-resolution 3D printing and soft lithography to produce microcylinders made of biodegradable polymers, which can be loaded with drugs and release them over time.
Pharmacokinetic analysis reveals Omomyc's lasting anti-cancer effects, with structural integrity persisting in tumor tissue for at least 72 hours. This finding is significant for clinical trials evaluating Omomyc as a MYC inhibitor.
A new antimalarial drug, tafenoquine, is found to require a higher dose of 450mg to achieve cure rates of 85% compared to the current 300mg dose of 70%. The study suggests that the single-dose tafenoquine is not as effective as optimal primaquine treatment in preventing vivax malaria relapses in all endemic regions.
Researchers propose a temporo-spatial pharmacometabolomics method based on ambient mass spectrometry imaging to evaluate the microregional effect of olanzapine on brain tissue, demonstrating its effectiveness in characterizing pharmacokinetics and pharmacodynamics. The method accurately illustrates levels dynamics and microregional dis...
Researchers developed a mathematical model to predict the efficiency of nanoparticle delivery into cells, particularly in stem cells. They found that nanoparticles become trapped in bubble-like vesicles, preventing them from reaching their targets.
A new study found that Black kidney transplant recipients exhibit a faster clearance rate of tacrolimus, an immunosuppressive drug. The study suggests that considering both sex and race when dosing tacrolimus may reduce adverse effects and enhance transplant outcomes.
A new animal study suggests that combining marijuana compounds like CBD and THC with opioids may not increase the risk of addiction. The research found that these compounds do not enhance the rewarding effects of opioids, which could lead to a lowered risk of addiction or physical dependence.
Researchers at NTU Singapore have developed a new method to generate sulphur pharmacophores, which are crucial for drug discovery. The method uses a catalyst called pentanidium and can produce multiple variations of pharmacophores, making the process more efficient and fruitful.
Researchers at Tokyo University of Science have developed bionanoparticles derived from corn that selectively target and inhibit the growth of cancer cells, inducing tumor necrosis factor-α release. These findings suggest a novel, economical, and safe anti-cancer therapy approach.
A comprehensive study investigates the metabolism of four drugs in rabbit eyes, revealing different enzyme profiles from liver metabolism. The findings provide valuable information for advancing ophthalmic drug development.
New research suggests that cannabis use can lead to harmful drug-drug interactions by interfering with two families of enzymes that metabolize a wide range of drugs. This could result in unintended side effects such as toxicity or accidental overdose, particularly for older individuals using medications.
A study found that microgravity significantly impacts P-glycoprotein expression and function in rats, with higher levels of P-gp expression in long-term microgravity exposure. The researchers identified 26 proteins interacting with P-gp, which regulated ATP hydrolysis-coupled transmembrane transport and other functions.
Researchers discovered novel diarylamides with excellent in vitro UT inhibitory activity, leading to the identification of a promising preclinical candidate. Oral administration of the compound showed a superior diuretic effect in vivo without causing electrolyte imbalance or toxicity.
A phase 1b study and a phase 2 proof of concept study have generated positive results for SNF472, demonstrating a linear pharmacokinetic behavior and improved safety profile. A randomized, placebo-controlled phase 2b study is evaluating the effect of SNF472 on cardiovascular calcification over 1 year in haemodialysis patients.
This article reviews the impact of pyridine modifications on tubulin inhibitors, highlighting improved binding modes and activity. The study identifies new insights into tubulin targeting and future perspectives for site-specific agents.
A new study by University of South Florida researchers found that lithium salicylate produced steady blood and brain lithium levels for up to 48 hours after oral dose, reducing the risk of toxicity associated with current lithium therapy. This could lead to a less frequent dosing regimen and fewer side effects.
The European Journal of Drug Metabolism and Pharmacokinetics will be published by Springer starting in 2010, covering aspects of drug delivery and bioavailability. The journal focuses on pharmacokinetics, drug metabolism, and drug development, publishing original articles and conference proceedings.
A study published in BMC Medicine found that standard doses of Rifampin, a first-line antituberculosis drug, result in low serum concentrations in children. The researchers suggest increasing the dose to 10-20mg/kg may be more effective. This could lead to increased treatment duration and risk of relapse in severe forms of tuberculosis.
The study shows that Perforomist Inhalation Solution delivers bronchodilation comparable to DPI delivery and has similar linear kinetics and excreted drug levels. This offers an effective, long-term treatment option for patients with COPD who may have difficulty coordinating other devices.
A study found that daily use of ginseng or ginkgo biloba supplements, or their combination, do not significantly alter the pharmacokinetics of most prescription drugs. Researchers tested 72 healthy adults with a cocktail of five drugs and found no differences in absorption or metabolism regardless of supplement use.
A Phase IV study found that Kadian's extended-release mechanism is maintained even in the presence of significant amounts of alcohol. The concomitant use of tested levels of alcohol with Kadian has no significant impact on morphine blood levels or release timing.
Researchers found that high doses of acetaminophen (up to 8g/day) were quickly eliminated from the bloodstream, with no accumulation or liver damage. The study's findings suggest that consumers can safely take higher doses than recommended, but emphasize the importance of adhering to the standard daily limit.
The Lancet's editor urges caution on expanding nurse prescribing rights in the UK, citing concerns over inadequate training and potential risks to patient care. The government's plan to extend prescribing powers to all nurses is criticized for its haste and lack of regard for nursing professional boundaries.