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About 15,075 results

Translation of liver stage activity of M5717, a Plasmodium elongation factor 2 inhibito...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9107587
Malaria Journal; Khandelwal A, Arez F et. al.

May 16th, 2022 - Targeting the asymptomatic liver stage of Plasmodium infection through chemoprevention could become a key intervention to reduce malaria-associated incidence and mortality. M5717, a Plasmodium elongation factor 2 inhibitor, was assessed in vitro and in vivo with readily accessible Plasmodium berghei parasites. In an animal refinement, reduction, replacement approach, the in vitro IC99 value was...

A Pharmacokinetic Analysis of Tobramycin in Patients Less than Five Years of Age with C...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9112897
Antimicrobial Agents and Chemotherapy; Downes KJ, Grim A et. al.

Apr 29th, 2022 - Extended interval dosing of tobramycin is recommended for treatment of pulmonary exacerbations in adults and older children with cystic fibrosis (CF), but data are limited in patients less than 5 years of age. We performed a retrospective population pharmacokinetic (PK) analysis of hospitalized children with CF <5 years of age prescribed intravenous tobramycin for a pulmonary exacerbation from ...

Childhood Abuse May Increase MS Risk in Adults
https://www.medscape.com/viewarticle/972449

Apr 20th, 2022 - Emotional or sexual abuse in childhood may increase risk of multiple sclerosis (MS) in women, and risk may increase further with exposure to multiple kinds of abuse, according to the first prospective cohort study of its kind. More research is needed to uncover underlying mechanisms of action, according to lead author Karine Eid, MD, a PhD candidate at Haukeland University Hospital, Bergen, Nor...

Emerging and Novel Therapeutics in the Management of Psoriatic Arthritis
https://www.medscape.com/viewarticle/959157

Apr 18th, 2022 - This transcript has been edited for clarity. Elaine Husni, MD, MPH: Welcome to this Medscape InDiscussion episode six. We're going to talk about emerging and novel therapeutics in the treatment of psoriatic arthritis. I'm particularly excited today because we have Dr Ana-Maria Orbai, who's both a friend and colleague. She is an assistant professor of medicine in the division of rheumatology at ...

A Phase I, Open-label, Randomized, Crossover Study of the Relative Bioavailability of C...
https://doi.org/10.1016/j.clinthera.2022.02.009
Clinical Therapeutics; Cohen-Rabbie S, Mattinson A et. al.

Apr 13th, 2022 - Selumetinib (ARRY-142886) is an oral, potent, and highly selective allosteric mitogen-activated protein kinase kinase 1/2 inhibitor approved for the treatment of pediatric patients (≥2 years of age) with neurofibromatosis type 1 who have symptomatic, inoperable plexiform neurofibromas. This Phase I crossover study (NCT03649165) evaluated the pharmacokinetic properties and palatability of a new ...

Aconitine: A review of its pharmacokinetics, pharmacology, toxicology and detoxification.
https://doi.org/10.1016/j.jep.2022.115270
Journal of Ethnopharmacology; Gao Y, Fan H et. al.

Apr 12th, 2022 - Aconitine, a C19-norditerpenoid alkaloid, derives from many medicinal plants such as Aconitum carmichaelii Debx. (Chinese:), Aconitum kusnezoffii Reichb (Chinese:), which were used to rheumatic fever, painful joints and some endocrinal disorders. The present paper reviews research progress relating to the pharmacokinetics, physiological and pathological processes of aconitine, while some promis...

Population pharmacokinetics of rucaparib in patients with advanced ovarian cancer or ot...
https://doi.org/10.1007/s00280-022-04413-7 10.1038/nbt.2121 10.1158/1535-7163.MCT-06-0552 10.1093/jnci/djq509 10.1038/bjc.2017.36 10.1158/1078-0432.CCR-16-2796 10.1002/cpdd.575 10.1016/S1470-2045(16)30559-9 10.1038/s41467-021-22582-6 10.1016/s0140-6736(17)32440-6 10.1158/1078-0432.CCR-20-0394 10.1200/JCO.20.01035 10.1007/s10637-019-00815-2 10.1158/1078-0432.CCR-08-1223 10.1016/j.cmpb.2003.11.003 10.1016/j.cmpb.2005.04.005 10.1208/s12248-011-9289-2 10.1208/s12248-009-9133-0 10.1016/j.ygyno.2021.03.015
Cancer Chemotherapy and Pharmacology; Green ML, Ma SC et. al.

Apr 11th, 2022 - To develop a population pharmacokinetics (PPK) model for rucaparib, an oral poly(ADP-ribose) polymerase inhibitor. The PPK analysis used PK data from patients in Study 1014 (NCT01009190, n = 35), Study 10 (NCT01482715, n = 123), and ARIEL2 (NCT01891344, n = 300), including intensive intravenous data (12-40 mg), intensive and sparse oral data (12-360 mg single-dose, 40-500 mg once daily, and 240...

Novel Drug Significantly Reduces Tics in Tourette's ― Without Side Effects
https://www.medscape.com/viewarticle/971335

Mar 31st, 2022 - An investigational drug that blocks the dopamine-1 (D1) receptor reduces tics and is safe and well tolerated in children with Tourette syndrome (TS), a new study shows. Importantly, unlike current medications for the disorder, ecocipam does not lead to weight gain, anxiety, depression, or tardive dyskinesia compared to placebo ― a factor that may lead to better adherence. Dr Donald Gilbert For ...

A Developer's Perspective on Clinical Evidence and Benefits for Rituximab Biosimilar Up...
https://doi.org/10.1007/s40261-022-01133-x 10.1016/j.clml.2021.08.005
Clinical Drug Investigation; Choi D, Lee S et. al.

Mar 25th, 2022 - To date, four rituximab biosimilars have received regulatory approval from the European Medicines Agency and/or US Food and Drug Administration. CT-P10 was the first rituximab biosimilar to be approved by each agency, in 2017 and 2018, respectively. Regulatory approval of CT-P10 followed demonstration of pharmacokinetic equivalence to the reference product in a phase I study in patients with rh...

First-in-Human Clinical Trial to Assess the Safety, Tolerability and Pharmacokinetics o...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9017376
Antimicrobial Agents and Chemotherapy; Raja SM, Guptill JT et. al.

Mar 22nd, 2022 - Botulism is a rare, life-threatening paralytic disease caused by botulinum neurotoxin (BoNT). Available treatments including an equine antitoxin and human immune globulin are given postexposure and challenging to produce and administer. NTM-1633 is an equimolar mixture of 3 human IgG monoclonal antibodies, E1, E2, and E3, targeting BoNT serotype E (BoNT/E). This first-in-human study assessed th...

Pharmacokinetics of mycophenolic acid and external evaluation of two limited sampling s...
https://doi.org/10.1007/s00228-022-03295-1 10.1016/j.clim.2019.108274 10.1136/annrheumdis-2017-211898 10.1016/j.rdc.2013.05.001 10.1002/art.21955 10.1016/j.berh.2018.02.001 10.1080/1744666X.2016.1212659 10.1007/s00467-020-04733-x 10.1097/FTD.0000000000000671 10.1016/S0162-3109(00)00188-0 10.1016/j.semarthrit.2010.05.007 10.1080/17425255.2021.1843633 10.2165/00003088-199834060-00002 10.1002/jcph.1565 10.1093/ndt/gfu184 10.1097/FTD.0000000000000871 10.1111/bcp.12392 10.1097/01.ftd.0000162231.90811.38 10.2165/00003088-200544080-00005 10.1097/FTD.0b013e31819c077c 10.1097/01.ftd.0000159784.25872.f6 10.1186/ar3202 10.1038/ki.2010.170 10.1093/ndt/gfy026 10.1097/FTD.0b013e31821633a6 10.2215/CJN.07111009 10.1016/j.phrs.2011.01.009 10.2215/CJN.00320116 10.1517/17425255.2016.1170806 10.1111/j.1365-2125.2010.03615.x 10.2165/00003088-200847040-00005 10.1097/FTD.0b013e3181a23f1a 10.1097/01.ASN.0000051598.12824.DA 10.1002/art.27495
European Journal of Clinical Pharmacology; Beaulieu Q, Zhang D et. al.

Mar 17th, 2022 - Mycophenolate mofetil (MMF), a pro-drug of mycophenolic acid (MPA), has become a major therapeutic option in juvenile systemic lupus erythematosus (jSLE). Monitoring MPA exposure using area under curve (AUC) has proved its value to increase efficacy and safety in solid organ transplantation both in children and adults, but additional data are required in patients with autoimmune diseases. In or...

Physiologically-Based Pharmacokinetic-Led Guidance for Patients With Cystic Fibrosis Ta...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9087007
Clinical Pharmacology and Therapeutics; Hong E, Almond LM et. al.

Mar 17th, 2022 - Cystic fibrosis transmembrane conductance regulator (CFTR) modulating therapies, including elexacaftor-tezacaftor-ivacaftor, are primarily eliminated through cytochrome P450 (CYP) 3A-mediated metabolism. This creates a therapeutic challenge to the treatment of coronavirus disease 2019 (COVID-19) with nirmatrelvir-ritonavir in people with cystic fibrosis (CF) due to the potential for significant...

Peginterferon beta-1a concentrations in breast milk of lactating multiple sclerosis pat...
https://doi.org/10.1016/j.msard.2022.103700
Multiple Sclerosis and Related Disorders; Houtchens M, Mahlanza T et. al.

Mar 10th, 2022 - Peginterferon beta-1a is an interferon beta-1a formulation that has been pegylated, resulting in a longer half-life than other interferon beta formulations. We examined concentrations of peginterferon beta-1a in breast milk of lactating patients with multiple sclerosis (MS) receiving peginterferon beta-1a as their postpartum disease-modifying therapy. After completion of titration to a full dos...

Prediction of lung exposure to anti-tubercular drugs using plasma pharmacokinetic data:...
https://doi.org/10.1016/j.ejps.2022.106163
European Journal of Pharmaceutical Sciences : Official Jo... Muliaditan M, Teutonico D et. al.

Mar 7th, 2022 - The development of novel candidate molecules for tuberculosis remains challenging, as drug distribution into the target tissue is not fully characterised in preclinical models of infection. Often antitubercular human dose selection is derived from pharmacokinetic data in plasma. Here, we explore whether whole-body physiologically-based pharmacokinetic (PBPK) modelling enables the prediction of ...

Regression Analysis to Estimate the Factor VIII Activity of Patients with Hemophilia A ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8894944
Clinical and Applied Thrombosis/hemostasis : Official Jou... Hatayama Y, Motokura T et. al.

Mar 1st, 2022 - Emicizumab, a bispecific monoclonal antibody for hemophilia A (HA), has strong pharmacodynamic effects in several coagulation assays resulting in dosing difficulties with Factor VIII (FVIII) concentrates during bleeding emergencies. Single and multiple regression models were studied to estimate FVIII activity using 27 archived plasma samples from three patients with HA without inhibitor under e...

Evaluation of the pharmacokinetics of trazpiroben (TAK-906) in the presence and absence...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9099131
Clinical and Translational Science; Kaur Mukker J, Dukes G et. al.

Feb 27th, 2022 - Trazpiroben, a dopamine D2 /D3 receptor antagonist under development to treat gastroparesis, displays decreasing solubility with increasing pH. This single-sequence, open-label, two-period, crossover study evaluated the effect of esomeprazole, a proton pump inhibitor that raises gastric pH, on the single-dose pharmacokinetics, safety, and tolerability of trazpiroben in healthy adults (NCT038496...

Prognostic value of 11C-methionine volume-based PET parameters in IDH wild type gliobla...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8880430
PloS One; van Dijken BRJ, Ankrah AO et. al.

Feb 26th, 2022 - 11C-Methionine (11C-MET) PET prognostication of isocitrate dehydrogenase (IDH) wild type glioblastomas is inadequate as conventional parameters such as standardized uptake value (SUV) do not adequately reflect tumor heterogeneity. We retrospectively evaluated whether volume-based parameters such as metabolic tumor volume (MTV) and total lesion methionine metabolism (TLMM) outperformed SUV for s...

The oral protease inhibitor (PF-07321332) protects Syrian hamsters against infection wi...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8847371
Nature Communications; Abdelnabi R, Foo CS et. al.

Feb 17th, 2022 - There is an urgent need for potent and selective antivirals against SARS-CoV-2. Pfizer developed PF-07321332 (PF-332), a potent inhibitor of the viral main protease (Mpro, 3CLpro) that can be dosed orally and that is in clinical development. We here report that PF-332 exerts equipotent in vitro activity against the four SARS-CoV-2 variants of concerns (VoC) and that it can completely arrest rep...

Pharmacodynamics and pharmacokinetics of PLGA-based doxorubicin-loaded implants for tum...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8843208
Drug Delivery; He P, Xu S et. al.

Feb 12th, 2022 - The traditional systemic chemotherapy through intravenous infusion of doxorubicin (DOX) has many side effects. The aim of this study was to develop a PLGA-based DOX-loaded implant and to evaluate the efficacy and drug metabolism distribution of the implant in intratumoral chemotherapy for osteosarcoma (OS). In this study, implants containing DOX, poly(d,l-lactide-co-glycolide), and polyethylene...

Comparative assessment of pharmacokinetic parameters between HS016, an adalimumab biosi...
https://doi.org/10.17219/acem/145947
Advances in Clinical and Experimental Medicine : Official... Zeng X, Zhang J et. al.

Feb 12th, 2022 - The HS016 is an adalimumab biosimilar related to the immunoglobulin G1 (IgG1) antibody, with a similar amino acid sequence. To quantify the differences in the pharmacokinetic (PK) parameters of HS016 and adalimumab in healthy individuals and patients with ankylosing spondylitis (AS). The PK data for HS016 and adalimumab were obtained in a randomized, double-blind, phase 1 clinical study in Chin...