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About 164,808 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...

Application of Modeling and Simulation to Identify a Shortened Study Duration and Novel...
https://doi.org/10.1208/s12248-022-00715-z 10.1002/jcph.1710 10.1089/jwh.2015.5191 10.1097/aog.0b013e318273eb56 10.1056/NEJMoa1400506 10.1363/4308811 10.1363/4309411 10.1208/s12248-008-9010-2 10.2147/PPA.S36948 10.1097/00004347-198609000-00005 10.1363/46e1714 10.1016/j.jpag.2012.10.006
The AAPS Journal; Sharan S, Choi S et. al.

May 3rd, 2022 - An intrauterine system (IUS) can be implanted in the uterus and deliver drug directly at the site of pharmacological action. Mirena was the first FDA-approved levonorgestrel (LNG) releasing IUS without an approved generic form. Its 5-year application duration presents challenges for bioequivalence (BE) assessment using the conventional in vivo studies with pharmacokinetic and/or comparative cli...

Effect of the Size of Protein Therapeutics on Brain Pharmacokinetics Following Systemat...
https://doi.org/10.1208/s12248-022-00701-5 10.1007/s10928-013-9301-9 10.1517/17425247.2016.1171315 10.1002/path.1711340107 10.1007/s40259-018-0309-y 10.1080/19420862.2021.1874121 10.3233/HAB-160306 10.1111/j.1471-4159.2007.04591.x 10.1016/j.nbd.2005.04.007 10.1021/mp300495e 10.1073/pnas.0509425103 10.1113/JP275105 10.1124/jpet.111.183483 10.1096/fj.14-253369 10.1186/s12987-018-0093-6 10.1080/19420862.2018.1473910 10.1007/s10928-019-09641-8 10.1038/clpt.1994.134 10.1124/dmd.119.087809 10.1002/jps.10410 10.1016/j.xphs.2017.03.033 10.1016/j.xphs.2016.08.016 10.1046/j.1365-2133.2000.03535.x 10.1016/j.npep.2011.07.008 10.1023/A:1016255124336 10.1016/j.neuron.2018.09.022 10.1172/JCI90603 10.1007/s10143-019-01133-0
The AAPS Journal; Chang HY, Wu S et. al.

May 3rd, 2022 - Here, we have investigated the effect of size of protein therapeutics on brain pharmacokinetics (PK) following systemic administration in rats. All tested proteins were derived from trastuzumab that do not bind to any targets in rats. PK data generated with F(ab)2 (100 kDa), Fab (50 kDa), and scFv (27 kDa) fragments of trastuzumab, along with published PK data for FcRn non-binding and wild-type...

Comparison of three galenic forms of lamivudine in young West African children living w...
https://doi.org/10.1177/13596535211058267
Antiviral Therapy; Pressiat C, Dainguy E et. al.

Apr 30th, 2022 - Few pharmacokinetic data were reported on dispersible tablets despite their increasing use. One hundred fifty HIV-infected children receiving lamivudine were enrolled in the MONOD ANRS 12,206 trial. Three galenic forms were administered: liquid formulation, tablet form and dispersible scored tablet. HIV-infected children <4 years old were enrolled in the MONOD ANRS 12,206 trial designed to asse...

Pharmacokinetic-Pharmacodynamic Analysis of Concentration-Response Relationship in Schi...
https://doi.org/10.1017/S1092852922000451
CNS Spectrums; Sun L, Mills R et. al.

Apr 29th, 2022 - A combination of olanzapine and samidorphan (OLZ/SAM) that provides the efficacy of olanzapine while mitigating weight gain was recently approved by the Food and Drug Administration for the treatment of schizophrenia and bipolar I disorder. This exploratory population pharmacokinetic-pharmacodynamic analysis evaluated potential relationships between drug exposure and treatment effects. Positive...

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 ...

The Effect of Particle Size on the Absorption of Cyclosporin A Nanosuspensions.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9034871
International Journal of Nanomedicine; Sun W, Gao J et. al.

Apr 27th, 2022 - Cyclosporin A (CsA) is a hydrophobic drug widely used as an immunosuppressant and anti-rejection drug in solid organ transplantation. On the market, there are two oral CsA formulations available containing polyoxyethylene castor oil, which can cause serious allergic reactions and nephrotoxicity. In order to eliminate polyoxyethylene castor oil, CsA was formulated into a nanosuspension. This stu...

Implementation of a Vancomycin Dose-Optimization Protocol in Neonates: Impact on Vancom...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9112885
Antimicrobial Agents and Chemotherapy; Gomez L, Boegler D et. al.

Apr 26th, 2022 - Vancomycin dosing used in neonates results frequently in insufficient concentrations. A vancomycin dose-optimization protocol consisting of an individualization of loading and maintenance doses (administered during continuous infusion) through a previously validated pharmacokinetic model was implemented in our center. This monocenter retrospective study aimed to compare vancomycin average conce...

Design and Development of Solid SMEDDS and Liquisolid Formulations of Lovastatin, for I...
https://doi.org/10.1208/s12249-022-02272-2 10.1080/10717544.2019.1686086 10.1016/S1056-8719(00)00107-6 10.1016/j.colsurfb.2014.11.022 10.1016/j.apsb.2013.11.001 10.1517/17425247.2013.798297 10.1016/j.ajps.2014.12.006 10.1016/j.ijpharm.2013.03.054 10.1208/s12249-012-9787-2 10.1016/0378-5173(94)00222-Q 10.1016/j.colsurfb.2018.03.034 10.1016/S0928-0987(02)00051-9 10.1016/j.apsb.2017.02.002 10.1016/j.jconrel.2008.03.021 10.15171/apb.2016.050 10.3390/molecules201219745 10.1007/s11095-004-9004-4 10.1016/0003-9861(91)90551-S 10.1080/00498254.2019.1662136 10.1208/pt0801024 10.1208/s12249-008-9171-4 10.30574/gscbps.2019.8.1.0082 10.1016/j.ajps.2014.08.003 10.1080/03639045.2020.1742142 10.2174/1567201815666180723115141 10.1007/s40005-017-0344-6 10.2478/acph-2013-0013 10.1248/bpb.32.1600 10.1016/j.jconrel.2016.06.017 10.1016/j.jddst.2016.04.011 10.1081/DDC-100102156 10.1016/j.ejpb.2008.02.017 10.1016/j.powtec.2008.01.029 10.1208/s12249-008-9046-8 10.1208/s12249-008-9143-8 10.1016/j.ijpharm.2006.11.004 10.3390/pharmaceutics2040351 10.1002/jps.2600561005 10.1007/s580-002-8080-5 10.1016/j.ejpb.2016.10.022 10.2147/IJN.S241120
AAPS PharmSciTech; Suram D, Veerabrahma K

Apr 24th, 2022 - Lovastatin (Lov) is a lipid-lowering agent, with 5% bioavailability (BA) due to extensive first pass metabolism and poor solubility. To enhance dissolution and in vivo effects, Lov solid self microemulsifying drug delivery system (SMEDDS) and liquisolid systems were developed and evaluated to select superior one. Solubilities were determined in oils, surfactants, and cosurfactants. Ternary phas...

Vancomycin Pharmacokinetics in a Pregnancy Rat Model.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9112916
Antimicrobial Agents and Chemotherapy; Avedissian SN, Pais GM et. al.

Apr 22nd, 2022 - Vancomycin usage is often unavoidable in pregnant patients; however, literature suggests vancomycin can cross the placental barrier and reach the fetus. Understanding the mass transit of vancomycin to the fetus is important in pregnancy. We aimed to (i) identify a relevant population pharmacokinetic (PK) model for vancomycin in pregnancy and (ii) estimate PK parameters and describe the mass tra...

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...

Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, includi...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9054876
Cancer Chemotherapy and Pharmacology; Xiong W, Papasouliotis O et. al.

Apr 8th, 2022 - Tepotinib is a highly selective, potent, mesenchymal-epithelial transition factor (MET) inhibitor, approved for the treatment of non-small cell lung cancer (NSCLC) harboring MET exon 14 skipping. Objectives of this population pharmacokinetic (PK) analysis were to evaluate the dose-exposure relationship of tepotinib and its major circulating metabolite, MSC2571109A, and to identify the intrinsic...

Pharmacokinetics of Daprodustat and Metabolites in Individuals with Normal and Impaired...
https://doi.org/10.1002/cpdd.1090
Clinical Pharmacology in Drug Development; Mahar KM, Shaddinger BC et. al.

Apr 1st, 2022 - Daprodustat is a hypoxia-inducible factor-prolyl hydroxylase inhibitor in development for treatment of anemia of chronic kidney disease. We evaluated the role of hepatic impairment on daprodustat pharmacokinetics, pharmacodynamics, and tolerability. Participants with mild (Child-Pugh Class A, score 5-6) and moderate (Child-Pugh Class B, score 7-9) hepatic impairment and matched healthy controls...

Pharmacokinetics of Clavulanic Acid in the Pediatric Population: A Systematic Literatur...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9095526
Clinical Pharmacokinetics; Keij FM, Tramper-Stranders GA et. al.

Apr 1st, 2022 - Clavulanic acid is a commonly used β-lactam inhibitor in pediatrics for a variety of infections. Clear insight into its mode of action is lacking, however, and a target has not been identified. The dosing of clavulanic acid is currently based on that of the partner drug (amoxicillin or ticarcillin). Still, proper dosing of the compound is needed because clavulanic acid has been associated with ...

Olanzapine-samidorphan combination tablets for the treatment of schizophrenia and bipol...
https://doi.org/10.1080/14737175.2022.2060742
Expert Review of Neurotherapeutics; Faden J, Serdenes R et. al.

Apr 1st, 2022 - Although olanzapine remains one of the most efficacious antipsychotic medications for the treatment of schizophrenia, there are significant tolerability concerns related to its weight and metabolic profile. Olanzapine-samidorphan combination tablets (OLZ/SAM), branded as Lybalvi, is a newly FDA approved formulation aimed at attenuating antipsychotic induced weight gain via modulation of the end...

Development, Characterization, and Investigation of In Vivo Targeted Delivery Efficacy ...
https://doi.org/10.1208/s12249-022-02255-3 10.1002/hep.31150 10.1016/j.metabol.2015.12.012 10.1038/nrgastro.2016.85 10.1038/pr.2014.157 10.1016/j.biopha.2019.108612 10.1021/acs.jnatprod.6b00146 10.3945/ajcn.116.136051 10.1016/j.bcp.2017.04.033 10.1016/j.abb.2021.109019 10.1002/smll.201900262 10.1016/j.ijpharm.2015.06.007 10.1016/j.jconrel.2005.02.011 10.1016/S0168-3659(98)00029-7 10.1016/j.ijpharm.2017.08.076 10.1016/j.jconrel.2014.03.039 10.1211/0022357011776658 10.3389/fchem.2020.00407 10.3389/fmed.2021.794299 10.1021/acsnano.5b03876 10.1021/mp800051m 10.1016/j.colsurfb.2009.09.001 10.1007/s10856-015-5641-x 10.1016/j.ijpharm.2020.120138 10.1016/j.ijbiomac.2017.10.103 10.1098/rsos.181457. 10.1016/0026-2862(83)90016-X 10.1161/01.RES.79.3.581 10.1054/bjoc.1999.1171 10.15171/apb.2020.001 10.2147/IJN.S46613 10.1080/08982104.2021.1999974 10.1016/S0378-5173(01)00574-9
AAPS PharmSciTech; Liu X, Zhang M et. al.

Mar 30th, 2022 - Luteolin (Lu) is a kind of flavonoid that has been proved to treat non-alcoholic fatty liver disease by alleviating intestinal microbiota disorder. In this study, luteolin was coated with methoxy poly(ethylene glycol)-poly(dl-lactide-co-glycolic acid) (mPEG-PLGA) using an emulsion solvent evaporation method, and the optimum preparation process was determined by a single-factor experiment combin...

Role of the efflux transporters Abcb1 and Abcg2 in the brain distribution of olaparib i...
https://doi.org/10.1016/j.ejps.2022.106177
European Journal of Pharmaceutical Sciences : Official Jo... Song YK, Kim MJ et. al.

Mar 29th, 2022 - Olaparib is a first-in-class poly (ADP-ribose) polymerase oral inhibitor used to treat various tumors. In this study, we clarified the roles of ABCB1/Abcb1 and ABCG2/Abcg2 transporters in restricting olaparib distribution to the brain. Olaparib was efficiently transported by human ABCG2, human ABCB1, and mouse Abcg2 in vitro. In the in vivo disposition study of olaparib using single or combinat...

Pharmacokinetic drug interactions with oral haloperidol in adults: dose correction fact...
https://doi.org/10.1080/17425255.2022.2057297
Expert Opinion on Drug Metabolism & Toxicology; McGrane I, Spina E et. al.

Mar 26th, 2022 - Pharmacokinetic (PK) drug-drug interactions (DDIs) of oral haloperidol, a first-generation antipsychotic, are systematically reviewed. After exclusions, the search for DDIs with oral haloperidol provided 47 articles as victim and 7 as perpetrator. Changes in mean haloperidol concentration-to-dose (C/D) ratios after weighting each study's size were used to calculate the effects of other drugs (i...

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...