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About 15,295 results

IVIVC of Octreotide in PLGA-Glucose Microsphere Formulation, Sandostatin® LAR.
https://doi.org/10.1208/s12249-022-02359-w
AAPS PharmSciTech; Song JS, Kim SY et. al.

Sep 20th, 2022 - In vitro-in vivo correlation (IVIVC) analysis reveals a relationship between in vitro release and in vivo pharmacokinetic response of the drug of interest. Sandostatin LAR Depot (SLD) for endocrine tumors and acromegaly is a sustained-release formulation of octreotide, a cyclic oligomer of 8 amino acids, which prolongs therapeutic efficacy and enhances medication compliance of octreotide. Since...

Your Posture Can Determine How Your Body Absorbs Drugs
https://www.medscape.com/viewarticle/980557

Sep 12th, 2022 - Your posture can significantly affect the way your body absorbs medication, with bad posture delaying effects of a drug by as much as an hour, according to researchers from Johns Hopkins University and Johns Hopkins School of Medicine. What to know: How a swallowed drug is absorbed in the gastrointestinal tract depends on the medication's ingredients, the stomach's physiologic environment at th...

Effect of fluconazole on the pharmacokinetics of a single dose of fedratinib in healthy...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9399588
Cancer Chemotherapy and Pharmacology; Chen Y, Ogasawara K et. al.

Aug 25th, 2022 - Fedratinib is an orally administered Janus kinase (JAK) 2-selective inhibitor for the treatment of adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis. In vitro, fedratinib is predominantly metabolized by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP2C19. Coadministration of fedratinib with CYP3A4 inhibitors is predicted to increase systemic exposure to ...

New Perspectives on Antimicrobial Agents: Isavuconazole.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9487460
Antimicrobial Agents and Chemotherapy; Lewis JS, Wiederhold NP et. al.

Aug 16th, 2022 - Isavuconazole is the newest of the clinically available advanced generation triazole antifungals and is active against a variety of yeasts, molds, and dimorphic fungi. Its current FDA-approved indications include the management of invasive aspergillosis as well as mucormycosis, though the latter indication is supported by limited clinical data. Isavuconazole did not achieve noninferiority to ca...

Engineered IL13 variants direct specificity of IL13Rα2-targeted CAR T cell therapy.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9388138
Proceedings of the National Academy of Sciences of the Un... Stern LA, Gholamin S et. al.

Aug 9th, 2022 - IL13Rα2 is an attractive target due to its overexpression in a variety of cancers and rare expression in healthy tissue, motivating expansion of interleukin 13 (IL13)-based chimeric antigen receptor (CAR) T cell therapy from glioblastoma into systemic malignancies. IL13Rα1, the other binding partner of IL13, is ubiquitously expressed in healthy tissue, raising concerns about the therapeutic win...

Pharmacokinetic parameter driven outcomes model predicts a reduction in bleeding events...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9356410
BMC Medical Research Methodology; Chen R, Gultyaev D et. al.

Aug 6th, 2022 - Long-term prophylactic therapy is considered the standard of care for hemophilia A patients. This study models the long-term clinical and cost outcomes of two factor VIII (FVIII) products using a pharmacokinetic (PK) simulation model in a Chinese population. Head-to-head PK profile data of BAY 81-8973 (KOVALTRY®) and antihemophilic factor (recombinant) plasma/albumin-free method (rAHF-PFM, ADVA...

Low-Dose Subcutaneous or Intravenous Monoclonal Antibody to Prevent Malaria.
https://doi.org/10.1056/NEJMoa2203067
The New England Journal of Medicine; Wu RL, Idris AH et. al.

Aug 4th, 2022 - New approaches for the prevention and elimination of malaria, a leading cause of illness and death among infants and young children globally, are needed. We conducted a phase 1 clinical trial to assess the safety and pharmacokinetics of L9LS, a next-generation antimalarial monoclonal antibody, and its protective efficacy against controlled human malaria infection in healthy adults who had never...

Piperaquine Pharmacokinetic and Pharmacodynamic Profiles in Healthy Volunteers of Papua...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9380548
Antimicrobial Agents and Chemotherapy; Millat-Martínez P, Salman S et. al.

Jul 22nd, 2022 - Mass drug administration (MDA) with monthly dihydroartemisinin-piperaquine (DHA-PQP) appears useful in malaria control and elimination strategies. Determining the relationship between consecutive piperaquine phosphate (PQP) exposure and its impact on QT interval prolongation is a key safety consideration for MDA campaigns. Healthy volunteers from Papua New Guinea received a 3-day course of DHA-...

A long-acting C-natriuretic peptide for achondroplasia.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9335275
Proceedings of the National Academy of Sciences of the Un... Schneider EL, Carreras CW et. al.

Jul 21st, 2022 - The C-natriuretic peptide (CNP) analog vosoritide has recently been approved for treatment of achondroplasia in children. However, the regimen requires daily subcutaneous injections in pediatric patients over multiple years. The present work sought to develop a long-acting CNP that would provide efficacy equal to or greater than that of vosoritide but require less frequent injections. We used a...

Influence of N-acetyltransferase 2 (NAT2) genotype/single nucleotide polymorphisms on c...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9482569
European Journal of Clinical Pharmacology; Thomas L, Raju AP et. al.

Jul 20th, 2022 - Significant pharmacokinetic variabilities have been reported for isoniazid across various populations. We aimed to summarize population pharmacokinetic studies of isoniazid in tuberculosis (TB) patients with a specific focus on the influence of N-acetyltransferase 2 (NAT2) genotype/single-nucleotide polymorphism (SNP) on clearance of isoniazid. A systematic search was conducted in PubMed and Em...

Clinical Pharmacokinetics and Pharmacodynamics of Fostamatinib and Its Active Moiety R406.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9250994
Clinical Pharmacokinetics; Matsukane R, Suetsugu K et. al.

Jul 6th, 2022 - Fostamatinib is the first approved spleen tyrosine kinase inhibitor for chronic immune thrombocytopenia. This review summarizes the clinical development, pharmacokinetics, pharmacodynamics, drug-drug interactions, adverse events, and comprehensive analyses of fostamatinib. While integrating these findings, we discuss the fostering and improvement of fostamatinib for further clinical application...

A personalized limited sampling approach to better estimate terminal half-life of FVIII...
https://doi.org/10.1111/jth.15803
Journal of Thrombosis and Haemostasis : JTH; Chelle P, Iorio A et. al.

Jun 27th, 2022 - Hemophilia A is a bleeding disorder characterized by a deficiency of a coagulation factor VIII and optimally treated using pharmacokinetics (PK)-guided prophylactic replacement therapy. To decrease patient burden, PK can be estimated from sparse sampling leveraging population PK modeling. However, recommendations for sampling times meant for patients with hemophilia A as a group may not be opti...

Population Pharmacokinetic Modelling and Limited Sampling Strategies for Therapeutic Dr...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9295566
Antimicrobial Agents and Chemotherapy; Abolhassani-Chimeh R, Akkerman OW et. al.

Jun 22nd, 2022 - Pyrazinamide is one of the first-line antituberculosis drugs. The efficacy of pyrazinamide is associated with the ratio of 24-h area under the concentration-time curve (AUC24) to MIC. The objective of this study was to develop and validate a limited sampling strategy (LSS) based on a population pharmacokinetic (popPK) model to predict AUC24. A popPK model was developed using an iterative two-st...

Pharmacokinetics and Exposure-Response Analysis of Venetoclax + Obinutuzumab in Chronic...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9309146
Advances in Therapy; Samineni D, Gibiansky L et. al.

Jun 17th, 2022 - This study aims to investigate pharmacokinetics (PK) and exposure-response parameters of the 400 mg once-daily venetoclax dose regimen in combination with obinutuzumab, which was approved for the first-line (1L) treatment of chronic lymphocytic leukemia (CLL) based on data from the phase 3 CLL14 study and the phase 1b dose-finding GP28331 study. Parameter estimates and uncertainty, which were e...

Multi-model averaging improves the performance of model-guided infliximab dosing in pat...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9381887
CPT: Pharmacometrics & Systems Pharmacology; Kantasiripitak W, Outtier A et. al.

Jun 17th, 2022 - Infliximab dosage de-escalation without prior knowledge of drug concentrations may put patients at risk for underexposure and trigger the loss of response. A single-model approach for model-informed precision dosing during infliximab maintenance therapy has proven its clinical benefit in patients with inflammatory bowel diseases. We evaluated the predictive performances of two multi-model appro...

Epicatechin exerts dual action to shield sickling and hydroxyurea-induced myelosuppress...
https://doi.org/10.1016/j.taap.2022.116113
Toxicology and Applied Pharmacology; Gour A, Kour D et. al.

Jun 13th, 2022 - Hydroxyurea (HU) is the key drug to treat Sickle cell anemia (SCA). However, its treatment is associated with the liability of myelosuppression. The present study aimed to investigate the potential of epicatechin as a supplementation therapy for the symptomatic management of SCA under HU therapy. A panel of experiments were performed at first to observe epicatechin's effect on sickling and hemo...

Distribution Pattern of the Monoamine Oxidase B Ligand, 18F-THK5351, in the Healthy Brain.
https://doi.org/10.1097/RLU.0000000000004272
Clinical Nuclear Medicine; Ishibashi K, Miura Y et. al.

Jun 9th, 2022 - 18F-THK5351 PET estimates the concentrations of monoamine oxidase B (MAO-B) that are preferentially located in astrocytes and can be used to visualize and quantify ongoing astrogliosis. To study images of astrogliosis in neurological disorders, it is essential to understand the detailed binding sites of 18F-THK5351 as the MAO-B ligand under normal conditions. In this study, we examined the deta...

Pre-clinical evaluation of LASSBio-1491: From in vitro pharmacokinetic study to in vivo...
https://doi.org/10.1371/journal.pone.0269447
PloS One; de Queiroz AC, Barbosa G et. al.

Jun 7th, 2022 - Leishmaniasis is a public health issue. It is among the top five parasitic illnesses worldwide and is one of the most neglected diseases. The current treatment disease includes limitations of toxicity, variable efficacy, high costs and inconvenient doses and treatment schedules. LASSBio-1736 was described as antileishmanial drug-candidate to cutaneous leishmaniasis, displaying plasma stability ...

Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resist...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9349160
Clinical Pharmacokinetics; Tanneau L, Karlsson MO et. al.

Jun 7th, 2022 - Delamanid is a nitroimidazole, a novel class of drug for treating tuberculosis, and is primarily metabolized by albumin into the metabolite DM-6705. The aims of this analysis were to develop a population pharmacokinetic (PK) model to characterize the concentration-time course of delamanid and DM-6705 in adults with drug-resistant tuberculosis and to explore a potential drug-drug interaction wit...

Identification of Infigratinib as a Potent Reversible Inhibitor and Mechanism-Based Ina...
https://doi.org/10.1124/jpet.122.001222
The Journal of Pharmacology and Experimental Therapeutics; Tang LWT, Wu G et. al.

Jun 1st, 2022 - Infigratinib (INF) is a fibroblast growth factor receptor inhibitor that was recently United States Food and Drug Administration-approved for the treatment of advanced or metastatic cholangiocarcinoma. We previously established that INF inhibited and inactivated cytochrome P450 3A4 (CYP3A4). Here, in a follow up to our previous study, we identified for the first time that INF also elicited pote...