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About 15,450 results

Population Pharmacokinetic Model and Optimal Sampling Strategies for Micafungin in Crit...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9765295
Antimicrobial Agents and Chemotherapy; Boonstra JM, van der Elst KC et. al.

Nov 16th, 2022 - Candida bloodstream infections are associated with high attributable mortality, where early initiation of adequate antifungal therapy is important to increase survival in critically ill patients. The exposure variability of micafungin, a first-line agent used for the treatment of invasive candidiasis, in critically ill patients is significant, potentially resulting in underexposure in a substan...

An overview of micafungin as a treatment option for invasive candidiasis in pediatric p...
https://doi.org/10.1080/14656566.2022.2147824
Expert Opinion on Pharmacotherapy; Bassetti M, Giacobbe DR et. al.

Nov 15th, 2022 - Invasive candidiasis remains a leading cause of morbidity and mortality in various categories of patients at risk. Structure and mechanism of action, pharmacokinetics and pharmacodynamics, clinical studies, safety, and regulatory status of micafungin are explored in the present review, focusing on pediatric patients younger than 4 months old. Although limited, the available data on the efficacy...

Efficacy and Safety of Trametinib Monotherapy or in Combination With Dabrafenib in Pedi...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9870224
Journal of Clinical Oncology : Official Journal of the Am... Bouffet E, Geoerger B et. al.

Nov 15th, 2022 - BRAF V600 mutations occur in many childhood cancers, including approximately 20% of low-grade gliomas (LGGs). Here, we describe a phase I/II study establishing pediatric dosing and pharmacokinetics of trametinib with or without dabrafenib, as well as efficacy and safety in a disease-specific cohort with BRAF V600-mutant LGG; other cohorts will be reported elsewhere. This is a four-part, phase I...

Association of CYP2D6*4 Polymorphism with the Steady-State Concentration of Haloperidol...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9611797
Psychopharmacology Bulletin; Parkhomenko AA, Zastrozhin MS et. al.

Nov 8th, 2022 - CYP2D6 subfamily isoenzymes play an important role in the biotransformation of haloperidol, and their activity may influence the efficacy and safety of haloperidol. The use of haloperidol is often associated with the occurrence of adverse drug reactions (ADRs), such as dyskinesia, acute dystonia, and orthostatic hypotension. Previous studies have demonstrated the relationship between the CYP2D6...

Population pharmacokinetics analysis of camidanlumab tesirine in patients with relapsed...
https://doi.org/10.1007/s00280-022-04486-4
Cancer Chemotherapy and Pharmacology; Toukam M, Wuerthner J et. al.

Nov 6th, 2022 - The objective of this analysis was to develop a population pharmacokinetic (PPK) model to characterize camidanlumab tesirine (Cami) pharmacokinetics based on the phase 1 study in relapsed/refractory lymphoma (NCT02432235). An initial PPK model was developed based on a two-compartment model with parallel linear and nonlinear elimination pathways. Pharmacokinetic parameters were evaluated for cor...

Bruton's Tyrosine Kinase Inhibition in Multiple Sclerosis.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9607648
Current Neurology and Neuroscience Reports; Schneider R, Oh J

Oct 28th, 2022 - Multiple sclerosis (MS) is an inflammatory disease of the central nervous system (CNS) with a chronic and often progressive disease course. The current disease-modifying treatments (DMTs) limit disease progression primarily by dampening immune cell activity in the peripheral blood or hindering their migration from the periphery into the CNS. New therapies are needed to target CNS immunopatholog...

Baicalin lipid nanocapsules for treatment of glioma: characterization, mechanistic cyto...
https://doi.org/10.1080/17425247.2022.2139370
Expert Opinion on Drug Delivery; Ibrahim A, Abdel Gaber SA et. al.

Oct 27th, 2022 - Baicalin is a promising anticancer nutraceutical compound, but its application is hindered by its low water solubility and bioavailability, which can be remedied by its encapsulation in nanoparticles. Lipid nanocapsules (LNCs) were developed to enhance baicalin delivery via intravenous and intranasal routes, and potentiate its therapeutic activity in treatment of glioma. LNCs displayed a partic...

Safety, tolerability, pharmacokinetics and preliminary antitumour activity of an antise...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9594513
BMJ Open; Nishina T, Fujita T et. al.

Oct 22nd, 2022 - We assessed the safety, tolerability, pharmacokinetics, preliminary antitumour activity and pharmacodynamics of danvatirsen, an antisense oligonucleotide targeting signal transducer and activator of transcription 3 (STAT3), monotherapy and danvatirsen plus durvalumab, an antiprogrammed cell death ligand 1 monoclonal antibody, in patients with advanced solid malignancies. Phase 1, open-label stu...

Evaluation of Absorption and Metabolism-Based DDI Potential of Pexidartinib in Healthy ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9652259
Clinical Pharmacokinetics; Zahir H, Greenberg J et. al.

Oct 21st, 2022 - Pexidartinib is a novel oral small-molecule inhibitor that selectively targets colony-stimulating factor 1 receptor, KIT proto-oncogene receptor tyrosine kinase, and FMS-like tyrosine kinase 3 harboring an internal tandem duplication mutation. It is approved in the United States for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT) associated with severe morb...

Safety and efficacy of risdiplam in patients with type 1 spinal muscular atrophy (FIREF...
https://doi.org/10.1016/S1474-4422(22)00339-8
The Lancet. Neurology; Masson R, Mazurkiewicz-Bełdzińska M et. al.

Oct 17th, 2022 - Risdiplam is an orally administered therapy that modifies pre-mRNA splicing of the survival of motor neuron 2 (SMN2) gene and is approved for the treatment of spinal muscular atrophy. The FIREFISH study is investigating the safety and efficacy of risdiplam in treated infants with type 1 spinal muscular atrophy versus historical controls. The primary endpoint of part 2 of the FIREFISH study show...

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...

Population Pharmacokinetic Modeling of Bedaquiline among Multidrug-Resistant Pulmonary ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9578397
Antimicrobial Agents and Chemotherapy; Zou J, Chen S et. al.

Sep 16th, 2022 - Bedaquiline has been widely used as a part of combination dosage regimens for the treatment of multidrug-resistant tuberculosis (MDR-TB) patients with limited options. Although the effectiveness and safety of bedaquiline have been demonstrated in clinical trials, limited studies have investigated the significant pharmacokinetics and the impact of genotype on bedaquiline disposition. Here, we de...

Brain-restricted mTOR inhibition with binary pharmacology.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9492542
Nature Zhang Z, Fan Q et. al.

Sep 15th, 2022 - On-target-off-tissue drug engagement is an important source of adverse effects that constrains the therapeutic window of drug candidates1,2. In diseases of the central nervous system, drugs with brain-restricted pharmacology are highly desirable. Here we report a strategy to achieve inhibition of mammalian target of rapamycin (mTOR) while sparing mTOR activity elsewhere through the use of the b...

Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fum...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9578392
Antimicrobial Agents and Chemotherapy; Shimizu R, Sonoyama T et. al.

Sep 13th, 2022 - Ensitrelvir is a novel selective inhibitor of the 3C-like protease of SARS-CoV-2, which is essential for viral replication. This phase 1 study of ensitrelvir assessed its safety, tolerability, and pharmacokinetics of single (part 1, n = 50) and multiple (part 2, n = 33) ascending oral doses. Effect of food on the pharmacokinetics of ensitrelvir, differences in pharmacokinetics of ensitrelvir be...

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...

Ibrexafungerp: A new triterpenoid antifungal.
https://doi.org/10.1093/ajhp/zxac256
American Journal of Health-system Pharmacy : AJHP : Offic... Sucher AJ, Thai A et. al.

Sep 10th, 2022 - The pharmacology, microbiology, pharmacokinetics, pharmacodynamics, efficacy, safety, and role of ibrexafungerp in the treatment of fungal infections are reviewed. Ibrexafungerp is the first triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistanc...

Effects of Enzyme Induction and Polymorphism on the Pharmacokinetics of Isoniazid and R...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9578428
Antimicrobial Agents and Chemotherapy; Sundell J, Bienvenu E et. al.

Sep 8th, 2022 - Tuberculosis is the most common cause of death in HIV-infected individuals. Rifampin and isoniazid are the backbones of the current first-line antitubercular therapy. The aim of the present study was to describe the time-dependent pharmacokinetics and pharmacogenetics of rifampin and isoniazid and to quantitatively evaluate the drug-drug interaction between rifampin and isoniazid in patients co...

Altered Bioavailability and Pharmacokinetics in Crohn's Disease: Capturing Systems Para...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9553790
Clinical Pharmacokinetics; Alrubia S, Mao J et. al.

Sep 3rd, 2022 - Crohn's disease (CD) is a chronic inflammatory bowel disease that affects a wide age range. Hence, CD patients receive a variety of drugs over their life beyond those used for CD itself. The changes to the integrity of the intestine and its drug metabolising enzymes and transporters (DMETs) can alter the oral bioavailability of drugs. However, there are other changes in systems parameters deter...

Prediction of the pharmacokinetics of pemetrexed with a low test dose: A proof-of-conce...
https://doi.org/10.1111/bcp.15520
British Journal of Clinical Pharmacology; Boosman RJ, de Rouw N et. al.

Sep 3rd, 2022 - Pemetrexed is a cytotoxic drug used for the treatment of lung cancer and mesothelioma. The use of a low test dosing of cytotoxic drugs may aid in dose individualization without causing harm. The aim of this proof-of-concept study was to assess if the pharmacokinetics (PKs) of a test dose could predict the PKs of a therapeutic pemetrexed dose. Ten patients received both a low test dose (100 μg) ...

Bioequivalence and Relative Bioavailability Studies to Assess a New Acalabrutinib Formu...
https://doi.org/10.1002/cpdd.1153
Clinical Pharmacology in Drug Development; Sharma S, Pepin X et. al.

Aug 28th, 2022 - Acalabrutinib is a Bruton tyrosine kinase (BTK) inhibitor approved to treat adults with chronic lymphocytic leukemia, small lymphocytic lymphoma, or previously treated mantle cell lymphoma. As the bioavailability of the acalabrutinib capsule (AC) depends on gastric pH for solubility and is impaired by acid-suppressing therapies, coadministration with proton-pump inhibitors (PPIs) is not recomme...