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Phase 1 Studies to Assess Inhaled Seralutinib as a Perpetrator or a Victim of Drug-Drug Interactions in Healthy Participants.
Clin Pharmacol Drug Dev
December 2024
Gossamer Bio, Inc., San Diego, CA, USA.
Seralutinib, an inhaled, small-molecule tyrosine kinase inhibitor in clinical development for the treatment of pulmonary arterial hypertension (PAH), was evaluated for its potential as a perpetrator or victim of a metabolic and transporter-based drug-drug interactions in 2 phase 1 studies. In study 1, 24 participants received a cocktail of probe substrates: caffeine (CYP1A2), montelukast (CYP2C8), flurbiprofen (CYP2C9), midazolam (CYP3A), and pravastatin (OATP1B1/1B3), plus digoxin (P-gp) with or without seralutinib. In study 2, 19 participants received seralutinib with/without itraconazole, a strong CYP3A inhibitor, or fosaprepitant, a weak CYP3A inhibitor.
View Article and Find Full Text PDFImprove Solubility and Develop Personalized Itraconazole Dosages via Forming Amorphous Solid Dispersions with Hydrophilic Polymers Utilizing HME and 3D Printing Technologies.
Polymers (Basel)
November 2024
Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Article Synopsis
- Itraconazole (ITZ) is a broad-spectrum antifungal with low oral bioavailability due to poor solubility and potential dose-related side effects.
- Researchers aimed to improve ITZ's solubility using various water-soluble polymers and developed personalized, programmable release tablets.
- The study found that using hot melt extrusion (HME) combined with 3D printing can enhance ITZ solubility and allow for precise control of its release, offering a promising method for personalized drug delivery.
Deconvoluting zavegepant drug-drug interactions: A phase I study to evaluate the effects of rifampin and itraconazole on zavegepant pharmacokinetics.
Clin Transl Sci
December 2024
Pfizer Inc., Groton, Connecticut, USA.
Zavegepant is a calcitonin gene-related peptide receptor antagonist for acute migraine treatment. This Phase I, open-label, fixed-sequence study evaluated the effects of itraconazole (a strong cytochrome P450 3A4 [CYP3A4] and P-glycoprotein [P-gp] inhibitor) on the pharmacokinetics of intranasal/oral zavegepant and the effects of rifampin (a strong inducer of CYP3A4 and P-gp; and an inhibitor of organic anion transporting polypeptide 1B3 [OATP1B3]) on oral zavegepant in healthy participants. In the intranasal/oral zavegepant-itraconazole cohort, participants received a single 10-mg dose of zavegepant nasal spray on Day 1, followed by oral zavegepant (50 mg) on Day 3.
View Article and Find Full Text PDFIntratracheal Administration of Itraconazole-Loaded Hyaluronated Glycerosomes as a Promising Nanoplatform for the Treatment of Lung Cancer: Formulation, Physiochemical, and In Vivo Distribution.
Pharmaceutics
November 2024
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Nile Valley University, Fayoum 63518, Egypt.
Background: Itraconazole (ITZ) is an antiangiogenic agent recognized as a potent suppressor of endothelial cell growth that suppresses angiogenesis. Nevertheless, its exploitation is significantly restricted by its low bioavailability and systematic side effects. The objective of this study was to utilize glycerosomes (GLY), glycerol-developed vesicles, as innovative nanovesicles for successful ITZ pulmonary drug delivery.
View Article and Find Full Text PDFClinical and Physiologically Based Pharmacokinetic Model Evaluations of Adagrasib Drug-Drug Interactions.
Clin Pharmacol Ther
November 2024
Clinical Pharmacology and Nonclinical Development, Mirati Therapeutics Inc. (A Bristol Myers Squib Company), San Diego, California, USA.
Adagrasib is a potent, highly selective, orally available, small molecule, covalent inhibitor of G12C mutated KRAS. As both a substrate and strong inhibitor of cytochrome P450 (CYP) 3A4, adagrasib inhibits its own CYP3A4-mediated metabolism following multiple dosing, resulting in time-dependent drug-drug interaction (DDI) liabilities. A physiologically-based pharmacokinetic (PBPK) model was developed and verified using a combination of physicochemical, in vitro and clinical pharmacokinetic (PK) data from healthy volunteers and cancer patients.
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