Publications by authors named "R Bertz"
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 PDFObjective: To compare the rate and extent of absorption of zavegepant 10 mg (therapeutic dose) or 20 mg (supratherapeutic dose) nasal spray during a migraine attack versus non-migraine period, assess safety, and explore efficacy and the relationship between zavegepant concentration and therapeutic response.
Background: Physiologic changes occurring during a migraine attack could affect the pharmacokinetics of treatments for migraine.
Methods: This was a Phase 1, multicenter, open-label, randomized, single-dose, two-period, fixed-sequence, comparative bioavailability study.
Article Synopsis
- The study aimed to investigate how the intranasal drug zavegepant affects the pharmacokinetics of the oral contraceptive ethinyl estradiol and levonorgestrel (EE-LNG) when taken together.
- It involved healthy females aged 18-45, who received a single dose of EE-LNG followed by multiple doses of zavegepant, with blood samples collected to analyze drug concentrations.
- Results indicated minor and statistically insignificant changes in the levels of EE and LNG when zavegepant was co-administered, with some common side effects noted such as dysgeusia and throat irritation.
Article Synopsis
- Zavegepant (ZAVZPRET™) is a selective medication for treating acute migraines in adults, targeting specific receptors related to migraine pathways.
- A comprehensive analysis of its pharmacokinetics determined how zavegepant is absorbed, distributed, and eliminated from the body, utilizing data from multiple clinical trials.
- The findings revealed that zavegepant has low bioavailability rates when taken intranasally (5.1%) or orally (0.65%), with factors like age and sex not significantly affecting its pharmacokinetics, but certain conditions (like moderate liver impairment) could impact its clearance.
Article Synopsis
- The study aimed to assess how zavegepant and sumatriptan interact pharmacodynamically (PD) and pharmacokinetically (PK) when administered together in healthy adults to understand their effects on migraine treatment.
- Zavegepant, a nasal spray for migraine, and sumatriptan, an injectable triptan, have different mechanisms and possible side effects, particularly concerning blood pressure, making their interaction important for possible joint use in patients.
- The Phase 1 study involved 42 participants and found that blood pressure and safety were generally unchanged when both drugs were taken together, suggesting they may be safe to coadminister.