FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4367296502> ?p ?o ?g. }

• W4367296502 abstract "<h3>Objective:</h3> To assess mass balance recovery, pharmacokinetics, disposition, biotransformation, and elimination after a single intravenous (IV) dose of carbon-14 ([¹⁴C])-zavegepant. To conduct metabolite profiling and structural identification using plasma, urine, and fecal samples. To provide additional safety and tolerability information. <h3>Background:</h3> Zavegepant (BHV-3500) is a high-affinity, selective, small-molecule calcitonin gene-related peptide receptor antagonist in development for migraine treatment. <h3>Design/Methods:</h3> In this phase 1, open-label, single-center, single-period study, subjects received one 15-minute IV infusion of 5 mg [¹⁴C]-zavegepant containing ≤3.6 MBq [¹⁴C]. Over a 192-hour sampling period, multiple blood, urine, and fecal samples were collected to evaluate mass balance, pharmacokinetics (using noncompartmental analysis methods), and metabolite profiling and identification (using liquid chromatography radio detection and subsequent high-resolution mass spectrometry where appropriate). Safety assessments included treatment-emergent adverse events (TEAEs), Sheehan Suicidality Tracking Scale (S-STS), physical examinations, electrocardiograms, and clinical laboratory assessments. <h3>Results:</h3> Six healthy male participants (aged 39–60 years, body mass index 23.6–32.0 kg/m², S-STS score 0) were included. Of all radioactivity administered, 96.6% (range 92.1%–102.4%) was recovered in excreta, primarily in feces (mean 84.9% [range 79.7%–94.0%]). The geometric mean volume of distribution during the terminal phase, total clearance values, and plasma terminal half-life of zavegepant were 129 L, 220 mL/min, and 6.8 hours, respectively. Exposure to zavegepant accounted for ~90% of circulating plasma total reactivity of the area under the curve (time 0 extrapolated to infinity). Profiling identified zavegepant, but no metabolites representing ≥10% of radioactivity. Urine and feces contained 11.1% and 80.5% of the administered zavegepant dose, respectively. Three subjects (50.0%) reported ≥1 TEAE; all were mild and considered unrelated to zavegepant. No clinically significant changes were observed in safety parameters. <h3>Conclusions:</h3> An IV infusion of 5 mg [¹⁴C]-zavegepant in healthy men was primarily (>80%) recovered in feces indicating biliary excretion, underwent minimal metabolism, had substantial distribution into tissue, and was safe and well tolerated. <b>Disclosure:</b> The institution of Dr. Bhardwaj has received personal compensation in the range of $0-$499 for serving as a Consultant for Certara. Ms. Donohue has received personal compensation for serving as an employee of Biohaven Pharmaceuticals, Inc.. Ms. Donohue has received stock or an ownership interest from Biohaven Pharmaceuticals, Inc.. Joseph Stringfellow has nothing to disclose. Jennifer Madonia has received personal compensation for serving as an employee of Biohaven Pharmaceuticals. Jennifer Madonia has stock in Biohaven Pharmaceuticals. Matt Anderson has received personal compensation for serving as an employee of Certara. An immediate family member of Matt Anderson has received personal compensation for serving as an employee of Bristol Myers Squibb. Matt Anderson has received personal compensation in the range of $100,000-$499,999 for serving as a Consultant for Certara Strategic Consulting. An immediate family member of Matt Anderson has received stock or an ownership interest from Bristol Myers Squibb. Beth Morris has received personal compensation for serving as an employee of Biohaven Pharmaceuticals Inc. Beth Morris has received stock or an ownership interest from Biohaven Pharmaceuticals Inc. Vlad Coric has received personal compensation for serving as an employee of Biohaven. Vlad Coric has received stock or an ownership interest from Biohaven. Vlad Coric has received intellectual property interests from a discovery or technology relating to health care. Dr. Croop has received personal compensation for serving as an employee of Biohaven Pharmaceuticals, Inc. Dr. Croop has stock in Biohaven Pharmaceutical Holding Co Ltd. Dr. Croop has received intellectual property interests from a discovery or technology relating to health care. Richard Bertz has received personal compensation for serving as an employee of Biohaven Pharmaceuticals. Richard Bertz has stock in Biohaven Pharmaceuticals." @default.
• W4367296502 created "2023-04-29" @default.
• W4367296502 creator A5020246660 @default.
• W4367296502 creator A5023069774 @default.
• W4367296502 creator A5026430249 @default.
• W4367296502 creator A5060859207 @default.
• W4367296502 creator A5066209993 @default.
• W4367296502 creator A5069362203 @default.
• W4367296502 creator A5077048090 @default.
• W4367296502 creator A5086458638 @default.
• W4367296502 creator A5090664407 @default.
• W4367296502 date "2023-04-25" @default.
• W4367296502 modified "2023-09-26" @default.
• W4367296502 title "Pharmacokinetics, Disposition, and Biotransformation of 5 mg [14C]-Zavegepant in Healthy Male Subjects After a Single Intravenous Infusion Dose (P9-12.008)" @default.
• W4367296502 doi "https://doi.org/10.1212/wnl.0000000000203200" @default.
• W4367296502 hasPublicationYear "2023" @default.
• W4367296502 type Work @default.
• W4367296502 citedByCount "0" @default.
• W4367296502 crossrefType "proceedings-article" @default.
• W4367296502 hasAuthorship W4367296502A5020246660 @default.
• W4367296502 hasAuthorship W4367296502A5023069774 @default.
• W4367296502 hasAuthorship W4367296502A5026430249 @default.
• W4367296502 hasAuthorship W4367296502A5060859207 @default.
• W4367296502 hasAuthorship W4367296502A5066209993 @default.
• W4367296502 hasAuthorship W4367296502A5069362203 @default.
• W4367296502 hasAuthorship W4367296502A5077048090 @default.
• W4367296502 hasAuthorship W4367296502A5086458638 @default.
• W4367296502 hasAuthorship W4367296502A5090664407 @default.
• W4367296502 hasConcept C112705442 @default.
• W4367296502 hasConcept C126322002 @default.
• W4367296502 hasConcept C139254425 @default.
• W4367296502 hasConcept C151730666 @default.
• W4367296502 hasConcept C185592680 @default.
• W4367296502 hasConcept C197934379 @default.
• W4367296502 hasConcept C2777477808 @default.
• W4367296502 hasConcept C2778375690 @default.
• W4367296502 hasConcept C2780026642 @default.
• W4367296502 hasConcept C43617362 @default.
• W4367296502 hasConcept C61716771 @default.
• W4367296502 hasConcept C71924100 @default.
• W4367296502 hasConcept C86803240 @default.
• W4367296502 hasConcept C98274493 @default.
• W4367296502 hasConceptScore W4367296502C112705442 @default.
• W4367296502 hasConceptScore W4367296502C126322002 @default.
• W4367296502 hasConceptScore W4367296502C139254425 @default.
• W4367296502 hasConceptScore W4367296502C151730666 @default.
• W4367296502 hasConceptScore W4367296502C185592680 @default.
• W4367296502 hasConceptScore W4367296502C197934379 @default.
• W4367296502 hasConceptScore W4367296502C2777477808 @default.
• W4367296502 hasConceptScore W4367296502C2778375690 @default.
• W4367296502 hasConceptScore W4367296502C2780026642 @default.
• W4367296502 hasConceptScore W4367296502C43617362 @default.
• W4367296502 hasConceptScore W4367296502C61716771 @default.
• W4367296502 hasConceptScore W4367296502C71924100 @default.
• W4367296502 hasConceptScore W4367296502C86803240 @default.
• W4367296502 hasConceptScore W4367296502C98274493 @default.
• W4367296502 hasLocation W43672965021 @default.
• W4367296502 hasOpenAccess W4367296502 @default.
• W4367296502 hasPrimaryLocation W43672965021 @default.
• W4367296502 hasRelatedWork W1976890451 @default.
• W4367296502 hasRelatedWork W2033723429 @default.
• W4367296502 hasRelatedWork W2046684621 @default.
• W4367296502 hasRelatedWork W2046827994 @default.
• W4367296502 hasRelatedWork W2071248898 @default.
• W4367296502 hasRelatedWork W2107461711 @default.
• W4367296502 hasRelatedWork W2148177218 @default.
• W4367296502 hasRelatedWork W2169566797 @default.
• W4367296502 hasRelatedWork W2415732068 @default.
• W4367296502 hasRelatedWork W3120625362 @default.
• W4367296502 isParatext "false" @default.
• W4367296502 isRetracted "false" @default.
• W4367296502 workType "article" @default.