{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T00:46:00Z","timestamp":1787013960534,"version":"build-2736575974"},"reference-count":67,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2024,2,6]],"date-time":"2024-02-06T00:00:00Z","timestamp":1707177600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100003246","name":"Nederlandse Organisatie voor Wetenschappelijk Onderzoek","doi-asserted-by":"publisher","award":["Vici grant 09150181910040"],"award-info":[{"award-number":["Vici grant 09150181910040"]}],"id":[{"id":"10.13039\/501100003246","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[2024,6]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:sec>\n                    <jats:title>Background and Purpose<\/jats:title>\n                    <jats:p>Multiple drugs targeting the calcitonin gene\u2010related peptide (CGRP) receptor have been developed for migraine treatment. Here, the effect of the monoclonal antibody erenumab on CGRP\u2010induced vasorelaxation was investigated in human isolated blood vessels, as well as the effect of combining erenumab with the small molecule drugs, namely rimegepant, olcegepant, or sumatriptan.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Experimental Approach<\/jats:title>\n                    <jats:p>\n                      Concentration\u2013response curves to CGRP, adrenomedullin or pramlintide were constructed in human coronary artery (HCA) and human middle meningeal artery (HMMA) segments, incubated with or without erenumab and\/or olcegepant. pA\n                      <jats:sub>2<\/jats:sub>\n                      or pK\n                      <jats:sub>b<\/jats:sub>\n                      values were calculated to determine the potency of erenumab in both tissues. To study whether acutely acting antimigraine drugs exerted additional CGRP\u2010blocking effects on top of erenumab, HCA segments were incubated with a maximally effective concentration of erenumab (3\u00a0\u03bcM), precontracted with KCl and exposed to CGRP, followed by rimegepant, olcegepant, or sumatriptan in increasing concentrations.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Key Results<\/jats:title>\n                    <jats:p>Erenumab shifted the concentration\u2010response curve to CGRP in both vascular tissues. However, in HCA, the Schild plot slope was significantly smaller than unity, whereas this was not the case in HMMA, indicating different CGRP receptor mechanisms in these tissues. In HCA, rimegepant, olcegepant and sumatriptan exerted additional effects on CGRP on top of a maximal effect of erenumab.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Conclusions and Implications<\/jats:title>\n                    <jats:p>Gepants have additional effects on top of erenumab for CGRP\u2010induced relaxation and could be effective in treating migraine attacks in patients already using erenumab as prophylaxis.<\/jats:p>\n                  <\/jats:sec>","DOI":"10.1111\/bph.16322","type":"journal-article","created":{"date-parts":[[2024,2,7]],"date-time":"2024-02-07T02:10:29Z","timestamp":1707271829000},"page":"1720-1733","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Pharmacology of erenumab in human isolated coronary and meningeal arteries: Additional effect of gepants on top of a maximum effect of erenumab"],"prefix":"10.1111","volume":"181","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5078-6764","authenticated-orcid":false,"given":"Tessa","family":"de Vries","sequence":"first","affiliation":[{"name":"Division of Vascular Medicine and Pharmacology, Department of Internal Medicine Erasmus University Medical Center  Rotterdam The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elo\u00edsa","family":"Rubio\u2010Beltr\u00e1n","sequence":"additional","affiliation":[{"name":"Division of Vascular Medicine and Pharmacology, Department of Internal Medicine Erasmus University Medical Center  Rotterdam The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Antoon","family":"van den Bogaerdt","sequence":"additional","affiliation":[{"name":"Heart Valve Department ETB\u2010BISLIFE  Beverwijk The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ruben","family":"Dammers","sequence":"additional","affiliation":[{"name":"Department of Neurosurgery Erasmus University Medical Center  The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5052-3585","authenticated-orcid":false,"given":"A. H. Jan","family":"Danser","sequence":"additional","affiliation":[{"name":"Division of Vascular Medicine and Pharmacology, Department of Internal Medicine Erasmus University Medical Center  Rotterdam The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Josefin","family":"Snellman","sequence":"additional","affiliation":[{"name":"Novartis Pharma AG  Basel Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jeanine","family":"Bussiere","sequence":"additional","affiliation":[{"name":"Amgen Inc  Thousand Oaks California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Antoinette","family":"MaassenVanDenBrink","sequence":"additional","affiliation":[{"name":"Division of Vascular Medicine and Pharmacology, Department of Internal Medicine Erasmus University Medical Center  Rotterdam The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2024,2,6]]},"reference":[{"key":"e_1_2_12_2_1","unstructured":"AbbVie Inc. (2021).FDA Approves QULIPTA\u2122 (atogepant) the First and Only Oral CGRP Receptor Antagonist Specifically Developed for the Preventive Treatment of Migraine. InPR Newswire.https:\/\/www.prnewswire.com\/news-releases\/fda-approves-qulipta-atogepant-the-first-and-only-oral-cgrp-receptor-antagonist-specifically-developed-for-the-preventive-treatment-of-migraine-301387297.html"},{"key":"e_1_2_12_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.15538"},{"key":"e_1_2_12_4_1","unstructured":"Allergan plc. (2019).Allergan receives U.S. FDA approval for UBRELVY\u2122 for the acute treatment of migraine with or without aura in adults.https:\/\/www.prnewswire.com\/news-releases\/allergan-receives-us-fda-approval-for-ubrelvy-for-the-acute-treatment-of-migraine-with-or-without-aura-in-adults-300979082.html: PR Newswire."},{"key":"e_1_2_12_5_1","unstructured":"Amgen Inc. (2021).AIMOVIG (erenumab\u2010aooe) prescribing information.https:\/\/www.accessdata.fda.gov\/drugsatfda_docs\/label\/2021\/761077s009lbl.pdf"},{"key":"e_1_2_12_6_1","doi-asserted-by":"publisher","DOI":"10.1111\/head.13930"},{"key":"e_1_2_12_7_1","doi-asserted-by":"publisher","DOI":"10.1177\/0333102420983282"},{"key":"e_1_2_12_8_1","unstructured":"Biohaven Pharmaceutical Company Holding Ltd. (2020a).Biohaven's NURTEC\u2122 ODT (rimegepant) receives FDA approval for the acute treatment of migraine in adults.https:\/\/www.prnewswire.com\/news-releases\/biohavens-nurtec-odt-rimegepant-receives-fda-approval-for-the-acute-treatment-of-migraine-in-adults-301013021.html: PR Newswire."},{"key":"e_1_2_12_9_1","unstructured":"Biohaven Pharmaceutical Company Holding Ltd. (2020b).Rimegepant (Nurtec\u2122 ODT): US prescribing information. Available fromhttps:\/\/www.accessdata.fda.gov\/drugsatfda_docs\/label\/2020\/212728s000lbl.pdf(accessed 2023)"},{"key":"e_1_2_12_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.yrtph.2019.05.013"},{"key":"e_1_2_12_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejphar.2005.12.039"},{"key":"e_1_2_12_12_1","doi-asserted-by":"publisher","DOI":"10.1007\/s40263-013-0136-0"},{"key":"e_1_2_12_13_1","doi-asserted-by":"crossref","unstructured":"Conway C. M. Croop R. Dubowchik G. M. Coric V. &Lipton R. B.(2019).Cardiovascular safety of rimegepant 75 mg in 3 randomized clinical trials and systematic evaluations from in vitro ex vivo and in vivo nonclinical assays. In American Headache Society 2019 Annual Scientific Meeting. Philadelphia PA.","DOI":"10.1212\/WNL.94.15_supplement.2141"},{"key":"e_1_2_12_14_1","volume-title":"American Headache Society 61st Annual Scientific Meeting","author":"Conway C. 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