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Elimusertib (BAY\u20101895344) is an orally available small\u2010molecule ATR inhibitor currently in preclinical and clinical development for cancer treatment. To support these studies and define elimusertib pharmacokinetics, we developed a HPLC\u2013MS method for its quantitation. A 50\u2010\u03bcL volume of plasma was subjected to acetonitrile protein precipitation and then chromatographic separation using a Phenomenex Polar\u2010RP column (2\u2009\u00d7\u200950\u2009mm, 4\u00a0\u03bcm) and a gradient mobile phase consisting of 0.1% formic acid in acetonitrile and water during a 7\u2010min run time. Mass spectrometric detection was achieved using a SCIEX 4000 triple\u2010stage mass spectrometer with electrospray positive\u2010mode ionization. With a stable isotopic internal standard, the assay was linear from 30 to 5000\u2009ng\/mL and proved to be both accurate (93.5\u2013108.2%) and precise (&lt;6.3% coefficient of variation) fulfilling criteria from the Food and Drug Administration guidance on bioanalytical method validation. This LC\u2013MS\/MS assay will support several ongoing clinical studies by defining elimusertib pharmacokinetics.<\/jats:p>","DOI":"10.1002\/bmc.5455","type":"journal-article","created":{"date-parts":[[2022,7,25]],"date-time":"2022-07-25T10:54:20Z","timestamp":1658746460000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Quantitation of the ataxia\u2010telangiectasia\u2010mutated and Rad3\u2010related inhibitor elimusertib (BAY\u20101895344) in human plasma using LC\u2013MS\/MS"],"prefix":"10.1002","volume":"36","author":[{"given":"Brian F.","family":"Kiesel","sequence":"first","affiliation":[{"name":"Cancer Therapeutics Program UPMC Hillman Cancer Center  Pittsburgh Pennsylvania USA"},{"name":"Department of Pharmaceutical Sciences, School of Pharmacy University of Pittsburgh  Pittsburgh Pennsylvania USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert A.","family":"Parise","sequence":"additional","affiliation":[{"name":"Cancer Therapeutics Program UPMC Hillman Cancer Center  Pittsburgh Pennsylvania USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Anuradha","family":"Krishnamurthy","sequence":"additional","affiliation":[{"name":"Division of Hematology\u2010Oncology, Department of Medicine University of Pittsburgh School of Medicine  Pittsburgh Pennsylvania USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Steven","family":"Gore","sequence":"additional","affiliation":[{"name":"Investigational Drug Branch, Cancer Therapy Evaluation Program, Division of Cancer Treatment and Diagnosis National Cancer Institute  Bethesda Maryland USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8978-9401","authenticated-orcid":false,"given":"Jan H.","family":"Beumer","sequence":"additional","affiliation":[{"name":"Cancer Therapeutics Program UPMC Hillman Cancer Center  Pittsburgh Pennsylvania USA"},{"name":"Department of Pharmaceutical Sciences, School of Pharmacy University of Pittsburgh  Pittsburgh Pennsylvania USA"},{"name":"Division of Hematology\u2010Oncology, Department of Medicine University of Pittsburgh School of Medicine  Pittsburgh Pennsylvania USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2022,8,8]]},"reference":[{"issue":"8","key":"e_1_2_6_2_1","first-page":"755","article-title":"The pivotal role of drug metabolism and pharmacokinetics in the discovery and development of new medicines","volume":"7","author":"Alavijeh M. 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