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The aim of reported development program of novel dasatinib anhydrate containing formulation was to demonstrate improved absorption and lower pharmacokinetic variability compared to dasatinib monohydrate. In a bioavailability study comparing formulations containing 110.6\u2009mg and 140\u2009mg of dasatinib as anhydrate and monohydrate, respectively, both C<jats:sub>max<\/jats:sub> and AUC of dasatinib were within standard 80.00\u2013125.00% range, while the intra- and inter-subject variability for AUC<jats:sub>0-inf<\/jats:sub> after the test product was approximately 3-fold and 1.5-fold less than after the reference, respectively.<\/jats:p><jats:p>In a drug\u2013drug interaction study, omeprazole 40\u2009mg reduced the mean AUC<jats:sub>0-inf<\/jats:sub> of dasatinib by 19%, when the test was ingested 2\u2009h before the 5th omeprazole dose. This decrease of exposure is clinically irrelevant and substantially less than after the reference. Co-prescription analysis supports the importance of pH-dependent solubility of dasatinib, as &gt;21% of patients were treated concomitantly with a PPI and dasatinib despite warnings against this co-medication in the SmPC.<\/jats:p><jats:p>The novel dasatinib anhydrate containing formulation demonstrated improved absorption and less pharmacokinetic variability compared to dasatinib monohydrate product, which may translate into improved clinical outcomes, although this needs to be proven by an appropriate trial.<\/jats:p>","DOI":"10.1038\/s41375-023-02045-1","type":"journal-article","created":{"date-parts":[[2023,10,3]],"date-time":"2023-10-03T14:02:55Z","timestamp":1696341775000},"page":"2486-2492","update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Dasatinib anhydrate containing oral formulation improves variability and bioavailability in humans"],"prefix":"10.1038","volume":"37","author":[{"given":"Ji\u0159\u00ed","family":"Hofmann","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ale\u0161","family":"Bart\u016fn\u011bk","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tom\u00e1\u0161","family":"Hauser","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gregor","family":"Sedmak","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Josef","family":"Ber\u00e1nek","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6727-1663","authenticated-orcid":false,"given":"Pavel","family":"Ry\u0161\u00e1nek","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6541-738X","authenticated-orcid":false,"given":"Martin","family":"\u0160\u00edma","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5357-7562","authenticated-orcid":false,"given":"Ond\u0159ej","family":"Slana\u0159","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"297","published-online":{"date-parts":[[2023,10,3]]},"reference":[{"key":"2045_CR1","doi-asserted-by":"publisher","first-page":"393","DOI":"10.1111\/bjh.17654","volume":"194","author":"P Rousselot","year":"2021","unstructured":"Rousselot P, Mollica L, Guilhot J, Guerci A, Nicolini FE, Etienne G, et al. 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