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The application of mechanistic absorption, distribution, metabolism and excretion studies and physiologically-based pharmacokinetic modeling in the discovery of the next-generation oral selective estrogen receptor degrader camizestrant to achieve an acceptable human pharmacokinetic profile.

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Title: The application of mechanistic absorption, distribution, metabolism and excretion studies and physiologically-based pharmacokinetic modeling in the discovery of the next-generation oral selective estrogen receptor degrader camizestrant to achieve an acceptable human pharmacokinetic profile.
Authors: Gangl ET; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts. Electronic address: eric.gangl@astrazeneca.com., Markandu R; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom., Sharma P; Clinical Pharmacology and Quantitative Pharmacology, Clinical Pharmacology Safety Science, R&D, AstraZeneca, Cambridge, United Kingdom., Sykes A; Clinical Pharmacology and Quantitative Pharmacology, Clinical Pharmacology Safety Science, R&D, AstraZeneca, Cambridge, United Kingdom., Pop-Damkov P; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts., Sarkar U; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts., Andersson L; Clinical Pharmacology Safety Science, AstraZeneca, Gothenburg, Sweden., Morentin-Gutierrez P; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom., Scott JS; Chemistry, Oncology R&D, AstraZeneca, Cambridge, United Kingdom., Fretland AJ; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts., Klinowska T; Late Development, Oncology R&D, AstraZeneca, Cambridge, United Kingdom., McGinnity DF; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.
Source: Drug metabolism and disposition: the biological fate of chemicals [Drug Metab Dispos] 2025 Aug; Vol. 53 (8), pp. 100110. Date of Electronic Publication: 2025 Jun 19.
Publication Type: Journal Article
Journal Info: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 9421550 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-009X (Electronic) Linking ISSN: 00909556 NLM ISO Abbreviation: Drug Metab Dispos Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1521-009X
DOI:10.1016/j.dmd.2025.100110