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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
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  Data: <searchLink fieldCode="AU" term="%22Gangl+ET%22">Gangl ET</searchLink>; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts. Electronic address: eric.gangl@astrazeneca.com.<br /><searchLink fieldCode="AU" term="%22Markandu+R%22">Markandu R</searchLink>; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Sharma+P%22">Sharma P</searchLink>; Clinical Pharmacology and Quantitative Pharmacology, Clinical Pharmacology Safety Science, R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Sykes+A%22">Sykes A</searchLink>; Clinical Pharmacology and Quantitative Pharmacology, Clinical Pharmacology Safety Science, R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Pop-Damkov+P%22">Pop-Damkov P</searchLink>; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts.<br /><searchLink fieldCode="AU" term="%22Sarkar+U%22">Sarkar U</searchLink>; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts.<br /><searchLink fieldCode="AU" term="%22Andersson+L%22">Andersson L</searchLink>; Clinical Pharmacology Safety Science, AstraZeneca, Gothenburg, Sweden.<br /><searchLink fieldCode="AU" term="%22Morentin-Gutierrez+P%22">Morentin-Gutierrez P</searchLink>; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Scott+JS%22">Scott JS</searchLink>; Chemistry, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22Fretland+AJ%22">Fretland AJ</searchLink>; DMPK, Oncology R&D, AstraZeneca, Boston, 35 Gatehouse Drive, Waltham, Massachusetts.<br /><searchLink fieldCode="AU" term="%22Klinowska+T%22">Klinowska T</searchLink>; Late Development, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.<br /><searchLink fieldCode="AU" term="%22McGinnity+DF%22">McGinnity DF</searchLink>; DMPK, Oncology R&D, AstraZeneca, Cambridge, United Kingdom.
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