Evaluating the Impact of CYP1A2 Inhibition on the Pharmacokinetics of Savolitinib: A Phase 1 Open-Label Study.

Kowser Miah¹, Jitendar Reddy², Pradeep Sharma², Ike Igwegbe³, Simon Nelson⁴, Caitlin Muldoon⁵, Ronald Goldwater⁶, Karthick Vishwanathan¹

¹Clinical Pharmacology and Quantitative Pharmacology, CPSS, AstraZeneca, Waltham, Massachusetts, USA.

²Clinical Pharmacology and Quantitative Pharmacology, CPSS, AstraZeneca, Cambridge, UK.

³Global Clinical Program, AstraZeneca, Gaithersburg, Maryland, USA.

⁴Patient Safety Oncology, AstraZeneca, Cambridge, UK.

⁵Late Oncology Statistics, AstraZeneca, Cambridge, UK.

⁶Early Phase Clinical Unit, Parexel, Baltimore, Maryland, USA.

PubMed DOI

Abstract

Savolitinib is an oral, potent, selective CNS-penetrant MET-tyrosine kinase inhibitor that in vitro studies indicate is metabolized by cytochrome P450 (CYP) enzymes, including CYP1A2, and by non-CYP enzymes, such as aldehyde oxidase (AO). Savolitinib primary metabolites, M2 and M3, are formed mainly by CYP1A2 and AO, respectively. This Phase 1, open-label study evaluated the impact of CYP1A2 inhib…

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