Pharmacokinetic profile and <i>in vivo</i> anticancer efficacy of anagrelide administered subcutaneously in rodents.

ABSTRACT: Anagrelide (ANA) is a phosphodiesterase 3A (PDE3A) inhibitor, commonly prescribed for essential thrombocythemia. It also functions as a molecular glue, inducing complex formation between PDE3A and Schlafen 12. This association either triggers apoptosis or inhibits proliferation in tumor cells, supporting its use in cancer therapy. Conventionally administered orally, ANA undergoes rapid metabolism and elimination, resulting in a short drug exposure time at the site of action. Here, we explored the pharmacokinetic profile of a subcutaneously (SC) injected ANA formulation in Sprague-Dawley rats by quantifying plasma ANA and metabolite concentrations using liquid-chromatography-tandem mass spectrometry. We further evaluated the in vivo tumor regression efficacy of orally and SC administ

SUBMITTER: Toivanen K 

PROVIDER: S-EPMC11816618 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature