biostudies-literatureUnknown11(7)Singh RSPZimlovisertib (PF-06650833) is a selective, reversible inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) with anti-inflammatory effects. This phase 1, open-label, fixed-sequence, two-period, single-dose study aimed to evaluate the mass balance and excretion rate of zimlovisertib in healthy male participants using a ¹⁴ C-microtracer approach. All six participants received 300 mg ¹⁴ C-zimlovisertib with lower radioactivity per mass unit orally in Period A, then unlabeled zimlovisertib 300 mg orally and ¹⁴ C-zimlovisertib 135 μg intravenously (IV) in Period B. Study objectives included extent and rate of excretion of ¹⁴ C-zimlovisertib, pharmacokinetics, and safety and tolerability of oral and IV zimlovisertib. Total radioactivity recoClinical pharmacology in drug development815-825https://www.ebi.ac.uk/biostudies/studies/S-EPMC9322294biostudies-literatureA Phase 1 Study to Assess Mass Balance and Absolute Bioavailability of Zimlovisertib in Healthy Male Participants Using a ¹⁴ C-Microtracer Approach.PMC9322294Salganik MSharma RWalker GSDowty MEBeebe JSSingh RSPDanto SIBrodfuehrer JIfalseA Phase 1 Study to Assess Mass Balance and Absolute Bioavailability of Zimlovisertib in Healthy Male Participants Using a ¹⁴ C-Microtracer Approach.Zimlovisertib (PF-06650833) is a selective, reversible inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) with anti-inflammatory effects. This phase 1, open-label, fixed-sequence, two-period, single-dose study aimed to evaluate the mass balance and excretion rate of zimlovisertib in healthy male participants using a ¹⁴ C-microtracer approach. All six participants received 300 mg ¹⁴ C-zimlovisertib with lower radioactivity per mass unit orally in Period A, then unlabeled zimlovisertib 300 mg orally and ¹⁴ C-zimlovisertib 135 μg intravenously (IV) in Period B. Study objectives included extent and rate of excretion of ¹⁴ C-zimlovisertib, pharmacokinetics, and safety and tolerability of oral and IV zimlovisertib. Total radioactivity reco2022-01-01T00:00:00Z2022 Jul2025-04-22T03:25:01.674Z2025-04-05T20:44:06.668ZS-EPMC93222943550650110.1002/cpdd.1109