A Phase 1 Mass Balance Study of 14C‐Labeled Talazoparib in Patients With Advanced Solid Tumors

• DOI: 10.1002/jcph.1415
• Publication Date: 2019-04-09T16:54:43Z
• Authors: Yanke Yu; Chin‐Hee Chung; Anna Plotka; Kevin Quinn; Haihong Shi; Zsuzsanna Pápai; Linh Nguyen; Diane Wang
• Keywords: Adult; Aged, 80 and over; Male; Administration, Oral; Middle Aged; 6. Clean water; 3. Good health; Feces; 03 medical and health sciences; 0302 clinical medicine; Neoplasms; Humans; Phthalazines; Female; Carbon Radioisotopes; Aged; Half-Life

Abstract This paper describes the pharmacokinetics (PK), mass balance, metabolic profiling, and safety of talazoparib after a single oral dose 14 C‐talazoparib in 6 patients with advanced solid tumors. Patients were aged ≥18 years, histologically confirmed tumor at screening. A 1‐mg solution supplemented 100 µCi C‐labeled was administered. Blood, urine, feces samples collected various time points analyzed for C radioactivity. Metabolic profiling identification also carried out. Mean recovery radioactivity 68.7% urine 19.7% feces. Talazoparib minimally metabolized. Renal excretion unchanged major route elimination, mean 54.6% administered dose, whereas fecal limited, 13.6% dose. No metabolites identified plasma, no that individually represented more than 10% recovered or The concentration‐time profiles talazoparib, total whole blood similar, median peak concentrations 30 minutes half‐life 89.8, 96.2, 77.6 hours, respectively. metabolized, renal elimination.