Pharmacokinetics, Metabolism, and Excretion of Intravenous [14C]Difelikefalin in Healthy Subjects and Subjects on Hemodialysis.

ABSTRACT:

Background and objective

Difelikefalin, a selective kappa-opioid receptor agonist, is the first approved treatment for moderate-to-severe pruritus in patients with end-stage renal disease (ESRD) on hemodialysis (HD) in the USA and Europe. The purpose of this open-label study was to investigate the pharmacokinetics and disposition of [¹⁴C]difelikefalin following a single intravenous dose in subjects with normal renal function and subjects on HD.

Methods

Twelve adult males (n = 6 healthy subjects; n = 6 subjects on HD) received single intravenous doses of [¹⁴C]difelikefalin containing 100 µCi (total doses of 1.7-3.0 μg/kg difelikefalin). Blood, urine, feces, and dialysate samples (when applicable) were collected after dosing.

Results

The median tim

SUBMITTER: Stark JG 

PROVIDER: S-EPMC10450003 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature