Single-dose of LC51-0255, a selective S1P₁ receptor modulator, showed dose-dependent and reversible reduction of absolute lymphocyte count in humans.

ABSTRACT: Reducing the peripheral absolute lymphocyte count (ALC) is a promising therapeutic approach in treating autoimmune diseases. LC51-0255 is a sphingosine-1-phosphate 1 receptor modulator, which is known to decrease the peripheral ALC. We aimed to assess the pharmacokinetics (PKs), pharmacodynamics (PDs), safety, and tolerability profiles of LC51-0255 after a single oral administration in healthy subjects. A randomized, double-blind, placebo-controlled, dose-escalation study was conducted in 50 healthy subjects. Each subject orally received LC51-0255 (0.25, 0.5, 1, 2, or 4 mg) or its matching placebo in an 8:2 ratio. Blood and urine samples were collected to assess the PKs, and PDs was evaluated using peripheral ALC and 24-h hourly heart rate data. Safety and tolerability were assessed by mon

SUBMITTER: Won Lee S 

PROVIDER: S-EPMC9010277 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature