Effects of GLPG3970 on Sulfasalazine and Methotrexate Pharmacokinetics in Healthy Adults: Two Open-Label, Phase I, Drug-Drug Interaction Studies.

ABSTRACT: GLPG3970 is a selective salt-inducible kinase 2/3 inhibitor intended for the treatment of inflammatory diseases. In vitro studies suggest GLPG3970 strongly inhibits breast cancer resistance protein (BCRP), indicating a possible interaction with BCRP substrates such as sulfasalazine (SSZ; a probe substrate for intestinal BCRP inhibition) and methotrexate (MTX), both inflammatory disease medications. Two open-label, nonrandomized, phase I, drug-drug interaction (DDI) studies assessed the pharmacokinetics of SSZ 1,000 mg (NCT04720183) and MTX 7.5 mg (EudraCT: 2020-000391-37) with and without GLPG3970 350 mg. Healthy participants aged 18-55 years with wild-type homozygous BCRP genotype (c421C/C) received: SSZ on day (D)1, GLPG3970 + SSZ on D5, and GLPG3970 2 hours after SSZ on D9 (N = 8; SSZ/G

SUBMITTER: van der Plas M 

PROVIDER: S-EPMC11739741 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature