Clinical assessment of mocravimod as a victim of drug-drug interactions via CYP3A4 metabolism and transporters.

ABSTRACT: Mocravimod, a novel immunomodulator targeting sphingosine-1-phosphate receptor (S1PR), is being developed as a maintenance treatment for patients with acute myeloid leukemia undergoing allogeneic hematopoietic cell transplantation. Preclinical data suggested that cytochrome (CYP) 3A4 is the primary enzyme involved in mocravimod metabolism. In vitro data showed that both mocravimod and its active metabolite mocravimod-phosphate are substrates for breast cancer resistance protein (BCRP) and P-glycoprotein (P-gp) but not for organic-anion-transporting polypeptides (OATP1B1 and OATP1B3). As mocravimod is co-administered with CYP3A4 inhibitors such as azoles or cyclosporin, the potential for drug-drug interactions (DDIs) was evaluated. In addition, the effect of BCRP, P-gp, and OATP via cyclosp

SUBMITTER: Huntjens DR 

PROVIDER: S-EPMC12933224 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature