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The following is a summary of “Whole blood concentrations of fingolimod and its pharmacologically active metabolite fingolimod phosphate obtained during routine health care of patients with multiple sclerosis,” published in the December 2024 issue of Neurology by Kacirova et al.
Fingolimod, an orally administered immunomodulator, is used as a disease-modifying therapy (DMT) to treat people with relapsing-remitting multiple sclerosis (RRMS) by modulating sphingosine-1-phosphate (S1P) receptors.
Researchers conducted a prospective study to determine if therapeutic drug monitoring (TDM) of fingolimod and the active metabolite, fingolimod phosphate, could help personalize pharmacotherapy for people with MS.
They analyzed whole blood samples from 73 people with MS who were treated with oral fingolimod (0.5 mg daily) (July 2021 and January 2022). Fingolimod and fingolimod phosphate Concentrations were measured using ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS), and relationships with peripheral blood lymphocyte counts were assessed.
The results showed fingolimod concentrations ranged from 0.61 to 6.21 µg/L, and fingolimod phosphate concentrations ranged from 0.48 to 4.28 µg/L. Women had significantly higher fingolimod phosphate concentrations and fingolimod phosphate-to-fingolimod concentration ratios. The combined concentrations of fingolimod and phosphate were considerably higher in individuals with lower absolute peripheral blood lymphocyte counts.
They concluded that fingolimod exhibited wide inter-individual variability in blood concentrations, highlighting the potential for TDM to optimize treatment and support adherence in people with MS.
Source: msard-journal.com/article/S2211-0348(24)00822-8/abstract
