Siponimod (BAF312) penetrates, distributes, and acts in the central nervous system: Preclinical insights.

ABSTRACT:

Background

Siponimod (BAF312), a selective S1P₁/S1P₅ agonist, reduces disability progression in secondary progressive MS. Recent observations suggest it could act via S1P₁/S1P₅-dependent anti-inflammatory and pro-myelination effects on CNS-resident cells.

Objective

Generate preclinical evidence confirming siponimod's CNS penetration and activity.

Methods

Siponimod's CNS penetration and distribution was explored in rodents and non-human primates (NHPs) using: Liquid Chromatography coupled to tandem Mass Spectrometry (LC-MS/MS), quantitative whole-body autoradiography (QWBA) using ¹⁴C-radiolabeled siponimod or non-invasive single-photon emission CT (SPECT) with a validated ¹²³I-radiolabeled siponimod anal

SUBMITTER: Bigaud M 

PROVIDER: S-EPMC8573504 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature