Cenerimod is a sphingosine-1-phosphate 1 receptor modulator under development for treatment of systemic lupus erythematosus.

This single-centre, open-label, single-dose study investigated the mass balance and excretion routes and aimed at identifying and quantifying cenerimod metabolites in plasma, urine, and faeces after oral administration of 2 mg/100 μCi (3.7 MBq) of ¹⁴C-cenerimod.

Total mean cumulative recovery was 84% of the administered dose (58–100% in faeces and 4.6–12% in urine). In a 0–504 h cross-subject area under the curve plasma pool, cenerimod and two metabolites were detected accounting for 78, 6.0, and 4.9% of total radioactivity, respectively, i.e. no major metabolite was identified in plasma. Cenerimod was only detected in faeces and accounted for 17% of the radioactivity excreted in this matrix. The metabolite M32 was detected in both urine and faeces and represented 23% and 66% of radioactivity excreted in these matrices, respectively. Other metabolites of unknown structure were detected in small amounts. Overall, M32 and cenerimod accounted for 52% and 13%, respectively, of the total radioactivity recovered.

Among the excreted metabolites, only the non-enzymatically formed M32 represented more than 25% of total drug-related material. Therefore, no pharmacokinetic drug–drug interaction studies are foreseen.

Cenerimod是一种鞘氨醇-1-磷酸1受体调节剂，正在开发中，用于治疗系统性红斑狼疮。

这项单中心，开放标签，单剂量的研究调查了质量平衡和排泄途径，旨在鉴定和定量口服2 mg / 100μCi（3.7 MBq）的血浆，尿液和粪便中的cenerimod代谢物¹⁴ C-cenerimod。

平均总累积恢复率为给药剂量的84％（粪便中58–100％，尿液中4.6–12％）。在曲线血浆库下的0–504 h跨对象区域中，检出塞来莫德和两种代谢物分别占总放射性的78％，6.0％和4.9％，即血浆中未鉴定出主要代谢物。塞内莫德仅在粪便中检测到，占该基质中排泄放射性的17％。在尿液和粪便中均检测到代谢物M32，分别占这些基质中排泄的放射性的23％和66％。少量检测到其他未知结构的代谢物。总体而言，M32和西立莫德分别占回收的总放射性的52％和13％。

在排出的代谢产物中，仅非酶促形成的M32占药物相关物质总量的25％以上。因此，没有预见到药代动力学药物相互作用的研究。