Disposition and metabolism of safinamide, a novel drug for Parkinson's disease, in healthy male volunteers.
Article Details
- CitationCopy to clipboard
Leuratti C, Sardina M, Ventura P, Assandri A, Muller M, Brunner M
Disposition and metabolism of safinamide, a novel drug for Parkinson's disease, in healthy male volunteers.
Pharmacology. 2013;92(3-4):207-16. doi: 10.1159/000354805. Epub 2013 Oct 11.
- PubMed ID
- 24136086 [ View in PubMed]
- Abstract
BACKGROUND/AIMS: Absorption, biotransformation and elimination of safinamide, an enantiomeric alpha-aminoamide derivative developed as an add-on therapy for Parkinson's disease patients, were studied in healthy volunteers administered a single oral dose of 400 mg (14)C safinamide methanesulphonate, labelled in metabolically stable positions. METHODS: Pharmacokinetics of the parent compound were investigated up to 96 h, of (14)C radioactivity up to 192/200 h post-dose. RESULTS/CONCLUSIONS: Maximum concentration was achieved at 1 h (plasma, median Tmax) for parent drug and at 7 and 1.5 h for plasma and whole blood (14)C radioactivity, respectively. Terminal half-lives were about 22 h for unchanged safinamide and 80 h for radioactivity. Safinamide deaminated acid and the N-dealkylated acid were identified as major metabolites in urine and plasma. In urine, the beta-glucuronide of the N-dealkylated acid and the monohydroxy safinamide were also characterized. In addition, the glycine conjugate of the N-dealkylated acid and 2-[4-hydroxybenzylamino]propanamide were tentatively identified as minor urinary metabolites.
DrugBank Data that Cites this Article
- Drugs
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Safinamide Cytochrome P450 3A4 Protein Humans UnknownSubstrateDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Safinamide Solute carrier organic anion transporter family member 3A1 Protein Humans UnknownSubstrateDetails