General
Preferred name
SAFINAMIDE
Synonyms
PNU-151774E,FCE28073 ()
EMD 1195686 mesylate ()
NW-1015 ()
PNU-151774E ()
SAFINAMIDE MESYLATE ()
FCE 26743 ()
EMD 1195686 ()
FCE 26743 (mesylate) ()
EMD 1195686 (mesylate) ()
Safinamide (mesylate) ()
EMD-1195686, PNU-15774E ()
EMD-1195686 ()
Safinamida ()
Xadago ()
Safinamide ()
Safinamide mesilate ()
Safinamide methanesulfonate ()
PNU 151774E ()
Safinamide methansulfonate ()
NW 1015 ()
Safinamide (mesylate) ()
Safinamide-d4 ()
P&D ID
PD012205
CAS
202825-46-5
133865-89-1
2748522-33-8
Tags
available
drug
Approved by
EMA
PMDA
FDA
First approval
2015
2014
Drug indication
Idiopathic parkinson disease
Parkinson disease
Drug Status
investigational
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY
uncontrolled involuntary movement, falls, nausea, and trouble sleeping or falling asleep (insomnia); Patients who have an overdose may experience hypertension (high blood pressure), orthostatic hypotension, hallucinations, psychomotor agitation, nausea, vomiting, and dyskinesia.
METABOLISM
The principal step is mediated by amidases which have not been identified, and produces safinamide acid. It is also metabolized to O-debenzylated safinamide and N-delkylated amine. The N-dealkylated amine is then oxidized to a carboxylic acid and finally glucuronidated. Dealkylation reactions are mediated by cytochrome P450s (CYPs), especially CYP3A4. Safinamide acid binds to organic anion transporter 3 (OAT3), but no clinical relevance of this interaction has been determined. Safinamide also binds to ABCG2 transiently. No other transporter affinities have been found in preliminary studies.
DESCRIPTION
Safinamide is an alpha-aminoamide. The clinically administered formulation may be the mesylate salt (PubChem CID 3038502).
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
24
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
62
Molecular Weight
302.14
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
2.37
TPSA
64.35
Fraction CSP3
0.24
Chiral centers
1.0
Largest ring
6.0
QED
0.83
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Metabolism
Neuroscience
Neuronal Signaling
Target
MAO
MAOB
Monoamine Oxidase
MOA
dopamine reuptake inhibitor, glutamate inhibitor, monoamine oxidase inhibitor
Indication
Parkinson's Disease
VGSC Target
Nav1.7
Source data
