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Details

Stereochemistry ABSOLUTE
Molecular Formula C17H19FN2O2.CH4O3S
Molecular Weight 398.4508
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SAFINAMIDE MESYLATE

SMILES

C[C@@]([H])(C(=N)O)NCc1ccc(cc1)OCc2cccc(c2)F.CS(=O)(=O)O

InChI

InChIKey=YKOCHIUQOBQIAC-YDALLXLXSA-N
InChI=1S/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14;1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21);1H3,(H,2,3,4)/t12-;/m0./s1

HIDE SMILES / InChI

Molecular Formula CH4O3S
Molecular Weight 96.1068
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C17H19FN2O2
Molecular Weight 302.344
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/27536120 | http://adisinsight.springer.com/drugs/800009612

Safinamide (FCE 26743, NW 1015, PNU 151774, PNU 151774E, trade name Xadago) combines potent, selective, and reversible inhibition of MAO-B with blockade of voltage-dependent Na+ and Ca2+ channels and inhibition of glutamate release. Safinamide is under development with Newron, Zambon and Meiji Seika Pharma for the treatment of Parkinson's disease. Safinamide has been launched in the EU, Iceland and Liechtenstein. Safinamide was well tolerated and safe in the clinical development program that demonstrated the amelioration of motor symptoms and OFF phenomena by safinamide when combined with dopamine agonists or levodopa.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
98 nM [IC50]
8 µM [IC50]
56.3999999999999986 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
XADAGO

Approved Use

Xadago (safinamide) is indicated for the treatment of adult patients with idiopathic Parkinson’s disease (PD) as add-on therapy to a stable dose of Levodopa (L-dopa) alone or in combination with other PD medicinal products in mid-to late-stage fluctuating patients.

Launch Date

1424649600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
650 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SAFINAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
19000 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SAFINAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
26 h
single, intravenous
SAFINAMIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
11.5%
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SAFINAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
400 mg 1 times / day single, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: single
Dose: 400 mg, 1 times / day
Sources:
healthy, mean age 28.7 years
Health Status: healthy
Age Group: mean age 28.7 years
Sex: M
Sources:
Other AEs: Headache...
Other AEs:
Headache (grade 1, 16.7%)
Sources:
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Other AEs: Diarrhea, Headache...
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Disc. AE: ALT increased...
Other AEs: Palpitations, Nausea...
AEs leading to
discontinuation/dose reduction:
ALT increased (5.5%)
Other AEs:
Palpitations (5.5%)
Nausea (5.5%)
Pharyngitis (5.5%)
Headache (5.5%)
Sources:
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Other AEs: Headache, Dizziness...
Other AEs:
Headache (11.9%)
Dizziness (5.1%)
Nausea (3.4%)
Nasopharyngitis (1.7%)
Fatigue (3.4%)
Vomiting (1.7%)
Diarrhea (1.7%)
Skin laceration (1.7%)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Angina pectoris, Aortic valve incompetence...
AEs leading to
discontinuation/dose reduction:
Angina pectoris (0.3%)
Aortic valve incompetence (0.3%)
Atrial flutter (0.3%)
Creatine phosphokinase increased (0.3%)
Vertigo (0.3%)
Cataract (0.3%)
Lacrimation increased (0.3%)
Macular oedema (0.3%)
Maculopathy (0.3%)
Ocular vascular disorder (0.3%)
Papilloedema (0.3%)
Paraesthesia (0.3%)
Pain of skin (0.3%)
Rash erythematous (0.3%)
Anaemia iron deficiency (0.3%)
Depressed mood (0.3%)
Bronchospasm (0.3%)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Dyskinesia, Parkinson's disease...
AEs leading to
discontinuation/dose reduction:
Dyskinesia (1.4%)
Parkinson's disease (0.6%)
Dizziness (0.2%)
Paraesthesia (0.2%)
Cognitive disorder (0.2%)
Presyncope (0.2%)
Abdominal pain (0.2%)
Vomiting (0.2%)
Hallucination, visual (0.6%)
Hallucination (0.2%)
Sleep terror (0.2%)
Asthenia (0.2%)
Muscle spasms (0.4%)
Basal cell carcinoma (0.2%)
Breast cancer (0.2%)
Non-Hodgkin's lymphoma (0.2%)
Arrhythmia (0.2%)
Ventricular tachycardia (0.2%)
Cataract subcapsular (0.2%)
Vision blurred (0.2%)
Change in ECG (0.2%)
QT interval prolonged (0.2%)
Blister (0.2%)
Hyperhidrosis (0.2%)
Fall (0.2%)
Subdural haematoma (0.2%)
Cachexia (0.2%)
Sources:
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Myocardial infarction, Palpitations...
AEs leading to
discontinuation/dose reduction:
Myocardial infarction (0.4%)
Palpitations (0.4%)
Ventricular tachycardia (0.4%)
QT interval prolonged (0.9%)
Blood glucose increased (0.4%)
Vertigo (0.4%)
Muscle spasms (0.4%)
Tremor (0.4%)
Nausea (0.4%)
Sources:
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Dyskinesia, Dizziness...
AEs leading to
discontinuation/dose reduction:
Dyskinesia (1.3%)
Dizziness (0.4%)
Paraesthesia (0.4%)
Balance disorder (0.4%)
Tremor (0.4%)
Abdominal pain (0.4%)
Vomiting (0.4%)
Aphthous stomatitis (0.4%)
Constipation (0.4%)
Nausea (0.4%)
Asthenia (0.4%)
Chest discomfort (0.4%)
Muscle rigidity (0.4%)
Dyspnoea (0.9%)
Pneumonitis (0.4%)
Palpitations (0.4%)
Urinary tract infection (0.4%)
Sources:
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Swollen tongue, Dyspnea...
AEs leading to
discontinuation/dose reduction:
Swollen tongue
Dyspnea
Redness mouth
Gingival swelling
Rash trunk
Decreased appetite
Increased appetite
Inner restlessness
Redness of face
Pruritus
Hyperhidrosis
Dry mouth
Hoarseness
Malaise
Sources:
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Head titubation, Nausea...
AEs leading to
discontinuation/dose reduction:
Head titubation (1.1%)
Nausea (2.2%)
Diarrhea (1.1%)
GERD (1.1%)
Vomiting (1.1%)
Anxiety (1.1%)
Nightmare (1.1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Headache grade 1, 16.7%
400 mg 1 times / day single, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: single
Dose: 400 mg, 1 times / day
Sources:
healthy, mean age 28.7 years
Health Status: healthy
Age Group: mean age 28.7 years
Sex: M
Sources:
Diarrhea 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Headache 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Headache 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Nausea 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Palpitations 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Pharyngitis 5.5%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
ALT increased 5.5%
Disc. AE
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy, mean age 41.2 years
Diarrhea 1.7%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Nasopharyngitis 1.7%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Skin laceration 1.7%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Vomiting 1.7%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Headache 11.9%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Fatigue 3.4%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Nausea 3.4%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Dizziness 5.1%
350 mg 1 times / day multiple, oral
Higher than recommended
Dose: 350 mg, 1 times / day
Route: oral
Route: multiple
Dose: 350 mg, 1 times / day
Sources:
healthy
Anaemia iron deficiency 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Angina pectoris 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Aortic valve incompetence 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Atrial flutter 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Bronchospasm 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Cataract 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Creatine phosphokinase increased 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Depressed mood 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Lacrimation increased 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Macular oedema 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Maculopathy 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Ocular vascular disorder 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Pain of skin 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Papilloedema 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Paraesthesia 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Rash erythematous 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Vertigo 0.3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Abdominal pain 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Arrhythmia 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Asthenia 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Basal cell carcinoma 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Blister 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Breast cancer 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Cachexia 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Cataract subcapsular 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Change in ECG 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Cognitive disorder 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Dizziness 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Fall 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Hallucination 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Hyperhidrosis 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Non-Hodgkin's lymphoma 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Paraesthesia 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Presyncope 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
QT interval prolonged 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Sleep terror 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Subdural haematoma 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Ventricular tachycardia 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Vision blurred 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Vomiting 0.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Muscle spasms 0.4%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Hallucination, visual 0.6%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Parkinson's disease 0.6%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Dyskinesia 1.4%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy
Blood glucose increased 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Muscle spasms 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Myocardial infarction 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Nausea 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Palpitations 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Tremor 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Ventricular tachycardia 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Vertigo 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
QT interval prolonged 0.9%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Abdominal pain 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Aphthous stomatitis 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Asthenia 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Balance disorder 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Chest discomfort 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Constipation 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Dizziness 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Muscle rigidity 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Nausea 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Palpitations 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Paraesthesia 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Pneumonitis 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Tremor 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Urinary tract infection 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Vomiting 0.4%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Dyspnoea 0.9%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Dyskinesia 1.3%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Decreased appetite Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Dry mouth Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Dyspnea Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Gingival swelling Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Hoarseness Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Hyperhidrosis Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Increased appetite Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Inner restlessness Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Malaise Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Pruritus Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Rash trunk Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Redness mouth Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Redness of face Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Swollen tongue Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Anxiety 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Diarrhea 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
GERD 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Head titubation 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Nightmare 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Vomiting 1.1%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
Nausea 2.2%
Disc. AE
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 43 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 3.7 uM]
yes [IC50 35 uM]
yes [IC50 47.7 uM]
yes
yes
yes
yes
Drug as victimTox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Safinamide (Newron Pharmaceuticals).
2001 Jun
Progress report on new antiepileptic drugs: a summary of the Sixth Eilat Conference (EILAT VI).
2002 Sep
Safinamide: FCE 26743, NW 1015, PNU 151774, PNU 151774E.
2004
Improvement of motor function in early Parkinson disease by safinamide.
2004 Aug 24
Pharmacokinetics and pharmacodynamics of safinamide, a neuroprotectant with antiparkinsonian and anticonvulsant activity.
2004 Jul
Crystal structures of monoamine oxidase B in complex with four inhibitors of the N-propargylaminoindan class.
2004 Mar 25
Progress report on new antiepileptic drugs: a summary of the Seventh Eilat Conference (EILAT VII).
2004 Sep-Oct
Voltage gated ion channels: targets for anticonvulsant drugs.
2005
Bioassay of safinamide in biological fluids of humans and various animal species.
2006
New pharmacologic horizons in the treatment of Parkinson disease.
2006 Oct 10
Symptom relief in Parkinson disease by safinamide: Biochemical and clinical evidence of efficacy beyond MAO-B inhibition.
2006 Oct 10
Safinamide: from molecular targets to a new anti-Parkinson drug.
2006 Oct 10
Monoamine oxidase-B inhibition in the treatment of Parkinson's disease.
2007 Dec
Safinamide.
2007 Jan
Safinamide for the treatment of Parkinson's disease, epilepsy and restless legs syndrome.
2007 Jul
Structures of human monoamine oxidase B complexes with selective noncovalent inhibitors: safinamide and coumarin analogs.
2007 Nov 15
Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase.
2007 Oct 4
An expert opinion on safinamide in Parkinson's disease.
2008 Jul
Computational systems analysis of dopamine metabolism.
2008 Jun 18
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions.
2009 Mar-Apr
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs.
2010 Apr
The Movement Disorder Society--14th International Congress of Parkinson's Disease and Movement Disorders.
2010 Aug
Superpose3D: a local structural comparison program that allows for user-defined structure representations.
2010 Aug 5
Safinamide in the treatment of Parkinson's disease.
2010 Sep
Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones.
2011 Dec 8
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: a new scaffold for the selective inhibition of monoamine oxidase B.
2011 Sep 22
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.
2013 Dec 1
A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency.
2013 Feb 5
Patents

Sample Use Guides

Treatment with Xadago (Safinamide) should be started at 50 mg per day. This daily dose may be increased to 100 mg/day on the basis of individual clinical need.
Route of Administration: Oral
Safinamide (PNU-151774E) reduces sustained repetitive firing in a use-dependent manner without modifying the first action potential in hippocampal cultured neurons. The inhibition of the currents by PNU-151774E was concentration-related from 10 to 200 μM.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:39:38 UTC 2021
Edited
by admin
on Fri Jun 25 21:39:38 UTC 2021
Record UNII
YS90V3DTX0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SAFINAMIDE MESYLATE
USAN  
USAN  
Official Name English
SAFINAMIDE METHANESULFONATE
MI  
Common Name English
SAFINAMIDE MESILATE
WHO-DD  
Common Name English
XADAGO
Brand Name English
(S)-2-((4-((3-FLUOROBENZYL)OXY)BENZYL)AMINO)PROPANAMIDE METHANESULFONATE
Systematic Name English
SAFINAMIDE MESYLATE [ORANGE BOOK]
Common Name English
NW-1015
Code English
SAFINAMIDE MESILATE [WHO-DD]
Common Name English
PNU 151774E
Code English
NW 1015
Code English
PNU-151774E
Code English
SAFINAMIDE METHANESULFONATE [MI]
Common Name English
SAFINAMIDE MESYLATE [USAN]
Common Name English
SAFINAMIDE METHANSULFONATE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C264
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
NCI_THESAURUS C667
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
EMA ASSESSMENT REPORTS XADAGO (AUTHORIZED: PARKINSON DISEASE)
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
Code System Code Type Description
FDA UNII
YS90V3DTX0
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
RXCUI
1922449
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
NCI_THESAURUS
C81331
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
PUBCHEM
3038502
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
DRUG BANK
DBSALT002034
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
MESH
C092797
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
ChEMBL
CHEMBL396778
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
MERCK INDEX
M9720
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY Merck Index
EVMPD
SUB130363
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
CAS
202825-46-5
Created by admin on Fri Jun 25 21:39:38 UTC 2021 , Edited by admin on Fri Jun 25 21:39:38 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
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IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY