Scroll

safinamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4921	133865-89-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: EMD-1195686 safinamide xadago EMD 1195686 safinamide mesylate safinamide mesilate safinamide methanesulfonate	Safinamide acts through both dopaminergic and non-dopaminergic mechanisms of action. Safinamide is a highly selective and reversible MAO-B inhibitor causing an increase in extracellular levels of dopamine in the striatum. Safinamide is associated with state-dependent inhibition of voltage-gated sodium (Na+) channels, and modulation of stimulated release of glutamate. To what extent the nondopaminergic effects contribute to the overall effect has not been established. Molecular weight: 302.35 Formula: C17H19FN2O2 CLOGP: 2.49 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 64.35 ALOGS: -4.49 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

EMD-1195686
safinamide
xadago
EMD 1195686
safinamide mesylate
safinamide mesilate
safinamide methanesulfonate

Safinamide acts through both dopaminergic and non-dopaminergic mechanisms of action. Safinamide is a highly selective and reversible MAO-B inhibitor causing an increase in extracellular levels of dopamine in the striatum. Safinamide is associated with state-dependent inhibition of voltage-gated sodium (Na+) channels, and modulation of stimulated release of glutamate. To what extent the nondopaminergic effects contribute to the overall effect has not been established.

Molecular weight: 302.35
Formula: C17H19FN2O2
CLOGP: 2.49
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 64.35
ALOGS: -4.49
ROTB: 7

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
75	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	2.19 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.17 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	21.67 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	80 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company
Dec. 18, 2014	EMA	Zambon SpA
March 21, 2017	FDA	NEWRON PHARMS US INC
Sept. 20, 2019	PMDA	Meiji Seika Pharma Co., Ltd.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyskinesia	105.84	52.42	29	541	31973	63456479
On and off phenomenon	73.89	52.42	13	557	1822	63486630
Parkinsonism hyperpyrexia syndrome	70.16	52.42	9	561	144	63488308

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	59.97	46.25	25	574	51473	34904859
Dyskinesia	55.80	46.25	19	580	22394	34933938
Freezing phenomenon	55.52	46.25	11	588	1525	34954807

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyskinesia	120.39	46.57	38	1045	44735	79698570
On and off phenomenon	90.44	46.57	18	1065	3222	79740083
Freezing phenomenon	74.16	46.57	14	1069	1900	79741405
Hallucination	72.31	46.57	31	1052	85714	79657591
Parkinsonism hyperpyrexia syndrome	62.06	46.57	9	1074	239	79743066
Bradykinesia	59.05	46.57	15	1068	8028	79735277
Hypokinesia	54.53	46.57	17	1066	19043	79724262

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N04BD03	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Monoamine oxidase B inhibitors
FDA MoA	N0000175761	Monoamine Oxidase-B Inhibitors
FDA EPC	N0000175762	Monoamine Oxidase Type B Inhibitor
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.92	acidic
pKa2	7.54	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 100MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8278485	June 8, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES
EQ 50MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8278485	June 8, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES
EQ 100MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8076515	Dec. 10, 2028	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES
EQ 50MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8076515	Dec. 10, 2028	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES
EQ 100MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8283380	March 21, 2031	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES
EQ 50MG BASE	XADAGO	MDD US	N207145	March 21, 2017	RX	TABLET	ORAL	8283380	March 21, 2031	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE EXPERIENCING OFF EPISODES

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN	INHIBITOR	Ki	6.35	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Amine oxidase [flavin-containing] A	Enzyme	P21397	AOFA_HUMAN		IC50	4.35	CHEMBL
Sodium channel protein type 9 subunit alpha	Ion channel	Q15858	SCN9A_HUMAN		IC50	4.48	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor		SGMR1_RAT		IC50	7.71	CHEMBL
Amine oxidase [flavin-containing] A	Enzyme		AOFA_RAT		IC50	5.55	CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel		SCN1A_RAT SCN2A_RAT SCN3A_RAT		IC50	5.09	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_RAT		IC50	7.59	CHEMBL

External reference:

ID	Source
90ENL74SIG	UNII
D10158	KEGG_DRUG
202825-46-5	SECONDARY_CAS_RN
4036707	VANDF
C1098261	UMLSCUI
CHEBI:134718	CHEBI
SAG	PDB_CHEM_ID
CHEMBL396778	ChEMBL_ID
131682	PUBCHEM_CID
DB06654	DRUGBANK_ID
CHEMBL48582	ChEMBL_ID
8013	INN_ID
C092797	MESH_SUPPLEMENTAL_RECORD_UI
8291	IUPHAR_LIGAND_ID
1922448	RXNORM
241367	MMSL
d08444	MMSL
016557	NDDF
016558	NDDF
1217565003	SNOMEDCT_US
718852000	SNOMEDCT_US
763521008	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xadago	HUMAN PRESCRIPTION DRUG LABEL	1	27505-110	TABLET, FILM COATED	50 mg	ORAL	NDA	31 sections
Xadago	HUMAN PRESCRIPTION DRUG LABEL	1	27505-110	TABLET, FILM COATED	50 mg	ORAL	NDA	31 sections
Xadago	HUMAN PRESCRIPTION DRUG LABEL	1	27505-111	TABLET, FILM COATED	100 mg	ORAL	NDA	31 sections
Xadago	HUMAN PRESCRIPTION DRUG LABEL	1	27505-111	TABLET, FILM COATED	100 mg	ORAL	NDA	31 sections