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

Stem definitionDrug idCAS RN
4921 133865-89-1

Description:

MoleculeDescription

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: ONP

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

Drug dosage:

DoseUnitRoute
75 mg O

ADMET properties:

PropertyValueReference
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

Approvals:

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

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dyskinesia 81.38 53.03 23 440 27838 50576823
Parkinsonism hyperpyrexia syndrome 62.22 53.03 8 455 128 50604533

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hallucination 53.31 44.32 21 405 44691 29529410
Freezing phenomenon 46.95 44.32 9 417 1254 29572847
Dyskinesia 44.79 44.32 15 411 20046 29554055

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dyskinesia 95.81 47.47 31 848 39357 64458496
On and off phenomenon 64.31 47.47 13 866 2506 64495347
Bradykinesia 62.06 47.47 15 864 6545 64491308
Hallucination 60.27 47.47 26 853 72762 64425091
Freezing phenomenon 57.93 47.47 11 868 1535 64496318
Parkinsonism hyperpyrexia syndrome 54.80 47.47 8 871 222 64497631

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.92 acidic
pKa2 7.54 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE XADAGO MDD US N207145 March 21, 2017 RX TABLET ORAL March 21, 2022 NEW CHEMICAL ENTITY
EQ 50MG BASE XADAGO MDD US N207145 March 21, 2017 RX TABLET ORAL March 21, 2022 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Amine oxidase [flavin-containing] B Enzyme INHIBITOR Ki 6.35 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 9 subunit alpha Ion channel IC50 4.48 CHEMBL
Amine oxidase [flavin-containing] A Enzyme IC50 4.35 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor IC50 7.71 CHEMBL
Amine oxidase [flavin-containing] B Enzyme IC50 7.59 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.09 CHEMBL

External reference:

IDSource
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
718852000 SNOMEDCT_US
763521008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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