safinamide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4921 | 133865-89-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 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 | 73.46 | 50.67 | 21 | 371 | 28904 | 46656766 |
| Parkinsonism hyperpyrexia syndrome | 60.99 | 50.67 | 8 | 384 | 165 | 46685505 |
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 |
|---|
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 (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Parkinson's disease | indication | 49049000 | DOID:14330 |
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)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG | XADAGO | MDD US | N207145 | March 21, 2017 | RX | TABLET | ORAL | March 21, 2022 | NEW CHEMICAL ENTITY |
| 50MG | XADAGO | MDD US | N207145 | March 21, 2017 | RX | TABLET | ORAL | March 21, 2022 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 | |||||
| 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 | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 7.71 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10158 | KEGG_DRUG |
| 202825-46-5 | SECONDARY_CAS_RN |
| 4036707 | VANDF |
| C1098261 | UMLSCUI |
| CHEBI:134718 | CHEBI |
| SAG | PDB_CHEM_ID |
| CHEMBL48582 | ChEMBL_ID |
| CHEMBL396778 | ChEMBL_ID |
| 131682 | PUBCHEM_CID |
| 8291 | IUPHAR_LIGAND_ID |
| C092797 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8013 | INN_ID |
| DB06654 | DRUGBANK_ID |
| 90ENL74SIG | UNII |
| 1922448 | RXNORM |
| 241367 | MMSL |
| d08444 | MMSL |
| 016557 | NDDF |
| 016558 | NDDF |
| 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 | 27505-111 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 31 sections |