amifampridine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4336 54-96-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • amifampridine
  • firdapse
  • amifampridin
  • amifampridine phosphate
  • DAP
  • 3,4-DAP
4-Aminopyridine derivative that acts as a POTASSIUM CHANNEL blocker to increase release of ACETYLCHOLINE from nerve terminals. It is used in the treatment of CONGENITAL MYASTHENIC SYNDROMES.
  • Molecular weight: 109.13
  • Formula: C5H7N3
  • CLOGP: 0.39
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 64.93
  • ALOGS: 0.16
  • ROTB: 0

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 2009 EMA BioMarin Europe Ltd
Nov. 28, 2018 FDA CATALYST PHARMS

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
Myasthenic syndrome 61.36 32.06 8 281 217 46685556

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

Pharmacologic Action:

SourceCodeDescription
ATC N07XX05 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
FDA MoA N0000175448 Potassium Channel Antagonists
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D026902 Potassium Channel Blockers
FDA EPC N0000192795 Potassium Channel Blocker
CHEBI has role CHEBI:76971 e.coli metabolites

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Eaton-Lambert syndrome indication 56989000 DOID:0050214

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.89 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL Nov. 28, 2023 NEW CHEMICAL ENTITY
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL Nov. 28, 2025 INDICATED FOR THE TREATMENT OF LAMBERT-EATON MYASTHENIC SYNDROME (LEMS) IN ADULTS
10MG RUZURGI JACOBUS PHARM CO INC N209321 May 6, 2019 RX TABLET ORAL May 6, 2026 TREATMENT OF LAMBERT-EATON MYASTHENIC SYNDROME (LEMS) IN PATIENTS 6 TO LESS THAN 17 YEARS OF AGE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-gated potassium channel Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
RU4S6E2G0J UNII
D10228 KEGG_DRUG
446254-47-3 SECONDARY_CAS_RN
4027572 VANDF
4038075 VANDF
C0046948 UMLSCUI
CHEBI:135948 CHEBI
L89 PDB_CHEM_ID
CHEMBL354077 ChEMBL_ID
CHEMBL3301611 ChEMBL_ID
5918 PUBCHEM_CID
DB11640 DRUGBANK_ID
D000077770 MESH_DESCRIPTOR_UI
8804 INN_ID
8032 IUPHAR_LIGAND_ID
2106337 RXNORM
177374 MMSL
23312 MMSL
NOCODE MMSL
d06641 MMSL
011806 NDDF
013406 NDDF
422654000 SNOMEDCT_US
782983000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ruzurgi HUMAN PRESCRIPTION DRUG LABEL 1 49938-110 TABLET 10 mg ORAL NDA 28 sections
Firdapse HUMAN PRESCRIPTION DRUG LABEL 1 69616-211 TABLET 10 mg ORAL NDA 31 sections