amifampridine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 24 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR1B,ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK19,CDK5,CDK9,CHEK1,CLK4,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GRK3,GSK3B,IKBKB,IRAK1,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK12,MAPK7,MAPK9,MARK4,MELK,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2 71
kinase-selectivity-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK9,DYRK1B,ERBB2,GRK2,MAP2K6,MAP3K21,MAPK7,MARK4,SIK2,STK33 15
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

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

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
Myasthenia gravis crisis 36.30 32.35 6 441 1058 90626942

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

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 D009465 Neuromuscular Agents
MeSH PA D026902 Potassium Channel Blockers
MeSH PA D049990 Membrane Transport Modulators
FDA EPC N0000192795 Potassium Channel Blocker
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

N07XX Other nervous system drugs 23 drugs
arimoclomoldeutetrabenazinedextromethorphanedaravoneeplontersenfampridineinotersen laquinimodlevacetylleucineomaveloxolonepatisiranphenylbutanoic acid show all 23 →

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

DiseaseRelationSNOMED_IDDOID
Eaton-Lambert syndrome indication 56989000 DOID:0050214




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL 11060128 June 29, 2032 METHOD OF TREATING LAMBERT-EATON MYASTHENIC SYNDROME WITH AMIFAMPRIDINE
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL 11268128 June 29, 2032 METHOD OF TREATING LAMBERT-EATON MYASTHENIC SYNDROME WITH AMIFAMPRIDINE
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL 11274331 June 29, 2032 METHOD OF TREATING LAMBERT-EATON MYASTHENIC SYNDROME WITH AMIFAMPRIDINE
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL 11274332 June 29, 2032 METHOD OF TREATING LAMBERT-EATON MYASTHENIC SYNDROME WITH AMIFAMPRIDINE
EQ 10MG BASE FIRDAPSE CATALYST PHARMS N208078 Nov. 28, 2018 RX TABLET ORAL 10793893 May 26, 2034 METHOD OF TREATING LAMBERT-EATON MYASTHENIC SYNDROME WITH AMIFAMPRIDINE

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 Sept. 29, 2029 TREATMENT OF LAMBERT-EATON MYASTHENIC SYNDROME (LEMS) IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER

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
D10228 KEGG_DRUG
4027572 VANDF
4038075 VANDF
C0046948 UMLSCUI
CHEBI:135948 CHEBI
CHEMBL354077 ChEMBL_ID
CHEMBL3301611 ChEMBL_ID
D000077770 MESH_DESCRIPTOR_UI
DB11640 DRUGBANK_ID
8032 IUPHAR_LIGAND_ID
8804 INN_ID
446254-47-3 SECONDARY_CAS_RN
RU4S6E2G0J UNII
5918 PUBCHEM_CID
2106337 RXNORM
177374 MMSL
23312 MMSL
NOCODE MMSL
d06641 MMSL
011806 NDDF
013406 NDDF
18038211000001106 SNOMEDCT_US
422654000 SNOMEDCT_US
782983000 SNOMEDCT_US
L89 PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Firdapse HUMAN PRESCRIPTION DRUG LABEL 1 69616-211 TABLET 10 mg ORAL NDA 33 sections