Details of the Drug

General Information of Drug (ID: DMK08L3)

Drug Name

Amifampridine

Synonyms

3,4-DIAMINOPYRIDINE; pyridine-3,4-diamine; 3,4-Pyridinediamine; Firdapse; Diamino-3,4 pyridine; 4,5-Diaminopyridine; 3,4-DAP; SC10; amifampridin; Zenas; UNII-RU4S6E2G0J; EINECS 200-220-9; NSC 521760; BRN 0110232; RU4S6E2G0J; OYTKINVCDFNREN-UHFFFAOYSA-N; WT559; NCGC00167560-01; SMR000752913

Indication

Disease Entry	ICD 11	Status	REF
LambertEaton myasthenic syndrome	8C62	Approved	[1]
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Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

109.13

Logarithm of the Partition Coefficient (xlogp)

-0.5

Rotatable Bond Count (rotbonds)

0

Hydrogen Bond Donor Count (hbonddonor)

2

Hydrogen Bond Acceptor Count (hbondacc)

3

ADMET Property

Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 16-137 mcg/L []
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 0.6-1.3 h []
Bioavailability: The bioavailability of drug is 93-100% []
Elimination: Following oral administration, more than 93% of total amifampridine is renally eliminated within 24 hours [2]
Half-life: The concentration or amount of drug in body reduced by one-half in 2.5 hours []

Chemical Identifiers

Formula: C5H7N3
IUPAC Name: pyridine-3,4-diamine
Canonical SMILES: C1=CN=CC(=C1N)N
InChI: InChI=1S/C5H7N3/c6-4-1-2-8-3-5(4)7/h1-3H,7H2,(H2,6,8)
InChIKey: OYTKINVCDFNREN-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 5918
ChEBI ID: CHEBI:135948
CAS Number: 54-96-6
DrugBank ID: DB11640
TTD ID: D0HE0Y
INTEDE ID: DR1747
ACDINA ID: D00831

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Potassium channel unspecific (KC)	TT1VOHK	NOUNIPROTAC	Blocker	[1]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
N-acetyltransferase 1 (NAT1)	DE7OAB3	ARY1_HUMAN	Substrate	[3]
N-acetyltransferase 2 (NAT2)	DER7TA0	ARY2_HUMAN	Substrate	[3]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Brushite	E00392	104805	Diluent
Calcium stearate	E00244	15324	lubricant
Magnesium stearate	E00208	11177	lubricant
Hydrophobic colloidal silica	E00285	24261	Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Amifampridine 10 mg tablet	10 mg	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
2	Haroldsen PE, Musson DG, Hanson B, Quartel A, O'Neill CA: Effects of Food Intake on the Relative Bioavailability of Amifampridine Phosphate Salt in Healthy Adults. Clin Ther. 2015 Jul 1;37(7):1555-63. doi: 10.1016/j.clinthera.2015.05.498. Epub 2015 Jun 20.
3	Genetic variation in aryl N-acetyltransferase results in significant differences in the pharmacokinetic and safety profiles of amifampridine (3,4-diaminopyridine) phosphate. Pharmacol Res Perspect. 2015 Feb;3(1):e00099.