AMIFAMPRIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C5H7N3
Molecular Weight	109.1294
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

c1c[nH]cc(c1=N)N

InChI

InChIKey=OYTKINVCDFNREN-UHFFFAOYSA-N

InChI=1S/C5H7N3/c6-4-1-2-8-3-5(4)7/h1-3H,7H2,(H2,6,8)

HIDE SMILES / InChI

Description
Sources: http://www.biomarin.com/products/firdapse/ | https://ec.europa.eu/health/documents/community-register/2011/20110412101013/anx_101013_en.pdf | http://www.catalystpharma.com/amifampridine-phosphate.shtml

Amifampridine (Firdapse), currently approved in the European Union, is the first and only approved drug for the symptomatic treatment of Lambert-Eaton Myasthenic Syndrome (LEMS) in adults, a rare autoimmune disease with the primary symptoms of muscle weakness. In LEMS, the body’s own immune system attacks connections between nerves and muscles and disrupts the ability of nerve cells to send signals to muscle cells. Amifampridine blocks voltage-dependent potassium channels, thereby prolonging pre-synaptic cell membrane depolarization. Prolonging the action potential enhances the transport of calcium into the nerve ending. The resulting increase in intracellular calcium concentrations facilitates exocytosis of acetylcholine containing vesicles, which in turn enhances neuromuscular transmission. Amifampridine phosphate has been granted Orphan Drug Designation and Breakthrough Therapy designation by the FDA for the treatment of Lambert-Eaton Myasthenic Syndrome (LEMS).

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
voltage-gated potassium channel activity Target ID: GO:0005249 Sources: https://ec.europa.eu/health/documents/community-register/2011/20110412101013/anx_101013_en.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/8358554	Blocker 231		2.0 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Lambert-Eaton myasthenic syndrome Sources: https://ec.europa.eu/health/documents/community-register/2011/20110412101013/anx_101013_en.pdf	Palliative		Approved 4033	Firdapse Approved Use Symptomatic treatment of Lambert-Eaton myasthenic syndrome (LEMS) in adults. Launch Date 1.26152645E12

C_max

Value	Dose	Analyte	Population
59.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
40.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
189 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
268 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
117 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
109 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1220 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1444 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
2.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.28 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
4.03 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
4.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26101174/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	3-N-ACETYL-AMIFAMPRIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
10 mg 3 times / day multiple, oral Recommended Dose: 10 mg, 3 times / day Route: oral Route: multiple Dose: 10 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf	healthy, adult n = 52 Health Status: healthy Age Group: adult Population Size: 52 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf	Other AEs: Paresthesia, Dysesthesia... Other AEs: Paresthesia (69%) Dysesthesia (69%) Oral dysesthesia (69%) Abdominal pain (25%) Upper abdominal pain (25%) Dyspepsia (17%) Dizziness (12%) Nausea (10%) Back pain (8%) Hypoesthesia (6%) Muscle spasms (6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
75 mg 1 times / day multiple, oral (typical) Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf	unhealthy, adult n = 162 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 162 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf	Other AEs: Convulsion, Head titubation... Other AEs: Convulsion (0.6%) Head titubation (0.6%) Tremor (0.6%) Unresponsive to stimuli (0.6%) Small cell lung cancer (0.6%) Metastases to central nervous system (0.6%) Lung cancer metastatic (0.6%) Pulmonary mass (0.6%) Bradycardia (0.6%) Pneumonia (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 753 inducer 374	inhibitor 825	inhibitor 894	inhibitor 775

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
Kv1.3 8 Kv1.5 8 P-gp 666 OATP1B3 319 CYP1A2 725 CYP2A6 334 CYP2B6 371 CYP2C8 417 CYP2C19 700 CYP2E1 424	P-gp 724 CYP450 32 FMO 18	CYP1A2 329 CYP2B6 243

Drug as perpetrator

Target	Modality	Activity	Metabolite
OATP1B3 326	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no [Inhibition 30 uM]
CYP1A2 805	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no	3-N-acetyl-BMN125
CYP1A2 805	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2A6 356	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2B6 465	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no	3-N-acetyl-BMN125
CYP2B6 465	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2C19 738	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2C8 448	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2C9 851	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2D6 908	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP2E1 467	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
CYP3A4 920	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no	3-N-acetyl-BMN125
CYP3A4 920	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
Kv1.3 18	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=25 Page: 25.0	no	3-N-acetyl-BMN125
Kv1.5 18	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=25 Page: 25.0	no	3-N-acetyl-BMN125
P-gp 754	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
Kv1.5 18	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=25 Page: 25.0	yes [IC50 490.9 uM]
Kv1.3 18	inhibitor 1612 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=25 Page: 25.0	yes [IC50 524.8 uM]
CYP1A2 805	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	yes
CYP2B6 465	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	yes
CYP3A4 920	inducer 772 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	yes

Drug as victim

Target	Modality	Activity
CYP450 32	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
FMO 18	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no
P-gp 724	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=27 Page: 27.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 796	inhibitor 786 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=26 Page: 26.0
hERG 796	inhibitor 786 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208078Orig1s000PharmR.pdf#page=26 Page: 26.0		3-N-acetyl-BMN125

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	NO22778	https://www.001chemical.com/chem/54-96-6
3B Scientific (Wuhan) Corp	3B3-000017	http://www.3bsc.com/index/pro_info.php?id=21905
AA Blocks	AA003ICP	http://www.aablocks.com/goods/Goods/detail?id=AA003ICP
AEchem Scientific Corp., USA	AE1-018071	http://www.aechemsc.com/info_products/AE1-018071.php
AHH Chemical co.,ltd	MT-07842	http://www.ahhchemical.com/product/MT-07842.html
AK Scientific, Inc. (AKSCI)	L421	http://www.aksci.com/item_detail.php?cat=L421
Aaron Chemicals	AR003J4H	http://www.aaronchem.com/54-96-6
AbMole Bioscience	M5406	http://www.abmole.com/products/amifampridine.html
Acadechem	ACDX-013489	http://acadechemical.com/product/88181
Acadechem	ACDS-033271	http://www.acadechemical.com/product/107970
Aceschem	ACS010096	https://www.aceschem.com/catalog/54-96-6.html
Achemica	ACMC-209lkh	http://www.achemica.com/prodinfo/?id=128901
Achemo Scientific Limited	AC-11438	http://www.achemo.com/search/?Keyword= 54-96-6
Achemtek	0104-046130	http://www.achemtek.com/54-96-6
Acros Organics	AC112390050	https://www.fishersci.com/shop/products/3-4-diaminopyridine-98-acros-organics-1/AC112390050
Acros Organics	AC112390250	https://www.fishersci.com/shop/products/3-4-diaminopyridine-98-acros-organics/AC112390250
Alfa Aesar	A12465	https://www.alfa.com/en/catalog/A12465/
Alinda	ALBB-005969	http://alinda.ru/finechem_en_.html?i=ALBB-005969
Allbio Pharm Co., Ltd	AF09092	http://www.allbiopharm.com/product/n/AF09092
Ampyridine	AM11000	https://www.ampyridine.com/pyridine/54-96-6.html
Anward	ANW-32223	http://www.anward.com/pro_result/13214
Ark Pharm	AK-26114	http://www.arkpharminc.com/products/54-96-6.html
Aromalake	3,4-Diaminopyridine	http://www.aromalake.com/34-Diaminopyridine-p42.html
Aromalake	LS00018	http://www.aromalake.com/34-Diaminopyridine-p42.html
AstaTech, Inc.	CL0116	http://www.astatechinc.com/CPSResult.php?CRNO=11308
Aurora Fine Chemicals LLC	A00.299.131	http://online.aurorafinechemicals.com/info?ID=A00.299.131
Aurora Fine Chemicals LLC	K01.795.664	http://online.aurorafinechemicals.com/info?ID=K01.795.664
Aurum Pharmatech LLC	M-3620	http://www.Aurumpharmatech.com/Product/ProductDetails/M_3620
Avantor Inc	BT218670-1G	https://us.vwr.com/store/product/16902257/3-4-diaminopyridine-98
Avantor Inc	BT218670-25G	https://us.vwr.com/store/product/16902257/3-4-diaminopyridine-98
Avantor Inc	BT218670-5G	https://us.vwr.com/store/product/16902257/3-4-diaminopyridine-98
BLD Pharm	BD9613	http://www.bldpharm.com/products/54-96-6.html
Beijing Acemol Technology	AMPD00217	http://www.acemol.com/products/PAMPD00217.shtml
BioChemPartner	BCP22343	http://www.biochempartner.com/54-96-6-BCP22343
BioCrick	BCC5185	http://www.biocrick.com/Amifampridine-BCC5185.html
BioSynth	W-105592	https://www.biosynth.com/en/products/chemical-intermediates/basic-intermediates/products/W-105592.html
BioSynth	J-610017	https://www.biosynth.com/en/products/life-science/other-biochemicals/products/J-610017.html
Boerchem	BC222447	http://www.boerchem.com/?product_41833.html
BroadPharm	BP-12781	http://www.broadpharm.com/web/product.php?catalog=BP-12781
CSNpharm	CSN19508	https://www.csnpharm.com/products/amifampridine.html
Capot Chemical	1295	http://www.capotchem.com/en/1295.htm
Capot Chemical	PubChem1295	http://www.capotchem.com/en/1295.htm
Chem Scene	CS-2778	http://www.chemscene.com/54-96-6.html
ChemMol	1201412	http://www.chemmol.com/chemmol/1201412.html
ChemMol	44006862	http://www.chemmol.com/chemmol/44006862.html
ChemMol	49425879	http://www.chemmol.com/chemmol/49425879.html
ChemMol	81407478	http://www.chemmol.com/chemmol/81407478.html
ChemMol	81412195	http://www.chemmol.com/chemmol/81412195.html
ChemReagents	813047	http://www.chemreagents.com/Product/Product.asp?ProductID=813047
Chemenu	CM108190	http://www.chemenu.com/products/CM108190
Chemspace	CSSB00000752140	https://chem-space.com/CSSB00000752140
Coresyn	CM14022	http://www.coresyn.com/Cas54-96-6.html
Debye Scientific	DB-011105	http://www.debyesci.com/cas_54-96-6.html
Finetech	FT-0614203	http://www.finetechnology-ind.com/prod/detail/pub/54-96-6.html
Glentham Life Sciences	GK1922	http://www.glentham.com/products/product/GK1922/
Hairui	HR1295	http://www.hairuichem.com/en/product/54-96-6.html
Hefei Hirisun Pharmatech Co., Ltd	HR013379	http://www.hirisunpharm.com/54-96-6.html
LGC Standards	MM3483.00	https://www.lgcstandards.com/US/en/p/MM3483.00
Lab Network	LN00007606	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00007606
Lumtec	K0349	http://www.lumtec.com.tw/portal_c1_cnt_page.php?owner_num=c1_290785&button_num=c1&folder_id=32214&cnt_id=259189&search_field=&search_word=&search_field2=&search_word2=&search_field3=&search_word3=&bool1=&bool2=&search_type=1&up_page=1
MIC Scientific	HC150250	http://www.michemical.com/mkdetail.php?id=867
Matrix Scientific	11183	https://www.matrixscientific.com/011183.html
MedChem Express	HY-14946	https://www.medchemexpress.com/Amifampridine.html
Molcore	CS22778	https://www.molcore.com/product/54-96-6
MuseChem	I004036	https://www.musechem.com/product/I004036.html
OChem	2159	http://www.ocheminc.com/index.php?act=psearch&pid=006D401
Oakwood	43674	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=37550&ExtHyperLink=1
Oakwood	47550	http://www.oakwoodchemical.com/p-57797-047550.aspx
Parchem	28175	http://www.parchem.com/chemical-supplier-distributor/Amifampridine-018175.aspx
R&D Chemicals	D219	http://www.rdchemicals.com/chemicals.php?mode=details&mol_id=6534
Renno Tech	RP00483	http://www.rennotech.com/product_show.asp?id=6873
Sigma-Aldrich	D7148_ALDRICH	https://www.sigmaaldrich.com/catalog/product/aldrich/d7148?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sinfoo Biotech	S017614	http://www.sinfoobiotech.com/product/1021012
Smolecule	S518476	http://www.smolecule.com/products/s518476
Smolecule	S748722	https://www.smolecule.com/products/s748722
TCI (Tokyo Chemical Industry)	D1149	http://www.tcichemicals.com/eshop/en/us/commodity/D1149/index.html
THE BioTek	bt-259134	https://www.thebiotek.com/product/inhibitors/bt-259134
THE BioTek	bt-308561	https://www.thebiotek.com/product/others/bt-308561
VladaChem	VL141657	https://www.vladachem.com/product.php?products=54-96-6
VladaChem	VL263634-25G	https://www.vladachem.com/product.php?products=54-96-6
Yuhao Chemical	LQ0029	http://www.chemyuhao.com/54-96-6.html
abcr GmbH	AB115247	http://www.abcr.com/shop/en/AB115247
eNovation Chemicals	K02926	https://www.enovationchem.com/ProductDetails.asp?ProductID=K02926
eNovation Chemicals	K15425	https://www.enovationchem.com/ProductDetails.asp?ProductID=K15425
iChemical	EBD541096	http://www.ichemical.com/products/54-96-6.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
mcule	MCULE-5478459845	https://mcule.com/MCULE-5478459845/

PubMed

Title	Date	PubMed
Validation of a CE assay for the analysis of isomeric aminopyridines and diaminopyridines.	2001 Feb	11272328
Persistence of botulinum neurotoxin A demonstrated by sequential administration of serotypes A and E in rat EDL muscle.	2001 Feb-Mar	10978741
Theoretical analysis of the molecular determinants responsible for the K(+) channel blocking by aminopyridines.	2001 Jun 15	11403883
Aminopyridines for symptomatic treatment in multiple sclerosis.	2002	12804404
Improvement of dy/dy dystrophic diaphragm by 3,4-diaminopyridine.	2002 Jul	12115951
Treatment for Lambert-Eaton myasthenic syndrome.	2003	12804456
Wheel-running exercise alters rat diaphragm action potentials and their regulation by K+ channels.	2003 Aug	12704092
Electrophysiological and pharmacological characterization of K+-currents in muscle fibres isolated from the ventral sucker of Fasciola hepatica.	2004 Dec	15648701
Enhanced brain motor activity in patients with MS after a single dose of 3,4-diaminopyridine.	2004 Jun 8	15184612
NCAM 180 acting via a conserved C-terminal domain and MLCK is essential for effective transmission with repetitive stimulation.	2005 Jun 16	15953420
Taicatoxin inhibits the calcium-dependent slow motility of mammalian outer hair cells.	2005 May	15855042
Fetal exposure to 3,4-diaminopyridine in a pregnant woman with congenital myasthenia syndrome.	2006 Apr	16537815
Inotropic effects of the K+ channel blocker 3,4-diaminopyridine: differential responses of rat soleus and extensor digitorum longus.	2006 Dec	17190034
[Fatigue and episodic exhaustion as a feature of multiple sclerosis].	2006 Mar	16585884
Childhood myasthenia: clinical subtypes and practical management.	2007 Aug	17635211
Beneficial effects of 3,4-diaminopyridine on positioning downbeat nystagmus in a circumscribed uvulo-nodular lesion.	2007 Aug	17410325
Myasthenia gravis and Lambert-Eaton myasthenic syndrome in the same patient.	2007 Jul	17206662
[Treatment of Lambert-Eaton syndrome with 3,4- diaminopyridine and pyridostigmine].	2007 Jul-Aug	18052623
Molecular docking study of the binding of aminopyridines within the K+ channel.	2007 May	17340113
Long-lasting in vivo inotropic effects of the K(+) channel blocker 3,4-diaminopyridine during fatigue-inducing stimulation.	2008 Dec	19016549
[Lambert-Eaton Myasthenic Syndrome associated with vocal cord carcinoma].	2008 Jan	18342060
Autoantibodies in neuromuscular transmission disorders.	2008 Jul	19893659
Onset dynamics of type A botulinum neurotoxin-induced paralysis.	2008 Jun	18551355
Therapeutic strategies in congenital myasthenic syndromes.	2008 Oct	19019305
[A case of Lambert-Eaton myasthenic syndrome with small cell lung cancer, treated with 3,4-diaminopyridine].	2009 Jan	19198242
3,4-Diaminopyridine is more effective than placebo in a randomized, double-blind, cross-over drug study in LEMS.	2009 Nov	19722254
3,4-diaminopyridine safety in clinical practice: an observational, retrospective cohort study.	2010 Jun	20058019

Patents

Sample Use Guides

In Vivo Use Guide

Amifampridine (Firdapse) should be given in divided doses, three or four times a day. The recommended starting dose is 15 mg a day, which can be increased in 5 mg increments every 4 to 5 days, to a maximum of 60 mg per day. No single dose should exceed 20 mg. Tablets are to be taken with food. For oral use only.

Route of Administration: Oral

In Vitro Use Guide

In nerve terminal regions of axons in rat olfactory cortex in the presence of tetraethylammonium (TEA, 5 mM) and Cd2+ (100 uM), the K(+)-component was depressed by Amifampridine (3,4-DAP; 1 to 20 uM; IC50 2.0 +/- 0.4 uM).

Name

Type

Language

AMIFAMPRIDINE

Official Name

English

AMIFAMPRIDINE [MI]

Common Name

English

3,4 DIAMINOPYRIDINE

Systematic Name

English

AMIFAMPRIDINE [ORANGE BOOK]

Common Name

English

NSC-521760

Code

English

AMIFAMPRIDINE [INN]

Common Name

English

PYRIDINE, 3,4-DIAMINO-

Systematic Name

English

DAP

Common Name

English

AMIFAMPRIDINE [MART.]

Common Name

English

3,4-DIAMINOPYRIDINE

Systematic Name

English

AMIFAMPRIDINE [USAN]

Common Name

English

3,4 DIAMINOPYRIDINE [VANDF]

Common Name

English

3,4-DAP

Code

English

DYNAMINE

Brand Name

English

AMIFAMPRIDINE [WHO-DD]

Common Name

English

RUZURGI

Brand Name

English

AMIFAMPRIDINE [EMA EPAR]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

56090