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

Stem definitionDrug idCAS RN
4163 504-24-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fampyra
  • dalfampridine
  • ampyra
  • pyridin-4-amine
  • 4-aminopyridine
  • fampridine
One of the POTASSIUM CHANNEL BLOCKERS with secondary effect on calcium currents which is used mainly as a research tool and to characterize channel subtypes.
  • Molecular weight: 94.12
  • Formula: C5H6N2
  • CLOGP: 0.32
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 38.91
  • ALOGS: 0.46
  • ROTB: 0

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 90.30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.04 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 2.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2010 FDA ACORDA

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
Urinary tract infection 3044.33 32.03 892 5805 29050 2322338
Gait disturbance 1915.54 32.03 588 6109 21957 2329431
Laboratory test abnormal 1896.54 32.03 433 6264 4857 2346531
Drug ineffective 1401.66 32.03 707 5990 100917 2250471
Multiple sclerosis relapse 1142.27 32.03 336 6361 10607 2340781
Balance disorder 1104.18 32.03 319 6378 9428 2341960
Urine analysis abnormal 1042.80 32.03 185 6512 444 2350944
Fall 1023.51 32.03 451 6246 46648 2304740
Insomnia 827.92 32.03 327 6370 25460 2325928
Dizziness 805.98 32.03 410 6287 58255 2293133
Therapy cessation 546.77 32.03 161 6536 5032 2346356
Multiple sclerosis 542.68 32.03 165 6532 5769 2345619
Muscular weakness 529.92 32.03 204 6493 14693 2336695
Seizure 527.16 32.03 234 6463 24232 2327156
Inappropriate schedule of product administration 520.81 32.03 191 6506 12013 2339375
Asthenia 484.23 32.03 272 6425 46654 2304734
Escherichia urinary tract infection 446.49 32.03 103 6594 1181 2350207
Fatigue 412.21 32.03 306 6391 84567 2266821
Headache 364.31 32.03 278 6419 79901 2271487
Therapeutic response unexpected 308.90 32.03 97 6600 3762 2347626
Gait inability 267.62 32.03 97 6600 5858 2345530
Hypoaesthesia 265.65 32.03 138 6559 20077 2331311
Paraesthesia 265.35 32.03 142 6555 21946 2329442
Culture urine positive 257.52 32.03 55 6642 427 2350961
Condition aggravated 251.56 32.03 156 6541 31823 2319565
Nausea 249.77 32.03 260 6437 111929 2239459
Urine leukocyte esterase positive 235.65 32.03 45 6652 181 2351207
B-lymphocyte count decreased 231.52 32.03 42 6655 118 2351270
Memory impairment 231.49 32.03 109 6588 12814 2338574
Product dose omission 223.64 32.03 155 6542 38102 2313286
Constipation 218.26 32.03 124 6573 21505 2329883
Back pain 217.91 32.03 142 6555 31517 2319871
Dysuria 202.75 32.03 71 6626 3870 2347518
Depression 200.46 32.03 129 6568 28003 2323385
Feeling abnormal 197.91 32.03 120 6577 23461 2327927
Adverse drug reaction 186.57 32.03 82 6615 8201 2343187
Pollakiuria 183.03 32.03 65 6632 3691 2347697
Muscle spasms 176.43 32.03 108 6589 21458 2329930
Tremor 175.52 32.03 106 6591 20555 2330833
Head injury 167.39 32.03 62 6635 3972 2347416
Mobility decreased 150.56 32.03 72 6625 8738 2342650
Malaise 139.66 32.03 138 6559 55447 2295941
Flushing 138.59 32.03 75 6622 11796 2339592
Walking aid user 137.89 32.03 36 6661 706 2350682
Pain in extremity 134.41 32.03 120 6577 42420 2308968
Dysstasia 132.39 32.03 48 6649 2891 2348497
Muscle spasticity 129.86 32.03 41 6656 1612 2349776
Generalised tonic-clonic seizure 126.82 32.03 55 6642 5317 2346071
Lymphocyte count decreased 126.08 32.03 48 6649 3315 2348073
White blood cells urine positive 125.86 32.03 30 6667 398 2350990
Micturition urgency 123.45 32.03 37 6660 1219 2350169
Burning sensation 121.76 32.03 60 6637 7768 2343620
Central nervous system lesion 120.33 32.03 41 6656 2053 2349335
Pain 115.20 32.03 131 6566 61726 2289662
Movement disorder 111.93 32.03 42 6655 2786 2348602
Confusional state 110.93 32.03 85 6612 24259 2327129
Abdominal discomfort 109.44 32.03 74 6623 17382 2334006
Urinary incontinence 108.68 32.03 46 6651 4187 2347201
T-lymphocyte count increased 108.44 32.03 18 6679 23 2351365
CD4 lymphocytes increased 105.60 32.03 18 6679 30 2351358
Red blood cells urine positive 102.52 32.03 23 6674 229 2351159
Musculoskeletal stiffness 101.72 32.03 62 6635 12185 2339203
Epilepsy 101.39 32.03 45 6652 4594 2346794
Urine abnormality 98.25 32.03 26 6671 538 2350850
Glycosylated haemoglobin increased 97.95 32.03 34 6663 1800 2349588
Urine odour abnormal 96.28 32.03 27 6670 699 2350689
Peroneal nerve palsy 95.85 32.03 27 6670 711 2350677
Haemoglobin urine present 95.26 32.03 17 6680 42 2351346
Cystitis 92.98 32.03 45 6652 5597 2345791
Cognitive disorder 88.92 32.03 43 6654 5338 2346050
T-lymphocyte count decreased 88.28 32.03 17 6680 72 2351316
Hypokinesia 87.85 32.03 31 6666 1723 2349665
Pruritus 87.79 32.03 96 6601 43244 2308144
Secondary progressive multiple sclerosis 86.97 32.03 21 6676 295 2351093
Full blood count abnormal 86.84 32.03 21 6676 297 2351091
Loss of consciousness 86.48 32.03 66 6631 18701 2332687
Urinary tract infection bacterial 86.36 32.03 23 6674 488 2350900
JC polyomavirus test positive 86.05 32.03 20 6677 236 2351152
Trigeminal neuralgia 85.16 32.03 24 6673 633 2350755
Dysgraphia 85.02 32.03 23 6674 519 2350869
Wheelchair user 84.02 32.03 22 6675 436 2350952
Loss of personal independence in daily activities 83.43 32.03 41 6656 5270 2346118
Influenza like illness 82.26 32.03 54 6643 12060 2339328
Stress 81.37 32.03 44 6653 6894 2344494
Therapeutic product effect decreased 80.42 32.03 51 6646 10738 2340650
Contusion 79.52 32.03 54 6643 12756 2338632
Escherichia test positive 78.61 32.03 19 6678 268 2351120
Status epilepticus 73.97 32.03 30 6667 2448 2348940
Vitamin B12 increased 73.69 32.03 15 6682 89 2351299
CD4 lymphocytes decreased 68.49 32.03 18 6679 362 2351026
Skin laceration 68.34 32.03 29 6668 2653 2348735
Red blood cell count decreased 64.22 32.03 32 6665 4234 2347154
Protein urine present 63.25 32.03 19 6678 630 2350758
Diarrhoea 62.77 32.03 115 6582 83449 2267939
Urinary tract infection pseudomonal 60.59 32.03 13 6684 103 2351285
Bacterial test positive 60.27 32.03 18 6679 585 2350803
Feeling hot 59.87 32.03 36 6661 6892 2344496
Speech disorder 59.54 32.03 35 6662 6429 2344959
Discomfort 58.49 32.03 32 6665 5127 2346261
Depressed mood 58.26 32.03 32 6665 5166 2346222
Rash 57.94 32.03 92 6605 59466 2291922
Vision blurred 57.67 32.03 47 6650 14621 2336767
CD8 lymphocytes decreased 57.04 32.03 11 6686 47 2351341
Urine ketone body present 55.80 32.03 15 6682 330 2351058
Neutrophil count increased 55.50 32.03 23 6674 1982 2349406
Haematocrit decreased 55.17 32.03 29 6668 4289 2347099
Vertigo 54.54 32.03 38 6659 9346 2342042
Dysphagia 54.53 32.03 43 6654 12762 2338626
Urinary tract infection enterococcal 54.47 32.03 14 6683 257 2351131
Vomiting 53.04 32.03 98 6599 71504 2279884
Tongue biting 52.56 32.03 14 6683 297 2351091
Anxiety 52.48 32.03 61 6636 29298 2322090
Lymphocyte count abnormal 51.75 32.03 12 6685 140 2351248
Urinary retention 50.78 32.03 26 6671 3641 2347747
Blood immunoglobulin M decreased 50.64 32.03 11 6686 93 2351295
White blood cell count decreased 48.88 32.03 47 6650 18161 2333227
Neurogenic bladder 48.30 32.03 14 6683 409 2350979
Temperature intolerance 47.57 32.03 17 6680 980 2350408
Dysarthria 47.46 32.03 30 6667 6272 2345116
Extra dose administered 47.38 32.03 18 6679 1233 2350155
Red blood cell count abnormal 47.30 32.03 11 6686 130 2351258
Adverse event 46.82 32.03 32 6665 7627 2343761
Nasopharyngitis 46.56 32.03 50 6647 22006 2329382
Vitamin D decreased 46.53 32.03 17 6680 1044 2350344
Abdominal pain upper 46.48 32.03 50 6647 22050 2329338
Ankle fracture 46.37 32.03 21 6676 2244 2349144
Lymphocyte percentage decreased 45.00 32.03 13 6684 375 2351013
Hip fracture 44.67 32.03 26 6671 4686 2346702
Urinary sediment present 44.57 32.03 11 6686 170 2351218
Dyskinesia 44.28 32.03 26 6671 4763 2346625
Syncope 44.24 32.03 43 6654 16832 2334556
Motor dysfunction 43.95 32.03 17 6680 1223 2350165
Migraine 43.69 32.03 35 6662 10618 2340770
Nitrite urine present 43.58 32.03 10 6687 111 2351277
Palpitations 43.27 32.03 42 6655 16414 2334974
Somnolence 42.29 32.03 49 6648 23436 2327952
B-lymphocyte count abnormal 41.72 32.03 7 6690 10 2351378
Lymphopenia 41.70 32.03 20 6677 2434 2348954
Amnesia 41.27 32.03 29 6668 7224 2344164
Hemiparesis 40.77 32.03 22 6675 3428 2347960
Initial insomnia 40.46 32.03 14 6683 733 2350655
Primary progressive multiple sclerosis 40.13 32.03 8 6689 42 2351346
Feeling jittery 39.83 32.03 18 6679 1914 2349474
Influenza 39.63 32.03 36 6661 12942 2338446
Oropharyngeal pain 39.26 32.03 34 6663 11484 2339904
Ataxia 38.41 32.03 19 6678 2473 2348915
Mental status changes 38.15 32.03 25 6672 5557 2345831
Throat irritation 38.01 32.03 24 6673 5006 2346382
Diplopia 37.91 32.03 21 6676 3444 2347944
Transferrin saturation decreased 37.67 32.03 8 6689 60 2351328
Dyspepsia 37.53 32.03 31 6666 9813 2341575
White blood cell count increased 37.28 32.03 27 6670 7051 2344337
Blood thyroid stimulating hormone increased 36.52 32.03 14 6683 983 2350405
Alopecia 36.46 32.03 44 6653 21957 2329431
Coordination abnormal 36.22 32.03 17 6680 1971 2349417
Blood thyroid stimulating hormone decreased 35.70 32.03 12 6685 575 2350813
Sepsis 35.69 32.03 40 6657 18448 2332940
Mean cell haemoglobin decreased 35.39 32.03 10 6687 266 2351122
Red cell distribution width increased 35.39 32.03 12 6685 591 2350797
Urinary tract disorder 35.13 32.03 11 6686 420 2350968
Dermatomyositis 34.98 32.03 11 6686 426 2350962
Arthralgia 34.86 32.03 70 6627 54215 2297173
Visual impairment 34.71 32.03 32 6665 11723 2339665
Proteus test positive 34.46 32.03 7 6690 41 2351347
Progressive multiple sclerosis 33.96 32.03 9 6688 187 2351201
Muscle tightness 33.81 32.03 16 6681 1889 2349499
Muscle twitching 33.70 32.03 18 6679 2747 2348641
Blood glucose increased 33.49 32.03 32 6665 12258 2339130
Weight decreased 33.45 32.03 48 6649 28323 2323065
Neck pain 33.08 32.03 26 6671 7671 2343717
Optic neuritis 32.87 32.03 15 6682 1631 2349757
Nervousness 32.47 32.03 22 6675 5167 2346221

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
Drug ineffective 671.64 37.29 307 1986 63494 1680994
Gait disturbance 669.03 37.29 201 2092 12469 1732019
Laboratory test abnormal 612.65 37.29 150 2143 4209 1740279
Urinary tract infection 487.03 37.29 150 2143 10003 1734485
Multiple sclerosis relapse 451.65 37.29 110 2183 2990 1741498
Fall 336.13 37.29 148 2145 27066 1717422
Balance disorder 303.80 37.29 92 2201 5720 1738768
Insomnia 261.67 37.29 107 2186 16169 1728319
Multiple sclerosis 207.75 37.29 55 2238 2077 1742411
Muscular weakness 201.35 37.29 78 2215 10171 1734317
Seizure 161.30 37.29 82 2211 20359 1724129
Inappropriate schedule of product administration 157.89 37.29 60 2233 7399 1737089
B-lymphocyte count decreased 151.88 37.29 25 2268 71 1744417
Dizziness 148.94 37.29 93 2200 34268 1710220
Therapy cessation 139.57 37.29 44 2249 3095 1741393
Therapeutic response unexpected 120.41 37.29 37 2256 2387 1742101
Fatigue 116.12 37.29 93 2200 50688 1693800
Asthenia 113.89 37.29 79 2214 34591 1709897
Condition aggravated 100.90 37.29 61 2232 21089 1723399
Back pain 100.70 37.29 56 2237 16557 1727931
Headache 91.48 37.29 69 2224 34307 1710181
Constipation 86.61 37.29 49 2244 14951 1729537
Gait inability 81.78 37.29 30 2263 3333 1741155
Flushing 76.28 37.29 34 2259 6245 1738243
Muscle spasticity 67.20 37.29 21 2272 1428 1743060
Paraesthesia 65.33 37.29 36 2257 10415 1734073
Adverse drug reaction 65.14 37.29 28 2265 4710 1739778
Memory impairment 61.99 37.29 30 2263 6633 1737855
Secondary progressive multiple sclerosis 60.81 37.29 12 2281 114 1744374
Full blood count abnormal 58.84 37.29 13 2280 222 1744266
Nausea 58.66 37.29 64 2229 51132 1693356
JC polyomavirus test positive 58.41 37.29 12 2281 142 1744346
Urine analysis abnormal 55.30 37.29 13 2280 296 1744192
Product dose omission 55.04 37.29 43 2250 22397 1722091
Dysuria 54.77 37.29 23 2270 3649 1740839
Walking aid user 53.16 37.29 12 2281 227 1744261
Movement disorder 52.35 37.29 18 2275 1652 1742836
Vitamin B12 increased 50.15 37.29 9 2284 48 1744440
Depression 49.88 37.29 36 2257 16633 1727855
Trigeminal neuralgia 48.43 37.29 11 2282 214 1744274
Tremor 47.81 37.29 32 2261 13099 1731389
Muscle spasms 46.39 37.29 30 2263 11591 1732897
Mobility decreased 46.33 37.29 21 2272 3999 1740489
Haematocrit decreased 45.11 37.29 21 2272 4252 1740236
Peroneal nerve palsy 44.55 37.29 12 2281 480 1744008
Hip fracture 44.13 37.29 16 2277 1714 1742774
Central nervous system lesion 43.97 37.29 14 2279 1010 1743478
Influenza like illness 43.80 37.29 23 2270 6030 1738458
Generalised tonic-clonic seizure 43.07 37.29 20 2273 4026 1740462
Cystitis 40.58 37.29 14 2279 1297 1743191
Pain in extremity 40.14 37.29 33 2260 18439 1726049
Feeling abnormal 40.12 37.29 27 2266 11139 1733349
Glycosylated haemoglobin increased 39.13 37.29 15 2278 1876 1742612

Pharmacologic Action:

SourceCodeDescription
ATC N07XX07 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D026902 Potassium Channel Blockers
CHEBI has role CHEBI:71031 orphan drug
CHEBI has role CHEBI:33289 avicide
FDA EPC N0000192795 Potassium Channel Blocker
FDA MoA N0000175448 Potassium Channel Antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Multiple sclerosis indication 24700007 DOID:2377
Seizure disorder contraindication 128613002
Impaired renal function disorder contraindication 197663003

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.58 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG AMPYRA ACORDA N022250 Jan. 22, 2010 RX TABLET, EXTENDED RELEASE ORAL 8440703 April 8, 2025 IMPROVEMENT OF WALKING IN PATIENTS WITH MULTIPLE SCLEROSIS (MS)
10MG AMPYRA ACORDA N022250 Jan. 22, 2010 RX TABLET, EXTENDED RELEASE ORAL 8354437 Dec. 22, 2026 IMPROVEMENT OF WALKING IN PATIENTS WITH MULTIPLE SCLEROSIS (MS)
10MG AMPYRA ACORDA N022250 Jan. 22, 2010 RX TABLET, EXTENDED RELEASE ORAL 8007826 May 26, 2027 IMPROVEMENT OF WALKING IN PATIENTS WITH MULTIPLE SCLEROSIS (MS)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-gated potassium channel Ion channel BLOCKER CHEMBL CHEMBL
Potassium voltage-gated channel subfamily C member 1 Unclassified BLOCKER IC50 4.50 IUPHAR
Potassium voltage-gated channel subfamily C member 2 Unclassified BLOCKER IC50 4.60 IUPHAR

External reference:

IDSource
4029704 VUID
N0000180628 NUI
C0000477 UMLSCUI
D04127 KEGG_DRUG
80994002 SNOMEDCT_US
413355004 SNOMEDCT_US
NOCODE MMSL
4025700 VANDF
4025705 VANDF
897018 RXNORM
26967 MMSL
d07546 MMSL
4029704 VANDF
006829 NDDF
BH3B64OKL9 UNII
7283 INN_ID
CHEMBL284348 ChEMBL_ID
4AP PDB_CHEM_ID
DB06637 DRUGBANK_ID
CHEBI:34385 CHEBI
D015761 MESH_DESCRIPTOR_UI
1727 PUBCHEM_CID
2416 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 0054-0479 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 0378-0509 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA authorized generic 17 sections
AMPYRA HUMAN PRESCRIPTION DRUG LABEL 1 10144-427 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 18 sections
Dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 16729-292 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
DALFAMPRIDINE HUMAN PRESCRIPTION DRUG LABEL 1 42571-275 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 51407-246 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 62756-429 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
DALFAMPRIDINE HUMAN PRESCRIPTION DRUG LABEL 1 65862-863 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Dalfampridine HUMAN PRESCRIPTION DRUG LABEL 1 67877-444 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections