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

Stem definitionDrug idCAS RN
vasodilators 1814 38304-91-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • minoxidil
  • loniten
  • rogaine
A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371)
  • Molecular weight: 209.25
  • Formula: C9H15N5O
  • CLOGP: 0.02
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 93.63
  • ALOGS: -1.02
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.20 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.83 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 95 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11.50 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) 1.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 18, 1979 FDA

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
Hypertrichosis 208.18 19.95 39 3411 901 46681711
Product formulation issue 155.73 19.95 29 3421 647 46681965
Hair texture abnormal 57.86 19.95 17 3433 2839 46679773
Alopecia 57.22 19.95 65 3385 162349 46520263
Application site pruritus 44.18 19.95 15 3435 3998 46678614
Dermatitis contact 40.48 19.95 17 3433 8106 46674506
Wrong patient received product 38.10 19.95 11 3439 1726 46680886
Hair colour changes 37.77 19.95 11 3439 1781 46680831
Dandruff 36.96 19.95 7 3443 171 46682441
Hair growth abnormal 33.91 19.95 11 3439 2547 46680065
Product use in unapproved indication 33.19 19.95 37 3413 90236 46592376
Hypertension 30.39 19.95 53 3397 196303 46486309
Product use issue 30.10 19.95 36 3414 94608 46588004
Hypertensive crisis 29.30 19.95 16 3434 13599 46669013
Cardiac hypertrophy 29.12 19.95 8 3442 1049 46681563
Vanishing bile duct syndrome 22.80 19.95 6 3444 668 46681944
Application site exfoliation 21.67 19.95 5 3445 323 46682289
Hypertensive emergency 21.62 19.95 7 3443 1611 46681001
Arrhythmia 21.59 19.95 19 3431 34822 46647790
Hirsutism 20.50 19.95 6 3444 988 46681624

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
Hypertrichosis 376.71 19.44 60 4265 229 29947924
Product formulation issue 293.25 19.44 53 4272 485 29947668
Pericardial effusion 159.16 19.44 72 4253 21072 29927081
Product label on wrong product 55.42 19.44 8 4317 12 29948141
Alopecia 46.60 19.44 31 4294 19244 29928909
Ceruloplasmin increased 42.91 19.44 6 4319 6 29948147
Blood copper increased 42.43 19.44 6 4319 7 29948146
Nephrogenic systemic fibrosis 39.65 19.44 17 4308 4354 29943799
Erectile dysfunction 36.41 19.44 26 4299 18076 29930077
Scrotal oedema 32.51 19.44 11 4314 1478 29946675
Sexual dysfunction 31.55 19.44 16 4309 5985 29942168
Dermatitis contact 30.74 19.44 13 4312 3218 29944935
Hypertension 30.35 19.44 59 4266 121295 29826858
Cardiac failure congestive 30.13 19.44 48 4277 84359 29863794
Fluid overload 26.49 19.44 22 4303 19070 29929083
Libido decreased 26.44 19.44 13 4312 4553 29943600
Affective disorder 24.65 19.44 11 4314 3097 29945056
Dizziness 23.06 19.44 71 4254 194838 29753315
Palpitations 22.57 19.44 26 4299 33547 29914606
Oedema peripheral 22.34 19.44 48 4277 105784 29842369
Chorioretinopathy 21.35 19.44 8 4317 1444 29946709
Skin induration 21.35 19.44 9 4316 2210 29945943
Application site reaction 21.30 19.44 6 4319 438 29947715
Skin fibrosis 19.71 19.44 7 4318 1086 29947067

Pharmacologic Action:

SourceCodeDescription
ATC C02DC01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON
Pyrimidine derivatives
ATC D11AX01 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
FDA PE N0000175379 Arteriolar Vasodilation
FDA EPC N0000175564 Arteriolar Vasodilator
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator
CHEBI has role CHEBI:35674 antihypertensive

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Alopecia indication 56317004 DOID:987
Pericarditis contraindication 3238004 DOID:1787
Myocardial infarction contraindication 22298006 DOID:5844
Orthostatic hypotension contraindication 28651003
Cardiac tamponade contraindication 35304003 DOID:115
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Cerebrovascular disease contraindication 62914000 DOID:6713
Kidney disease contraindication 90708001 DOID:557
Angina pectoris contraindication 194828000
Cerebrovascular accident contraindication 230690007
Pheochromocytoma contraindication 302835009
Pericardial effusion contraindication 373945007 DOID:118
Dermatosis of scalp contraindication 402694007 DOID:3136

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.35 Basic
pKa2 2.62 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 2, Kir6.2 Ion channel OPENER CHEMBL SCIENTIFIC LITERATURE
ATP-sensitive inward rectifier potassium channel 1 Ion channel IC50 6.97 WOMBAT-PK

External reference:

IDSource
4018077 VUID
N0000146416 NUI
D00418 KEGG_DRUG
4018077 VANDF
C0699464 UMLSCUI
CHEBI:6942 CHEBI
MXD PDB_CHEM_ID
CHEMBL802 ChEMBL_ID
D008914 MESH_DESCRIPTOR_UI
DB00350 DRUGBANK_ID
4254 IUPHAR_LIGAND_ID
2987 INN_ID
5965120SH1 UNII
4201 PUBCHEM_CID
202706 RXNORM
1335 MMSL
2064 MMSL
5119 MMSL
7147 MMSL
d00135 MMSL
000637 NDDF
387272001 SNOMEDCT_US
49577002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Good Sense Hair Regrowth Treatmentfor Men HUMAN OTC DRUG LABEL 1 0113-0798 SOLUTION 3 g TOPICAL ANDA 16 sections
Good Sense Hair Regrowth Treatment HUMAN OTC DRUG LABEL 1 0113-1032 SOLUTION 5 g TOPICAL ANDA 16 sections
Good Sense Hair Regrowth Treatment HUMAN OTC DRUG LABEL 1 0113-1129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7202 SOLUTION 2 g TOPICAL ANDA 16 sections
basic care hair regrowth treatment HUMAN OTC DRUG LABEL 1 0113-7294 AEROSOL, FOAM 5 g TOPICAL ANDA 16 sections
Basic Care Hair Regrowth HUMAN OTC DRUG LABEL 1 0113-7798 SOLUTION 3 g TOPICAL ANDA 16 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-0032 SOLUTION 5 g TOPICAL ANDA 16 sections
minoxidil HUMAN OTC DRUG LABEL 1 0363-0294 AEROSOL, FOAM 5 g TOPICAL ANDA 16 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-1129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
Solution HUMAN OTC DRUG LABEL 1 0363-2173 SOLUTION 0.02 g TOPICAL ANDA 13 sections
Solution HUMAN OTC DRUG LABEL 1 0363-2173 SOLUTION 0.02 g TOPICAL ANDA 13 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-2294 AEROSOL, FOAM 5 g TOPICAL ANDA 16 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-2798 SOLUTION 3 g TOPICAL ANDA 16 sections
hair regrowth treatment HUMAN OTC DRUG LABEL 1 0363-7202 SOLUTION 2 g TOPICAL ANDA 16 sections
MinoxidilRegular Strength for Men HUMAN OTC DRUG LABEL 1 0472-0066 SOLUTION 2 g TOPICAL ANDA 15 sections
MinoxidilExtra Strength for Men HUMAN OTC DRUG LABEL 1 0472-0094 SOLUTION 50 mg TOPICAL ANDA 16 sections
minoxidil HUMAN OTC DRUG LABEL 1 0472-1660 AEROSOL, FOAM 5 g TOPICAL ANDA 15 sections
minoxidil HUMAN OTC DRUG LABEL 1 0472-1665 AEROSOL, FOAM 5 g TOPICAL ANDA 15 sections
Minoxidil HUMAN PRESCRIPTION DRUG LABEL 1 0591-5642 TABLET 2.50 mg ORAL ANDA 26 sections
Minoxidil HUMAN PRESCRIPTION DRUG LABEL 1 0591-5643 TABLET 10 mg ORAL ANDA 26 sections
just for men minoxidil HUMAN OTC DRUG LABEL 1 11509-0798 SOLUTION 3 g TOPICAL ANDA 16 sections
up and up hair regrowth treatment for women HUMAN OTC DRUG LABEL 1 11673-189 SOLUTION 2 g TOPICAL ANDA 16 sections
up and up hair regrowth treatment for women HUMAN OTC DRUG LABEL 1 11673-431 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
up and up hair regrowth treatment for men HUMAN OTC DRUG LABEL 1 11673-632 SOLUTION 5 g TOPICAL ANDA 16 sections
up and up hair regrowth treatment for men HUMAN OTC DRUG LABEL 1 11673-707 AEROSOL, FOAM 5 g TOPICAL ANDA 16 sections
Minoxidil HUMAN OTC DRUG LABEL 1 11822-0129 AEROSOL, FOAM 50 mg TOPICAL ANDA 16 sections
Minoxidil HUMAN OTC DRUG LABEL 1 11822-0202 SOLUTION 2 g TOPICAL ANDA 16 sections
Daylogic For Men HUMAN OTC DRUG LABEL 1 11822-0606 AEROSOL, FOAM 5 g TOPICAL ANDA 16 sections
minoxidil HUMAN OTC DRUG LABEL 1 11822-0798 SOLUTION 3 g TOPICAL ANDA 16 sections