Minoxidil

Summary

Minoxidil (CHEMBL802) is an approved small-molecule vasodilator agent (ATC C02DC01) targeting KCNJ8 and KCNJ11; indicated across 6 conditions including androgenetic alopecia and hypertensive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C02DC01 (+1 more)
• Targets: 2 (KCNJ8, KCNJ11)
• Indications: 6 conditions
• Clinical trials: 59
• Chemistry: 209.25 Da · C9H15N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL802
Name	Minoxidil
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4201
ChEBI	CHEBI:6942
ATC	C02DC01, D11AX01
Molecular formula	C9H15N5O
Molecular weight	209.25
InChIKey	ZIMGGGWCDYVHOY-UHFFFAOYSA-N

SMILES: C1CCN(CC1)C2=NC(=N)N(C(=C2)N)O

IUPAC name: 3-hydroxy-2-imino-6-piperidin-1-ylpyrimidin-4-amine

ChEBI definition: A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.

Pharmacological roles (ChEBI): vasodilator agent, antihypertensive agent.

Also known as: Alopexil, Alostil, Loniten, Lonolox, Men’s rogaine, Minodyl, Minoxidil, Minoxidil (for men), Minoxidil (for women), Minoxidil extra strength (for men), Minoximen, Mintop

Patent coverage: 11,194 distinct patent families (34,950 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 34,826 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
KCNJ8	Kir6.1			0%	Q15842
KCNJ11	Kir6.2			0.1%	Q14654

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Inositol monophosphatase 1, 4’-phosphopantetheinyl transferase ffp, Histone-lysine N-methyltransferase 2A, Thyrotropin receptor, Cytochrome P450 1A2, Lethal factor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P97697	6.05	Potency	891.3	nM	CHEMBL_ACT_4407990
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_3938189
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_4743268
KMT2A	5.05	Potency	8912	nM	CHEMBL_ACT_3792418

Target pathways

Aggregated over 2 target gene(s): KCNJ8, KCNJ11.

Top Reactome pathways

17 total, by targets touching each:

Pathway	Targets	Genes
Neuronal System	2	KCNJ11, KCNJ8
ATP sensitive Potassium channels	2	KCNJ11, KCNJ8
Inwardly rectifying K+ channels	2	KCNJ11, KCNJ8
Potassium Channels	2	KCNJ11, KCNJ8
Metabolism	1	KCNJ11
Integration of energy metabolism	1	KCNJ11
Disease	1	KCNJ11
Transport of small molecules	1	KCNJ11
ABC-family protein mediated transport	1	KCNJ11
Muscle contraction	1	KCNJ11
Regulation of insulin secretion	1	KCNJ11
Cardiac conduction	1	KCNJ11
Ion homeostasis	1	KCNJ11
ABC transporter disorders	1	KCNJ11
Disorders of transmembrane transporters	1	KCNJ11
Defective ABCC9 causes CMD10, ATFB12 and Cantu syndrome	1	KCNJ11
Defective ABCC8 can cause hypo- and hyper-glycemias	1	KCNJ11

Dominant GO biological processes

GO term	Targets
response to hypoxia	2
response to ischemia	2
ventricular cardiac muscle tissue development	2
potassium ion transport	2
apoptotic process	2
determination of adult lifespan	2
response to xenobiotic stimulus	2
response to ATP	2
regulation of monoatomic ion transmembrane transport	2
CAMKK-AMPK signaling cascade	2
potassium ion transmembrane transport	2
obsolete inorganic cation transmembrane transport	2
response to resveratrol	2
potassium ion import across plasma membrane	2
action potential	2

Indications & clinical

Indications

6 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
androgenetic alopecia	4	MONDO:0005339	EFO:0004191
hypertensive disorder	4	MONDO:0005044	EFO:0000537
alopecia	4	MONDO:0004907	MONDO:0003037
ovarian cancer	2	MONDO:0008170	MONDO:0008170
acne	1	MONDO:0011438	EFO:0003894

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 59.

Phase distribution

Phase	Trials
PHASE3	14
PHASE2	13
Not specified	12
PHASE4	7
PHASE1/PHASE2	4
EARLY_PHASE1	4
PHASE1	3
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04207931	PHASE4	RECRUITING	Treatment Results for Patients With Central Centrifugal Cicatricial Alopecia (CCCA): a Multicenter Prospective Study
NCT07459933	PHASE4	NOT_YET_RECRUITING	Topical Methotrexate vs Minoxidil for Localized Alopecia Areata
NCT07518342	PHASE4	NOT_YET_RECRUITING	The Effect of Nanofat Injection on Androgenetic Alopecia
NCT03535233	PHASE4	COMPLETED	Topical 5% Minoxidil and Potent Topical Corticosteroid Versus Intralesional Corticosteroid in the Treatment of Alopecia Areata
NCT04090801	PHASE4	COMPLETED	Comparison of Topical Minoxidil 5% in Ethanol Plus Propylene Glycol Versus Minoxidil 5% in Ethanol Alone in Treatment of Women With Female Pattern Hair Loss
NCT04209803	PHASE4	COMPLETED	N-Acetyl-Cysteine for Treatment of AGA in Men
NCT04293822	PHASE4	UNKNOWN	Topical Cetirizine 1% vs Minoxidil 5% Gel in Treatment of Androgenetic Alopecia
NCT04594018	PHASE3	RECRUITING	Efficacy and Safety of Finlândia Hair Lotion Association on Androgenetic Alopecia
NCT05888922	PHASE3	RECRUITING	Evaluation of Efficacy and Safety of Oral Minoxidil 1 mg in Female Androgenetic Alopecia
NCT06501924	PHASE3	NOT_YET_RECRUITING	Clinical Study of DA-002 and DA-005 As a Treatment for Hair Loss
NCT07273799	PHASE3	NOT_YET_RECRUITING	Comparison of Outcomes Between Topical Minoxidil Versus Oral Minoxidil for the Treatment of Androgenetic Alopecia
NCT07435012	PHASE3	RECRUITING	Androgenic Alopecia TH07 Clinical Trial
NCT07529977	PHASE3	NOT_YET_RECRUITING	Phase 3 Study to Evaluate the Efficacy and Safety of Oral Minoxidil (N1087) in Men With Androgenetic Alopecia.
NCT00151515	PHASE3	COMPLETED	A Study to Evaluate the Effectiveness and Safety of 5 Percent Minoxidil Foam in the Treatment of Male Pattern Hair Loss
NCT00958750	PHASE3	COMPLETED	Efficacy and Safety Study to Compare Two Minoxidil Formulations on Women With Androgenetic Alopecia
NCT01655108	PHASE3	UNKNOWN	Efficacy and Safety of Mesotherapy With Minoxidil 0.5%/2ml for Androgenetic Alopecia in Female Patients
NCT03753113	PHASE3	COMPLETED	Evaluating the Topical Herbal Solution on the Treatment of Male Pattern Hair Loss and Comparison With Minoxidil 5%
NCT04481412	PHASE2/PHASE3	COMPLETED	Topical Cetirizine in Androgenetic Alopecia in Females
NCT04721548	PHASE3	COMPLETED	Treatment of Androgenetic Alopecia in Men for 24 Weeks
NCT05989165	PHASE3	COMPLETED	Effectiveness of Combination Therapy of Microneedling and Minoxidil in Androgenetic Alopecia of Indonesian Men
NCT05990400	PHASE2/PHASE3	UNKNOWN	Effectiveness and Safety of Topical Finasteride and Minoxidil Combination Compared to Topical Minoxidil for The Treatment of Male Androgenetic Alopecia
NCT06484881	PHASE3	WITHDRAWN	Clinical Study of Probiotic Treatment for Androgenetic Alopecia
NCT06924632	PHASE3	COMPLETED	Efficacy & Safety of Minoxidil SL Tablets in Men With AGA
NCT05778825	PHASE2	ACTIVE_NOT_RECRUITING	A Study of Oral Minoxidil to Treat Hair Loss in Children, Teens, and Young Adults Who Are Cancer Survivors
NCT06826001	PHASE2	NOT_YET_RECRUITING	Various Procedural Treatment Options for Androgenetic Alopecia
NCT07011485	PHASE2	ACTIVE_NOT_RECRUITING	A Safety and Efficacy Study of PDFE-2304 Topical Solution for the Treatment of Androgenic Alopecia.
NCT07203599	PHASE1/PHASE2	RECRUITING	A Study on the Treatment of Androgenetic Alopecia in Young Men With Umbilical Cord Mesenchymal Stem Cell Exosomes
NCT07594678	PHASE2	NOT_YET_RECRUITING	Minoxidil With or Without Low-Level Red-Light Therapy for Improving Chemotherapy-Induced Alopecia in Breast Cancer Patients
NCT00175617	PHASE2	COMPLETED	Efficacy of Therapy With the Spironolactone Pills Compared to Minoxidil Lotion in Female Pattern Hair Loss
NCT00876200	PHASE2	COMPLETED	Efficacy of Minoxidil in Children With Williams-Beuren Syndrome
NCT01319370	PHASE2	COMPLETED	Effectiveness and Safety of Minoxidil Foam Versus Placebo Foam for Androgenetic Alopecia
NCT01325337	PHASE2	COMPLETED	Safety and Efficacy Study of Bimatoprost in the Treatment of Men With Androgenic Alopecia
NCT01325350	PHASE2	COMPLETED	Safety and Efficacy Study of Bimatoprost in the Treatment of Women With Female Pattern Hair Loss
NCT01900041	PHASE2	COMPLETED	A Study to Evaluate the Superiority, Efficacy and Tolerability of Combination Pantovigar With 2% Minoxidil vs 2% Minoxidil in Women With Female Pattern Hair Loss
NCT03488108	PHASE1/PHASE2	COMPLETED	Platelet Rich Plasma Versus Minoxidil Foam for Treatment of Androgenic Alopecia in Women
NCT03852992	PHASE2	WITHDRAWN	Laser Assisted Delivery of Minoxidil in Androgenetic Alopecia
NCT05272462	PHASE2	UNKNOWN	Oral Minoxidil for the Treatment of Recurrent Platinum Resistant Epithelial Ovarian Cancer
NCT05636904	PHASE1/PHASE2	COMPLETED	Safety and Efficacy Study of Topical DLQ01 in the Treatment of Androgenetic Alopecia (AGA) in Men
NCT06333600	PHASE1/PHASE2	UNKNOWN	Efficacy and Safety of Topical Vitamin D Analogue in Treatment of Female Pattern Hair Loss
NCT07076706	PHASE2	COMPLETED	Clinical Trial to Evaluate CG2001 in Chinese Adult Male Participants With Androgenetic Alopecia

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

8 molecules share ≥1 primary target. Top 8 by shared-target count:

Molecule	Source	Status	Shared targets
glyburide	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11, KCNJ8
CROMAKALIM	ChEMBL	Phase 2	KCNJ11, KCNJ8
DIAZOXIDE	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11
PROPAFENONE	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11
PINACIDIL	ChEMBL	Phase 4 (approved)	KCNJ11
CLAMIKALANT	ChEMBL	Phase 2	KCNJ11
TIFENAZOXIDE	ChEMBL	Phase 2	KCNJ11
Berberine Chloride	PubChem	Approved	KCNJ11