Capsaicin

Summary

Capsaicin (CHEMBL294199) is an approved small-molecule non-narcotic analgesic (ATC N01BX04) targeting TRPV1, KCNA1, and KCNA2; indicated across 41 conditions including arthritic joint disease and frozen shoulder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01BX04 (+1 more)
• Targets: 6 (TRPV1, KCNA1, KCNA2…)
• Indications: 41 conditions
• Clinical trials: 137
• Chemistry: 305.4 Da · C18H27NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL294199
Name	Capsaicin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	1548943
ChEBI	CHEBI:3374
ATC	N01BX04, M02AB01
Molecular formula	C18H27NO3
Molecular weight	305.4
InChIKey	YKPUWZUDDOIDPM-SOFGYWHQSA-N

SMILES: CC(C)/C=C/CCCCC(=O)NCC1=CC(=C(C=C1)O)OC

IUPAC name: (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide

Pharmacological roles (ChEBI): non-narcotic analgesic, voltage-gated sodium channel blocker, TRPV1 agonist.

Also known as: ALGRX 4975, ALGRX-4975, Ausanil, Axsain, Capsaicin, Capsaicina, Capsaicine, Capzasin-hp, Cntx-4975, Dolenon, FEMA NO. 3404, Mioton

Patent coverage: 19,060 distinct patent families (52,939 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 52,501 (99%) 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
TRPV1	TRPV1	Agonist	7.5	0.3%	Q8NER1
KCNA1	Kv1.1		4.5	0%	Q09470
KCNA2	Kv1.2	Pore blocker	4.4	0.7%	P16389
KCNA7	Kv1.7		4.6	0.5%	Q96RP8
KCNC1	Kv3.1		3.8	1.7%	P48547
CFTR	CFTR	Potentiation		0.1%	P13569

Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Transient receptor potential cation channel subfamily M member 8, Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, Inositol monophosphatase 1, 4’-phosphopantetheinyl transferase ffp, Menin/Histone-lysine N-methyltransferase MLL, Vanilloid receptor, Polyunsaturated fatty acid 5-lipoxygenase.

Bioactivity

ChEMBL activities: 58 potent at pChembl ≥ 5 of 86 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
TRPV1	8.6	EC50	2.51	nM	CHEMBL_ACT_3292346
TRPV1	8.41	EC50	3.9	nM	CHEMBL_ACT_8032045
TRPV1	8.3	EC50	5	nM	CHEMBL_ACT_25536712
TRPV1	8.28	EC50	5.3	nM	CHEMBL_ACT_15161504
TRPV1	8.28	EC50	5.3	nM	CHEMBL_ACT_22772984
TRPV1	8.22	Ki	6	nM	CHEMBL_ACT_3597070
TRPV1	8.14	EC50	7.2	nM	CHEMBL_ACT_19190324
TRPV1	8.1	IC50	8	nM	CHEMBL_ACT_15161499
TRPV1	8.1	IC50	8	nM	CHEMBL_ACT_22772989
TRPV1	8.1	IC50	8	nM	CHEMBL_ACT_25536741
O35433	7.72	IC50	19	nM	CHEMBL_ACT_3597072
TRPV1	7.7	EC50	19.95	nM	CHEMBL_ACT_1204433
TRPV1	7.7	EC50	20	nM	CHEMBL_ACT_2528363
DRD3	7.64	AC50	23	nM	CHEMBL_ACT_25194183
TRPV1	7.59	EC50	25.9	nM	CHEMBL_ACT_19148118
TRPV1	7.54	EC50	29	nM	CHEMBL_ACT_24785206
O35433	7.52	EC50	30	nM	CHEMBL_ACT_509493
TRPV1	7.4	EC50	40	nM	CHEMBL_ACT_1951532
TRPV1	7.4	EC50	40	nM	CHEMBL_ACT_3074188
O35433	7.35	EC50	44.8	nM	CHEMBL_ACT_19148123
TRPV1	7.35	EC50	44.8	nM	CHEMBL_ACT_22994496
O35433	7.35	EC50	44.8	nM	CHEMBL_ACT_2389124
O35433	7.35	EC50	44.8	nM	CHEMBL_ACT_998806
TRPV1	6.7	EC50	200	nM	CHEMBL_ACT_29059684
O35433	6.52	EC50	300	nM	CHEMBL_ACT_786105
O35433	6.52	EC50	300	nM	CHEMBL_ACT_848468
O35433	6.52	EC50	300	nM	CHEMBL_ACT_88485
O35433	6.52	EC50	300	nM	CHEMBL_ACT_93421
O35433	6.52	EC50	300	nM	CHEMBL_ACT_950964
TRPV1	6.5	IC50	313	nM	CHEMBL_ACT_25706563

Target pathways

Aggregated over 6 target gene(s): TRPV1, KCNA1, KCNA2, KCNA7, KCNC1, CFTR.

Top Reactome pathways

15 total, by targets touching each:

Pathway	Targets	Genes
Neuronal System	4	KCNA1, KCNA2, KCNA7, KCNC1
Potassium Channels	4	KCNA1, KCNA2, KCNA7, KCNC1
Voltage gated Potassium channels	4	KCNA1, KCNA2, KCNA7, KCNC1
TRP channels	1	TRPV1
ABC-family protein mediated transport	1	CFTR
RHO GTPases regulate CFTR trafficking	1	CFTR
Defective CFTR causes cystic fibrosis	1	CFTR
Ub-specific processing proteases	1	CFTR
Cargo recognition for clathrin-mediated endocytosis	1	CFTR
Clathrin-mediated endocytosis	1	CFTR
RHOQ GTPase cycle	1	CFTR
Chaperone Mediated Autophagy	1	CFTR
Late endosomal microautophagy	1	CFTR
Aggrephagy	1	CFTR
Developmental Lineage of Pancreatic Ductal Cells	1	CFTR

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	6
monoatomic ion transmembrane transport	6
transmembrane transport	6
action potential	4
protein homooligomerization	4
potassium ion transmembrane transport	4
potassium ion transport	4
sensory perception of pain	2
neuronal action potential	2
corpus callosum development	2
optic nerve development	2
regulation of presynaptic membrane potential	2
negative regulation of transcription by RNA polymerase II	1
fever generation	1
diet induced thermogenesis	1

Indications & clinical

Indications

41 indications (13 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
arthritic joint disease	4	MONDO:0005578	EFO:0005856
frozen shoulder	4	MONDO:0006763	EFO:1000941
disease of the tendon	4	MONDO:0100010	EFO:1001434
neuralgia	4	MONDO:0021667	EFO:0005762
osteoarthritis	4	MONDO:0005178	MONDO:0005178
diabetic neuropathy	3	MONDO:0006626	EFO:1000783
head and neck cancer	3	MONDO:0005627	EFO:0006859
osteoarthritis, knee	3	MONDO:0005416	EFO:0004616
peripheral nervous system disorder	3	MONDO:0003620	EFO:0009387
breast neoplasm	3	MONDO:0021100	MONDO:0007254
herpes zoster	3	MONDO:0005609	EFO:0006510
common cold	3	MONDO:0005709	EFO:0009364
peripheral neuropathy	3	MONDO:0005244	EFO:0003100
pulmonary arterial hypertension	2	MONDO:0015924	EFO:0001361
HIV infectious disease	2	MONDO:0005109	EFO:0000764
myofascial pain syndrome	2	MONDO:0006862	EFO:1001054
neuroma	2	MONDO:0002173	EFO:0009619
epicondylitis	2	MONDO:0001875	EFO:1001896
cardiovascular disorder	2	MONDO:0004995	EFO:0000319
pulmonary hypertension	2	MONDO:0005149	MONDO:0005149
stroke disorder	1	MONDO:0005098	EFO:0000712
brain injury	0	MONDO:0043510	MONDO:0043510
amyotrophic lateral sclerosis	0	MONDO:0004976	MONDO:0004976
migraine disorder	0	MONDO:0005277	MONDO:0005277

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

Clinical trials

Total trials: 137.

Phase distribution

Phase	Trials
Not specified	49
PHASE2	25
PHASE4	17
PHASE3	15
PHASE1	13
EARLY_PHASE1	11
PHASE1/PHASE2	4
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00176969	PHASE4	COMPLETED	Response of Topical Capsaicin in Alopecia Areata
NCT00655811	PHASE4	COMPLETED	Ethnic Differences in Response to Topical Capsaicin: A Psychophysical Study on Healthy Subjects
NCT00697034	PHASE4	TERMINATED	Effects of Capsaicin on the Structure, Distribution, and Function of Cutaneous Small Nerve Fibers in Psoriatic Skin
NCT00771511	PHASE4	WITHDRAWN	Cervical Capsaicin for Labor Induction and Pain Relief
NCT01223820	PHASE4	COMPLETED	Neuro-immunological Analysis of Idiopathic Rhinitis Patients and Controls Treated With Capsaicin.
NCT01252160	PHASE4	COMPLETED	Safety and Effectiveness of Repeated Administration of QUTENZA Patches for Treatment of Pain Caused by Nerve Damage
NCT01416116	PHASE4	COMPLETED	Method of Pre-treatment for Application of QUTENZA Capsaicin 8% Patch
NCT01704339	PHASE4	UNKNOWN	Qutenza for Critical Ischaemia in End Stage Renal Failure
NCT01713426	PHASE4	COMPLETED	A Study to Compare QUTENZA With Pregabalin for the Treatment of Peripheral Neuropathic Pain (PNP) After 8 Weeks of Treatment
NCT01862523	PHASE4	COMPLETED	Mechanisms of Capsaicin Treatment in Idiopathic Rhinitis Patients and Controls
NCT01974037	PHASE4	COMPLETED	Capsaicin on Salty Gustatory Cortices
NCT02288156	PHASE4	COMPLETED	Elaboration of Patient-friendly Treatment Strategy With Capsaicin Nasal Spray in Patients With Idiopathic Rhinitis
NCT03124407	PHASE4	COMPLETED	Osteoarthritis Knee Pain Relief Study of 0.25% 920-CGS-200
NCT03348735	PHASE4	TERMINATED	Localized Neuropathic Pain: Topical Treatment Versus Systemic Treatment
NCT04238208	PHASE4	COMPLETED	The Efficacy and Safety Profile of Capsaicin 8% Patch Versus 5% Lidocaine Patch in Males With Diabetic Neuropathy
NCT04283292	PHASE4	COMPLETED	Capsaicin for the Treatment of Cannabinoid Hyperemesis Syndrome
NCT05298202	PHASE4	COMPLETED	The Influence of Capsaicin Gel During Exercise Within the Heat
NCT05840562	PHASE3	RECRUITING	Capsaicin 179 mg Patch Versus Oral Duloxetine in Patients With Chemotherapy-induced Peripheral Neuropathy
NCT05997979	PHASE3	RECRUITING	Analgesic Effectiveness of Capsaicin 8% Cutaneous Patch in Children
NCT00003610	PHASE3	COMPLETED	Capsaicin Lozenges in Treating Patients With Mucositis Caused by Radiation Therapy
NCT00115310	PHASE3	COMPLETED	Study of NGX-4010 for the Treatment of Postherpetic Neuralgia
NCT00300222	PHASE3	COMPLETED	Study of NGX-4010 for the Treatment of Postherpetic Neuralgia
NCT00321672	PHASE3	COMPLETED	Study of NGX-4010 for the Treatment of Painful HIV-Associated Neuropathy
NCT00993070	PHASE2/PHASE3	COMPLETED	Efficacy and Safety Study of Topical Capsaicin in Painful Diabetic Neuropathy
NCT01231750	PHASE3	TERMINATED	Efficacy of Topical Capsaicin Cream for Stable Angina
NCT01478607	PHASE3	COMPLETED	A Study to Evaluate the Long-term Safety of Repeated QUTENZA Administration for Treatment of Pain Caused by Nerve Damage in Diabetic Patients
NCT01533428	PHASE3	COMPLETED	A Study to Evaluate Efficacy and Safety of a Single Application of Capsaicin 8%Transdermal Delivery System Compared to Placebo in Reducing Pain Intensity in Subjects With Painful Diabetic Peripheral Neuropathy (PDPN)
NCT02700815	PHASE3	COMPLETED	Capsaicin + Diclofenac Gel in Acute Back Pain or Neck Pain
NCT02823912	PHASE2/PHASE3	UNKNOWN	Capsaicin Effect on Cytokines Profile in Dyslipidemia
NCT02854670	PHASE2/PHASE3	TERMINATED	A Study of the Effects of Topical Capsaicin in the Treatment of Provoked Vestibulodynia
NCT03153813	PHASE3	TERMINATED	Capsaicin Patches In Knee Osteoarthritis In Obese Patients
NCT03794388	PHASE3	COMPLETED	Evaluation in the Treatment of Neuropathic Pain Post Breast Surgery
NCT04967664	PHASE3	COMPLETED	Comparison of Qutenza (8% Capsaicin) With a Low-dose Capsaicin for Treatment of Nerve Pain After Surgery
NCT05029297	PHASE3	COMPLETED	Study With Two Capsaicin Topic Treatments in Diabetic Neuropathy.
NCT05093478	PHASE3	COMPLETED	The Prevalence of Local Immunoglobulin E (IgE) Elevation and Its Effect on Intranasal Capsaicin Therapy in the Non-allergic Rhinitis Population
NCT06807164	PHASE2	RECRUITING	Serratus Plane Block (SPB) Versus Capsaïcine Versus Botox-A for Chronic Neuropathic Pain in Post-mastectomy Syndrome
NCT00004316	PHASE1/PHASE2	COMPLETED	Phase I/II Randomized, Placebo-Controlled Study of Capsaicin for Interstitial Cystitis and Vulvar Vestibulitis
NCT00008476	PHASE2	COMPLETED	Capsaicin to Control Pain Following Third Molar Extraction
NCT00034710	PHASE2	COMPLETED	Pilot Study of High-Dose Capsaicin Patches to Treat Postherpetic Neuralgia Pain
NCT00130949	PHASE2	COMPLETED	ALGRX 4975 in the Treatment of Tennis Elbow

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.

42 molecules share ≥1 primary target. Top 42 by shared-target count:

Molecule	Source	Status	Shared targets
Flecainide	PubChem	Approved	KCNA1, KCNA7
DALFAMPRIDINE	ChEMBL + PubChem	Phase 4 (approved)	KCNA1
IVACAFTOR	ChEMBL + PubChem	Phase 4 (approved)	CFTR
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	KCNA1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	TRPV1
ELEXACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
GLYBURIDE	ChEMBL	Phase 4 (approved)	CFTR
LUMACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
PROPOFOL	ChEMBL	Phase 4 (approved)	TRPV1
TEZACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
CORTISONE	ChEMBL + PubChem	Phase 3 (approved)	KCNA1
BAMOCAFTOR	ChEMBL	Phase 3	CFTR
BERGAPTEN	ChEMBL	Phase 3	KCNA2
CANNABINOL	ChEMBL	Phase 3	TRPV1
FRAMYCETIN	ChEMBL	Phase 3	TRPV1
QUERCETIN	ChEMBL	Phase 3	CFTR
RESINIFERATOXIN	ChEMBL	Phase 3	TRPV1
RUTIN	ChEMBL	Phase 3	CFTR
ZUCAPSAICIN	ChEMBL	Phase 3	TRPV1
CANNABIDIVARIN	ChEMBL	Phase 2	TRPV1
CANNABIGEROL	ChEMBL	Phase 2	TRPV1
GALICAFTOR	ChEMBL	Phase 2	CFTR
GENISTEIN	ChEMBL	Phase 2	CFTR
GLPG-2737	ChEMBL	Phase 2	CFTR
ICENTICAFTOR	ChEMBL	Phase 2	CFTR
ILEPCIMIDE	ChEMBL	Phase 2	TRPV1
JTS-653	ChEMBL	Phase 2	TRPV1
MAVATREP	ChEMBL	Phase 2	TRPV1
NAVOCAFTOR	ChEMBL	Phase 2	CFTR
NGD-8243	ChEMBL	Phase 2	TRPV1
OLVANIL	ChEMBL	Phase 2	TRPV1
PIPERINE	ChEMBL	Phase 2	TRPV1
RISELCAFTOR	ChEMBL	Phase 2	CFTR
SB-705498	ChEMBL	Phase 2	TRPV1
TETRAHYDROCANNABIVARIN	ChEMBL	Phase 2	TRPV1
TETRYLAMMONIUM	ChEMBL	Phase 2	KCNA1
Amiodarone	PubChem	Approved	KCNA7
Diltiazem	PubChem	Approved	KCNA1
methoxsalen	PubChem	Approved	KCNA1
Quinidine	PubChem	Approved	KCNA7
Tadalafil	PubChem	Approved	CFTR
Verapamil	PubChem	Approved	KCNA7