Amorolfine

drug
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Also known as AmorolfinaAmorolfine (as hydrochloride)Amorolfine hclAmorolfine hydrochlorideLocerylLoceryl curanailOmicurSID50112777rel-AmorolfineSID144206074SID174007380SID170466078

Summary

Amorolfine (CHEMBL489411) is an approved small-molecule EC 1.14.13.132 (squalene monooxygenase) inhibitor (ATC D01AE16) targeting SCN9A; indicated across 1 condition including tinea unguium.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: D01AE16
  • Targets: 1 (SCN9A)
  • Indications: 1 condition
  • Clinical trials: 13
  • Chemistry: 317.5 Da · C21H35NO

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL489411
NameAmorolfine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID54260
ChEBICHEBI:599440
ATCD01AE16
Molecular formulaC21H35NO
Molecular weight317.5
InChIKeyMQHLMHIZUIDKOO-AYHJJNSGSA-N

SMILES: CCC(C)(C)C1=CC=C(C=C1)CC(C)CN2C[C@H](O[C@H](C2)C)C

IUPAC name: (2S,6R)-2,6-dimethyl-4-[2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine

ChEBI definition: A member of the class of morpholines that is cis-2,6-dimethylmorpholine in which the hydrogen attached to the nitrogen is replaced by a racemic 2-methyl-3-[p-(2-methylbutan-2-yl)phenyl]propyl group. An inhibitor of the action of squalene monooxygenase, Δ14 reductase and D7-D8 isomerase and an antifungal agent, it is used (generally as its hydrochloride salt) for the topical treatment of fungal nail and skin infections.

Pharmacological roles (ChEBI): EC 1.14.13.132 (squalene monooxygenase) inhibitor, EC 5.3.3.5 (cholestenol Δ-isomerase) inhibitor, EC 1.3.1.70 (Δ14-sterol reductase) inhibitor.

Also known as: Amorolfina, Amorolfine, Amorolfine (as hydrochloride), Amorolfine hcl, Amorolfine hydrochloride, Loceryl, Loceryl curanail, Omicur, SID50112777, rel-Amorolfine, AMOROLFINE, SID144206074

Parent form; salt/anhydrous children: CHEMBL4303363

Patent coverage: 2,280 distinct patent families (7,765 SureChEMBL compound mentions), from 1 matched compound structure(s). 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).

GeneTargetActionpAffinityCancer dependencyUniProt
SCN9ANav1.74.020%Q15858

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Nuclear receptor ROR-gamma, Muscarinic acetylcholine receptor M1, D(3) dopamine receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Adenosine receptor A3.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): SCN9A.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Developmental Biology1SCN9A
L1CAM interactions1SCN9A
Muscle contraction1SCN9A
Axon guidance1SCN9A
Interaction between L1 and Ankyrins1SCN9A
Cardiac conduction1SCN9A
Phase 0 - rapid depolarisation1SCN9A
Nervous system development1SCN9A
Sensory Perception1SCN9A
Sensory perception of taste1SCN9A
Sensory perception of sweet, bitter, and umami (glutamate) taste1SCN9A

Dominant GO biological processes

GO termTargets
inflammatory response1
circadian rhythm1
response to toxic substance1
post-embryonic development1
neuronal action potential1
sensory perception of pain1
sodium ion transmembrane transport1
behavioral response to pain1
detection of temperature stimulus involved in sensory perception of pain1
detection of mechanical stimulus involved in sensory perception1
cardiac muscle cell action potential involved in contraction1
action potential propagation1
action potential1
regulation of heart rate1
monoatomic ion transport1

Indications & clinical

Indications

1 indication (0 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).

IndicationTrial phaseMONDOEFO
tinea unguium3MONDO:0001628MONDO:0001628

Clinical trials

Total trials: 13.

Phase distribution

PhaseTrials
Not specified8
PHASE43
PHASE31
PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01014637PHASE4UNKNOWNEfficacy, Safety and Cost-effectiveness of a Sequential Therapy With RV4104A Ointment, Ciclopiroxolamine Cream and Ciclopirox Film-forming Solution Compared With Amorolfine Nail Lacquer in Dermatophytic Onychomycosis
NCT01851590PHASE4COMPLETEDResin vs. Amorolfine vs. Terbinafine Treatment in Onychomycosis
NCT02812043PHASE4COMPLETEDComparison Between Long-pulsed Nd:YAG, Amorolfine and Combination Treatment in Treating Non-dermatophyte Onychomycosis
NCT02549001PHASE3COMPLETEDStudy to Evaluate the Efficacy and Safety of P-3058 10% Nail Solution in the Treatment of Toenail Onychomycosis
NCT01528813PHASE2UNKNOWNErbium-doped Yttrium Aluminium Garnet Laser(Er:Yag)Associated With Amorolfine Lacquer in the Treatment of Onychomycosis
NCT05482763Not specifiedACTIVE_NOT_RECRUITINGMycosis Culture Collection From Dermatological Isolated
NCT06689852Not specifiedRECRUITINGCLINICAL INVESTIGATION FOR THE EVALUATION OF EFFICACY AND SAFETY OF TWO PRODUCTS FOR THE TREATMENT OF ONYCHOMYCOSIS
NCT01929187Not specifiedUNKNOWNA Randomized Study to Evaluate the Efficacy of Herbal Ingredients Combined With a Carrier System (Phytonail) Compared With Amorolfine 5% Nail Lacquer (Loceryl) in the Treatment of Toenail Onychomycosis
NCT03098342Not specifiedCOMPLETEDComparison of Efficacy and Safety Between Methylene Blue-mediated Photodynamic Therapy and 5% Amorolfine Nail Lacquer for Toenail Onychomycosis Treatment
NCT03289871Not specifiedCOMPLETEDClinical Evaluation of the Efficacy of a Medical Device in Treatment of Toenail Onychomycosis
NCT03382717Not specifiedCOMPLETEDEfficacy and Safety of a Medical Device for the Treatment of Toenail Onychomycosis
NCT04961684Not specifiedCOMPLETEDClinical Evaluation of Efficacy and Safety of a Medical Device for the Treatment of Toenail Onychomycosis
NCT06254027Not specifiedUNKNOWNClinical Investigation for the Evaluation of Efficacy and Safety of Two Medical Devices for Onychomycosis Treatment

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

31 molecules share ≥1 primary target. Top 31 by shared-target count:

MoleculeSourceStatusShared targets
SAFINAMIDEChEMBL + PubChemPhase 4 (approved)SCN9A
AMIODARONEChEMBLPhase 4 (approved)SCN9A
AMITRIPTYLINEChEMBLPhase 4 (approved)SCN9A
CANNABIDIOLChEMBLPhase 4 (approved)SCN9A
CARBAMAZEPINEChEMBLPhase 4 (approved)SCN9A
CHLORPROMAZINEChEMBLPhase 4 (approved)SCN9A
DILTIAZEMChEMBLPhase 4 (approved)SCN9A
HALOPERIDOLChEMBLPhase 4 (approved)SCN9A
IMIPRAMINEChEMBLPhase 4 (approved)SCN9A
LACOSAMIDEChEMBLPhase 4 (approved)SCN9A
LAMOTRIGINEChEMBLPhase 4 (approved)SCN9A
LIDOCAINEChEMBLPhase 4 (approved)SCN9A
MEXILETINEChEMBLPhase 4 (approved)SCN9A
MIBEFRADILChEMBLPhase 4 (approved)SCN9A
NIFEDIPINEChEMBLPhase 4 (approved)SCN9A
PIMOZIDEChEMBLPhase 4 (approved)SCN9A
RILUZOLEChEMBLPhase 4 (approved)SCN9A
SERTINDOLEChEMBLPhase 4 (approved)SCN9A
TETRACAINEChEMBLPhase 4 (approved)SCN9A
AJMALINEChEMBLPhase 3SCN9A
ELECLAZINEChEMBLPhase 3SCN9A
NITRENDIPINEChEMBLPhase 3SCN9A
RALFINAMIDEChEMBLPhase 3SCN9A
TEDISAMILChEMBLPhase 3SCN9A
TETRODOTOXINChEMBLPhase 3SCN9A
VIXOTRIGINEChEMBLPhase 3SCN9A
CIFENLINEChEMBLPhase 2SCN9A
DS-1971ChEMBLPhase 2SCN9A
FUNAPIDEChEMBLPhase 2SCN9A
PF-04531083ChEMBLPhase 2SCN9A
PF-05089771ChEMBLPhase 2SCN9A