Amorolfine
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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
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL489411 |
| Name | Amorolfine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 54260 |
| ChEBI | CHEBI:599440 |
| ATC | D01AE16 |
| Molecular formula | C21H35NO |
| Molecular weight | 317.5 |
| InChIKey | MQHLMHIZUIDKOO-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).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| SCN9A | Nav1.7 | 4.02 | 0% | 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:
| Pathway | Targets | Genes |
|---|---|---|
| Developmental Biology | 1 | SCN9A |
| L1CAM interactions | 1 | SCN9A |
| Muscle contraction | 1 | SCN9A |
| Axon guidance | 1 | SCN9A |
| Interaction between L1 and Ankyrins | 1 | SCN9A |
| Cardiac conduction | 1 | SCN9A |
| Phase 0 - rapid depolarisation | 1 | SCN9A |
| Nervous system development | 1 | SCN9A |
| Sensory Perception | 1 | SCN9A |
| Sensory perception of taste | 1 | SCN9A |
| Sensory perception of sweet, bitter, and umami (glutamate) taste | 1 | SCN9A |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| inflammatory response | 1 |
| circadian rhythm | 1 |
| response to toxic substance | 1 |
| post-embryonic development | 1 |
| neuronal action potential | 1 |
| sensory perception of pain | 1 |
| sodium ion transmembrane transport | 1 |
| behavioral response to pain | 1 |
| detection of temperature stimulus involved in sensory perception of pain | 1 |
| detection of mechanical stimulus involved in sensory perception | 1 |
| cardiac muscle cell action potential involved in contraction | 1 |
| action potential propagation | 1 |
| action potential | 1 |
| regulation of heart rate | 1 |
| monoatomic ion transport | 1 |
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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| tinea unguium | 3 | MONDO:0001628 | MONDO:0001628 |
Clinical trials
Total trials: 13.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 8 |
| PHASE4 | 3 |
| PHASE3 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01014637 | PHASE4 | UNKNOWN | Efficacy, 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 |
| NCT01851590 | PHASE4 | COMPLETED | Resin vs. Amorolfine vs. Terbinafine Treatment in Onychomycosis |
| NCT02812043 | PHASE4 | COMPLETED | Comparison Between Long-pulsed Nd:YAG, Amorolfine and Combination Treatment in Treating Non-dermatophyte Onychomycosis |
| NCT02549001 | PHASE3 | COMPLETED | Study to Evaluate the Efficacy and Safety of P-3058 10% Nail Solution in the Treatment of Toenail Onychomycosis |
| NCT01528813 | PHASE2 | UNKNOWN | Erbium-doped Yttrium Aluminium Garnet Laser(Er:Yag)Associated With Amorolfine Lacquer in the Treatment of Onychomycosis |
| NCT05482763 | Not specified | ACTIVE_NOT_RECRUITING | Mycosis Culture Collection From Dermatological Isolated |
| NCT06689852 | Not specified | RECRUITING | CLINICAL INVESTIGATION FOR THE EVALUATION OF EFFICACY AND SAFETY OF TWO PRODUCTS FOR THE TREATMENT OF ONYCHOMYCOSIS |
| NCT01929187 | Not specified | UNKNOWN | A 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 |
| NCT03098342 | Not specified | COMPLETED | Comparison of Efficacy and Safety Between Methylene Blue-mediated Photodynamic Therapy and 5% Amorolfine Nail Lacquer for Toenail Onychomycosis Treatment |
| NCT03289871 | Not specified | COMPLETED | Clinical Evaluation of the Efficacy of a Medical Device in Treatment of Toenail Onychomycosis |
| NCT03382717 | Not specified | COMPLETED | Efficacy and Safety of a Medical Device for the Treatment of Toenail Onychomycosis |
| NCT04961684 | Not specified | COMPLETED | Clinical Evaluation of Efficacy and Safety of a Medical Device for the Treatment of Toenail Onychomycosis |
| NCT06254027 | Not specified | UNKNOWN | Clinical 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.
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.
31 molecules share ≥1 primary target. Top 31 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| SAFINAMIDE | ChEMBL + PubChem | Phase 4 (approved) | SCN9A |
| AMIODARONE | ChEMBL | Phase 4 (approved) | SCN9A |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | SCN9A |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | SCN9A |
| CARBAMAZEPINE | ChEMBL | Phase 4 (approved) | SCN9A |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | SCN9A |
| DILTIAZEM | ChEMBL | Phase 4 (approved) | SCN9A |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | SCN9A |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | SCN9A |
| LACOSAMIDE | ChEMBL | Phase 4 (approved) | SCN9A |
| LAMOTRIGINE | ChEMBL | Phase 4 (approved) | SCN9A |
| LIDOCAINE | ChEMBL | Phase 4 (approved) | SCN9A |
| MEXILETINE | ChEMBL | Phase 4 (approved) | SCN9A |
| MIBEFRADIL | ChEMBL | Phase 4 (approved) | SCN9A |
| NIFEDIPINE | ChEMBL | Phase 4 (approved) | SCN9A |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | SCN9A |
| RILUZOLE | ChEMBL | Phase 4 (approved) | SCN9A |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | SCN9A |
| TETRACAINE | ChEMBL | Phase 4 (approved) | SCN9A |
| AJMALINE | ChEMBL | Phase 3 | SCN9A |
| ELECLAZINE | ChEMBL | Phase 3 | SCN9A |
| NITRENDIPINE | ChEMBL | Phase 3 | SCN9A |
| RALFINAMIDE | ChEMBL | Phase 3 | SCN9A |
| TEDISAMIL | ChEMBL | Phase 3 | SCN9A |
| TETRODOTOXIN | ChEMBL | Phase 3 | SCN9A |
| VIXOTRIGINE | ChEMBL | Phase 3 | SCN9A |
| CIFENLINE | ChEMBL | Phase 2 | SCN9A |
| DS-1971 | ChEMBL | Phase 2 | SCN9A |
| FUNAPIDE | ChEMBL | Phase 2 | SCN9A |
| PF-04531083 | ChEMBL | Phase 2 | SCN9A |
| PF-05089771 | ChEMBL | Phase 2 | SCN9A |
Related Atlas pages
- Genes: SCN9A
- Diseases: tinea unguium
- Drugs: Safinamide, Amiodarone, Amitriptyline, Cannabidiol, Carbamazepine, Chlorpromazine, Diltiazem, Haloperidol, Imipramine, Lacosamide, Lamotrigine, Lidocaine, Mexiletine, Mibefradil, Nifedipine, Pimozide, Riluzole, Sertindole, Tetracaine, Ajmaline, Eleclazine, Nitrendipine, Ralfinamide, Tedisamil, Tetrodotoxin, Vixotrigine