Amiloride
Amiloride, Midamor (amiloride) is a small molecule pharmaceutical. Amiloride was first approved as Midamor on 1982-01-01. It is used to treat ascites, cystic fibrosis, edema, heart failure, and hypertension amongst others in the USA. It is known to target sodium/hydrogen exchanger 5, transient receptor potential cation channel subfamily V member 2, gonadotropin-releasing hormone receptor, acid-sensing ion channel 3, short transient receptor potential channel 7, transient receptor potential cation channel subfamily A member 1, acid-sensing ion channel 2, polycystin-2-like protein 1, alpha-2A adrenergic receptor, short transient receptor potential channel 6, sodium/hydrogen exchanger 2, sodium/hydrogen exchanger 3, sodium/hydrogen exchanger 1, and acid-sensing ion channel 1.
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Commercial
Therapeutic Areas
Trade Name
FDA
EMA
Midamor (generic drugs available since 1986-01-22)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Amiloride hydrochloride
Amiloride hydrochloride
+
Hydrochlorothiazide
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| MODURETIC 5-50 | Merck KGaA | N-018201 DISCN | 1982-01-01 | 1 products, RLD |
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FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| amiloride hydrochloride | ANDA | 2023-11-28 |
| amiloride hydrochloride and hydrochlorothiazide | ANDA | 2023-02-04 |
| amiloride hydrocloride | New Drug Application | 2021-12-11 |
Agency Specific
FDA
EMA
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Patent Expiration
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HCPCS
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Clinical
Clinical Trials
67 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hypertension | D006973 | EFO_0000537 | I10 | 3 | 1 | 5 | 6 | 8 | 23 |
| Chronic renal insufficiency | D051436 | — | N18 | — | 1 | — | 2 | — | 3 |
| Essential hypertension | D000075222 | — | I10 | — | — | — | 1 | 1 | 2 |
| Proteinuria | D011507 | HP_0000093 | R80 | 1 | — | — | 1 | — | 2 |
| Prehypertension | D058246 | — | — | — | — | 1 | 1 | — | 2 |
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | — | — | — | 1 | — | 1 |
| Bipolar disorder | D001714 | EFO_0000289 | F30.9 | — | — | — | 1 | — | 1 |
| Autosomal dominant polycystic kidney | D016891 | EFO_1001496 | Q61.2 | — | — | — | 1 | — | 1 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Heart failure | D006333 | HP_0001635 | I50 | 2 | — | 1 | — | — | 3 |
| Cardiovascular diseases | D002318 | HP_0001626 | — | — | — | 2 | — | — | 2 |
| Insulin resistance | D007333 | HP_0000855 | E88.819 | — | 1 | 1 | — | 1 | 2 |
| Coronary disease | D003327 | — | — | — | 1 | 1 | — | — | 1 |
| Coronary artery disease | D003324 | — | I25.1 | — | 1 | 1 | — | — | 1 |
| Primary hyperparathyroidism | D049950 | EFO_0008519 | E21.0 | — | 1 | 1 | — | — | 1 |
| Sleep apnea syndromes | D012891 | HP_0010535 | G47.3 | — | — | 1 | — | — | 1 |
| Obstructive sleep apnea | D020181 | EFO_0003918 | G47.33 | — | — | 1 | — | — | 1 |
| Overweight | D050177 | — | E66.3 | — | 1 | 1 | — | — | 1 |
| Nephrotic syndrome | D009404 | EFO_0004255 | N04 | — | — | 1 | — | — | 1 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Cystic fibrosis | D003550 | EFO_0000390 | E84 | 5 | 1 | — | — | 1 | 7 |
| Optic neuritis | D009902 | EFO_0007405 | H46 | — | 2 | — | — | — | 2 |
| Hypoparathyroidism | D007011 | HP_0000829 | E20 | — | 1 | — | — | — | 1 |
| Chronic progressive multiple sclerosis | D020528 | EFO_0003840 | — | — | 1 | — | — | — | 1 |
| Gitelman syndrome | D053579 | Orphanet_358 | N15.8 | 1 | 1 | — | — | — | 1 |
| Migraine with aura | D020325 | EFO_0005295 | G43.1 | — | 1 | — | — | — | 1 |
| Albuminuria | D000419 | EFO_0004285 | R80.9 | — | 1 | — | — | — | 1 |
| Multiple sclerosis | D009103 | EFO_0003885 | G35 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Mucociliary clearance | D009079 | — | — | 3 | — | — | — | — | 3 |
| Pharmacokinetics | D010599 | — | — | 1 | — | — | — | — | 1 |
| Gastroesophageal reflux | D005764 | EFO_0003948 | K21 | 1 | — | — | — | — | 1 |
| Heartburn | D006356 | — | R12 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Covid-19 | D000086382 | — | U07.1 | — | — | — | — | 1 | 1 |
| Microvascular angina | D017566 | — | — | — | — | — | — | 1 | 1 |
| Bone fractures | D050723 | EFO_0003931 | T14.8 | — | — | — | — | 1 | 1 |
| Nephrogenic diabetes insipidus | D018500 | — | N25.1 | — | — | — | — | 1 | 1 |
| Hyperaldosteronism | D006929 | HP_0011736 | E26 | — | — | — | — | 1 | 1 |
| Diabetic nephropathies | D003928 | EFO_0000401 | — | — | — | — | — | 1 | 1 |
| Acromegaly | D000172 | — | — | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Amiloride |
| INN | amiloride |
| Description | Amiloride is a member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid. It has a role as a sodium channel blocker and a diuretic. It is a member of pyrazines, an organochlorine compound, an aromatic amine and a member of guanidines. It is a conjugate base of an amiloride(1+). |
| Classification | Small molecule |
| Drug class | epithelial sodium channel (ENaC) inhibitors, amiloride derivatives |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | N=C(N)NC(=O)c1nc(Cl)c(N)nc1N |
Identifiers
| PDB | — |
| CAS-ID | 2609-46-3 |
| RxCUI | — |
| ChEMBL ID | CHEMBL945 |
| ChEBI ID | 2639 |
| PubChem CID | 16231 |
| DrugBank | DB00594 |
| UNII ID | 7DZO8EB0Z3 (ChemIDplus, GSRS) |
Target
Agency Approved
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Alternate
PKD2L1
PKD2L1
SLC9A3
SLC9A3
Organism
Homo sapiens
Gene name
PKD2L1
Gene synonyms
PKD2L, PKDL, TRPP3
NCBI Gene ID
Protein name
polycystin-2-like protein 1
Protein synonyms
Polycystic kidney disease 2-like 1 protein, Polycystin-2 homolog, polycystin-2L1, Polycystin-L, Polycystin-L1, transient receptor potential cation channel, subfamily P, member 3
Uniprot ID
Mouse ortholog
Pkd2l1 (329064)
polycystin-2-like protein 1; polycystic kidney disease 2-like 1 protein (Q80ZH4)
Variants
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Estimated US medical usage
Amiloride
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Amiloride
+
Hydrochlorothiazide
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Safety
Black-box Warning
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Adverse Events
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1,640 adverse events reported
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