Metolazone
Metolazone (metolazone) is a small molecule pharmaceutical. Metolazone was first approved as Diulo on 1982-01-01. It is used to treat edema, heart failure, hypertension, and nephrotic syndrome in the USA. The pharmaceutical is active against solute carrier family 12 member 3.
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Commercial
Therapeutic Areas
Trade Name
FDA
EMA
Metolazone (discontinued: Diulo, Metolazone, Mykrox, Zaroxolyn)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Metolazone
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| MYKROX | Chartwell Pharmaceuticals | N-019532 DISCN | 1987-10-30 | 1 products |
| DIULO | G.D. Searle | N-018535 DISCN | 1982-01-01 | 3 products |
| ZAROXOLYN | i3 Pharmaceuticals | N-017386 DISCN | 1982-01-01 | 3 products, RLD |
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FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| metolazone | ANDA | 2025-07-22 |
| mykrox tablets | 2006-01-12 | |
| zaroxolyn | New Drug Application | 2016-08-06 |
Indications
FDA
EMA
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
C: Cardiovascular system drugs
— C03: Diuretics
— C03B: Low-ceiling diuretics, excl. thiazides
— C03BA: Sulfonamides, low-ceiling diuretics, plain
— C03BA08: Metolazone
— C03E: Diuretics and potassium-sparing agents in combination
— C03EA: Low-ceiling diuretics and potassium-sparing agents
— C03EA12: Metolazone and potassium-sparing agents
HCPCS
No data
Clinical
Clinical Trials
35 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Heart failure | D006333 | EFO_0003144 | I50 | 1 | 2 | 4 | 11 | 7 | 25 |
| Water intoxication | D014869 | — | — | — | 1 | — | 2 | 1 | 4 |
| Hypertension | D006973 | EFO_0000537 | I10 | — | — | — | 1 | 2 | 3 |
| Acute liver failure | D017114 | — | — | — | — | — | 2 | 1 | 3 |
| Covid-19 | D000086382 | — | U07.1 | — | — | — | 1 | 1 | 2 |
| Iron overload | D019190 | — | — | — | 1 | — | 1 | — | 2 |
| Coronavirus infections | D018352 | EFO_0007224 | B34.2 | — | — | — | 1 | — | 1 |
| Renal insufficiency | D051437 | — | N19 | — | — | — | 1 | — | 1 |
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | — | — | — | 1 | — | 1 |
| Edema | D004487 | — | R60.9 | — | — | — | 1 | — | 1 |
Indications Phases 3
No data
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Chronic renal insufficiency | D051436 | — | N18 | — | 1 | — | — | — | 1 |
| Chronic kidney failure | D007676 | EFO_0003884 | N18.6 | — | 1 | — | — | — | 1 |
| Respiratory distress syndrome | D012128 | EFO_1000637 | J80 | — | 1 | — | — | — | 1 |
| Critical illness | D016638 | — | — | — | 1 | — | — | — | 1 |
| Sepsis | D018805 | EFO_0001420 | A41.9 | — | 1 | — | — | — | 1 |
| Wounds and injuries | D014947 | — | T14.8 | — | 1 | — | — | — | 1 |
| Multiple trauma | D009104 | — | T07 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 3 | — | — | — | — | 3 |
| Cardiomyopathies | D009202 | EFO_0000318 | I42 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Respiratory insufficiency | D012131 | — | J96.9 | — | — | — | — | 1 | 1 |
| Hypernatremia | D006955 | — | E87.0 | — | — | — | — | 1 | 1 |
| Systolic heart failure | D054143 | EFO_1001207 | I50.20 | — | — | — | — | 1 | 1 |
| Diastolic heart failure | D054144 | EFO_1000899 | I50.30 | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Metolazone |
| INN | metolazone |
| Description | Metolazone is a quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics. It has a role as a diuretic, an antihypertensive agent and an ion transport inhibitor. It is a member of quinazolines, an organochlorine compound and a sulfonamide. |
| Classification | Small molecule |
| Drug class | — |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | Cc1ccccc1N1C(=O)c2cc(S(N)(=O)=O)c(Cl)cc2NC1C |
Identifiers
| PDB | — |
| CAS-ID | 17560-51-9 |
| RxCUI | — |
| ChEMBL ID | CHEMBL878 |
| ChEBI ID | 64354 |
| PubChem CID | 4170 |
| DrugBank | DB00524 |
| UNII ID | TZ7V40X7VX (ChemIDplus, GSRS) |
Target
Agency Approved
SLC12A3
SLC12A3
Organism
Homo sapiens
Gene name
SLC12A3
Gene synonyms
NCC, TSC
NCBI Gene ID
Protein name
solute carrier family 12 member 3
Protein synonyms
Na-Cl cotransporter, Na-Cl symporter, NaCl electroneutral thiazide-sensitive cotransporter, NCC, sodium-chloride co-transporter, solute carrier family 12 (sodium/chloride transporter), member 3, thiazide-sensitive Na-Cl cotransporter, Thiazide-sensitive sodium-chloride cotransporter
Uniprot ID
Mouse ortholog
Slc12a3 (20497)
solute carrier family 12 member 3 (P59158)
Alternate
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Variants
No data
Financial
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Estimated US medical usage
Metolazone
Total medical expenditures per year (USD, in millions)
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Number of persons purchased
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Number of purchases
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 1,385 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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7,080 adverse events reported
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