Allopurinol
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1966
- First approval year
- 1966
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Allopurinol
- Molecular weight
- 136.11
- Structure (SMILES)
- Oc1ncnc2[nH]ncc12
- allopurinol
- Allopurinol
- allopurinol component of duzallo
- Allopurinol component of duzallo
- aloral
- Aloral
- aluline 100
- Aluline 100
- aluline 300
- Aluline 300
- caplenal
- Caplenal
- cosuric
- Cosuric
- hamarin 100
- Hamarin 100
- hamarin 300
- Hamarin 300
- ledopur
- Ledopur
- lopurin
- Lopurin
- uricto
- Uricto
- xanthomax 100
And 9 more, listed on the interactive page.
- allopurinol
- Allopurinol
- Allopurinol (ALLO)
- ALLOPURINOL [EP IMPURITY]
- ALLOPURINOL [EP MONOGRAPH]
- ALLOPURINOL [HSDB]
- allopurinol [INN]
- ALLOPURINOL [JAN]
- ALLOPURINOL [MART.]
- ALLOPURINOL [MI]
- ALLOPURINOL [ORANGE BOOK]
- ALLOPURINOL [USAN]
- ALLOPURINOL [USP MONOGRAPH]
- ALLOPURINOL [USP-RS]
- Allopurinol [WHO-DD]
- ALLOPURINOL [WHO-IP]
- allopurinol 300 mg
- Allopurinol 300 mg
- allopurinol allo
- allopurinol ep impurity
- allopurinol ep monograph
- allopurinol hsdb
- allopurinol inn
- allopurinol jan
- allopurinol mart
And 28 more, listed on the interactive page.
- CAS registry numbers
- 315-30-0
- ChEMBL ID
- CHEMBL1467
- InChIKey
- OFCNXPDARWKPPY-UHFFFAOYSA-N
- PubChem compound IDs
- 135401907
- RxNorm IDs (RxCUI)
- 519
- FDA ingredient codes (UNII)
- 63CZ7GJN5I
- M04AA01
- M04AA51
Sources for recorded values
- Applicant
- CASPER PHARMA LLC
- Approval date
- 19 Aug 1966
- Application number
- NDA016084
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- Pharmacology name
- allopurinol
- Type
- Synthetic organic
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- xanthine dehydrogenase
- Gene symbol
- XDH
- Protein identifier
- P47989
- Median affinity
- 5.38
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- xanthine dehydrogenase
- Gene symbol
- XDH
- Protein identifier
- P47989
- Median affinity
- 5.15
- Affinity units
- pKi
- Primary target
- Yes
- Mechanism
- Xanthine dehydrogenase inhibitor
- Action type
- Inhibitor
- Target
- Xanthine dehydrogenase/oxidase
- Protein identifier
- P47989
Open Targets mechanisms
- Mechanism
- Xanthine dehydrogenase inhibitor
- Action type
- Inhibitor
- Target
- Xanthine dehydrogenase/oxidase
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- XDH
- Protein identifier
- P47989
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Response Evaluation Criteria in Solid Tumors
- Highest recorded phase
- 4
- Subject identifier
- D066066
- Condition
- Leukemia, Biphenotypic, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000094
- Subject identifier
- D015456
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Metabolic Syndrome
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000195
- Subject identifier
- D024821
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Neoplasms, Plasma Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000200
- Subject identifier
- D054219
- Condition
- Leukemia, Biphenotypic, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000209
- Subject identifier
- D015456
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Cardiovascular Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000319
- Subject identifier
- D002318
- Condition
- Heart Failure
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000373
- Subject identifier
- D006333
- Condition
- Diabetes Mellitus
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000400
- Subject identifier
- D003920
- Condition
- Hypertension
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000537
- Subject identifier
- D006973
- Condition
- Wounds and Injuries
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000546
- Subject identifier
- D014947
- Condition
- Leukemia
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Colitis, Ulcerative
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000729
- Subject identifier
- D003093
- Condition
- Obesity
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001073
- Subject identifier
- D009765
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Liver Cirrhosis
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001422
- Subject identifier
- D008103
- Condition
- Heart Failure
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003144
- Subject identifier
- D006333
- Condition
- Inflammatory Bowel Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003767
- Subject identifier
- D015212
- Condition
- Heart Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003777
- Subject identifier
- D006331
- Condition
- Renal Insufficiency, Chronic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003884
- Subject identifier
- D051436
And 21 more, listed on the interactive page.
- Condition identifier
- EFO_0000195
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000220
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000319
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000373
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000400
- Condition identifier
- EFO_0000401
- Condition identifier
- EFO_0000407
- Condition identifier
- EFO_0000495
- Condition identifier
- EFO_0000537
- Condition identifier
- EFO_0000546
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000565
- Condition identifier
- EFO_0000574
- Condition identifier
- EFO_0001422
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003144
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003767
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003884
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003896
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003913
- Condition identifier
- EFO_0003913
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003918
- Condition identifier
- EFO_0004194
- Condition identifier
- EFO_0004253
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004274
- Condition identifier
- EFO_0004517
- Highest recorded phase
- 2
And 64 more, listed on the interactive page.
Warnings
- Warning
- Black Box Warning
Open Targets warnings
- Warning
- Black Box Warning
- Country
- United States
- Event
- acute generalised exanthematous pustulosis
- Reports
- 97
- Reporting signal score
- 144.028
- Event
- acute kidney injury
- Reports
- 683
- Reporting signal score
- 697.574
- Event
- agranulocytosis
- Reports
- 132
- Reporting signal score
- 144.382
- Event
- cholestasis
- Reports
- 146
- Reporting signal score
- 167.762
- Event
- dermatitis exfoliative
- Reports
- 105
- Reporting signal score
- 198.543
- Event
- dermatitis exfoliative generalised
- Reports
- 91
- Reporting signal score
- 225.741
- Event
- drug interaction
- Reports
- 375
- Reporting signal score
- 132.786
- Event
- drug rash with eosinophilia and systemic symptoms
- Reports
- 185
- Reporting signal score
- 501.659
- Event
- drug reaction with eosinophilia and systemic symptoms
- Reports
- 1,697
- Reporting signal score
- 5,560.52
- Event
- eczema
- Reports
- 118
- Reporting signal score
- 134.256
- Event
- eosinophilia
- Reports
- 375
- Reporting signal score
- 812.549
- Event
- erythema
- Reports
- 353
- Reporting signal score
- 197.832
- Event
- erythema multiforme
- Reports
- 97
- Reporting signal score
- 130.31
- Event
- face oedema
- Reports
- 126
- Reporting signal score
- 141.066
- Event
- gout
- Reports
- 139
- Reporting signal score
- 230.693
- Event
- headache
- Reports
- 72
- Reporting signal score
- 147.143
- Event
- hepatitis
- Reports
- 139
- Reporting signal score
- 133.693
- Event
- hepatocellular injury
- Reports
- 159
- Reporting signal score
- 184.297
- Event
- human herpesvirus 6 infection
- Reports
- 55
- Reporting signal score
- 135.677
- Event
- hyperkalaemia
- Reports
- 201
- Reporting signal score
- 204.38
- Event
- pancytopenia
- Reports
- 255
- Reporting signal score
- 233.157
- Event
- pruritus
- Reports
- 484
- Reporting signal score
- 213.802
- Event
- purpura
- Reports
- 98
- Reporting signal score
- 154.24
- Event
- pyrexia
- Reports
- 622
- Reporting signal score
- 221.75
- Event
- rash maculo-papular
- Reports
- 408
- Reporting signal score
- 802.396
And 8 more, listed on the interactive page.
- NCT00000658
- NCT00276003
- NCT00003700
- NCT00039130
- NCT00053196
- NCT00061945
- NCT00109837
- NCT00602693
- NCT01200485
- NCT05536349
- NCT00004755
- NCT00199043
- NCT03570983
- NCT00102440
- NCT00174915
- NCT00175019
- NCT00430248
- NCT00819585
- NCT01001338
- NCT01109121
- NCT01129648
- NCT01310673
- NCT01391325
- NCT01399008
- NCT01451645
And 66 more, listed on the interactive page.
- Dose
- 100 mg
- Route
- Oral
- How often
- Once daily
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 74.69
- Calculated partition coefficient (ALogP)
- 0.06
- Calculated partition coefficient (XLogP)
- -0.7
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 0
- Heavy atoms
- 10
- Molecular formula
- C5H4N4O
- Monoisotopic mass
- 136.03851076
- Natural product
- Yes
- 0378-0137
- 0378-0181
- 0591-5543
- 0591-5544
- 0603-2115
- 0603-2116
- 0615-8385
- 0615-8517
- 0904-6572
- 0904-7041
- 14445-170
- 14445-171
- 14445-172
- 16571-883
- 16571-884
- 16571-885
- 16714-576
- 16714-577
- 16729-134
- 16729-135
- 23155-693
- 23155-694
- 29300-349
- 29300-350
- 31722-252
And 135 more, listed on the interactive page.
- Recorded assays
- 6,518
- Active assays
- 138
- Confirmatory
- Other
- Screening
- Summary
- Antimetabolites
- Enzyme Inhibitors
- Gout Suppressants
- Free Radical Scavengers
Distribution coefficient (LogD)
- Median
- -0.495
- Mean
- -0.495
- Minimum
- -0.55
- Maximum
- -0.44
- Unit
- unitless
- Assays
- 2
- Standard deviation
- 0.0777817
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Solubility
- Median
- 695
- Mean
- 695
- Minimum
- 490
- Maximum
- 900
- Unit
- ug/mL
- Assays
- 2
- Standard deviation
- 289.914
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Related records
Trials (177)
- A Controlled Study of Uric Acid on the Progression of IgA Nephropathy
- A Multicenter Clinical Trial of Allopurinol to Prevent Kidney Function Loss in Type 1 Diabetes
- A Multicentre, Randomized, Double-blind, Allopurinol Controlled Study to Evaluate the Efficacy and Safety of SHR4640 in Subjects With Gout
- A Phase III Randomized Trial of Low-Dose Versus Standard-Dose mBACOD Chemotherapy With rGM-CSF for Treatment of AIDS-Associated Non-Hodgkin's Lymphoma
- A Pilot Study of Allopurinol As A Modifier of 6-MP Metabolism in Pediatric ALL
- A Study in Healthy Subjects to Assess Drug Availability of 4 Different Formulations of Verinurad and Allopurinol
- A Study of Dotinurad Versus Allopurinol in Participants With Gout
- A Study of Dotinurad Versus Allopurinol in Tophaceous Gout
- A Study of Evaluating the Efficacy and Safety of SHR4640 in Subjects With Gout
- A Study of the Efficacy of Canakinumab in Prevention of Acute Flares in Chronic Gout Patients Initiating Allopurinol Therapy (Core Study) and a Long-term Study of the Efficacy and Safety of Canakinumab in Patients With Gout (Extension Study)
- A Study of Verinurad and Allopurinol in Patients With Chronic Kidney Disease and Hyperuricaemia
- A Study to Assess the Effect of Verinurad on the Electric Activity of the Heart
- A Study to Assess the Safety and Pharmacokinetics of Verinurad and Allopurinol in Asian and Chinese Subjects
- A Study to Evaluate Safety and Efficacy of Oral Febuxostat in Patients With Gout
- A Trial Comparing Single Agent Melphalan to Carmustine, Etoposide, Cytarabine, and Melphalan (BEAM) as a Preparative Regimen for Patients With Multiple Myeloma Undergoing High Dose Therapy Followed by Autologous Stem Cell Reinfusion
- Alemtuzumab and Combination Chemotherapy in Treating Patients With Untreated Acute Lymphoblastic Leukemia
- Allo HSCT Using RIC and PTCy for Hematological Diseases
- Allo HSCT Using RIC for Hematological Diseases
- Allogeneic Natural Killer Cells in Patients With Recurrent Ovarian Cancer, Fallopian Tube, and Primary Peritoneal Cancer
- Allopurinol Add-on Treatment for Refractory Mania
Approved for (4)
In development for (54)
- Acute lymphoblastic leukemia Phase 3
- Acute myeloid leukemia Phase 2
- Adenylosuccinate lyase deficiency Phase 2
- Autism Phase 2
- B-cell acute lymphoblastic leukemia Phase 1
- B-cell chronic lymphocytic leukemia Phase 2
- Bipolar disorder Phase 3
- Bone marrow neoplasm Phase 2
- Brain disorder Phase 3
- Brain injury Phase 3
- Burkitt lymphoma Phase 2
- Cardiovascular disorder Phase 3
- Chronic kidney disease Phase 2
- Cirrhosis of liver Phase 2
- Congenital heart disease Phase 3
- Congestive heart failure Phase 2
- Coronary artery disorder Phase 2
- Cutaneous leishmaniasis Phase 2
- Diabetes mellitus Phase 2
- Diabetic autonomic neuropathy Phase 3
Other linked conditions (8)
- Diabetic kidney disease
- Diabetic retinopathy
- Fetal growth restriction
- IgA glomerulonephritis
- Kidney disorder
- Mucocutaneous leishmaniasis
- Prediabetes syndrome
- Schizophrenia
Targets (1)
- XDH Xanthine dehydrogenase inhibitor