Drug ID:Drug175
Drug Name:Allopurinol
CID:135401907
DrugBank ID:DB00437
Modality:Small Molecule
Groups:approved
US Approved:YES
Other Approved:YES
Identifier: NCT03101800
Molecular Formula:C5H4N4O
Molecular Weight:136.11 g/mol
Isomeric SMILES:C1=NNC2=C1C(=O)NC=N2
Synonyms:allopurinol; 315-30-0; 1H-Pyrazolo[3,4-d]pyrimidin-4-ol; 4-Hydroxypyrazolo[3,4-d]pyrimidine; Allopurinolum; 4-HPP; Alopurinol; 1H-Pyrazolo(3,4-d)pyrimidin-4-ol; 4-Hydroxypyrazolopyrimidine; 4-Hydroxy-1H-pyrazolo(3,4-d)pyrimidine
Phase 0: 4
Phase 1: 36
Phase 2: 76
Phase 3: 46
Phase 4: 40
Description:A xanthine oxidase inhibitor that decreases uric acid production. It also acts as an antimetabolite on some simpler organisms. [PubChem]

Molecular Structure

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
dt1276 135401907 Allopurinol 1576 CYP3A4 Homo sapiens (human) None
dt1277 135401907 Allopurinol 2646 GCKR Homo sapiens (human) Inhibitor
dt1278 135401907 Allopurinol 54657 UGT1A4 Homo sapiens (human) None
dt1279 135401907 Allopurinol 23040 MYT1L Homo sapiens (human) None
dt1280 135401907 Allopurinol 54579 UGT1A5 Homo sapiens (human) None
dt1281 135401907 Allopurinol 5311 PKD2 Homo sapiens (human) None
dt1282 135401907 Allopurinol 54659 UGT1A3 Homo sapiens (human) None
dt1283 135401907 Allopurinol 1557 CYP2C19 Homo sapiens (human) None
dt1284 135401907 Allopurinol 1565 CYP2D6 Homo sapiens (human) None
dt1285 135401907 Allopurinol 360158 CYCSP5 Homo sapiens (human) None

  • No data available

Phase Distribution
Phase Description
  • Phase 0: Exploratory trials to assess drug behavior in humans
  • Phase 1: Safety trials to determine safe dosage range
  • Phase 2: Efficacy trials to evaluate therapeutic effects
  • Phase 3: Large-scale trials to confirm efficacy and safety
  • Phase 4: Post-marketing surveillance for long-term safety and efficacy

Trial IDTitlePhaseStatusSponsorIndicationsInterventions
EUCTR2016-004112-35-SE Low-dose azathioprine and allopurinol- versus azathioprine monotherapy in patients with Inflammatory Bowel Disease: An investigator-initiated, open, multicentre, parallel-arm, randomized controlled trial __A SOIBD (The Swedish Organisation for the study of Inflammatory Bowel Diseases) study __ PHASE4 Authorised SOIBD (The Swedish Organisation for the study of Inflammatory Bowel Diseases) Patients with inflammatory bowel diseae (Ulcerati… Trade Name: Imurel Product Name: Azathioprine Pro… Details
ACTRN12613001347752 A randomized controlled trial of patients with IBD attending specialist clinics comparing de novo combination allopurinol and thiopurine versus thiopurine and placebo (ie standard practice) in terms of objective and clinical outcomes at six months PHASE3|PHASE4 Recruiting Eastern Health Inflammatory Bowel Disease; Inflammatory Bowel D… De novo combination therapy with allopurinol 100m… Details
EUCTR2013-001503-37-DK Effect of low-dose Azathioprine and Allopurinol compared to Azathioprine on clinical outcomes in Inflammatory Bowel Disease PHASE3 Not Recruiting Marianne Kiszka-Kanowitz Inflammatory Bowel Disease, (Ulcerativ colitis, C… Trade Name: Imurel Pharmaceutical Form: Tablet IN… Details
ACTRN12612001107819 Febuxostat-thiopurine combination therapy in patients with moderately severe inflammatory bowel disease (IBD): a pilot study of a novel drug combination that may influence thiopurine bioavailability PHASE1 Not Recruiting Prof Tim Florin inflammatory bowel disease; inflammatory bowel d… To use the combination of febuxostat and 6-mercap… Details
ACTRN12611000363987 The Triple A (Adjunctive Allopurinol and Azathioprine) Study: Use of Ajunctive Allopurinol in Azathioprine/6-Mercaptopurine Non-responders to Optimize 6-Thioguanine Nucleotide Production and Improve Clinical Outcomes in Patients with Inflammatory Bowel Disease (IBD). PHASE3|PHASE4 Not Recruiting The Alfred Hospital Inflammatory Bowel Disease (IBD); Inflammatory B… Eligible IBD patients will be randomly allocated … Details
NCT00849368 Dose-effect Relationship Between Allopurinol, Azathioprine and 6-thioguanine Nucleotide Levels (6-TGN) in Inflammatory Bowel Disease Patients. PHASE1 Not recruiting University of Zurich Inflammatory Bowel Disease Drug: Azathioprine / Allopurinol Details
NCT03101800 Beneficial and Harmful Effects of Azathioprine and Allopurinol Versus Standard Azathioprine Therapy for Patients With Ulcerative Colitis PHASE3 UNKNOWN Hvidovre University Hospital Colitis, Ulcerative|Colitis Ulcerative Exacerbati… DRUG: Azathioprine and Allopurinol|DRUG: Azathiop… Details

Disease IDDisease NameDefinitionCategoryRelated DrugsMechanism
No data available

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
No data available

Thiopurine shunting in a renal transplant recipient: prepregnancy consideration…

PMID: 40675654
Year: 2025
Relationship Type: Treatment Score: 6.5

Fertility and reproductive counselling are integral for female kidney transplant recipients. Although classified as high-risk, successful pregnancies…

The fate of thiopurine metabolites after switching to low-dose thiopurine with …

PMID: 40421668
Year: 2025
Relationship Type: Treatment Score: 6.5

AIMS: Shunting (hypermethylating) thiopurine metabolism, characterized by excessive 6-MMPR production and (sub)therapeutic 6-TGN levels, poses a sign…

Multicentre study and systematic review: Allopurinol exposure during pregnancy

PMID: 38984819
Year: 2024
Relationship Type: Treatment Score: 6.5

BACKGROUND: Data about the safety of allopurinol in pregnant women are sparsely reported. AIMS: To investigate the risk of adverse pregnancy outcome …

Allopurinol Disrupts Purine Metabolism to Increase Damage in Experimental Colit…

PMID: 38474337
Year: 2024
Relationship Type: Treatment Score: 6.5

Inflammatory bowel disease (IBD) is marked by a state of chronic energy deficiency that limits gut tissue wound healing. This energy shortfall is par…

Clinical trial: Combination allopurinol-thiopurine versus standard thiopurine i…

PMID: 38095246
Year: 2024
Relationship Type: Treatment Score: 6.5

BACKGROUND: Thiopurines are established treatments for inflammatory bowel disease (IBD), yet concerns remain regarding their safety. AIM: To evaluate…

Safety and Efficacy of Split-Dose Thiopurine vs Low-Dose Thiopurine-Allopurinol…

PMID: 36729814
Year: 2023
Relationship Type: Treatment Score: 6.5

INTRODUCTION: Split-dose thiopurine and allopurinol-thiopurine cotherapy strategies have been suggested as rescue therapeutic options for children wi…

Low-Dose Azathioprine in Combination with Allopurinol: The Past, Present and Fu…

PMID: 36242689
Year: 2022
Relationship Type: Treatment Score: 6.5

The inflammatory bowel diseases (IBD) are complex immune-mediated inflammatory diseases that are associated with significant morbidity around the wor…

Allopurinol to Prevent Mercaptopurine Adverse Effects in Children and Young Adu…

PMID: 33750748
Year: 2021
Relationship Type: Treatment Score: 6.5

Mercaptopurine (6MP) is used to treat acute lymphoblastic leukemia (ALL) and is metabolized by hypoxanthine guanine phosphoribosal transferase to for…

Influence of allopurinol on thiopurine associated toxicity: A retrospective pop…

PMID: 33118191
Year: 2021
Relationship Type: Treatment Score: 6.5

AIMS: Thiopurines are important for treating inflammatory bowel disease, but are often discontinued due to adverse effects. Concomitant use of allopu…

Use of Allopurinol to Mitigate 6-Mercaptopurine Associated Gastrointestinal Tox…

PMID: 32766146
Year: 2020
Relationship Type: Treatment Score: 6.5

An essential component of acute lymphoblastic leukemia (ALL) therapy is the prolonged maintenance phase with daily 6-mercaptopurine (6-MP) as the cor…

Outcome of concomitant treatment with thiopurines and allopurinol in patients w…

PMID: 32213059
Year: 2020
Relationship Type: Treatment Score: 6.5

BACKGROUND: Thiopurine and allopurinol in combination are associated with clinical remission in inflammatory bowel diseases but their influence on su…

Role of allopurinol and febuxostat in the amelioration of dextran-induced colit…

PMID: 31654756
Year: 2020
Relationship Type: Treatment Score: 6.5

Ulcerative colitis is a chronic auto-inflammatory disorder confined to the colorectal region. It is challenging to find an absolute treatment and cur…

Thiopurines with low-dose allopurinol (ThiLDA)-a prospective clinical one-way c…

PMID: 31587102
Year: 2019
Relationship Type: Treatment Score: 6.5

PURPOSE: Many patients with Crohn's disease (CD) and ulcerative colitis (UC) who have a high 6-methylmercaptopurine/6-thioguanine (6-MMP/6-TGN) ratio…

Addition of Allopurinol for Altering Thiopurine Metabolism to Optimize Therapy …

PMID: 29197117
Year: 2018
Relationship Type: Treatment Score: 6.3

Thiopurine drugs, including azathioprine and 6-mercaptopurine, are used commonly in patients with inflammatory bowel disease for maintenance of remis…

Histological remission of autoimmune hepatitis after the addition of allopurino…

PMID: 28740837
Year: 2017
Relationship Type: Treatment Score: 6.3

The standard therapy for some autoimmune diseases consists of a combination of corticosteroids and thiopurines. In non-responders to thiopurine drugs…

Optimizing Thiopurine Therapy in Inflammatory Bowel Disease Among 2 Real-life I…

PMID: 28617756
Year: 2017
Relationship Type: Treatment Score: 6.3

BACKGROUND: Thiopurines (azathioprine and mercaptopurine) are frequently used immunosuppressive drugs to maintain remission in patients with inflamma…

Combination treatment with 6-mercaptopurine and allopurinol in HepG2 and HEK293…

PMID: 28278299
Year: 2017
Relationship Type: Treatment Score: 6.3

Combination treatment with low-dose thiopurine and allopurinol (AP) has successfully been used in patients with inflammatory bowel disease with a so …

Allopurinol enhanced thiopurine treatment for inflammatory bowel disease: safet…

PMID: 24438369
Year: 2014
Relationship Type: Treatment Score: 6.3

WHAT IS KNOWN AND OBJECTIVE: The thiopurine medications are standard inflammatory bowel disease treatments. Therapeutic failure is observed, however,…

Allopurinol use in pregnancy in three women with inflammatory bowel disease: sa…

PMID: 24345189
Year: 2013
Relationship Type: Treatment Score: 6.1

BACKGROUND: Allopurinol is a frequently prescribed drug. In inflammatory bowel disease patients who shunt thiopurine metabolism towards more toxic an…

Mechanism of allopurinol induced TPMT inhibition

PMID: 23770457
Year: 2013
Relationship Type: Treatment Score: 6.1

Up to 1/5 of patients with wildtype thiopurine-S-methyltransferase (TPMT) activity prescribed azathioprine (AZA) or mercaptopurine (MP) demonstrate a…

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