Drug ID:Drug79
Drug Name:Mercaptopurine
CID:667490
DrugBank ID:DB01033
Modality:Small Molecule
Groups:approved
US Approved:YES
Other Approved:YES
Identifier: NCT02413047, , NCT00514982, , NCT03370601
Molecular Formula:C5H4N4S
Molecular Weight:152.18 g/mol
Isomeric SMILES:C1=NC2=C(N1)C(=S)N=CN2
Synonyms:6-Mercaptopurine; mercaptopurine; 50-44-2; Purinethol; Mercapurin; 6-Thiopurine; 7H-purine-6-thiol; Mercaleukin; Leukerin; Leupurin
Phase 0: 0
Phase 1: 26
Phase 2: 90
Phase 3: 87
Phase 4: 24
Description:An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia. [PubChem]

Molecular Structure

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
dt665 667490 Mercaptopurine 3251 HPRT1 Homo sapiens (human) 15354273 Inhibitor
dt666 667490 Mercaptopurine 3614 IMPDH1 Homo sapiens (human) 37713619 Inhibitor
dt667 667490 Mercaptopurine 5471 PPAT Homo sapiens (human) Inhibitor
dt668 667490 Mercaptopurine 3614 IMPDH1 Homo sapiens (human) Inhibitor
dt669 667490 Mercaptopurine 3615 IMPDH2 Homo sapiens (human) Inhibitor
dt670 667490 Mercaptopurine 316 AOX1 Homo sapiens (human) Substrate
dt671 667490 Mercaptopurine 7172 TPMT Homo sapiens (human) 15354273 Substrate
dt672 667490 Mercaptopurine 7498 XDH Homo sapiens (human) 15354273 Substrate
dt673 667490 Mercaptopurine 9376 SLC22A8 Homo sapiens (human) Substrate|Inhibitor
dt674 667490 Mercaptopurine 10257 ABCC4 Homo sapiens (human) 11447229 Substrate

  • 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
NCT00514982 Medical Treatment of Colitis in Patients With Hermansky-Pudlak Syndrome PHASE2 WITHDRAWN National Institute of Allergy and Infectious Diseases (NIAID) Hermanski-Pudlak Syndrome|Colitis|Cytokines|Lymph… DRUG: Mesalamine|DRUG: Infliximab|DRUG: Corticost… Details
ISRCTN95420128 Subcutaneous CT-P13 monotherapy versus combination with immunomodulation when switching from intravenous infliximab in inflammatory bowel disease A multicentre, randomised withdrawal trial PHASE4 Recruiting Kings Health Partners Crohn's disease and ulcerative colitis Digestive… The intervention is the withdrawal of immunomodul… Details
EUCTR2019-002942-19-DK NORDTREAT_The Nordic IBD treatment strategy trial a randomized controlled trial of access to a protein profile_ PHASE4 Not Recruiting Region ebro l Crohn's disease and Ulcerative colitis MedDRA ve… Trade Name: Remicade Infliximab Pharmaceutical Fo… 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
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
NL-OMON22783 Long term hepatotoxicity of azathioprine, 6-mercaptopurine and 6-thioguanine in inflammatory bowel disease. Not Available Not Recruiting Department of Gastroenterology and Hepatology, VU University Medical Center, Amsterdam, The Netherlands Inflammatory bowel disease, azathioprine, 6-merca… 1. Liver biopsy; 2. Venapuncture; 3. Abdominal … Details
NCT02413047 Evaluate if Response to Infliximab or Adalimumab May be Regained With an Immunomodulator None TERMINATED Indiana University Inflammatory Bowel Disease|Ulcerative Colitis|Cro… DRUG: Azathioprine|DRUG: 6 mercaptopurine|DRUG: M… Details
NCT02910245 Mercaptopurine Therapy in Ulcerative Colitis PHASE3 UNKNOWN Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) Colitis, Ulcerative DRUG: Mercaptopurine (Purinethol)|DRUG: Placebo|D… Details
NCT00521950 Cost-effectiveness of TPMT Pharmacogenetics None COMPLETED ZonMw: The Netherlands Organisation for Health Research and Development Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… GENETIC: TPMT genotyping; Drug: azathioprine or 6… Details
NCT03370601 Evaluation of the Clinical and Immunological Impact of Two Therapeutic Strategies in Chronic Inflammatory Diseases None TERMINATED University Hospital, Lille Inflammatory Bowel Diseases DRUG: Infliximab|DRUG: Mercaptopurine|DRUG: Azath… Details

Disease IDDisease NameDefinitionCategoryRelated DrugsMechanism
No data available

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
S02 Immunosuppression Classic immunosuppressive drugs azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus Ciclosporin-A and tacrolimus bind to specific intracellular… Details

Oral administration of non-absorbable delayed release 6-mercaptopurine is local…

PMID: 25846055
Year: 2015
Relationship Type: Treatment Score: 10.0

Therapy for Crohn's disease (CD) with thiopurines is limited by systemic side effects. A novel formulation of fixed-dose, delayed-release 6-mercaptop…

[Intervention effect analysis of TPMT and NUDT15 genotyping on the tolerability…

PMID: 40393756
Year: 2025
Relationship Type: Treatment Score: 9.5

Objective: To investigate the impact of pre-treatment TPMT and NUDT15 genotyping on medication selection, tolerability and discontinuation rates of a…

Impact of the loss of slc43a3 on 6-mercaptopurine absorption and tissue distrib…

PMID: 40133022
Year: 2025
Relationship Type: Treatment Score: 9.5

6-Mercaptopurine (6-MP) is a nucleobase analog used in the therapy of acute lymphoblastic leukemia and inflammatory bowel disease. It is associated w…

Azathioprine and 6-mercaptopurine for maintenance of remission in ulcerative co…

PMID: 40013523
Year: 2025
Relationship Type: Treatment Score: 9.5

BACKGROUND: Maintenance of remission is essential in inflammatory bowel disease (IBD) in terms of disease course and long-term prognosis. The thiopur…

Azathioprine and 6-mercaptopurine-induced intrahepatic cholestasis of pregnancy…

PMID: 37679010
Year: 2023
Relationship Type: Treatment Score: 9.5

OBJECTIVE: Azathioprine, a prodrug of 6-mercaptopurine (6-MP), is used in the treatment of inflammatory bowel disease and may be continued during pre…

Commensal bacteria promote azathioprine therapy failure in inflammatory bowel d…

PMID: 37586320
Year: 2023
Relationship Type: Treatment Score: 9.5

Azathioprine (AZA) therapy failure, though not the primary cause, contributes to disease relapse and progression in inflammatory bowel disease (IBD).…

Enhanced Cytotoxic Activity of 6-Mercaptopurine-Loaded Solid Lipid Nanoparticle…

PMID: 37417972
Year: 2023
Relationship Type: Treatment Score: 9.5

6-Mercaptopurine (6-MCP) is an antiproliferative purine analog used in acute lymphoblastic leukemia, non-Hodgkin lymphoma, and inflammatory bowel dis…

Evaluation of FTO polymorphism in 6-mercaptopurine related intolerance in child…

PMID: 37256334
Year: 2023
Relationship Type: Treatment Score: 9.5

PURPOSE: Thiopurine drugs like 6-Mercaptopurine (6MP) are the cornerstone of maintenance therapy in acute lymphoblastic leukemia (ALL). A recently de…

Impact of Chronotherapy on 6-Mercaptopurine Metabolites in Inflammatory Bowel D…

PMID: 36730289
Year: 2023
Relationship Type: Treatment Score: 9.5

INTRODUCTION: Chronotherapy is the timing of medication according to biological rhythms of the host to optimize drug efficacy and minimize toxicity. …

Improved HPLC Quantification of 6-Mercaptopurine Metabolites in Red Blood Cells…

PMID: 36233187
Year: 2022
Relationship Type: Treatment Score: 9.5

Thiopurine drugs azathioprine (AZA) and 6-mercaptopurine (6-MP) are used extensively in pediatric and adult patients with inflammatory and neoplastic…

Impact of SLC43A3/ENBT1 Expression and Function on 6-Mercaptopurine Transport a…

PMID: 35798387
Year: 2022
Relationship Type: Treatment Score: 9.5

6-Mercaptopurine (6-MP) is used extensively in the treatment of acute lymphoblastic leukemia (ALL) and inflammatory bowel diseases. Our laboratory de…

A Comprehensive Approach to Compatibility Testing Using Chromatographic, Therma…

PMID: 33802871
Year: 2021
Relationship Type: Treatment Score: 9.5

In this work, a systematical compatibility investigation of 6-mercaptopurine and folic acid, two commonly used medications in the treatment of inflam…

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

PMID: 32766146
Year: 2020
Relationship Type: Treatment Score: 9.5

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

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

PMID: 28278299
Year: 2017
Relationship Type: Treatment Score: 9.3

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

Experts Opinion on the Practical Use of Azathioprine and 6-Mercaptopurine in In…

PMID: 27760078
Year: 2016
Relationship Type: Treatment Score: 9.3

The relevance of azathioprine and 6-mercaptopurine therapy in inflammatory bowel disease, Crohn's disease, and ulcerative colitis, has been challenge…

Azathioprine and 6-Mercaptopurine-induced Liver Injury: Clinical Features and O…

PMID: 27648552
Year: 2017
Relationship Type: Adverse Effect Score: 9.3

OBJECTIVE: The objective of the study was to define the clinical, biochemical, and histologic features of liver injury from thiopurines. BACKGROUND: …

Azathioprine and 6-mercaptopurine for maintenance of remission in ulcerative co…

PMID: 27192092
Year: 2016
Relationship Type: Treatment Score: 9.3

BACKGROUND: Maintenance of remission is a major issue in inflammatory bowel disease. In ulcerative colitis, the evidence for the effectiveness of aza…

Azathioprine or 6-mercaptopurine for maintenance of remission in Crohn's disease

PMID: 26517527
Year: 2015
Relationship Type: Treatment Score: 9.3

BACKGROUND: The therapeutic role of 6-mercaptopurine (6-MP) and azathioprine (AZA) remains controversial due to their perceived relatively slow-actin…

Factitious Disorder in Crohn's Disease: Recurrent Pancytopenia Caused by Surrep…

PMID: 26078732
Year: 2015
Relationship Type: Association Score: 9.3

Factitious disorder is a rare psychiatric illness characterized by the willful and deceptive induction of illness for the purpose of assuming the sic…

Azathioprine and 6-mercaptopurine for maintenance of surgically-induced remissi…

PMID: 25081347
Year: 2014
Relationship Type: Treatment Score: 9.3

BACKGROUND: Crohn's disease (CD) is a chronic relapsing inflammatory condition. Many patients fail to achieve remission with medical management and r…

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