| 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
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| 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 ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT03370601 | Evaluation of the Clinical and Immunological Impact of Two Therapeutic Strategies in Chronic Inflammatory Diseases | NA | TERMINATED | University Hospital, Lille | Inflammatory Bowel Diseases | DRUG: Infliximab|DRUG: Mercaptopurine|DRUG: Azath… | 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 |
| NCT02852694 | Reduce Risk for Crohn's Disease Patients | PHASE4 | COMPLETED | PIBD-Net | Crohn's Disease | DRUG: Methotrexate|DRUG: Adalimumab|DRUG: Azathio… | Details |
| NCT02413047 | Evaluate if Response to Infliximab or Adalimumab May be Regained With an Immunomodulator | NA | TERMINATED | Indiana University | Inflammatory Bowel Disease|Ulcerative Colitis|Cro… | DRUG: Azathioprine|DRUG: 6 mercaptopurine|DRUG: M… | Details |
| NCT02177071 | A proSpective Randomized Controlled Trial comParing infliximAb-antimetabolites Combination Therapy to Anti-metabolites monotheRapy and Infliximab monothErapy in Crohn's Disease Patients in Sustained Steroid-free Remission on Combination Therapy | PHASE4 | COMPLETED | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | Crohn's Disease | DRUG: INFLIXIMAB|DRUG: AZATHIOPRINE|DRUG: MERCAPT… | Details |
| NCT01629628 | Adalimumab for the Management of Post-operative Crohn's Disease (CD) | PHASE3 | UNKNOWN | Tel-Aviv Sourasky Medical Center | Crohn Disease | DRUG: Adalimumab|DRUG: 6 Mercaptopurine | Details |
| NCT01094613 | Multicenter Clinical Efficacy and Safety Study of Delayed Release 6MP in Crohn's Disease | PHASE1|PHASE2 | TERMINATED | Teva GTC | Crohn's Disease | DRUG: Delayed Release 6 mercaptopurine|DRUG: 6 Me… | Details |
| NCT00774982 | Pilot Comparative Bioavailability Study of 6Mercaptopurine (Delayed Release vs. Purinethol) in Crohns Disease Patients | PHASE1 | COMPLETED | Teva GTC | Crohns Disease | DRUG: Delayed Release 6 mercaptopurine|DRUG: 6 Me… | Details |
| NCT00521950 | Cost-effectiveness of TPMT Pharmacogenetics | NA | COMPLETED | ZonMw: The Netherlands Organisation for Health Research and Development | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | GENETIC: TPMT genotyping; Drug: azathioprine or 6… | Details |
| 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 |
| 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 Di… | 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 di… | 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 Di | PHASE3|PHASE4 | Not Recruiting | The Alfred Hospital | Inflammatory Bowel Disease (IBD); Inflammatory Bo… | Eligible IBD patients will be randomly allocated … | Details |
| NL-OMON22783 | Long term hepatotoxicity of azathioprine, 6-mercaptopurine and 6-thioguanine in inflammatory bowel disease. | NULL | Not Recruiting | Department of Gastroenterology and Hepatology, VU University Medical Center, Amsterdam, The Netherlands | Inflammatory bowel disease, azathioprine, 6-merca… | 1. Liver biopsy;<br />2. Venapuncture;<br />3. Ab… | Details |
| NCT00287170 | Efficacy Study of Targeted, Local Delivery of Drugs to Treat Crohn's Disease | PHASE1|PHASE2 | COMPLETED | Teva GTC | Crohn's Disease | DRUG: Delayed Release 6MP or Calcitriol vs. Purin… | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| 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…