| 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 | |
|---|---|---|---|---|---|---|---|
| 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 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 |
6-Mercaptopurine reduces macrophage activation and gut epithelium proliferation…
PMID: 25029617
Year: 2014
Relationship Type:
Treatment
Score: 9.3
BACKGROUND: Inflammatory bowel disease is characterized by chronic intestinal inflammation. Azathioprine and its metabolite 6-mercaptopurine (6-MP) a…
Acute Pancreatitis Induced by Azathioprine and 6-mercaptopurine Proven by Singl…
PMID: 24010098
Year: 2012
Relationship Type:
Adverse Effect
Score: 9.1
We report here a case of drug-induced acute pancreatitis proved by elimination and single, low dose challenge test in a child with Crohn disease. A 1…
Expert opinion: experience with 6-mercaptopurine in the treatment of inflammato…
PMID: 23716977
Year: 2013
Relationship Type:
Treatment
Score: 9.1
Arbitrarily, modern day treatment of inflammatory bowel disease begins with the introduction of immunosuppressives for ulcerative colitis. Clinical i…
Azathioprine and 6-mercaptopurine for maintenance of remission in ulcerative co…
PMID: 22972046
Year: 2012
Relationship Type:
Treatment
Score: 9.1
BACKGROUND: Maintenance of remission is a major issue in inflammatory bowel disease. In ulcerative colitis, the evidence for the effectiveness of aza…
A histopathologic pattern of centrilobular hepatocyte injury suggests 6-mercapt…
PMID: 22646267
Year: 2012
Relationship Type:
Treatment
Score: 9.1
CONTEXT: Hepatotoxicity is an important side effect of thiopurine analog treatment for inflammatory bowel disease. A variety of histopathologic findi…
Nutritional therapy versus 6-mercaptopurine as maintenance therapy in patients …
PMID: 22542605
Year: 2012
Relationship Type:
Treatment
Score: 9.1
BACKGROUND: 6-Mercaptopurine is often used as maintenance therapy in patients with Crohn's disease. However, toxicities like myelosuppression limit i…
Allopurinol might improve response to azathioprine and 6-mercaptopurine by corr…
PMID: 21175793
Year: 2011
Relationship Type:
Treatment
Score: 9.1
BACKGROUND AND AIM: Allopurinol potentiates azathioprine and 6-mercaptopurine (6-MP) by increasing 6-thioguanine nucleotide (6-TGN) metabolite concen…
IOIBD questionnaire on the clinical use of azathioprine, 6-mercaptopurine, cycl…
PMID: 10656204
Year: 2000
Relationship Type:
Treatment
Score: 9.1
BACKGROUND: Reactive oxygen and nitrogen derived species produced by activated neutrophils have been implicated in the damage of mucosal proteins in…
6-Mercaptopurine for Azathioprine Intolerant Inflammatory Bowel Disease: Litera…
PMID: 26728773
Year: 2015
Relationship Type:
Treatment
Score: 8.3
Thiopurines have been shown to effectively maintain remission of both Crohn's disease (CD) and ulcerative colitis (UC), and to behave as disease modi…
Key factors associated with 6-thioguanine and 6-methylmercaptopurine nucleotide…
PMID: 37621013
Year: 2024
Relationship Type:
Treatment
Score: 7.5
AIMS: Azathioprine (AZA) and 6-mercaptopurine are prescribed in acute lymphoblastic leukaemia (ALL) and inflammatory bowel diseases (IBD). Metabolism…
Exome sequencing and array-based comparative genomic hybridisation analysis of …
PMID: 25752523
Year: 2015
Relationship Type:
Treatment
Score: 7.3
Preferential conversion of azathioprine or 6-mercaptopurine into methylated metabolites is a major cause of thiopurine resistance. To seek potentiall…
Mercaptopurine Therapy and TPMT and NUDT15 Genotype
PMID: 28520348
Year: 2012
Relationship Type:
Treatment
Score: 7.1
Mercaptopurine (brand names Purinethol, Purixan) is an immunosuppressant and anti-neoplastic agent that belongs to the drug class of thiopurines. It …
Two brothers with skewed thiopurine metabolism in ulcerative colitis treated su…
PMID: 22147254
Year: 2012
Relationship Type:
Treatment
Score: 7.1
Thiopurine therapy effectively maintains remission in inflammatory bowel disease. However, many patients are unable to achieve optimum benefits from …
Pharmacogenomic studies of the anticancer and immunosuppressive thiopurines mer…
PMID: 18662289
Year: 2008
Relationship Type:
Adverse Effect
Score: 7.1
BACKGROUND: 6-Mercaptopurine (6-MP) and its prodrug azathioprine (AZA) are effective for the induction and maintenance of remission and reduction of…
Cost-effectiveness and cost-utility of optimized mercaptopurine treatment versu…
PMID: 39400525
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: We assessed the cost-effectiveness and cost-utility of therapeutic drug monitoring (TDM)-guided mercaptopurine treatment compare…
A novel turn-on fluorescence sensor based on the Nd (III) complex for the ultra…
PMID: 38447438
Year: 2024
Relationship Type:
Association
Score: 6.5
Evaluation of tolerance to mercaptopurine in patients with inflammatory bowel d…
PMID: 38072359
Year: 2024
Relationship Type:
Association
Score: 6.5
BACKGROUND: Thiopurines such as azathioprine (AZA) and mercaptopurine (MP) are commonly utilized to treat inflammatory bowel disease (IBD). Their use…
6-Mercaptopurine in ulcerative colitis: the potential of upfront dosing with al…
PMID: 37642331
Year: 2024
Relationship Type:
Association
Score: 6.5
Mercaptopurine for the Treatment of Ulcerative Colitis: A Randomized Placebo-Co…
PMID: 36847130
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Scepticism about the efficacy of thiopurines for ulcerative colitis [UC] is rising. This study aimed to evaluate mercaptopurine …
One Case of Epstein-Barr Virus Encephalitis from Pediatric Crohn's Disease Afte…
PMID: 36670326
Year: 2023
Relationship Type:
Treatment
Score: 6.5