| 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 metabolite levels in children with inflammatory bowel disease
PMID: 11698762
Year: 2001
Relationship Type:
Association
Score: 6.1
BACKGROUND: miR-143 and miR-145 are believed to function as colon cancer tumor suppressors, as they inhibit colon cancer cell growth and are downreg…
An open-label pilot study using thioguanine as a therapeutic alternative in Cro…
PMID: 11515842
Year: 2001
Relationship Type:
Treatment
Score: 6.1
Not found
Frequency of use and standards of care for the use of azathioprine and 6-mercap…
PMID: 11173323
Year: 2001
Relationship Type:
Treatment
Score: 6.1
Scid mice transplanted with CD4(+) T cells from congenic donor mice develop a chronic and lethal inflammatory bowel disease (IBD) 2-3 months post-t…
6-mercaptopurine or methotrexate added to prednisone induces and maintains remi…
PMID: 11111780
Year: 2000
Relationship Type:
Treatment
Score: 6.1
Hydrogen sulfide (H₂S) is a toxic gas that is now recognized as an important mediator of many physiological processes. In the colon, H₂S is produced…
Normal thiopurine methyltransferase levels do not eliminate 6-mercaptopurine or…
PMID: 10875470
Year: 2000
Relationship Type:
Adverse Effect
Score: 6.1
BACKGROUND: Calprotectin is released from neutrophils and monocytes, and increased calprotectin levels in stool may serve as a marker of intestinal …
Outcome of pregnancies when fathers are treated with 6-mercaptopurine for infla…
PMID: 10710057
Year: 2000
Relationship Type:
Association
Score: 6.1
BACKGROUND: A previous nationwide epidemiologic study of inflammatory bowel disease (IBD) in Iceland in 1950-79 showed a low but steadily rising inc…
Malignant neoplasms subsequent to treatment of inflammatory bowel disease with …
PMID: 10566724
Year: 1999
Relationship Type:
Treatment
Score: 6.1
Not found
Allergic reactions to 6-mercaptopurine during treatment of inflammatory bowel d…
PMID: 10372932
Year: 1999
Relationship Type:
Treatment
Score: 6.1
Crohn's disease (CD) and ulcerative colitis (UC) are inflammatory bowel diseases (IBD) of unknown etiology. Oral absorption studies have shown an in…
Shingles during the course of treatment with 6-mercaptopurine for inflammatory …
PMID: 10022640
Year: 1999
Relationship Type:
Treatment
Score: 6.1
Not found
6-Mercaptopurine metabolism in Crohn's disease: correlation with efficacy and t…
PMID: 8949645
Year: 1996
Relationship Type:
Adverse Effect
Score: 6.1
BACKGROUND: Tumor necrosis factor alpha (TNF alpha) and beta (TNF beta) appear to play an important role in the regulation of the inflammatory respo…
Combined use of cyclosporine and azathioprine or 6-mercaptopurine in pediatric …
PMID: 8708884
Year: 1996
Relationship Type:
Association
Score: 6.1
Human intestinal lamina propria T cells have a low expression of the CD45RA antigen and a high expression of the CD45RO antigen. This phenotype is …
6-Mercaptopurine and spermatogenesis in the young rat
PMID: 1935495
Year: 1991
Relationship Type:
Association
Score: 6.1
Cases of interest using affected sib-pair methods to distinguish between recessive and additive (dominant) modes of inheritance of a disease-predisp…