Overview

Generic Name(s):
mercaptopurine
Trade Name(s):
Leukerin, Ismipur, Puri-Nethol, Mercaptina, Alti-Mercaptopurine, Purinethol, Flocofil, Mercaptopurinum, and Mercaleukim
NCI Definition [1]:
A thiopurine-derivative antimetabolite with antineoplastic and immunosuppressive activities. Produced through the metabolism of mercaptopurine by hypoxanthine-guanine phosphoribosyltransferase (HGPRT), mercaptopurine metabolites 6-thioguanosine-5'-phosphate (6-thioGMP) and 6-thioinosine monophosphate (T-IMP) inhibit nucleotide interconversions and de novo purine synthesis, thereby blocking the formation of purine nucleotides and inhibiting DNA synthesis. This agent is also incorporated into DNA in the form of deoxythioguanosine, which results in the disruption of DNA replication. In addition, mercaptopurine is converted to 6-methylmercaptopurine ribonucleoside (MMPR) by 6-thiopurine methyltransferase; MMPRs are also potent inhibitors of de novo purine synthesis. (NCI04)

Mercaptopurine has been investigated in 32 clinical trials, of which 29 are open and 3 are closed. Of the trials investigating mercaptopurine, 2 are phase 1 (2 open), 2 are phase 1/phase 2 (2 open), 12 are phase 2 (9 open), 3 are phase 2/phase 3 (3 open), 9 are phase 3 (9 open), 2 are phase 4 (2 open), and 2 are no phase specified (2 open).

BCR-ABL1 Fusion, t(9;22)(q34;q11), and KMT2A Fusion are the most frequent biomarker inclusion criteria for mercaptopurine clinical trials.

B-cell acute lymphoblastic leukemia, acute lymphoblastic leukemia, and B-cell lymphoblastic lymphoma are the most common diseases being investigated in mercaptopurine clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Mercaptopurine
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Mercaptopurine
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating mercaptopurine and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
Mercaptopurinum, Purinethol, Alti-Mercaptopurine, Flocofil, Ismipur, Leukerin, purixan, bw 57 323h, Mercaleukim, Mercaptina, Puri-Nethol, mercaptopurine, 1226, mercaptopurine (substance), 24850, 6 mercaptopurine monohydrate, 6-thiohypoxanthine, purine-6-thiol monohydrate, 6-mercaptopurine monohydrate, mp, 6-mercaptopurine [chemical/ingredient], 6h-purine-6-thione, 1,7-dihydro- (9ci), purine-6-thiol, monohydrate, 6-thiopurine, 6 thiopurine, 6-mercaptopurine, 6-purinethiol, mercaptopurine, mercaptopurine a 06, 6112-76-1 (monohydrate), 6 mercaptopurine, 3h purine-6-thiol, 6-thioxopurine, bw 57-323h, purine-6-thiol, monohydrate, 50-44-2, purine-6-thiol monohydrate, leupurin, mercapto-6-purine, mercaptopurine (product), 6-mp, xaluprine, purine-6-thiol, monohydrate, 7-mercapto-1,3,4,6-tetrazaindene, purinethiol, azathiopurine, puri nethol, 6 mercaptopurine, 6h-purine-6-thione, 1,7-dihydro- (9ci), 1,7-dihydro-6h-purine-6-thione monohydrate, 6-thioxopurine, bw 57-323h, u-4748, azathiopurine, 755, 6 thiopurine, 6mp - mercaptopurine, 1,7 dihydro-6h-purine-6-thione monohydrate, 6-mercaptopurine monohydrate, mercaptopurina, 7-mercapto-1,3,4,6-tetrazaindene, 6-thiopurine, 6mp, mercaleukin, 3h-purine-6-thiol, mercapurin, wr-2785, bw 57323h, purine, 6-mercapto-, purine-6-thiol (8ci), purine-6-thiol (8ci), nci-c04886, 1,7-dihydro-6h-purine-6-thione, 6 thiohypoxanthine, 6 mp, mern, mercaptopurinum, purimethol, 6h-purine-6-thione, 1,7-dihydro-, 6 thiohypoxanthine, 6- mercaptopurine, 6-mercaptopurine, 6-purinethiol
Drug Categories [2]:
Antimetabolites
NCIT ID [1]:
C195
SNOMED ID [1]:
F-61ABE

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.