Drug · Small Molecule

Mercaptopurine

CI-DRUG-00000375Explore in graph →NCIt C195 CHEMBL1200751 CIViC Approved

Regulatory

Approvals (5)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory5 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as MERCAPTOPURINE TABLETS USP (DIN 02415275) under ATC L01BB02 MERCAPTOPURINE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Nov 27, 2013	health-canada-dpd

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 2 days agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	43	25	63	169	5	CA, EU, US	Sep 11, 1953	1992-10
Leukemia	Approved	Phase 4	38	22	55	149	3	EU, US	Sep 11, 1953	1992-10
Non-Hodgkin Lymphoma	Phase4	Phase 4	11	8	8	25	0	—	—	1993-03
Malignant Central Nervous System Neoplasm	Phase3	Phase 3	1	1	2	4	0

Curated evidence

Clinical evidence (31)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–31 of 31 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
NT5C2 R238W2
Mercaptopurine + Thioguanine

Clinical trials

Trials with this intervention (173)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 173 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT06124157	A Study Testing the Combination of Dasatinib or Imatinib to Chemotherapy Treatment With Blinatumomab for Children, Adolescents, and Young Adults With Philadelphia Chromosome Positive (Ph+) or ABL-Class Philadelphia Chromosome-Like (Ph-Like) B-cell Acute Lymphoblastic Leukemia (B-ALL)	recruiting	Phase 2	222	National Cancer Institute (NCI)NIH	4	Sep 28, 2026	clinicaltrials
NCT06317662	Testing the Addition of the Anti-cancer Drug Venetoclax and/or the Anti-cancer Immunotherapy Blinatumomab to the Usual Chemotherapy Treatment for Infants With Newly Diagnosed KMT2A-rearranged or KMT2A-non-rearranged Leukemia

Molecule

Record

Kind: Small Molecule
Mechanism: Amidophosphoribosyltransferase inhibitor; DNA inhibitor
Targets: 1 gene
UNII: E7WED276I5
Aliases: 1,7-Dihydro-6H-purine-6-thione, 1,7-Dihydro-6H-purine-6-thione Monohydrate, 3H-Purine-6-thiol, 6H-Purine-6-thione, 1,7-dihydro- (9CI), 6-Mercaptopurine, 6-Mercaptopurine Monohydrate, 6 MP, 6-Purinethiol, 6 Thiohypoxanthine, 6 Thiopurine, 6-Thioxopurine, 7-Mercapto-1,3,4,6-tetrazaindene, Alti-Mercaptopurine, Azathiopurine, BW 57-323H, Flocofil, Ismipur, Leukerin, Leupurin, Mercaleukim, Mercaleukin, Mercaptina, Mercapto-6-purine, Mercaptopurina, Mercaptopurine, Mercaptopurine hydrate, Mercaptopurinum, Mercapurin, Mern, NCI-C04886 … (+15)

Data updated 21 hours agoSource updated unknown

Identifiers

Codes (6)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01BB02	MERCAPTOPURINE
DIN (Health Canada)	00004723

PRPS1 A190T2
Lometrexol + MercaptopurineCombination	B Lymphoblastic Leukemia/LymphomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID7913 Treatment with the GART inhibitor, Lometrexol (de novo purine synthesis inhibitor), sensitized Reh cells overexpressing PRPS1 A190T to mercaptopurine (6-MP) as evidenced by significant reduction of th… (full text at CIViC) PMID 25962120 · Li et al., 2015 · Open in CIViC	civic
Mercaptopurine + ThioguanineSubstitutes	B Lymphoblastic Leukemia/LymphomaCURATED_BROADER	Predictive	D	Supports Resistance	5	accepted	EID7909 Lentiviral-mediated overexpression of PRPS1 A190T in Reh cells resulted in significant resistance against mercaptopurine (6-MP) and thioguanine (6-TG) as indicated by IC50 increases and reduced apopto… (full text at CIViC) PMID 25962120 · Li et al., 2015 · Open in CIViC	civic

PRPS1 S103T2
Lometrexol + MercaptopurineCombination	B Lymphoblastic Leukemia/LymphomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID7912 Treatment with the GART inhibitor, Lometrexol (de novo purine synthesis inhibitor), sensitized Reh cells overexpressing PRPS1 S103T to 6-MP as evidenced by significant reduction of the cell line's 6-M… (full text at CIViC) PMID 25962120 · Li et al., 2015 · Open in CIViC	civic
Mercaptopurine + ThioguanineSubstitutes	B Lymphoblastic Leukemia/LymphomaCURATED_BROADER	Predictive	D	Supports Resistance	5	accepted	EID7907 Lentiviral-mediated overexpression of PRPS1 S103T in Reh cells resulted in significant resistance against mercaptopurine (6-MP) and thioguanine (6-TG) as indicated by IC50 increases and reduced apopto… (full text at CIViC) PMID 25962120 · Li et al., 2015 · Open in CIViC	civic

NT5C2 R367Q3
Mercaptopurine + ThioguanineSubstitutes	Childhood Acute Lymphoblastic LeukemiaALIAS	Predictive	C	Supports Resistance	2	accepted	EID7812 71 Childhood B-cell acute lymphocytic leukemia relapse patients had their diagnosis and relapse samples sequenced for NT5C2 mutations. Sequencing revealed an early relapse case with NT5C2 R367Q enrich… (full text at CIViC) PMID 23377183 · Meyer et al., 2013 · Open in CIViC	civic
〃	Childhood Acute Lymphoblastic LeukemiaALIAS	Predictive	D	Supports Resistance	4	accepted	EID7862 Lentiviral-mediated overexpression of NT5C2 R367Q in Reh cells resulted in significant resistance against thiopurines (mercaptopurine and thioguanine) versus wildtype and GFP controls, as indicated by… (full text at CIViC) PMID 23377183 · Meyer et al., 2013 · Open in CIViC	civic
Mercaptopurine + ThioguanineSubstitutes	T Acute Lymphoblastic LeukemiaCURATED_BROADER	Predictive	D	Supports Resistance	4	accepted	EID630 CCRF-CEM and to a lesser extent CUTLL1 T-ALL cell lines expressing the NT5C2 R367Q mutation had increased resistance to 6-mercaptopurine and 6-thioguanine treatment than cells expressing wildtype NT5C… (full text at CIViC) PMID 23377281 · Tzoneva et al., 2013 · Open in CIViC	civic