Drug · Small Molecule

Thioguanine

CI-DRUG-00000590Explore in graph →NCIt C876 CHEMBL727 CIViC Approved

Regulatory

Approvals (2)

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-dpdRegulatory2 approval records from 2 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 LANVIS (DIN 00282081) under ATC L01BB03 TIOGUANINE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Dec 31, 1974	health-canada-dpd
US FDA	—	a) Acute Nonlymphocytic Leukemias TABLOID brand Thioguanine is indicated for remission induction and remission consolidation treatment of acute nonlymphocytic leukemias. However, it is not recommended for use during maintenance therapy or similar long-term continuous treatments due to the high risk of liver toxicity (see WARNINGS and ADVERSE REACTIONS). The response to this agent depends upon the age of the patient (younger patients faring better than older) and whether thioguanine is used in previously treated or previously untreated patients. Reliance upon thioguanine alone is seldom justified for initial remission induction of acute nonlymphocytic leukemias because combination chemotherapy including thioguanine results in more frequent remission induction and longer duration of remission than thioguanine alone. b) Other Neoplasms TABLOID brand Thioguanine is not effective in chronic lymphocytic leukemia, Hodgkin’s lymphoma, multiple myeloma, or solid tumors. Although thioguanine is one of several agents with activity in the treatment of the chronic phase of chronic myelogenous leukemia, more objective responses are observed with MYLERAN ® (busulfan), and therefore busulfan is usually regarded as the preferred drug.	approved	Jan 18, 1966	openfda

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 15 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	18	10	44	84	2	CA, US	Jan 18, 1966	1993-01
Leukemia	Phase4	Phase 4	16	8	39	72	0	—	—	1993-01
Non-Hodgkin Lymphoma	Phase4	Phase 4	6	4	6	15	0	—	—	2004-04
Malignant Central Nervous System Neoplasm	Phase3	Phase 3	1	1	2	3	0	—

Curated evidence

Clinical evidence (29)

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

civicCuratedShowing 1–29 of 29 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 (84)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 84 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: Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor; DNA inhibitor
Targets: 2 genes
UNII: FTK8U1GZNX
Aliases: 2-Amino-1,7-dihydro-6H-purine-6-thione, 2-Amino-6-mercaptopurine, 2-Amino 6MP, 2-Amino-6-purinethiol, 2-Aminopurin-6-thiol, 2-Aminopurine-6(1H)-thione, 2-Aminopurine-6-thiol, 2-Aminopurine-6-thiol Hemihydrate, 2-Mercapto-6-aminopurine, 6-Amino-2-mercaptopurine, 6H-Purine-6-thione, 2-amino-1,7-dihydro- (9CI), 6-Mercapto-2-aminopurine, 6 Mercaptoguanine, 6-TG, 6 Thioguanine, BW 5071, Lanvis, NSC-752, NSC-76504, Tabloid, Thioguanine, Thioguanine anhydrous, Thioguanine Hemihydrate, Thioguanine Hydrate, Tioguanin, Tioguanina, Tioguanine, Tioguanine hemihydrate, Wellcome U3B, WR-1141 … (+1)

Data updated 9 minutes agoSource updated unknown

Identifiers

Codes (3)

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

System	Code	Label
ATC (WHO)	L01BB03	TIOGUANINE
DIN (Health Canada)

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