Delving into the Latest Updates on Thioguanine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-Amino 6MP, 2-Amino-1,7-dihydro-6H-purine-6-thione, 2-amino-1,9-dihydropurine-6-thione

+ [26]

Target

DNA

Action

inhibitors

Mechanism

DNA inhibitors(DNA inhibitors)

Therapeutic Areas

NeoplasmsImmune System DiseasesHemic and Lymphatic Diseases

Active Indication

Acute Lymphoblastic LeukemiaAcute Myeloid LeukemiaPhiladelphia chromosome positive chronic myelogenous leukemia

Inactive Indication-

Originator Organization

Aspen Pharmacare Holdings Ltd.

Active Organization

Shanghai Donghai Pharmaceutical Co., Ltd.Waylis Therapeutics LLC

Inactive Organization

Only For Children Pharmaceuticals SA

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (18 Jan 1966),

Acute Myeloid LeukemiaPhiladelphia chromosome positive chronic myelogenous leukemia

RegulationOrphan Drug (European Union)

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Structure/Sequence

Molecular FormulaC5H5N5S

InChIKeyWYWHKKSPHMUBEB-UHFFFAOYSA-N

CAS Registry154-42-7

This phase II trial tests how well adding revumenib to usual treatment (blinatumomab) compared to usual treatment alone works in treating patients with B-cell acute lymphoblastic leukemia (B-ALL) or acute leukemia with ambiguous lineage (ALAL) with KMT2A-translocation. Revumenib binds to a protein called menin and keeps it from binding to another protein called KMT2A. This stops or slows the growth of leukemia cells with changes in the KMT2A gene. Blinatumomab binds to CD19, which is found on most B cells (a type of white blood cell) and some types of leukemia cells. It also binds to a protein called CD3, which is found on T cells (another type of white blood cell). This may help the immune system kill cancer cells. In addition to blinatumomab, usual treatment also includes dexamethasone, methotrexate, cyclophosphamide, cytarabine, mercaptopurine, calaspargase pegol, doxorubicin, thioguanine, daunorubicin, vincristine and leucovorin. Dexamethasone is in a class of medications called corticosteroids. It is used to reduce inflammation and lower the body's immune response to help lessen the side effects of chemotherapy drugs. Methotrexate is in a class of medications called antimetabolites. It is also a type of antifolate. Methotrexate stops cells from using folic acid to make deoxyribonucleic acid (DNA) and may kill cancer cells. Cyclophosphamide is in a class of medications called alkylating agents. It works by damaging the cell's DNA and may kill cancer cells. It may also lower the body's immune response. Chemotherapy drugs, such as cytarabine, mercaptopurine, calaspargase pegol, doxorubicin, thioguanine, and daunorubicin, work in different ways to stop the growth of cancer cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Vincristine is in a class of medications called vinca alkaloids. It works by stopping cancer cells from growing and dividing and may kill them. Leucovorin is also being studied in the treatment of cancer. It is a type of chemoprotective agent and a type of chemosensitizing agent. Adding revumenib to usual treatment with blinatumomab may be safe, tolerable and more effective than blinatumomab alone in lowering the amount of leukemia in patients with B-ALL or ALAL with the KMT2A translocation.

Start Date14 Oct 2026

Sponsor / Collaborator

SWOG

[+1]

NCT07072585

/ Not yet recruitingPhase 2/3IIT

A Phase 2/3 Randomized Trial Investigating Daratumumab on a Modified Augmented BFM (aBFM) Backbone in Newly Diagnosed T-Lymphoblastic Leukemia (T-ALL) and T-Lymphoblastic Lymphoma (T-LL)

This phase II/III trial tests the addition of daratumumab to chemotherapy for treating patients with newly-diagnosed T-ALL and T-LL. Daratumumab is in a class of medications called monoclonal antibodies. It binds to a protein called CD38, which is found on some types of immune cells and cancer cells. Daratumumab may block CD38 and help the immune system kill cancer cells. Chemotherapy drugs work in different ways to stop the growth of cancer cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Giving chemotherapy with daratumumab may kill more cancer cells.

Start Date28 Aug 2026

Sponsor / Collaborator

The Children's Oncology Group Foundation, Inc.

NCT06317662

/ RecruitingPhase 2IIT

A Phase 2 Study of Blinatumomab in Combination With Chemotherapy for Infants With Newly Diagnosed Acute Lymphoblastic Leukemia With Randomization of KMT2A-Rearranged Patients to Addition of Venetoclax

This phase II trial tests the addition of venetoclax and/or blinatumomab to usual chemotherapy for treating infants with newly diagnosed acute lymphoblastic leukemia (ALL) with a KMT2A gene rearrangement (KMT2A-rearranged [R]) or without a KMT2A gene rearrangement (KMT2A-germline [G]). Venetoclax is in a class of medications called B-cell lymphoma-2 (Bcl-2) inhibitors. It may stop the growth of cancer cells by blocking Bcl-2, a protein needed for cancer cell survival. Blinatumomab is a monoclonal antibody that may interfere with the ability of cancer cells to grow and spread. Chemotherapy drugs work in different ways to stop the growth of cancer cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Adding venetoclax and/or blinatumomab to standard chemotherapy may be more effective at treating patients with ALL than standard chemotherapy alone, but it may also cause more side effects. This clinical trial evaluates the safety and effectiveness of adding venetoclax and/or blinatumomab to chemotherapy for the treatment of infants with KMT2A-R or KMT2A-G ALL.

Start Date05 Jun 2025

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Thioguanine

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100 Translational Medicine associated with Thioguanine

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100 Patents (Medical) associated with Thioguanine

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3,146

Literatures (Medical) associated with Thioguanine

31 Dec 2026·Gut Microbes

Exploring the gut microbiome and metabolomic interactions of antimetabolite drugs to optimize therapy

Review

Author: Zhao, Libo ; Chen, Jingyang ; Wang, Yanan ; Xu, Lei ; Li, Xiaona

Antimetabolite drugs are cornerstones in treating various cancers and autoimmune diseases; however, their clinical utility is often hampered by systemic toxicity caused by drug-induced gut microbiota dysbiosis. Predicting patient responses remains a significant challenge. Several studies have highlighted the influence of gut microbiota on antimetabolite treatment outcomes, revealing complex bidirectional interactions between the drugs and microbial communities. This review synthesizes the effects of common antimetabolites (including 5-fluorouracil, methotrexate, gemcitabine, capecitabine, 6-mercaptopurine, and thioguanine) on gut microbial communities and outlines a framework (pharmacokinetics, endogenous metabolite production, immune modulation, and apoptotic pathway modulation) for assessing chemotherapy-microbiota interactions. Additionally, potential microbial biomarkers for predicting treatment responses and strategies for manipulating the gut microbiota to enhance therapeutic efficacy are discussed. Therefore, advances in methodologies such as metagenomics and real-time microbial monitoring will be essential for unraveling these interactions and promoting the precise application of antimetabolite drugs.

01 Dec 2026·Molecular & general genetics : MGG

Investigating the evolutionary history of the biosynthetic gene cluster for the cytotoxic purine analog, 6-thioguanine

Article

Author: Bateman, Adria ; Stavrinides, John ; Most, Kathryn

The aim of this study was to explore the distribution and evolution of the biosynthetic gene cluster that directs the synthesis of 6-thioguanine, a purine antimetabolite that has applications as a chemotherapeutic, and has been studied for anti-inflammatory, antibacterial, and antiviral properties. Some bacteria, like members of the genus Erwinia, carry the ycfRABCD operon that directs the synthesis of 6-thioguanine. To explore its evolution, we surveyed for the presence of the cluster across all bacteria available in the public databases, and identified two distinct configurations of the gene cluster. One configuration is found exclusively within the Erwiniaceae and the Yersiniaceae (Gammaproteobacteria), and the second, which carries an additional gene, is found within members of the Alpha- and Betaproteobacteria. We found that the genomic location of ycf operon is conserved across divergent bacteria, with phylogenetic and %GC analyses suggesting that the cluster is evolutionarily old and vertically inherited. In some lineages, the cluster has been lost, while in others it has been acquired horizontally from distantly related groups. Maintenance of the cluster across diverse bacterial species suggests multiple roles for 6-thioguanine in the general ecology of these species.

01 Sep 2026·MARINE POLLUTION BULLETIN

Chemical profile of Thalassia testudinum under coastal pollution: Assessment of mercury, VOCs and secondary metabolites in the Colombian Caribbean

Article

Author: Palacio-Herrera, Flor ; Olivero-Verbel, Jesus ; Sierra-Marquez, Lucellys

Seagrass meadows of Thalassia testudinum are key components of blue carbon ecosystems and effective bioindicators of environmental contamination due to their ability to incorporate both inorganic and organic pollutants. This study evaluated total mercury (T-Hg) concentrations and the qualitative occurrence of volatile organic compounds (VOCs) and secondary metabolites in T. testudinum collected from two sites with contrasting environmental pressures in the Colombian Caribbean: Cartagena Bay (CTG Bay) and the reference area within the Corales del Rosario and San Bernardo National Natural Park (RSBC-NNP). Total mercury was quantified using a direct mercury analyzer, while VOCs were identified by GC-MS. T-Hg concentrations in T. testudinum, expressed on a dry-weight basis, ranged from 9.7 to 32.4 μg/kg in CTG Bay and from 8.0 to 10.0 μg/kg in the RSBC-NNP, although both ranges remained substantially lower than values previously reported for sediments and fish from the same area, yet consistent with a moderate bioaccumulation capacity of this seagrass species. Subsequently, a total of 89 VOCs were identified, mainly including aliphatic and aromatic hydrocarbons, terpenes, fatty acids, and sterols. CTG Bay exhibited a higher chemical diversity, whereas the 23 compounds detected in the reference area were also present in the bay, with no exclusive compounds observed in the protected site. Metabolites such as phytol, squalene, and (Z)-9-octadecenamide were detected in both areas, suggesting common physiological processes related to basal metabolism and general stress responses. Overall, these findings demonstrate that T. testudinum integrates signals of exposure to both metallic and organic contaminants, reinforcing its value as a sentinel species for environmental assessment in tropical coastal ecosystems.

100 Deals associated with Thioguanine

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External Link

KEGG	Wiki	ATC	Drug Bank
D06109	Thioguanine	L01BB03	DB00352

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute Lymphoblastic Leukemia	China	Shanghai Donghai Pharmaceutical Co., Ltd.	01 Jan 1995
Acute Myeloid Leukemia	United States	Waylis Therapeutics LLC	18 Jan 1966
Philadelphia chromosome positive chronic myelogenous leukemia	United States	Waylis Therapeutics LLC	18 Jan 1966

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASH2025	Not Applicable	Hematologic Neoplasms	67	DecitabineThioguanine + DecitabineThioguanine	zkqyiohnwd(qzzpgdtyon) = xqakssmrua maxdzgwvdn (odfarrsdug ) View more	Positive	06 Dec 2025
NCT05276284 (TEMPLE, ESMO2025)	Phase 1/2	Metastatic Solid Tumor	30	Atezolizumab + 6-mercaptopurine + 6-thioguanine	laabnsjqwe(jjrnfyvrnr) = fnwcrsvvyf xhidnwkpha (vgivbbwjcs ) View more	Negative	17 Oct 2025
ECCO2024	Not Applicable	Inflammatory Bowel Diseases	307	Low-dose thioguanine	qodqqbeati(lopopnbadv) = ymvkgtpugz jjpgzqycjd (nhbgxbeacg ) View more	Positive	21 Feb 2024
ECCO2024	Not Applicable	Inflammatory Bowel Diseases	307	6-mercaptopurine	qodqqbeati(lopopnbadv) = vuzgzgkuvj jjpgzqycjd (nhbgxbeacg ) View more	Positive	21 Feb 2024
ECCO2022	Not Applicable	Inflammatory Bowel Diseases First line	103	Thioguanine	xwqzhxzbvy(edibasqgcz) = yrfikscgdm ngmioxyuyx (hgmmjsxyog ) View more	Positive	16 Feb 2022
ECCO2021	Not Applicable	Perianal fistula due to Crohn's disease	221	Methotrexate	qvbuhlsjzc(xdvbisoalb) = ddygsdongu kndguqfxhc (klevmnouvu ) View more	Positive	02 Jul 2021
ECCO2021	Not Applicable	Perianal fistula due to Crohn's disease	221	Tioguanine	rtywtovzja(jtmsqnanxs) = pyqgkdzddu toazapogyt (jonqogwymp ) View more	Positive	02 Jul 2021
UEGW2020	Not Applicable	Inflammatory Bowel Diseases	-	Thioguanine (TG)	pmpyjnwbfp(vrwuusmkzy) = veatidfihu qxckaqhhoo (qjjvicmsfv, 145 - 1761) View more	-	01 Oct 2020
ECCO2020	Not Applicable	Inflammatory Bowel Diseases	182	Thioguanine	gzlbidfong(bjeydckdvc) = lyoigblmsx rhlcsigxcu (lspzqtckiv ) View more	Positive	12 Feb 2020
ECCO2020	Not Applicable	Inflammatory Bowel Diseases	182	low dose thiopurines and allopurinol	gzlbidfong(bjeydckdvc) = risgmqquhk rhlcsigxcu (lspzqtckiv ) View more	Positive	12 Feb 2020
UEGW2019	Not Applicable	Inflammatory Bowel Diseases	-	Thioguanine	qzfpcqspwy(srgabbpefz) = NRH was diagnosed in two patients (1%) zqdbfgujko (kklhxmanxx ) View more	-	01 Oct 2019
NCT00866749 (CTgov)	Phase 2	Acute Lymphoblastic Leukemia \| Precursor T-Cell Lymphoblastic Leukemia-Lymphoma \| Adult Lymphoblastic Lymphoma	120	PEG-asparaginase+Cyclophosphamide+Doxorubicin+Methotrexate+Thioguanine+Mercaptopurine+Vincristine+Cytarabine+Daunorubicin	oydjqvqzup = uwamklozbl cajiviylze (bwqfpcpaxl, nehemrhbqq - ogsfftvlef) View more	-	10 Sep 2019
ECCO2019	Not Applicable	Inflammatory Bowel Diseases	274	Thioguanine	zekutjdhec(ualhrvymgb) = Beneficial therapeutic response was correlated with 6-thioguanine-nucleotide (6-TGN) threshold levels of > 682 pmol/8 × 108 RBC (p < 0.05). pjavggwevo (mijpvzqkvh ) View more	Positive	06 Mar 2019