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DRUG:

thioguanine

i
Other names: 6-TG
Company:
Generic mfg.
Drug class:
DNA synthesis inhibitor
Related drugs:
7d
Enrollment open
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JAK2 (Janus kinase 2) • RUNX1 (RUNX Family Transcription Factor 1) • KMT2A (Lysine Methyltransferase 2A) • ETV6 (ETS Variant Transcription Factor 6) • CRLF2 (Cytokine Receptor Like Factor 2) • IKZF1 (IKAROS Family Zinc Finger 1) • AFF1 (AF4/FMR2 Family Member 1) • TCF3 (Transcription Factor 3) • PBX1 (PBX Homeobox 1)
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KMT2A rearrangement
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cytarabine • doxorubicin hydrochloride • Jakafi (ruxolitinib) • cyclophosphamide • ifosfamide • etoposide IV • vincristine • daunorubicin • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine • vindesine
22d
Trial completion date
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cytarabine • doxorubicin hydrochloride • cyclophosphamide • methotrexate • vincristine • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine • Hemady (dexamethasone tablets) • Starasid (cytarabine ocfosfate)
22d
Phase classification
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ABL1 (ABL proto-oncogene 1) • CD19 (CD19 Molecule) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CSF1R (Colony stimulating factor 1 receptor)
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TruSight RNA Pan-Cancer Panel
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dasatinib • imatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • Blincyto (blinatumomab) • methotrexate • vincristine • daunorubicin • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • Asparlas (calaspargase pegol-mknl) • thioguanine • Starasid (cytarabine ocfosfate)
1m
Trial completion
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JAK2 (Janus kinase 2) • CRLF2 (Cytokine Receptor Like Factor 2) • JAK1 (Janus Kinase 1) • IL7R (Interleukin 7 Receptor) • EPOR (Erythropoietin Receptor) • SH2B3 (SH2B Adaptor Protein 3)
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cytarabine • doxorubicin hydrochloride • Jakafi (ruxolitinib) • cyclophosphamide • vincristine • prednisone • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine • Erwinase (erwinia asparaginase)
2ms
Ubiquitin-Specific Proteases in Breast Cancer: Unraveling Oncogenic Roles and Therapeutic Opportunities. (PubMed, DNA Cell Biol)
Pharmacological inhibitors of specific USPs, such as pimozide, trifluoperazine, rottlerin, 6-thioguanine, and costunolide, are highlighted for their potential to inhibit proliferation, metastasis, induce apoptosis, and circumvent therapy resistance across breast cancer subtypes (triple-negative and HER-2 positive). The review highlights the complex and often contradictory roles of USPs in breast cancer and points to the immense promise of targeting these enzymes to develop new and efficacious anticancer therapies.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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thioguanine
2ms
A041501: Inotuzumab Ozogamicin and Frontline Chemotherapy in Treating Young Adults With Newly Diagnosed B Acute Lymphoblastic Leukemia (clinicaltrials.gov)
P3, N=310, Suspended, Alliance for Clinical Trials in Oncology | Trial completion date: Aug 2026 --> Aug 2027 | Trial primary completion date: Mar 2026 --> Mar 2027
Trial completion date • Trial primary completion date
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CD20 (Membrane Spanning 4-Domains A1) • CD22 (CD22 Molecule) • ITGB1 (Integrin Subunit Beta 1)
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CD20 positive • CD22 positive
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Rituxan (rituximab) • cytarabine • doxorubicin hydrochloride • cyclophosphamide • Besponsa (inotuzumab ozogamicin) • vincristine • daunorubicin • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine
2ms
Placing purines in precision medicine: Targeting a metabolic reliance in KRAS-mutant tumors. (PubMed, iScience)
In KRAS-mutant cancer models, trametinib treatment caused dysregulation of the purine biosynthetic pathway driven by reductions in enzyme GART. This induced vulnerability nominated purine analog 6-thioguanine as a synergistic partner...In vivo, the treatment significantly increases overall survival without systemic toxicity. Integrating drug-induced multi-omic changes with functional screening identifies therapeutic strategies, supporting the use of purine analogs with MEK inhibitors for KRAS-mutant tumors.
Journal
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation
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Mekinist (trametinib) • thioguanine
2ms
Model-Based Strategy for 6-Mercaptopurine Treatment in Acute Lymphoblastic Leukemia Maintenance Phase: Prediction of 6-TGN and 6-MMP Concentrations to Optimize Treatment. (PubMed, Pediatr Blood Cancer)
Allopurinol co-treatment reduces toxicity while maintaining therapeutic efficacy at lower 6-MP doses. The proposed model warrants prospective evaluation for clinical relevance confirmation.
Journal
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MMP9 (Matrix metallopeptidase 9)
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mercaptopurine • thioguanine
2ms
AALL1732: Inotuzumab Ozogamicin and Post-Induction Chemotherapy in Treating Patients With High-Risk B-ALL, Mixed Phenotype Acute Leukemia, and B-LLy (clinicaltrials.gov)
P3, N=5951, Recruiting, Children's Oncology Group | Trial completion date: Mar 2030 --> Mar 2032 | Trial primary completion date: Mar 2030 --> Mar 2032
Trial completion date • Trial primary completion date
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cytarabine • doxorubicin hydrochloride • cyclophosphamide • Blincyto (blinatumomab) • methotrexate • Besponsa (inotuzumab ozogamicin) • vincristine • daunorubicin • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • Asparlas (calaspargase pegol-mknl) • thioguanine • Hemady (dexamethasone tablets) • Starasid (cytarabine ocfosfate)
3ms
TEMPLE: Thiopurine Enhanced Mutations for PD-1/Ligand-1 Efficacy (clinicaltrials.gov)
P1/2, N=18, Completed, Kristoffer Rohrberg | Recruiting --> Completed | N=39 --> 18
Trial completion • Enrollment change • Tumor mutational burden • IO biomarker
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TMB (Tumor Mutational Burden)
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Tecentriq (atezolizumab) • mercaptopurine • thioguanine
3ms
In silico identification of deleterious NT5C2 and PRPS1 mutations driving thiopurine resistance in relapsed acute lymphoblastic leukemia. (PubMed, Cancer Genet)
Protein-protein interaction networks indicate that these variations are involved in nucleotide metabolism and pharmacological responses, confirming their role in thiopurine resistance. In summary, NT5C2 and PRPS1 gene variations may act as potential biomarkers for resistance and hence require more experimental validation of VUS to determine their significance.
Journal
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NT5C2 (5'-Nucleotidase Cytosolic II) • PRPS1 (Phosphoribosyl Pyrophosphate Synthetase 1)
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thioguanine
4ms
Trial initiation date
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cytarabine • bortezomib • doxorubicin hydrochloride • cyclophosphamide • methotrexate • Darzalex (daratumumab) • vincristine • daunorubicin • Oncaspar liquid (pegaspargase) • nelarabine • Asparlas (calaspargase pegol-mknl) • thioguanine • Hemady (dexamethasone tablets) • Purixan (mercaptopurine oral suspension) • Starasid (cytarabine ocfosfate)