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DRUG:

temozolomide

i
Other names: CCRG-81045, MB 39831, NSC 362856, RP 46161, MK-7365, SCH-52365, MB-39831, RP-46161, SCH 52365, M & B 39831, SCH 052365, TOZ309
Company:
Generic mfg.
Drug class:
DNA synthesis inhibitor
Related drugs:
2d
Phase classification • Metastases
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AR (Androgen receptor) • HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset)
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HRD • BRCA mutation
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temozolomide • Partruvix (pamiparib)
3d
Enrollment open
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IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • MGMT (6-O-methylguanine-DNA methyltransferase)
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temozolomide
3d
A Dose-escalation Clinical Study of Intraoperative Photodynamic Therapy of Glioblastoma (clinicaltrials.gov)
P1/2, N=12, Recruiting, Hemerion Therapeutics | Trial completion date: Jul 2025 --> Jul 2026 | Trial primary completion date: Mar 2025 --> Dec 2025
Trial completion date • Trial primary completion date
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temozolomide
3d
New P3 trial • Metastases
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Keytruda (pembrolizumab) • Yervoy (ipilimumab) • carboplatin • temozolomide • albumin-bound paclitaxel • cyclophosphamide • dacarbazine • Opdualag (nivolumab/relatlimab-rmbw) • Amtagvi (lifileucel) • relatlimab (BMS-986016) • IMA203
4d
Fluorescent Polymer Nanocomposites as Novel Drug-Loading and Targeted Delivery Nanocarriers for Glioma Therapy by Modulating ERBB4. (PubMed, J Fluoresc)
Temozolomide (TMZ) is widely used in glioma therapy due to its excellent ability to penetrate the blood-brain barrier...Additionally, we evaluated the inhibitory effects and mechanisms of HA-PEG@ICG@1@TMZ on glioma cell proliferation. Our study lays the foundation for further exploration of TMZ-based therapies for glioma treatment.
Journal
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ERBB4 (erb-b2 receptor tyrosine kinase 4)
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temozolomide
4d
New P2 trial • Real-world evidence • Pan tumor • Real-world
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BRAF (B-raf proto-oncogene)
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Lynparza (olaparib) • Mekinist (trametinib) • Ibrance (palbociclib) • Tafinlar (dabrafenib) • Focus V (anlotinib) • temozolomide • Lenvima (lenvatinib) • Piqray (alpelisib) • pazopanib • Epidaza (chidamide) • Trodelvy (sacituzumab govitecan-hziy) • bozitinib (APL-101)
4d
Hypofractionated Radiotherapy (clinicaltrials.gov)
P=N/A, N=420, Recruiting, The First Hospital of Jilin University
New trial
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temozolomide
4d
CB2R activation enhances tumor-associated macrophages-mediated phagocytosis of glioma cell. (PubMed, Heliyon)
JHW133 also effectively augmented the chemotherapeutic efficacy of temozolomide. Overall, our findings show that CB2R activation promotes TAMs-mediated phagocytosis of tumor cells by enhancing CD36 expression, implying that JWH133 could be a useful therapeutic approach to improving chemotherapeutic efficacy against GBM.
Journal
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CD36 (thrombospondin receptor)
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temozolomide
4d
Multiparametic Metabolic and Hypoxic PET/MRI for Disease Assessment in High Grade Glioma (clinicaltrials.gov)
P1, N=20, Recruiting, University of Alabama at Birmingham | Trial primary completion date: Dec 2024 --> Feb 2026
Trial primary completion date
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temozolomide
5d
Epichaperome Inhibition by PU-H71-Mediated Targeting of HSP90 Sensitizes Glioblastoma Cells to Alkylator-Induced DNA Damage. (PubMed, Cancers (Basel))
These results confirm that HSP90 is a strong pro-survival factor in molecularly heterogeneous gliomas and suggest that epichaperome inhibition with HSP90 inhibitors warrants further investigation for the treatment of gliomas.
Journal
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EGFR (Epidermal growth factor receptor) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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temozolomide • zelavespib intravenous (PU-H71 IV)
6d
Comprehensive whole-genome sequencing reveals origins of mutational signatures associated with aging, mismatch repair deficiency and temozolomide chemotherapy. (PubMed, Nucleic Acids Res)
Blocking BER after abasic site formation results in large deletions and TMZ hypersensitization. Our findings reveal potential vulnerabilities of TMZ-resistant tumors.
Journal • Mismatch repair
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MSH2 (MutS Homolog 2)
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temozolomide
7d
A novel nuclear RNA HSD52 scaffolding NONO/SFPQ complex modulates DNA damage repair to facilitate temozolomide resistance. (PubMed, Neuro Oncol)
Our results revealed that HSD52 could serve as a promising therapeutic target to overcome TMZ resistance, improving the clinical efficacy of TMZ chemotherapy in GBM.
Journal
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DNMT1 (DNA methyltransferase 1)
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temozolomide
8d
Daily glucocorticoids promote glioblastoma growth and circadian synchrony to the host. (PubMed, Cancer Cell)
Finally, mouse and human GBM models have intrinsic circadian rhythms in clock gene expression in vitro and in vivo that entrain to the host through glucocorticoid signaling, regardless of tumor type or host immune status. We conclude that GBM entrains to the circadian circuit of the brain, modulating its growth through clock-controlled cues, like glucocorticoids.
Journal
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ARNTL (Aryl Hydrocarbon Receptor Nuclear Translocator Like) • CLOCK (Clock Circadian Regulator) • NR3C1 (Nuclear Receptor Subfamily 3 Group C Member 1)
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temozolomide
10d
B7-H3 in glioblastoma and beyond: significance and therapeutic strategies. (PubMed, Front Immunol)
Following diagnosis, the typical life expectancy ranges from 12 to 15 months, as current established treatments like surgical intervention, radiotherapy, and chemotherapy using temozolomide exhibit limited effectiveness...We delineate the receptors it binds to and its significance in glioblastoma and other cancer types. Lastly, we examine its role in immunotherapy and the utilization of nanobodies in this domain.
Review • Journal • IO biomarker
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CD276 (CD276 Molecule)
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temozolomide
10d
Phase 1 Study of INBRX-109 in Subjects with Locally Advanced or Metastatic Solid Tumors Including Sarcomas (clinicaltrials.gov)
P1, N=321, Recruiting, Inhibrx Biosciences, Inc | N=240 --> 321 | Trial completion date: Jul 2026 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Jun 2026
Enrollment change • Trial completion date • Trial primary completion date • Metastases
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cisplatin • carboplatin • 5-fluorouracil • temozolomide • pemetrexed • irinotecan • ozekibart (INBRX-109)
11d
The impact of timing of temozolomide chemoradiotherapy for newly diagnosed glioblastoma on patient overall survival: A multicenter retrospective study. (PubMed, Neurooncol Adv)
The timing of adjuvant TMZ chemoradiotherapy, if commenced within 12 weeks after glioblastoma diagnosis, did not influence OS regardless of EOR or pMGMT methylation status. Clinical judgment should be exercised in optimizing the timing of initiating adjuvant therapy.
Retrospective data • Journal
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MGMT (6-O-methylguanine-DNA methyltransferase)
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temozolomide
11d
NUTMEG: Nivolumab and Temozolomide Versus Temozolomide Alone in Newly Diagnosed Elderly Patients With GBM (clinicaltrials.gov)
P2, N=103, Active, not recruiting, University of Sydney | Completed --> Active, not recruiting | Trial primary completion date: Dec 2024 --> Jun 2024
Enrollment closed • Trial primary completion date
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Opdivo (nivolumab) • temozolomide
11d
The novel DNA cross-linking agent KL-50 is active against patient-derived models of new and recurrent post-temozolomide mismatch repair-deficient glioblastoma. (PubMed, Neuro Oncol)
KL-50-based compounds are a promising new strategy for the treatment of MGMT-deficient, MMR-deficient GBM that recurs after frontline TMZ.
Journal • Mismatch repair
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MSH6 (MutS homolog 6)
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MSI-H/dMMR
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temozolomide
12d
Trial primary completion date • Surgery • Metastases
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cisplatin • carboplatin • temozolomide • capecitabine • etoposide IV
14d
Clofazimine enhances anti-glioma effect of immunotherapy. (PubMed, Int Immunopharmacol)
Combination of clofazimine and immunotherapy enhances anti-glioma effect of TMZ in an in vivo model experiment.
Journal
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CD68 (CD68 Molecule) • CDH2 (Cadherin 2) • IL1B (Interleukin 1, beta)
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carboplatin • paclitaxel • temozolomide • lomustine
16d
A new nano approach to prevent tumor growth in the local treatment of glioblastoma: Temozolomide and rutin-loaded hybrid layered composite nanofiber. (PubMed, Asian J Pharm Sci)
This was evidenced by a decrease in the angiogenesis marker CD31, the absence of inflammation or necrosis in H&E staining of the cerebellum, increased production of IFN-γ, decreased levels of interleukin-4 in splenic T cells, and lower serum AST levels. Our findings collectively indicate that LHNTMZ +rutin is a promising biocompatible model for the local treatment of GB.
Journal • PARP Biomarker
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IFNG (Interferon, gamma) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • CD31 (Platelet and endothelial cell adhesion molecule 1) • IL4 (Interleukin 4) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
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temozolomide
16d
New trial
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temozolomide
17d
Hypoxia enhances IL-8 signaling through inhibiting miR-128-3p expression in glioblastomas. (PubMed, Biochim Biophys Acta Mol Cell Res)
Additionally, lower miR-128-3p levels existed in hypoxic GBM, leading to desensitizing temozolomide (TMZ)'s efficacy, a first-line therapeutic drug for GBM...Collectively, the HIF-1α/miR-128-3p/IL-8 signaling pathway plays a critical role in promoting the progression of hypoxic GBM. Targeting this signaling pathway holds promise as a potential therapeutic strategy.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • MIR128 (MicroRNA 128)
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CXCL8 elevation • HIF1A expression • CXCL8 expression • miR-128 expression
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temozolomide
17d
GRETeL: Tumor Response to Standard Radiotherapy and TMZ Patients With GBM (clinicaltrials.gov)
P=N/A, N=100, Suspended, Duke University | Recruiting --> Suspended
Trial suspension • Liquid biopsy • Biopsy
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temozolomide
18d
Unraveling molecular signatures and prognostic biomarkers in glioblastoma: a comprehensive study on treatment resistance and personalized strategies. (PubMed, Discov Oncol)
This study sheds light on the molecular intricacies governing GBM treatment response. The identified hub genes and the gene prognostic nomogram offer valuable tools for predicting patient outcomes and guiding personalized treatment strategies. These findings contribute to advancing our understanding of GBM biology and may pave the way for improved clinical management.
Journal
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IGFBP6 (Insulin Like Growth Factor Binding Protein 6)
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temozolomide
18d
Multiparametric MR-Guided High Dose Adaptive Radiotherapy With Concurrent Temozolomide in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P2, N=30, Recruiting, University of Michigan Rogel Cancer Center | Trial completion date: Nov 2024 --> Feb 2025 | Trial primary completion date: Nov 2024 --> Feb 2025
Trial completion date • Trial primary completion date
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temozolomide
18d
NAVIG-1: New Adjuvant Vaccine in Glioblastoma, a Phase 1/2a Study (clinicaltrials.gov)
P1/2, N=35, Recruiting, Assistance Publique - Hôpitaux de Paris | Not yet recruiting --> Recruiting
Enrollment open
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PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
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temozolomide
18d
Integrative Analysis Identifies NSUN2 as an Essential Coordinator for Glioma Malignancy and Glucose Metabolism. (PubMed, J Gene Med)
Our findings highlight NSUN2 as a critical regulator of glioma malignancy. Targeting NSUN2 disrupts key pathways in glioma progression, suggesting it as a promising therapeutic target. Our work underscores the potential of NSUN2 inhibition to enhance treatment efficacy and improve patient outcomes in glioma.
Journal
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EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1) • NSUN2 (NOP2/Sun RNA Methyltransferase 2)
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temozolomide
20d
Molecular Characterization and Clinical Relevance of MGMT-Silenced Pancreatic Cancer. (PubMed, Cancer Med)
MGMT silencing occurs in a small subgroup of PACs and is enriched in KRAS wild type cases, with a favorable prognostic impact. Our findings provide the rationale to explore combinations of alkylating with DNA damaging agents in MGMT-silenced PAC.
Journal
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS wild-type • RAS wild-type
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temozolomide
20d
Ginsenoside RK3 inhibits glioblastoma by modulating macrophage M2 polarization via the PPARG/CCL2 axis. (PubMed, Phytomedicine)
This study innovatively highlights the dual mechanism of ginsenoside RK3 in glioblastoma treatment: it impedes tumor progression by modulating the PPARG/CCL2 pathway and enhances the efficacy of temozolomide. Our research underscores the promising role of herbal medicine in the management of glioblastoma, paving the way for novel therapeutic strategies that integrate traditional approaches with conventional treatments.
Journal
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CCL2 (Chemokine (C-C motif) ligand 2) • PPARG (Peroxisome Proliferator Activated Receptor Gamma)
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temozolomide
20d
GlioVax: Efficiency of Vaccination with Lysate-loaded Dendritic Cells in Patients with Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P2, N=136, Active, not recruiting, Heinrich-Heine University, Duesseldorf | Recruiting --> Active, not recruiting | Trial primary completion date: Nov 2026 --> May 2027
Enrollment closed • Trial primary completion date
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MGMT (6-O-methylguanine-DNA methyltransferase)
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MGMT promoter methylation
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temozolomide
20d
UNITED2: UNITy-BasED MR-Linac Adaptive Simultaneous Integrated Hypofractionated Boost Trial for High Grade Glioma in the Elderly (clinicaltrials.gov)
P2, N=55, Recruiting, Sunnybrook Health Sciences Centre | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
Trial completion date • Trial primary completion date
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temozolomide
20d
NIVOGLIO: Nivolumab in Combination With Temozolomide and Radiotherapy in Children and Adolescents With Newly Diagnosed High-grade Glioma (clinicaltrials.gov)
P1/2, N=41, Completed, Gustave Roussy, Cancer Campus, Grand Paris | Recruiting --> Completed | Trial completion date: Jan 2024 --> Nov 2024 | Trial primary completion date: Jan 2023 --> Nov 2024
Trial completion • Trial completion date • Trial primary completion date • Combination therapy
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Opdivo (nivolumab) • temozolomide
20d
Trial completion • Combination therapy • Metastases
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Avastin (bevacizumab) • cisplatin • carboplatin • 5-fluorouracil • temozolomide • etoposide IV • irinotecan
23d
A detailed evaluation of the advantages among extracellular vesicles from three cell origins for targeting delivery of celastrol and treatment of glioblastoma. (PubMed, Int J Pharm)
Importantly, BMSC-EVs-Cel could effectively inhibit GBM growth, induce tumor tissue apoptosis and suppress intratumoral microvessel density in comparison with free Cel and temozolomide, while successfully decrease systemic toxicity. Overall, this study elucidates the properties of EVs derived from distinct cell origins and highlights the great potential of BMSC-EVs for brain tumor treatment.
Journal
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TSG101 (Tumor Susceptibility 101)
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temozolomide
24d
Design of Experiments to Tailor the Potential of BSA-Coated Peptide Nanocomplexes for Temozolomide/p53 Gene Co-Delivery. (PubMed, Pharmaceutics)
The reported findings instigate the development of future research to evaluate their potential utility to TMZ/p53 co-delivery. The DoE tool proved to be a powerful approach to explore and tailor the composition of BSA-coated TMZ-WRAP5/p53 complexes, which are expected to contribute to the progress toward a more efficient therapy against cancer and, more specifically, against glioblastoma.
Journal
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TP53 (Tumor protein P53)
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temozolomide
25d
Immunophenotypic Profile of Adult Glioblastoma IDH-Wildtype Microenvironment: A Cohort Study. (PubMed, Cancers (Basel))
All patients underwent surgery followed by temozolomide concurrent with and adjuvant to radiotherapy...The expression of PD-L1 in GBM IDH-wt patients is confined to a small subpopulation. While we found a significant association between low CD4+ lymphocyte density (≤10%) and survival, given the small numbers of our cohort, the prognostic value of CD4+ lymphocyte density will need to be validated in large-scale studies.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • MGMT (6-O-methylguanine-DNA methyltransferase) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD163 (CD163 Molecule) • CD4 (CD4 Molecule)
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PD-L1 expression • PD-1 expression
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temozolomide
25d
A Comparative Study of Methyl-BEAMing and Droplet Digital PCR for MGMT Gene Promoter Hypermethylation Detection. (PubMed, Diagnostics (Basel))
Background: O-6-methylguanine-DNA methyltransferase is responsible for the direct repair of O6-methylguanine lesions induced by alkylating agents, including temozolomide... Digital droplet PCR proved to be an efficient method for detecting gene promoter methylation. However, the Methyl-BEAMing method has proved more sensitive for detecting low quantities of DNA.
Journal • PD(L)-1 Biomarker • IO biomarker
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MGMT (6-O-methylguanine-DNA methyltransferase)
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MSI-H/dMMR
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temozolomide
25d
STARLITE for Unresectable High-Grade Gliomas (clinicaltrials.gov)
P1, N=24, Not yet recruiting, University of Miami | Trial completion date: May 2029 --> Mar 2030 | Initiation date: Nov 2024 --> Mar 2025 | Trial primary completion date: May 2028 --> Mar 2029
Trial completion date • Trial initiation date • Trial primary completion date
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temozolomide • ritonavir
26d
Novel Fibroblast Growth Factor Receptor 3-Fatty Acid Synthase Gene Fusion in Recurrent Epithelioid Glioblastoma Linked to Aggressive Clinical Progression. (PubMed, Curr Oncol)
Postoperative treatment included radiotherapy and temozolomide...The recurrence was managed with regorafenib and bevacizumab, though complications like hand-foot syndrome and radiation necrosis arose...The novel FGFR3-FASN fusion suggests potential implications for GBM recurrence and lipid metabolism. Further studies are warranted to explore FGFR3-FASN's role in GBM and its therapeutic targeting.
Journal
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PTEN (Phosphatase and tensin homolog) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • TERT (Telomerase Reverse Transcriptase) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • FASN (Fatty acid synthase)
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IDH2 mutation • PTEN deletion • PTEN mutation • CDKN2A deletion • CDKN2A mutation • TERT mutation • TERT promoter mutation
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Avastin (bevacizumab) • temozolomide • Stivarga (regorafenib)
26d
Flavored, Oral Irinotecan VAL-413 (Orotecan®) Given With Temozolomide for Treatment of Recurrent Pediatric Solid Tumors (clinicaltrials.gov)
P1, N=20, Recruiting, Valent Technologies, LLC | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Jun 2024 --> Jun 2025
Trial completion date • Trial primary completion date
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temozolomide
26d
Triapine in Combination with Temozolomide for the Treatment of Patients with Recurrent Glioblastoma (clinicaltrials.gov)
P1, N=30, Recruiting, Northwestern University | Active, not recruiting --> Recruiting
Enrollment open • Combination therapy
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temozolomide • Triapine (3-AP)