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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
Effect of radiochemotherapy on peripheral immune response in glioblastoma. (PubMed, Cancer Immunol Immunother)
Overall, these findings shed light on the peripheral immune landscape in GBM, emphasizing the immunosuppressive effects of treatment. Baseline immune parameters may serve as prognostic indicators for treatment response.
Journal • IO biomarker
|
CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
|
temozolomide
4d
Lapatinib With Temozolomide and Regional Radiation Therapy for Patients With Newly-Diagnosed Glioblastoma Multiforme (clinicaltrials.gov)
P2, N=50, Completed, Jonsson Comprehensive Cancer Center | Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> May 2024
Trial completion • Trial completion date • Combination therapy
|
temozolomide • lapatinib
4d
INO-5401 and INO-9012 Delivered by Electroporation (EP) in Combination With Cemiplimab (REGN2810) in Newly-Diagnosed Glioblastoma (GBM) (clinicaltrials.gov)
P1/2, N=52, Active, not recruiting, Inovio Pharmaceuticals | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Dec 2024
Trial completion date • Trial primary completion date • Combination therapy
|
temozolomide • Libtayo (cemiplimab-rwlc) • INO-5401 • rocakinogene sifuplasmid (INO-9012)
4d
BGB-A317-290-LTE1: Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (clinicaltrials.gov)
P3, N=300, Enrolling by invitation, BeiGene | Trial completion date: Aug 2024 --> Dec 2026 | Trial primary completion date: Aug 2024 --> Dec 2026
Trial completion date • Trial primary completion date • Metastases
|
temozolomide • Lenvima (lenvatinib) • Tevimbra (tislelizumab) • Fruzaqla (fruquintinib) • Partruvix (pamiparib) • zanidatamab (ZW25) • Avzivi (bevacizumab-tnjn) • ociperlimab (BGB-A1217) • sitravatinib (MGCD516) • BGB-15025 • BGB-A445 • LBL-007 • surzebiclimab (BGB-A425)
4d
VERITAS: Evaluation of 2 Intensification Treatment Strategies for Neuroblastoma Patients With a Poor Response to Induction (clinicaltrials.gov)
P2, N=34, Terminated, Gustave Roussy, Cancer Campus, Grand Paris | Trial completion date: Aug 2023 --> Mar 2024
Trial completion date • Metastases
|
temozolomide • irinotecan • topotecan • thiotepa
4d
9-ING-41 in Pediatric Patients With Refractory Malignancies. (clinicaltrials.gov)
P1, N=68, Recruiting, Actuate Therapeutics Inc. | Active, not recruiting --> Recruiting
Enrollment open
|
AFP (Alpha-fetoprotein)
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temozolomide • cyclophosphamide • irinotecan • topotecan • elraglusib (9-ING-41)
5d
GlioVax: Efficiency of Vaccination With Lysate-loaded Dendritic Cells in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P2, N=136, Recruiting, Heinrich-Heine University, Duesseldorf | Trial completion date: Jun 2025 --> Mar 2027 | Trial primary completion date: Sep 2024 --> Nov 2026
Trial completion date • Trial primary completion date
|
MGMT (6-O-methylguanine-DNA methyltransferase)
|
MGMT promoter methylation • IDH wild-type
|
temozolomide
5d
New P2 trial • Combination therapy
|
temozolomide • Verzenio (abemaciclib)
5d
Pilot Study of Mirtazapine for the Dual Tx of Depression and CINV in High-Grade Glioma Pts on TMZ (clinicaltrials.gov)
P2, N=120, Active, not recruiting, University of California, Irvine | Recruiting --> Active, not recruiting
Enrollment closed
|
temozolomide
5d
BEACON: Activity Study of Bevacizumab With Temozolomide ± Irinotecan for Neuroblastoma in Children (clinicaltrials.gov)
P2, N=225, Active, not recruiting, University of Birmingham | Phase classification: P2b --> P2 | Trial completion date: Dec 2026 --> Feb 2026
Phase classification • Trial completion date
|
Avastin (bevacizumab) • temozolomide • cyclophosphamide • irinotecan • topotecan • Qarziba (dinutuximab beta)
5d
PPAR-γ agonists reactivate the ALDOC-NR2F1 axis to enhance sensitivity to temozolomide and suppress glioblastoma progression. (PubMed, Cell Commun Signal)
The relationship and function of the ALDOC-PPAR-γ axis could serve as a potential prognostic indicator. Furthermore, PPAR-γ agonists offer a new treatment alternative for glioblastoma multiforme (GBM).
Journal
|
NR2F1 (Nuclear Receptor Subfamily 2 Group F Member 1) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
|
temozolomide
6d
New P1 trial • Combination therapy
|
temozolomide • Triapine (3-AP)
6d
Trial completion date • Combination therapy
|
MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1)
|
SMARCB1 mutation • IDH wild-type
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temozolomide • Kisqali (ribociclib) • topotecan
7d
Effects of Apatinib combined with Temozolomide on levels of sPD-1 and sPD-L1 in patients with drug-resistant recurrent glioblastoma. (PubMed, Clinics (Sao Paulo))
Apatinib combined with TMZ is safe and effective in the treatment of recurrent GB. The combined application of the two can reduce the levels of sPD-1 and sPD-L1, which has important clinical application value.
Journal
|
PD-1 (Programmed cell death 1)
|
temozolomide • AiTan (rivoceranib)
7d
Evaluation of a Combinatorial Immunotherapy Regimen That Can Cure Mice Bearing MYCN-Driven High-Risk Neuroblastoma That Resists Current Clinical Therapy. (PubMed, J Clin Med)
First, we demonstrate that 9464D-GD2 is nonresponsive to a preferred salvage regimen: anti-GD2 with temozolomide and irinotecan. Second, we have previously shown that adding agonist anti-CD40 mAb and CpG to a regimen of radiotherapy, anti-GD2/IL2 immunocytokine and anti-CTLA-4, cured a substantial fraction of mice bearing small 9464D-GD2 tumors; here, we further characterize this regimen by showing that radiotherapy and hu14.18-IL2 are necessary components, while anti-CTLA-4, anti-CD40, or CpG can individually be removed, and CpG and anti-CTLA-4 can be removed together, while maintaining efficacy. We have developed and characterized a regimen that can cure mice of a high-risk neuroblastoma that is refractory to the current clinical regimen for relapsed/refractory disease. Ongoing preclinical work is directed towards ways to potentially translate these findings to a regimen appropriate for clinical testing.
Preclinical • Journal
|
MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • IL2 (Interleukin 2)
|
MYCN amplification
|
temozolomide • irinotecan • lorukafusp alfa (APN301)
7d
Opaganib Downregulates N-Myc Expression and Suppresses In Vitro and In Vivo Growth of Neuroblastoma Cells. (PubMed, Cancers (Basel))
Amplified MYCN does not confer resistance to opaganib, and, in fact, the drug attenuates the expression of both c-Myc and N-Myc. The safety of opaganib has been established in clinical trials with adults with advanced cancer or severe COVID-19, and so opaganib has excellent potential for treating patients with NB, particularly in combination with temozolomide and irinotecan or anti-CTLA-4 antibody.
Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
|
MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
|
MYC expression
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temozolomide • irinotecan • Yeliva (opaganib)
7d
Pentraxin 3: A Main Driver of Inflammation and Immune System Dysfunction in the Tumor Microenvironment of Glioblastoma. (PubMed, Cancers (Basel))
The death rate for patients with GB remains high, occurring within a few months after diagnosis, even with the gold-standard therapies now available, such as surgery, radiation, or a pharmaceutical approach with Temozolomide...In several tumoral subtypes, via regulating complement-dependent and macrophage-associated tumor-promoting inflammation, it has been demonstrated that PTX3 may function as a promoter of cancer metastasis, invasion, and stemness. Our review aims to deeply evaluate the function of PTX3 in the pathological context of GB, considering its pivotal biological activities and its possible role as a molecular target for future therapies.
Review • Journal
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CRP (C-reactive protein)
|
temozolomide
9d
Targeting NKG2D ligands in glioblastoma with a bispecific T-cell engager is augmented with conventional therapy and enhances oncolytic virotherapy of glioma stem-like cells. (PubMed, J Immunother Cancer)
We propose a potential model for targeting GSCs in heterogeneous tumors, whereby differentiated GBM cells infected with G207-NKG2D BiTE produce NKG2D BiTE locally, directing T-cell cytotoxicity towards the GSC subpopulations in the tumor microenvironment.
Journal • Oncolytic virus
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NKG2D (killer cell lectin like receptor K1)
|
temozolomide
9d
Muscone restores anoikis sensitivity in TMZ-resistant glioblastoma cells by suppressing TOP2A via the EGFR/Integrin β1/FAK signaling pathway. (PubMed, Phytomedicine)
We first demonstrated that muscone suppressed TOP2A expression through the EGFR/Integrin β1/FAK pathway, hence restoring anoikis sensitivity in TMZ-resistant GBM cells. These data suggest that muscone may be a promising co-therapeutic agent for enhancing GBM treatment, particularly in cases of TMZ-resistant GBM with elevated TOP2A expression.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • CCNE1 (Cyclin E1) • TOP2A (DNA topoisomerase 2-alpha) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CDK2 (Cyclin-dependent kinase 2) • CASP9 (Caspase 9) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • ANXA5 (Annexin A5)
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EGFR overexpression • MGMT expression • TOP2A expression
|
temozolomide
10d
Diethyldithiocarbamate-ferrous oxide nanoparticles inhibit human and mouse glioblastoma stemness: aldehyde dehydrogenase 1A1 suppression and ferroptosis induction. (PubMed, Front Pharmacol)
DE-FeO NPs also revealed a higher inhibitory impact than standard chemotherapy (temozolomide, TMZ) on self-renewal, cancer repopulation, chemoresistance, and radioresistance potentials...This in vitro novel study declared the potency of DE-FeO NPs for collapsing GSCs and GSCs-RR with improving their sensitivity to chemotherapy and radiotherapy, indicating that DE-FeO NPs may be a promising remedy for GBM. Glioma animal models will be needed for in-depth studies on its safe effectiveness.
Preclinical • Journal
|
CTNNB1 (Catenin (cadherin-associated protein), beta 1) • GPX4 (Glutathione Peroxidase 4) • ALDH1A1 (Aldehyde Dehydrogenase 1 Family Member A1)
|
temozolomide
10d
Understanding the immunosuppressive microenvironment of glioma: mechanistic insights and clinical perspectives. (PubMed, J Hematol Oncol)
Despite the established treatment regimen comprising surgical intervention, radiotherapy, temozolomide administration, and the exploration of emerging modalities such as immunotherapy and integration of medicine and engineering technology therapy, the efficacy of these approaches remains constrained, resulting in suboptimal prognostic outcomes...Additionally, the review comprehensively surveys ongoing clinical trials and potential treatment strategies, envisioning a future where targeting MDSCs could reshape the immune landscape of GBM. Through the synergistic integration of immunotherapy with other therapeutic modalities, this approach can establish a multidisciplinary, multi-target paradigm, ultimately improving the prognosis and quality of life in patients with GBM.
Review • Journal
|
PTPRC (Protein Tyrosine Phosphatase Receptor Type C)
|
temozolomide
10d
Selinexor (KPT-330) in Combination With Temozolomide and Radiation Therapy in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P1, N=6, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting | N=24 --> 6 | Trial primary completion date: Aug 2025 --> Sep 2023
Enrollment closed • Enrollment change • Trial primary completion date • Combination therapy
|
temozolomide • Xpovio (selinexor)
10d
Phase 1 Study of Ibrutinib and Immuno-Chemotherapy Using Temozolomide, Etoposide, Doxil, Dexamethasone, Ibrutinib,Rituximab (TEDDI-R) in Primary CNS Lymphoma (clinicaltrials.gov)
P1, N=93, Recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2024 --> Jun 2027 | Trial primary completion date: Jun 2024 --> Jun 2025
Trial completion date • Trial primary completion date
|
Imbruvica (ibrutinib) • Rituxan (rituximab) • temozolomide • cytarabine • etoposide IV • pegylated liposomal doxorubicin • dexamethasone
10d
Temozolomide Resistance Mechanisms: Unveiling the role of Translesion DNA Polymerase Kappa in Glioblastoma Spheroids in vitro. (PubMed, Biosci Rep)
Collectively, the results suggest that TLS Polκ plays a vital role in the survival, cell death, genotoxicity, and metastatic potential of GBM spheroids in vitro when subjected to TMZ treatment. While the precise mechanisms underpinning this resistance remain elusive, TLS Polκ emerges as a potential therapeutic target for GBM patients.
Preclinical • Journal
|
CASP3 (Caspase 3) • CASP7 (Caspase 7) • TP53BP1 (Tumor Protein P53 Binding Protein 1) • POLK (DNA Polymerase Kappa)
|
temozolomide
11d
BETTER 2: Two Chemotherapy Regimens Plus or Minus Bevacizumab (clinicaltrials.gov)
P2, N=140, Active, not recruiting, Gustave Roussy, Cancer Campus, Grand Paris | Recruiting --> Active, not recruiting
Enrollment closed
|
Avastin (bevacizumab) • temozolomide • capecitabine • Zanosar (streptozocin)
11d
PERGOLA: Pembrolizumab for Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P2, N=56, Active, not recruiting, University of Zurich | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Feb 2024 --> Apr 2026
Trial completion date • Trial primary completion date
|
Keytruda (pembrolizumab) • temozolomide
11d
OU-SCC-Oblato-001: OKN-007 in Combination With Adjuvant Temozolomide Chemoradiotherapy for Newly Diagnosed Glioblastoma (clinicaltrials.gov)
P1, N=27, Active, not recruiting, University of Oklahoma | Trial completion date: Nov 2025 --> Nov 2026 | Trial primary completion date: Apr 2024 --> Apr 2025
Trial completion date • Trial primary completion date • Combination therapy
|
temozolomide • disufenton sodium (OKN-007)
11d
MEK inhibition enhances the antitumor effect of radiation therapy in NF1-deficient glioblastoma. (PubMed, Mol Cancer Ther)
No neurosphere lines exhibited enhanced sensitivity to temozolomide combined with mirdametinib. In sensitive models, benefits were observed at least three weeks beyond the completion of treatment, including sustained phosphor-ERK inhibition on immunoblot and decreased Ki-67 expression. These observations demonstrate synergistic activity between mirdametinib and irradiation in NF1-deficient glioma models and may have clinical implications for patients with gliomas that harbor germline or somatic NF1 alterations.
Journal
|
NF1 (Neurofibromin 1) • RAD51 (RAD51 Homolog A)
|
temozolomide • mirdametinib (PD-0325901)
12d
Glioblastoma stem cells deliver ABCB4 transcribed by ATF3 via exosomes conferring glioblastoma resistance to temozolomide. (PubMed, Cell Death Dis)
This mechanism may lead to drug resistance and recurrence of GBM. These findings contribute to a deeper understanding of the mechanisms underlying drug resistance in GBM and provide novel insights into its treatment.
Journal
|
ABCB4 (ATP Binding Cassette Subfamily B Member 4) • ATF3 (Activating Transcription Factor 3)
|
temozolomide
13d
PAZOGLIO: Phase I/II Study of Pazopanib+ Temozolomide in Patients With Newly Diagnosed Glioblastoma Multiforme (clinicaltrials.gov)
P1/2, N=51, Recruiting, Centre Antoine Lacassagne | Trial primary completion date: Aug 2025 --> Feb 2027
Trial primary completion date • Combination therapy • Surgery
|
temozolomide • Votrient (pazopanib)
13d
Enrollment closed • Combination therapy
|
temozolomide • Verzenio (abemaciclib) • irinotecan • Unituxin (dinutuximab)
15d
Gedunin modulates cellular growth and apoptosis in glioblastoma cell lines. (PubMed, Cancer Rep (Hoboken))
Our data provide in vitro support for the anticancer activity of gedunin in glioma cells by downregulating cancer survival proteins.
Preclinical • Journal • PARP Biomarker
|
EGFR (Epidermal growth factor receptor) • mTOR (Mechanistic target of rapamycin kinase) • BCL2L1 (BCL2-like 1)
|
temozolomide
16d
Trial initiation date • Metastases
|
temozolomide • SurVaxM (SVN53-67/M57-KLH peptide vaccine) • Leukine (sargramostim)
16d
Phase III Trial of Extended Temozolomide in Newly Diagnosed Glioblastoma (ACTRN12618001944224)
P3, N=315, Completed, The Walter and Eliza Hall Institute of Medical Research | Active, not recruiting --> Completed
Trial completion
|
temozolomide
17d
Enrollment open • Metastases
|
Mekinist (trametinib) • temozolomide • dacarbazine • naporafenib (ERAS-254)
17d
New P1 trial
|
IL6 (Interleukin 6)
|
temozolomide
17d
A Study of the Drugs Talazoparib and Temozolomide in Prostate Cancer (clinicaltrials.gov)
P1/2, N=16, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=44 --> 16
Enrollment closed • Enrollment change • Metastases
|
temozolomide • Talzenna (talazoparib)
17d
Pan-cancer analysis of prognostic and immunological role of IL4I1 in human tumors: a bulk omics research and single cell sequencing validation. (PubMed, Discov Oncol)
IL4I1 may play a role as promoter of cancer and prognostic indicator in patients. High expression of IL4I1 is associated with the state of tumor immunosuppression and may contribute to tumor-associated macrophage invasion. Therefore, IL4I1 may be a new therapeutic target for the treatment and prognosis of patients with cancer.
Journal • Pan tumor
|
IL4 (Interleukin 4) • IL4I1 (Interleukin 4 Induced 1)
|
docetaxel • temozolomide • BMS-754807
18d
FIORELLA: Study on Tailored Treatment in Elderly Patients With Newly Diagnosed Primary Lymphoma of Central Nervous System (clinicaltrials.gov)
P2, N=208, Recruiting, International Extranodal Lymphoma Study Group (IELSG) | Trial completion date: Oct 2023 --> Dec 2024 | Trial primary completion date: Oct 2023 --> Dec 2024
Trial completion date • Trial primary completion date
|
CD20 (Membrane Spanning 4-Domains A1)
|
Rituxan (rituximab) • lenalidomide • temozolomide • Matulane (procarbazine hydrochloride)
18d
Characterization of macrophages in head and neck squamous cell carcinoma and development of MRG-based risk signature. (PubMed, Sci Rep)
Finally, drugs with high sensitivity to HNSCC (such as 5-Fluorouracil, Temozolomide, Carmustine, and EPZ5676) were explored and analyze the malignant characteristics of HNSCC. Malignant features associated with HNSCC include angiogenesis, EMT, and the cell cycle. This study has opened up new prospects for the prognosis, prediction, and clinical treatment strategy of HNSCC.
Journal • IO biomarker
|
TGM2 (Transglutaminase 2) • AQP1 (Aquaporin 1) • MAP3K8 (Mitogen-Activated Protein Kinase Kinase Kinase 8) • ITGA5 (Integrin Subunit Alpha 5) • PIK3R3 (Phosphoinositide-3-Kinase Regulatory Subunit 3) • STC1 (Stanniocalcin 1)
|
5-fluorouracil • temozolomide • carmustine • pinometostat (EPZ-5676)
19d
Enrollment open • Surgery
|
ALK (Anaplastic lymphoma kinase) • TERT (Telomerase Reverse Transcriptase) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
|
cisplatin • carboplatin • temozolomide • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • irinotecan • vincristine • daunorubicin • topotecan • melphalan • thiotepa • Qarziba (dinutuximab beta) • Unituxin (dinutuximab) • dexrazoxane
20d
IGF2BP2 modulates autophagy and serves as a prognostic marker in glioma. (PubMed, Ibrain)
Additionally, our analysis suggested a link between IGF2BP2 expression and drug-resistant markers in TCGA-LGG samples, and Cell Counting Kit-8 cell viability assay revealed that knockdown of IGF2BP2 sensitized cells to temozolomide treatment. This comprehensive exploration unveils the role of IGF2BP2 in glioma progression, shedding light on autophagy modulation and chemosensitization strategies for glioma therapy.
Journal
|
IGF2 (Insulin-like growth factor 2) • IGF2BP2 (Insulin Like Growth Factor 2 MRNA Binding Protein 2)
|
IGF2 elevation
|
temozolomide