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DRUG CLASS:

TERT inhibitor

12ms
Enrollment open
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • RZ-001 • Valcyte (valganciclovir)
1year
New P1/2 trial • Combination therapy
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • RZ-001 • Valcyte (valganciclovir)
1year
Expanded Access Program for GBM Subjects (clinicaltrials.gov)
P=N/A, N=0, Temporarily Not Available, Rznomics, Inc.
New trial • Combination therapy
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RZ-001 • Valcyte (valganciclovir)
1year
Enrollment closed • Combination therapy
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TERT (Telomerase Reverse Transcriptase)
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RZ-001 • Valcyte (valganciclovir)
over1year
Enrollment open • Combination therapy
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TERT (Telomerase Reverse Transcriptase) • IFNG (Interferon, gamma) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CD4 (CD4 Molecule) • IL10 (Interleukin 10)
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RZ-001 • Valcyte (valganciclovir)
2years
New P1/2 trial • Combination therapy
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TERT (Telomerase Reverse Transcriptase)
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RZ-001 • Valcyte (valganciclovir)
over2years
Short-Term TERT Inhibition Impairs Cellular Proliferation via a Telomere Length-Independent Mechanism and Can Be Exploited as a Potential Anticancer Approach. (PubMed, Cancers (Basel))
The combination of BIBR1532 with antineoplastic drugs (cyclophosphamide or fludarabine) significantly reduced xenografted cells' proliferation rate compared to monotherapy in the zebrafish xenograft model. Overall, these findings indicate that short-term inhibition of TERT impairs cell growth through the downregulation of MYC via NF-κB signalling and supports the use of TERT inhibitors in combination with antineoplastic drugs as an efficient anticancer strategy.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • TERT (Telomerase Reverse Transcriptase) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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BRAF wild-type
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cyclophosphamide • fludarabine IV • BIBR1532
3years
New P1/2 trial • Combination therapy
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TERT (Telomerase Reverse Transcriptase)
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RZ-001 • Valcyte (valganciclovir)
3years
Combined targeting of telomerase reverse transcriptase and metabolism abrogates glioblastoma proliferation in vivo (SNO 2022)
Collectively, our results indicate that simultaneously targeting TERT and ASCT2 provides a novel therapeutic opportunity for GBMs and that hyperpolarized [1-13C]-alanine serves as a companion agent for imaging early response to therapy. Our findings pave the way for precision therapy and response assessment for GBM patients.
Preclinical
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TERT (Telomerase Reverse Transcriptase) • SLC1A5 (Solute Carrier Family 1 Member 5)
4years
Enhanced immortalization, HUWE1 mutations and other biological drivers of breast invasive carcinoma in Black/African American patients. (PubMed, Gene)
Relative to Caucasian non-responders to endocrine therapy, B/AA non-responders show suppressed expression of a signature gene set on which biological processes including signaling by interleukins, circadian clock, regulation of lipid metabolism by PPARα, FOXO-mediated transcription, and regulation of TP53 degradation are over-represented. Thus, we identify molecular expression patterns suggesting diminished response to oxidative stress, changes in regulation of tumor suppressors/facilitators, and enhanced immortalization in B/AA patients are likely important in defining the more aggressive molecular tumor phenotype reported in B/AA patients.
Clinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PTEN (Phosphatase and tensin homolog) • RB1 (RB Transcriptional Corepressor 1) • TERT (Telomerase Reverse Transcriptase) • MIR221 (MicroRNA 221) • HUWE1 (HECT UBA And WWE Domain Containing E3 Ubiquitin Protein Ligase 1) • MIR135B (MicroRNA 135b) • E2F1 (E2F transcription factor 1) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
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TP53 mutation • PIK3CA mutation • PTEN mutation • MYC expression • PTEN expression • HUWE1 mutation • miR-135-b expression
over4years
Long noncoding RNA SNHG1 promotes TERT expression by sponging miR-18b-5p in breast cancer. (PubMed, Cell Biosci)
Our results provide a comprehensive understanding of the oncogenic mechanism of lncRNA SNHG1 in breast cancer. Importantly, we identified a novel E2F1-SNHG1-miR-18b-5p-TERT axis, which may be a potential therapeutic target for breast cancer. Our results also provided a potential treatment for breast cancer when knockdown SNHG1 and TERT inhibitor administration simultaneously.
Journal
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TERT (Telomerase Reverse Transcriptase) • E2F1 (E2F transcription factor 1)