- |||||||||| temozolomide / Generic mfg.
RRM2-driven dNTP biosynthesis: a therapeutic vulnerability in temozolomide-resistant glioblastoma (Section 23; Poster Board No: 2) - Mar 25, 2025 - Abstract #AACR2025AACR_6803; These findings underscore the potential of targeting RRM2-mediated dNTP biosynthesis to overcome chemoresistance in GBM. We are conducting a Phase 1/1b clinical trial to assess the safety, toxicity, and maximum tolerated dose (MTD) of combining 3-AP with TMZ in recurrent GBM patients.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial completion date, Trial primary completion date: Testing the Effectiveness of an Anti-cancer Drug, Triapine, When Used With Targeted Radiation-based Treatment (Lutetium Lu 177 Dotatate), Compared to Lutetium Lu 177 Dotatate Alone for Metastatic Neuroendocrine Tumors (clinicaltrials.gov) - Mar 18, 2025 P2, N=94, Recruiting, We are conducting a Phase 1/1b clinical trial to assess the safety, toxicity, and maximum tolerated dose (MTD) of combining 3-AP with TMZ in recurrent GBM patients. Trial completion date: Mar 2025 --> Sep 2025 | Trial primary completion date: Mar 2025 --> Sep 2025
- |||||||||| Triapine (3-AP) / Vion, Northwestern University, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial completion date, Trial primary completion date: ETCTN 10388: Testing the Addition of an Anti-cancer Drug, Triapine, to the Usual Radiation-Based Treatment (Lutetium Lu 177 Dotatate) for Neuroendocrine Tumors (clinicaltrials.gov) - Mar 18, 2025 P1, N=33, Active, not recruiting, Trial completion date: Mar 2025 --> Sep 2025 | Trial primary completion date: Mar 2025 --> Sep 2025 Trial completion date: Mar 2025 --> Mar 2026 | Trial primary completion date: Mar 2025 --> Sep 2024
- |||||||||| Triapine (3-AP) / Vion, Northwestern University
Journal: Study on the effects and mechanism of RRM2 on three gynecological malignancies. (Pubmed Central) - Feb 24, 2025 These pro-tumorigenic effects may then be mediated through the involvement of RRM2 in the p53 and Akt/mTOR signaling pathways, altering the expression of p53 and Akt/mTOR. Thus, RRM2 is potentially a candidate gene for the unified diagnosis of cervical, endometrial, and ovarian cancers.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University
Journal, IO biomarker: Opposing effects of mycotoxins alternariol and deoxynivalenol on the immunomodulatory effects of oxaliplatin and triapine. (Pubmed Central) - Feb 12, 2025 While AOH generally suppressed a drug-induced activation and increased anti-inflammatory IL10 levels, DON potentiated activation and pro-inflammatory markers, such as CXCL8 and TNF in immune cells. In conclusion, AOH and DON have the potential to alter the immunological effects of anticancer therapies, which should be considered during therapy as well as in their future risk assessment.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University
Journal: DefNEtTrp: An Iron Dual Chelator Approach for Anticancer Application. (Pubmed Central) - Dec 30, 2024 In conclusion, AOH and DON have the potential to alter the immunological effects of anticancer therapies, which should be considered during therapy as well as in their future risk assessment. Two important chelators, deferasirox (Def) and triapine (Trp), attack the intracellular supply of iron (Fe) and inhibit Fe-dependent pathways responsible for cellular proliferation and metastasis...Its cytotoxicity (IC50 0.77
- |||||||||| Lutathera (lutetium Lu 177 dotatate) / Novartis
Enhancing [177Lu]Lu-DOTA-TATE therapeutic efficacy in vitro by combining it with chemotherapy (Hall Y4-Y9) - Sep 27, 2024 - Abstract #EANM2024EANM_490; Hydroxyurea, gemcitabine and triapine all increased cell size, SSTR2A expression, and [177Lu]Lu-DOTA-TATE uptake, whilst further reducing cell metabolic viability in U2OS+SSTR2A cells when compared to [177Lu]Lu-DOTA-TATE monotherapy. Further investigations could transform patient care and positively increase outcomes for patients treated with [177Lu] Lu-DOTA-TATE.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial completion date, Trial primary completion date: ETCTN 10388: Testing the Addition of an Anti-cancer Drug, Triapine, to the Usual Radiation-Based Treatment (Lutetium Lu 177 Dotatate) for Neuroendocrine Tumors (clinicaltrials.gov) - Jun 12, 2024 P1, N=29, Active, not recruiting, Both ligands down-regulated multiple key receptors that display inter-receptor cooperation that leads to aggressive and resistant breast cancer. Trial completion date: Jun 2024 --> Dec 2024 | Trial primary completion date: Jun 2024 --> Dec 2024
- |||||||||| Triapine (3-AP) / Vion
FDA event, Journal: Identification of several African swine fever virus replication inhibitors by screening of a library of FDA-approved drugs. (Pubmed Central) - Mar 13, 2024 Furthermore, molecular docking studies showed that triapine might interact with the active center Fe2+ in the small subunit of ASFV ribonucleotide reductase while cytarabine hydrochloride metabolite might interact with three residues (Arg589, Lys593, and Lys631) of ASFV DNA polymerase to block new DNA chain extension. Taken together, our results suggest that triapine and cytarabine hydrochloride displayed significant antiviral activity against ASFV in vitro.
- |||||||||| Triapine (3-AP) / Vion
Covalent conjugation of the deferasirox and triapine iron chelators to exploit dual chelation in anticancer therapy (In-person; Room 212 (Ernest N. Morial Convention Center)) - Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_12002; As seen in Jurkat cell viability experiments, the cytotoxicity of DefNEtTrp is superior to that of unconjugated Def and Trp ligands in single-drug and combination drug treatments, and is assessed in the context of intracellular labile Fe binding. Preliminary studies will also be presented for the Ti(IV)(DefNEtTrp) 2 complex, which appears to retain the cancer selectivity and promising potency of the free ligand.
- |||||||||| Triapine (3-AP) / Vion
Dual chelator conjugates express enhanced eelectivity than non-conjugated chelators | Poster Board #437 (In-person; Poster Board #437; Hall C (Ernest N. Morial Convention Center)) - Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_1246; The use of two iron binding compounds, deferasirox (def) and triapine (trp), are known to coordinate with intracellular iron (Fe) to inhibit the development cells, which depend on Fe to proliferate and is known to fuel cancer...MRC-5 treated cells present GI 50 /IC 50 and TGI values significantly greater than MDA-MB-468, indicating how DefNEtTrp is much more selective towards cancer cells. This development will increase the availability of a novel design of chemotherapeutics for widespread patient access and to overcome the limitations of present TNBC and NSCLC therapies.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial completion date, Trial primary completion date: ETCTN 10388: Testing the Addition of an Anti-cancer Drug, Triapine, to the Usual Radiation-Based Treatment (Lutetium Lu 177 Dotatate) for Neuroendocrine Tumors (clinicaltrials.gov) - Mar 2, 2024 P1, N=29, Active, not recruiting, This development will increase the availability of a novel design of chemotherapeutics for widespread patient access and to overcome the limitations of present TNBC and NSCLC therapies. Trial completion date: Jan 2024 --> Jun 2024 | Trial primary completion date: Jan 2024 --> Jun 2024
- |||||||||| Triapine (3-AP) / Vion, rabusertib (LY 2603618) / Eli Lilly
Journal, Combination therapy, Synthetic lethality: Inhibition of RRM2 radiosensitizes glioblastoma and uncovers synthetic lethality in combination with targeting CHK1. (Pubmed Central) - Aug 14, 2023 Collectively, our results suggest RRM2 is a promising therapeutic target for GBM, and targeting RRM2 with triapine sensitizes GBM cells to radiation and independently induces synthetic lethality of GBM cells with CHK1 inhibition. Our findings suggest combining triapine with radiation or rabusertib may improve therapeutic outcomes in GBM.
- |||||||||| Triapine (3-AP) / Vion
Journal: Human serum albumin as a copper source for anticancer thiosemicarbazones. (Pubmed Central) - Jul 28, 2023 Noteworthy, Fe-chelation from transferrin was not overserved, even not for Triapine. In summary, the labile Cu pool of HSA is a potential source for Cu-TSC complex formation and, consequently, distinctly influences the anticancer activity and pharmacological behavior of TSCs.
- |||||||||| Triapine (3-AP) / Vion, Northwestern University, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial initiation date: Testing the Effectiveness of an Anti-cancer Drug, Triapine, When Used With Targeted Radiation-based Treatment (Lutetium Lu 177 Dotatate), Compared to Lutetium Lu 177 Dotatate Alone for Metastatic Neuroendocrine Tumors (clinicaltrials.gov) - Jul 14, 2023 P2, N=94, Recruiting, In summary, the labile Cu pool of HSA is a potential source for Cu-TSC complex formation and, consequently, distinctly influences the anticancer activity and pharmacological behavior of TSCs. Initiation date: Mar 2023 --> Sep 2023
- |||||||||| Triapine (3-AP) / Vion, Northwestern University
Trial completion date, Trial primary completion date: NRG-GY006: Testing the Addition of a New Anti-Cancer Drug, Triapine, to the Usual Chemotherapy Treatment (Cisplatin) During Radiation Therapy for Advanced-stage Cervical and Vaginal Cancers (clinicaltrials.gov) - Jun 26, 2023 P3, N=437, Active, not recruiting, Suspended --> Active, not recruiting Trial completion date: Jul 2023 --> Jun 2024 | Trial primary completion date: Jul 2023 --> Jan 2023
- |||||||||| Triapine (3-AP) / Vion, VE-821 / EMD Serono, Vertex, didox (NSC-324360) / Molecules for Health
Journal: Synergistic anticancer activity of combined ATR and ribonucleotide reductase inhibition in Ewing's sarcoma cells. (Pubmed Central) - Apr 25, 2023 Clinical trial information: NCT02466971. Our study reveals that combined targeting of ATR and RNR was effective against Ewing's sarcoma in vitro and thus rationalises an in vivo exploration into the potential of combining ATR and RNR inhibitors as a new strategy for the treatment of this challenging disease.
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