- |||||||||| 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.
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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
Trial completion date, Combination therapy, Metastases: 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) - Sep 26, 2023 P3, N=437, Active, not recruiting, Inhibition of RRM2 may be a promising therapeutic strategy for NF1-associated MPNST. Trial completion date: Jun 2024 --> Sep 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, Lutathera (lutetium Lu 177 dotatate) / Novartis
Trial initiation date, Metastases: 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, Combination therapy, Metastases: 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.
- |||||||||| Triapine (3-AP) / Vion, COTI-2 / Cotinga Pharma
The role of protein disulfide isomerase and copper in the paraptotic cell death of clinically investigated anticancer thiosemicarbazones (Section 14; Poster Board #12) - Mar 14, 2023 - Abstract #AACR2023AACR_7245; To further improve the anticancer activity of TSCs, novel derivatives (such as DpC and COTI-2) have been developed and clinically investigated for their activity against solid tumors...The formation of the complex results in the interaction with thiol-containing proteins and subsequently in the disruption of the thiol-redox homeostasis, which leads to paraptotic cell death. Overall this work shed light on the paraptotic cell death and will be of interest for future clinical development of anticancer TSCs, as paraptosis is hypothesized to overcome apoptosis-resistance of cancer cells.
- |||||||||| Triapine (3-AP) / Vion
Pharmacokinetics, bioavailability, and pharmacodynamics of oral triapine (Section 18; Poster Board #23) - Mar 14, 2023 - Abstract #AACR2023AACR_5026; Correlation of methemoglobin with exposure highlights the importance of optimizing triapine exposure. Additional data may support the exploration of a dose specific to current smokers.
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