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A technology of evsomide and its purpose, applied in the field of efsomide, can solve the problem of inability to effectively target tumors for a long time
Pending Publication Date: 2020-03-20
SHENZHEN ASCENTAWITS PHARM TECH CO LTD
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[0010] The above researches have triggered the development of the compound as a targeted anti-cancer drug by international pharmaceutical giants. After Merck purchased TH-302-related research projects from Threshold Pharmaceuticals, it conducted phase III clinical trials of the anti-tumor drug TH-302. The trial was to investigate the drug's therapeutic effect on soft tissue sarcoma and pancreatic cancer. However, in 2015, Merck announced the failure of the trial. Threshold Pharmaceuticals stated that the failure of the TH-302 clinical trial showed that the drug could not effectively target tumors for a long time and became A stable anticancer drug
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[0272] Cell Proliferation Experiment
[0273] Exponentially growing cells were seeded with different concentrations of TH-302 24 hours after inoculation. After drug addition, the plates were incubated at 37°C for 2 hours in an anaerobic chamber (Bactron II), hypoxic chamber (Hypoxystation) or standard tissue culture incubator. After washing, cells were cultured in normoxic complete medium for 72 hours. Viable cells were quantified using AlamarBlue. 50% growth inhibition (IC50) was calculated using Prism software.
[0274] In vitro clonogenic assay
[0275] Cells were seeded 24 hours before starting treatment. Cells were then incubated with drugs for 2 hours at defined oxygen concentrations. At the end of treatment, the washed cells were plated and placed in an incubator for 10 days. For VC-8, UWB1.289 and FANCA strains, cells were plated in triplicate in 6-well plastic plates with 500 to 1,000 cells per well and processed. TH-302 was cultured under hypoxic conditions fo...
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Abstract
Evofosfamide (TH-302) or an analog thereof has a specific inhibitory effect on a cell having a specific gene mutation, in particular on a DNA repair-damaged cell. The cell or tissue has at least one or more gene mutations in BRCA1, BRCA2, FANCD1, FANCD2, ATM, ATR, CHEK1, CHEK2, CTP, BARD1, BRIP1, PALB2, RAD51D, RAD51C, RAD52, RAD54, RAD55, RAD57, FAM175, NBN, Rad50, MER11, p53, NBS1, XRS2, XRCC2,XRCC3, ERCC1, ERCC2, ERCC3, ERCC4, XRCC1, Ku80, MHS6, MGMT, PARP, and ERCC5. For this, a medical use of evofosfamide (TH-302) or an analog thereof in treating tumors or cancer in a cancer patient having the specific gene mutation(s) is provided.
Description
technical field [0001] The present invention relates to efsolamide, especially the treatment of efsolamide to the cancer or tumor of patients with specific gene mutation. Background technique [0002] TH-302 (Evofosfamide, cas number 918633-87-1) is a 2-nitroimidazole-triggered hypoxia-activated prodrug (HAP) bromoifosfamide. Under hypoxic conditions, the inactive TH-302 prodrug can release highly toxic Br-IPM (shown in Structural Formula 1 below). TH-302 has broad-spectrum biological activity in vivo and in vitro, specific hypoxia selective activation activity, induction of H2AX phosphorylation and DNA cross-linking activity, resulting in cell cycle arrest, so this compound has been developed by many pharmaceutical companies and scientific research institutes Development of anticancer drugs. [0003] [0004] However, in the past, when researchers screened the anticancer activity of TH-302, they often used the principle of hypoxia activation in structural formula 1 to ...
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