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tirapazamine (SR 4233)

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has high toxicity for hypoxic mammalian cells; structure given in first source

Also Known As:

SR 4233; 3-amino-1,2,4-benzothiadi- azine 1,1-dioxide; 3-amino-1,2,4-benzotriazine-1,4-dioxide; NSC 130181; SR-4233; Tirazone; WIN 59075; WIN-59075; 1,2,4-Benzotriazin-3-amine, 1,4-dioxide

Networked: 260 relevant articles (29 outcomes, 81 trials/studies)

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Bio-Agent Context: Research Results

Heterocyclic Compounds: 60
- 1-Ring Heterocyclic Compounds
  - Triazines: 37
    - tirapazamine: 260

Experts

1.	Wilson, William R: 19 articles (10/2015 - 01/2003)
2.	Hay, Michael P: 14 articles (03/2012 - 01/2003)
3.	Denny, William A: 13 articles (10/2010 - 01/2003)
4.	Pruijn, Frederik B: 12 articles (05/2014 - 01/2003)
5.	Hicks, Kevin O: 11 articles (01/2013 - 09/2003)
6.	Rischin, Danny: 10 articles (10/2015 - 01/2005)
7.	Gates, Kent S: 9 articles (08/2014 - 09/2002)
8.	Yang, Bo: 7 articles (03/2014 - 04/2003)
9.	Fisher, Richard: 7 articles (02/2014 - 01/2005)
10.	Brown, J Martin: 7 articles (10/2010 - 09/2002)

Related Diseases

1.	Neoplasms (Cancer) 01/01/1994 - "The radiation enhancement was significantly greater, however, for SR 4233 for two of the tumors with comparable results in the third. " 12/01/2012 - "Despite the promising results from early clinical trials, it has been shown that the addition of tirapazamine appears to confer no benefits on progression-free or overall survival in patients with cervical cancer. " 05/01/1993 - "Concentrations of SR 4233 required for effective in vitro cytotoxicity are achieved in vivo, and extensive bioreductive metabolism occurs in tumor and normal tissues." 12/01/2012 - "The addition of tirapazamine (TPZ) to conventional chemoradiation protocols in the management of cervical cancer held promise in the initial Phase I and II clinical trials in delaying recurrence and improving survival. " 10/15/2010 - "Pharmacokinetic/pharmacodynamic modeling identifies SN30000 and SN29751 as tirapazamine analogues with improved tissue penetration and hypoxic cell killing in tumors."
2.	Anoxia (Hypoxia) 02/15/2009 - "On the other hand, Pd(L3)(2), where L3 is 3-amino-6(7)-chloroquinoxaline-2-carbonitrile N(1),N(4)-dioxide, resulted in vitro more potent cytotoxin in hypoxia (P=5.0 microM) than the corresponding free ligand (P=9.0 microM) and tirapazamine (P=30.0 microM), the first bioreductive cytotoxic drug introduced into clinical trials. " 03/01/2008 - "In this study, stable CA9-expressing cell lines were established using the CA9 gene-defective human C33a cell line and the HeLa cell line to investigate the role of CA9 in response to ionizing radiation and hypoxia-selective cytotoxin, Tirapazamine (TPZ). " 10/07/2014 - "The drug testing results show an increase in A549 cell apoptosis due to the hypoxia-activated cytotoxicity of tirapazamine (TPZ) and also suggest great cell compatibility and gradient controllability of the device. " 02/21/2013 - "The results of the proof-of-concept experiment indicate the dose-dependent antitumor effect of the drugs and hypoxia-induced cytotoxicity of tirapazamine. " 04/01/2012 - "Tirapazamine induced apoptosis of colorectal tumour cells under hypoxia in vitro. "
3.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 12/01/1999 - "The first of these new drugs to be tested clinically, tirapazamine, a drug that is highly toxic to hypoxic but not aerobic cells, has already demonstrated efficacy in selective potentiation of cisplatin in randomized Phase III trials with non-small cell lung cancer. " 11/01/1998 - "A phase II study was conducted to evaluate the safety and efficacy of tirapazamine combined with cisplatin for the treatment of patients with advanced non-small-cell lung cancer (NSCLC). " 03/01/2000 - "Tirapazamine plus cisplatin versus cisplatin in advanced non-small-cell lung cancer: A report of the international CATAPULT I study group. " 11/01/1998 - "Tirapazamine with cisplatin in patients with advanced non-small-cell lung cancer: a phase II study." 06/01/1998 - "Tirapazamine has been clinically tested in combination with cisplatin at escalating doses in a phase I trial and at therapeutic doses in three separate phase II trials in patients with advanced non-small-cell lung cancer (NSCLC) in 11 study centres. "
4.	Carcinoma (Carcinomatosis) 11/01/1998 - "1994 to Nov. 1996, 40 patients with stage III or IV carcinomas of the head and neck were enrolled in a Phase II trial to receive conventional RT (70 Gy in 7 weeks) with concurrent tirapazamine (159 mg/m2 intravenously, 3 times per week for 12 doses). " 11/01/1998 - "The toxicity of RT with concurrent tirapazamine was acceptable in treating advanced head and neck carcinomas. " 10/14/1994 - "SR-4233 (500 microM, 1 h) killed about 70% of normally oxygenated and 99% of hypoxic human MCF-7 breast carcinoma cells. " 11/01/1998 - "Concurrent tirapazamine and radiotherapy for advanced head and neck carcinomas: a Phase II study." 11/01/1998 - "To evaluate the efficacy and toxicity of tirapazamine, a hypoxic cytotoxin, combined with conventional radiotherapy (RT) for advanced head and neck carcinomas. "
5.	Melanoma (Melanoma, Malignant) 12/01/1998 - "In this study the response of three melanoma cell lines to single doses of radiation, to the bioreductive drug tirapazamine (SR-4233) and to the combination of radiation and tirapazamine was determined. " 12/01/1998 - "Three melanoma cell lines (MM576, MM96L and murine B16-F10) were exposed to increasing concentrations of tirapazamine to assess cytotoxicity under aerobic and hypoxic conditions. " 12/01/1998 - "Effect of radiation and tirapazamine (SR-4233) on three melanoma cell lines." 12/01/1998 - "Since melanomas are known to contain hypoxic cells which may reduce their radiosensitivity, these in vitro results have demonstrated the potential of tirapazamine to overcome the radioresistance of hypoxia and give encouragement for further studies." 05/01/2000 - "Two human cell lines were studied: one cell line sensitive to tirapazamine, Na11+, a pigmented melanoma with a high percentage of hypoxic cells, and a less sensitive cell line to tirapazamine, HRT18, a rectal adenocarcinoma. "

Related Drugs and Biologics

1.	Cisplatin (Platino)
2.	Cyclophosphamide (Cytoxan)
3.	carbogen
4.	Niacinamide (Nicotinamide)
5.	irinotecan (Camptosar)
6.	Paclitaxel (Taxol)
7.	Carboplatin (JM8)
8.	Fluorouracil (Carac)
9.	Oxygen
10.	Cytotoxins

Related Therapies and Procedures

1.	Heterologous Transplantation (Xenotransplantation)
2.	Radiotherapy
3.	Drug Therapy (Chemotherapy)
4.	Therapeutics
5.	Stents