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Nimorazole

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Chemical Structure| 6506-37-2 同义名 : 尼莫唑 ;K-1900;Acterol;NSC 107524;Nitrimidazine;Naxogin;Naxofem
CAS号 : 6506-37-2
货号 : A394939
分子式 : C9H14N4O3
纯度 : 99%+
分子量 : 226.232
MDL号 : MFCD00866796
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(154.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Nimorazole is a nitroimidazole anti-infective. Follow-up tests in 100 patients treated with metronidazole and 97 treated with nimorazole indicated cure-rates of 95 and 82 percent, respectively[3]. Nimorazole significantly improves the effect of radiotherapeutic management of supraglottic and pharynx tumors and can be given without major side-effects[4]. Nimorazole, a 5-Nitromidazole compound has been shown in animal studies to have similar radiosensitizing properties to misonidazole at clinically acceptable dose levels. The drug is well absorbed in humans after oral administration with peak plasma levels occurring around 90 min after ingestion (range 35-135 min) and a plasma half life between 2 and 4.8 hours[5]. The compliance to nimorazole is fair, with tolerable acute, but neither persistent nor late, toxicity. It can be administered with chemotherapy and different radiotherapy fractionation schedules[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02976051 Locally Advanced Head and Neck... 展开 >> Cancer Radiotherapy 收起 << Phase 2 Recruiting December 2021 Denmark ... 展开 >> Department of Experimental Clinical Oncology, Aarhus University Hospital Recruiting Aarhus, Denmark, 8000 C Contact: Jens Overgaard, Prof., MD    +45 7846 2629    jens@oncology.au.dk    Contact: Mette Saxø, MD    +89492619    mette.saksoe@oncology.au.dk 收起 <<
NCT01733823 HNSCC,Larynx, Pharynx and Oral... 展开 >> Cavity 收起 << Phase 1 Phase 2 Completed - Denmark ... 展开 >> Aarhus Aarhus, Aarhus C, Denmark, 8000 Odense Odense, Odense C, Denmark, 5000 Aalborg Aalborg, Denmark, 9100 Herlev Herlev, Denmark, 2730 收起 <<
NCT01880359 Locally Advanced Head and Neck... 展开 >> HPV Negative Squamous Cell Cancers 收起 << Phase 3 Active, not recruiting December 2020 Australia ... 展开 >> Royal Brisbane And Women's Hospital Brisbane, Australia, QLD 4029 Princess Alexandra Hospital - University Of Queensland Brisbane, Australia, QLD 4102 Royal North Shore Hospital St Leonards, Australia, NSW 2065 Belgium Hopitaux Universitaires Bordet-Erasme - Institut Jules Bordet Brussels, Belgium, 1000 Cliniques Universitaires Saint-Luc Brussels, Belgium, 1200 U.Z. Leuven - Campus Gasthuisberg Leuven, Belgium, 3000 France Centre Georges-Francois-Leclerc Dijon, France, 21079 CHU de Tours - Hopital Bretonneau Tours, France, 37044 Institut Gustave Roussy Villejuif, France, 94805 Germany Charite - Universitaetsmedizin Berlin - Campus Virchow-Klinikum Berlin, Germany Ludwig-Maximilians-Universitaet Muenchen - Klinikum der Universitaet Muenchen - Campus Grosshadern Muenchen, Germany, 81377 Netherlands Vrije Universiteit Medisch Centrum Amsterdam, Netherlands, 7007MB Radboud University Medical Center Nijmegen Nijmegen, Netherlands, 6500 H Poland Medical University Of Gdansk Gdansk, Poland, 80 211 The Great Poland Cancer Centre Poznan, Poland Maria Sklodowska-Curie Memorial Cancer Centre Warsaw, Poland Lower Silesian Oncology Centre Wrocław, Poland Switzerland Hôpitaux universitaires de Genève - HUG - site de Cluse-Roseraie Geneva, Switzerland, 1211 UniversitaetsSpital Zurich Zurich, Switzerland, 8091 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.42mL

0.88mL

0.44mL

22.10mL

4.42mL

2.21mL

44.20mL

8.84mL

4.42mL
参考文献

[1]Overgaard J, Hansen HS, et al. A randomized double-blind phase III study of nimorazole as a hypoxic radiosensitizer of primary radiotherapy in supraglottic larynx and pharynx carcinoma. Results of the Danish Head and Neck Cancer Study (DAHANCA) Protocol 5-85. Radiother Oncol. 1998 Feb;46(2):135-46.

[2]Roy RB, Laird SM, et al. Treatment of trichomoniasis in the female. A comparison of metronidazole and nimorazole. Br J Vener Dis. 1975 Aug;51(4):281-4.

[3]Roy RB, Laird SM, Heasman L. Treatment of trichomoniasis in the female. A comparison of metronidazole and nimorazole. Br J Vener Dis. 1975;51(4):281‐284

[4]Overgaard J, Hansen HS, Overgaard M, et al. A randomized double-blind phase III study of nimorazole as a hypoxic radiosensitizer of primary radiotherapy in supraglottic larynx and pharynx carcinoma. Results of the Danish Head and Neck Cancer Study (DAHANCA) Protocol 5-85. Radiother Oncol. 1998;46(2):135‐146

[5]Timothy AR, Overgaard J, Overgaard M. A phase I clinical study of Nimorazole as a hypoxic radiosensitizer. Int J Radiat Oncol Biol Phys. 1984;10(9):1765‐1768

[6]Metwally MA, Frederiksen KD, Overgaard J. Compliance and toxicity of the hypoxic radiosensitizer nimorazole in the treatment of patients with head and neck squamous cell carcinoma (HNSCC). Acta Oncol. 2014;53(5):654‐661