Zhang Jiahui, Wang Junxiang, Chen Lingfan, Yu Xiangbin, Zhang Shuihua, Yu Yue
School of Pharmacy, Fujian Medical University, Fuzhou 350122, China.
Fujian Center for New Drug Safety Evaluation, Fuzhou 350122, China.
Pharmaceuticals (Basel). 2024 Jan 22;17(1):141. doi: 10.3390/ph17010141.
Levamisole (LVM) is considered an immunomodulatory agent that has the potential to treat various cancer and inflammation diseases. However, there is still much debate surrounding the toxicokinetic and toxicological information of LVM. Therefore, it is crucial to assess its toxicity to provide useful data for future human LVM risk assessments. In this study, a barrier environment was established under the guidance of good laboratory practice (GLP) at the Fujian Center for New Drug Safety Evaluation. Male beagle dogs were orally administered with 5, 15, and 30 mg/kg of LVM daily for four weeks. Toxicity assessment was based on various factors such as mortality, clinical signs, food and water consumption, body weight, body temperature, electrocardiogram, ophthalmological examination, hematology, serum biochemistry, organ/body coefficients, histopathological study, and toxicokinetic analysis. The results of this study showed that LVM did not exhibit any significant toxicological effects on beagle dogs at the exposure levels tested. A no observed adverse effect level (NOAEL) of LVM was set at 30 mg/kg/day for male beagle dogs, which is equivalent to a 12-fold clinical dose in humans. Moreover, the repeated exposure to LVM for four weeks did not lead to any bioaccumulation. These findings provide valuable insights for future human LVM risk assessments.
左旋咪唑(LVM)被认为是一种具有治疗多种癌症和炎症性疾病潜力的免疫调节剂。然而,围绕LVM的毒代动力学和毒理学信息仍存在诸多争议。因此,评估其毒性以提供未来人类LVM风险评估的有用数据至关重要。在本研究中,福建新药安全评价中心在良好实验室规范(GLP)的指导下建立了屏障环境。雄性比格犬每天口服5、15和30 mg/kg的LVM,持续四周。毒性评估基于多种因素,如死亡率、临床症状、食物和水消耗量、体重、体温、心电图、眼科检查、血液学、血清生物化学、器官/体重系数、组织病理学研究和毒代动力学分析。本研究结果表明,在所测试的暴露水平下,LVM对比格犬未表现出任何显著的毒理学效应。雄性比格犬LVM的无观察到有害作用水平(NOAEL)设定为30 mg/kg/天,这相当于人类临床剂量的12倍。此外,连续四周重复暴露于LVM未导致任何生物蓄积。这些发现为未来人类LVM风险评估提供了有价值的见解。