Radi Zaher A, Khan Nasir
Pfizer Worldwide Research, Development and Medical, Drug Safety R&D, 1 Portland Street, Cambridge, MA 02140, USA.
Pfizer Worldwide Research, Development and Medical, Drug Safety R&D, Eastern Point Road, Groton, CT 06340, USA.
Toxicol Appl Pharmacol. 2023 May 1;466:116471. doi: 10.1016/j.taap.2023.116471. Epub 2023 Mar 17.
Thymoma, a tumor of thymic lymphocytes or thymic epithelial cells (TECs), is a common spontaneous tumor in Wistar Han rats, especially in females with up to 18% incidence in controls. In addition to sex, there are rat strain differences in background incidence of thymomas such as Sprague Dawley versus Wistar Han rats. Human thymomas are very rare and without clear differences in incidence between males and females. Immunomodulatory and anti-inflammatory pharmaceutical drug classes, including Janus kinase inhibitors, increase the incidence of benign thymoma in two-year rat carcinogenicity studies. Potential non-genotoxic mechanisms that might contribute to the pathogenesis of thymoma development in one sex (female) Wistar Han rats include: (1) hormonal differences, (2) high proliferation rate of TECs, (3) delayed physiologic thymic involution, and/or (4) significant level of immunosuppression at high doses of a pharmaceutical drug. Factors to consider in the human cancer risk assessment of pharmaceutical-induced thymoma are: the genotoxicity of the test article, sex and strain of rats, exposure safety margins, and pathophysiologic differences and similarities of thymoma between rats and humans. Totality of weight of evidence approach and available data suggest thymomas observed in carcinogenicity studies of pharmaceutical drugs are not relevant for human risk at clinically relevant therapeutic doses.
胸腺瘤是一种胸腺淋巴细胞或胸腺上皮细胞(TECs)的肿瘤,是Wistar Han大鼠常见的自发肿瘤,尤其是在雌性大鼠中,对照组发病率高达18%。除了性别外,不同品系大鼠胸腺瘤的背景发病率也存在差异,如Sprague Dawley大鼠与Wistar Han大鼠。人类胸腺瘤非常罕见,男性和女性发病率无明显差异。在两年期大鼠致癌性研究中,包括Janus激酶抑制剂在内的免疫调节和抗炎药物类别会增加良性胸腺瘤的发病率。可能导致一种性别(雌性)Wistar Han大鼠胸腺瘤发病机制的潜在非遗传毒性机制包括:(1)激素差异,(2)TECs的高增殖率,(3)生理性胸腺退化延迟,和/或(4)高剂量药物时显著的免疫抑制水平。在药物诱导胸腺瘤的人类癌症风险评估中需要考虑的因素包括:受试物的遗传毒性、大鼠的性别和品系、暴露安全边际以及大鼠和人类胸腺瘤的病理生理差异和相似性。证据权重法和现有数据表明,在药物致癌性研究中观察到的胸腺瘤在临床相关治疗剂量下与人类风险无关。