UCLA Olympic Analytical Laboratory, David Geffen School of Medicine, Los Angeles, California, USA.
Institute of Biochemistry, German Sport University Cologne, Cologne, Germany.
Drug Test Anal. 2023 Nov-Dec;15(11-12):1449-1453. doi: 10.1002/dta.3573. Epub 2023 Sep 8.
Capromorelin is a growth hormone secretagogue. Despite promising results to alleviate muscle-wasting in the elderly, it has not advanced further in human development. Subsequent studies demonstrated capromorelin's ability to increase food intake in animals, leading to approval in the United States and Europe as an appetite stimulant for cats (Elura) and dogs (Entyce). Capromorelin is prohibited in sports due to its ability to stimulate growth hormone production and enhance performance. However, given that its veterinary preparation is formulated as a highly concentrated solution (20 or 30 mg/mL) delivered orally, incidental ingestion or dermal absorption may result in an adverse analytical finding (AAF) by way of direct exposure during oral administration to a pet. An administration study was conducted by either oral or transdermal application of capromorelin solution to mimic the scenario of inadvertent exposure to the drug. Ingestion of 30 μg of capromorelin orally (equivalent to 1 μL of Entyce) resulted in detectable amounts of capromorelin in urine for up to 48 h after administration with a maximum urinary concentration of 7 ng/mL. Importantly, when applied directly to the skin on the hands in larger quantities mimicking a pet administration exposure scenario (30 mg or 1 mL of Entyce), capromorelin was also detected reaching a maximum urinary concentration of 0.7 ng/mL. Athletes and testing authorities should be aware of the risk of an AAF arising due to incidental exposure to veterinary preparations of capromorelin. To our knowledge, before 2022, no positive test for capromorelin had ever been reported.
卡普莫瑞林是一种生长激素促分泌素。尽管有缓解老年人肌肉消耗的前景，但它在人体开发方面没有进一步进展。随后的研究表明，卡普莫瑞林能够增加动物的食物摄入量，因此在美国和欧洲获得批准，作为猫（Elura）和狗（Entyce）的食欲刺激剂。由于其刺激生长激素产生和提高性能的能力，卡普莫瑞林在运动中被禁止使用。然而，鉴于其兽医制剂被制成高浓度溶液（20 或 30mg/mL）口服给药，偶然摄入或皮肤吸收可能导致通过宠物口服给药直接暴露而出现不良分析发现（AAF）。进行了一项通过口服或经皮应用卡普莫瑞林溶液的管理研究，以模拟意外暴露于药物的情况。口服摄入 30μg 卡普莫瑞林（相当于 1μL 的 Entyce）后，在给药后长达 48 小时内可检测到尿液中的卡普莫瑞林，最大尿液浓度为 7ng/mL。重要的是，当直接涂抹在手上的皮肤时，模拟宠物管理暴露情况（30mg 或 1mL 的 Entyce）时，也检测到卡普莫瑞林，达到最大尿液浓度 0.7ng/mL。运动员和检测机构应意识到由于意外接触兽医制剂卡普莫瑞林而出现 AAF 的风险。据我们所知，在 2022 年之前，从未报告过卡普莫瑞林的阳性测试。
