评价药代动力学、药效学资料,和宽容Gadopiclenol,新高Relaxivity GBCA,在健康受试者和脑损伤患者(I /花絮研究阶段)。

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郝J, Bourrinet P, Desche P

评价药代动力学、药效学资料,和宽容Gadopiclenol,新高Relaxivity GBCA,在健康受试者和脑损伤患者(I /花絮研究阶段)。

Radiol投资。2019年7月,54 (7):396 - 402。doi: 10.1097 / RLI.0000000000000556。

PubMed ID
30870257 (在PubMed
]
文摘

目的:本研究的目的是评价药物动力学,安全性,和药效学gadopiclenol新高relaxivity大环的提醒造影剂,在健康受试者和脑损伤患者。材料与方法:这是一个提升剂量阶段I /花絮”研究。阶段我是双盲,随机,安慰剂对照,包括54健康受试者。在每个剂量组(0.025,0.05,0.075,0.1,0.2,和0.3更易/公斤),6收到gadopiclenol和3位接受静脉注射安慰剂(氯化钠0.9%)。阶段活动花絮是开放性脑损伤患者,包括12个,每个剂量组3(0.05,0.075,0.1,和0.2更易/公斤)。浓度测定血浆样品中之前收集管理和24小时postadministration和收集的尿液标本(第一阶段),直到政府后7天。noncompartmental方法用于药代动力学分析。可视化的药效学评价包括定性评价大脑结构/病变和定量测量(信噪比,contrast-to-noise比率)磁共振成像。临床和生物安全执行后续管理后7天期和后一天活动花絮管理阶段。结果:在健康受试者(男,50%; median age, 26.0 years), the pharmacokinetics of gadopiclenol is considered linear with mean maximum concentration Cmax values ranging from 248.7 to 3916.4 mug/mL. Gadopiclenol was excreted in an unchanged form via the kidneys, eliminated from plasma with a terminal elimination half-life (t1/2) of 1.5 to 2 hours. There was no difference in the pharmacokinetics between males and females. After administration of gadopiclenol, the contrast enhancement scores in brain structures were improved in all dose groups. Similar rates of related adverse events were observed with gadopiclenol (36.1%) and placebo (33.3%). No clinically significant modifications in biochemistry, hematology, urinalysis, electrocardiogram parameters, and vital signs were reported.In patients (male, 58%; median age, 53.0 years), a similar pharmacokinetic and safety profile was observed, and sufficient contrast enhancement was seen at all tested doses. CONCLUSIONS: The pharmacokinetics of gadopiclenol is dose-independent in healthy subjects and patients with brain lesions. Its good safety profile is in line with that reported for other macrocyclic gadolinium-based contrast agents. Preliminary pharmacodynamic results in patients suggest that gadopiclenol is a promising macrocyclic contrast agent with the potential use of lower dose for clinical routine magnetic resonance imaging scans.The study is registered on ClinicalTrials.gov under the trial registration number NCT03603106.

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