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MCT1 抑制剂 AZD3965 治疗后出现恶性高乳酸酸中毒 1 例。

A case of malignant hyperlactaemic acidosis appearing upon treatment with the mono-carboxylase transporter 1 inhibitor AZD3965.

机构信息

Newcastle upon Tyne Hospitals NHS Foundation Trust, Newcastle upon Tyne, UK.

Newcastle University, Newcastle upon Tyne, UK.

出版信息

Br J Cancer. 2020 Apr;122(8):1141-1145. doi: 10.1038/s41416-020-0727-8. Epub 2020 Feb 20.

Abstract

A 47-year-old man with metastatic melanoma presented with refractory hyperlactaemic acidosis following the first dose of the mono-carboxylase transporter 1 inhibitor AZD3965 within a "first time in man" clinical trial. The mechanism of the agent and the temporal relationship suggested that this event was potentially drug related and recruitment was suspended. However, urinary metabolomics showed extensive abnormalities even prior to drug administration, leading to investigations for an underlying metabolic disorder. The lack of clinical symptoms from the elevated lactate and low blood glucose suggested a diagnosis of "hyper-Warburgism", where the high tumour burden was associated with extensive glucose uptake and lactate efflux from malignant cells, and the subsequent impact on blood biochemistry. This was supported by an FDG-PET scan showing extensive glucose uptake in numerous metastases and lack of uptake in the brain. A review of the literature showed 16 case reports of "hyper-Warburgism" in non-haematological malignancies, none of them with melanoma, with most associated with a poor outcome. The patient was treated symptomatically, but died 2 months later. The development of AZD3965 continues with the exclusion of patients with elevated plasma lactate at screening added to the protocol as a safety measure.Trial identification number ClinicalTrials.Gov. NCT01791595.

摘要

一位 47 岁男性患有转移性黑色素瘤,在首次参加“首次人体临床试验”中接受单羧酸转运蛋白 1 抑制剂 AZD3965 治疗后,出现难治性高乳酸血症酸中毒。该药物的作用机制和时间关系表明,此次事件可能与药物有关,因此暂停了招募。然而,尿代谢组学显示,即使在给药之前,也存在广泛的异常,这导致对潜在代谢紊乱进行了调查。高乳酸血症和低血糖而无临床症状提示存在“高 Warburg 现象”,其高肿瘤负荷与恶性细胞中葡萄糖摄取和乳酸外流广泛相关,并对血液生化产生后续影响。这得到了 FDG-PET 扫描的支持,该扫描显示多个转移灶中葡萄糖摄取广泛,而大脑中无摄取。对文献的回顾显示,在非血液系统恶性肿瘤中有 16 例“高 Warburg 现象”的病例报告,其中没有黑色素瘤,大多数与不良预后相关。该患者接受了对症治疗,但两个月后死亡。AZD3965 的开发继续进行,在筛选时排除了血浆乳酸升高的患者,并将其作为安全措施添加到方案中。试验识别号 ClinicalTrials.Gov. NCT01791595。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe66/7156442/c36d5fc5fff6/41416_2020_727_Fig1_HTML.jpg

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