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111铟标记的抗前列腺酸性磷酸酶单克隆抗体经前列腺内和静脉注射后的体内行为。

In vivo behavior of 111In-labeled monoclonal anti-prostatic acid phosphatase antibody after intraprostatic and intravenous injections.

作者信息

Kairemo K J, Rannikko S, Nordling S, Savalainen S, Ahonen A, Taavitsainen M J, Alfthan O S

机构信息

Department of Radiology, Helsinki University Central Hospital, Finland.

出版信息

J Nucl Biol Med (1991). 1994 Dec;38(4 Suppl 1):151-5.

PMID:7632761
Abstract

The 111In-labeled monoclonal anti-prostatic acid phosphatase (PAP) monoclonal antibody F(ab')2 fragment was used for the radioimmunodetection of prostate cancer in two different patient groups: 15 patients with surgically verified T1-2 prostate cancer were imaged prior to staging lymphadenectomy and total prostatectomy using lymphatic administration (intraprostatic (ipr) injection), and 15 patients with verified metastatic prostatic cancer were imaged after intravenous (i.v.) injection. The patients were studied on several occasions (at 0-180 hours) after injecting a 1 mg MoAb fragment labeled with 75-150 MBq111In (DTPA-chelation). The extirpated tissues were counted for radioactivity, and studied immunohistochemically (IHC) and histologically. The anti-PAP MoAb was labeled with high efficiency (87-99%) and it demonstrated good immunoreactivity (90-95%) and a high affinity to the target antigen. In the excised prostates, cut into 12-18 smaller pieces, there was a clear correlation between the PAP content (as detected by IHC) and absolute radioactivity (% ID of 111In anti-PAP/g prostate). However, there was no correlation between radioactivity and the amount of cancer tissue (% of histological slices) inside the removed prostate tissue. In the pharmacokinetic studies, maximum activity in the serum was obtained within 3-5 hours after ipr injection; after that the kinetic behavior was similar to that after i.v. injection. After i.v. injection, two components could be distinguished the pharmacokinetic curves; the half-lives for mean distribution and elimination were 0.62 and 35.6 hours, respectively. The mean distribution half-life as well as the AUC from the pharmacokinetic curves correlated significantly with serum PAP (p < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

用铟 - 111标记的抗前列腺酸性磷酸酶(PAP)单克隆抗体F(ab')2片段,对两组不同患者进行前列腺癌的放射免疫检测:15例经手术证实为T1 - 2期前列腺癌的患者,在分期淋巴结清扫术和全前列腺切除术之前,通过淋巴管给药(前列腺内注射)进行成像;15例经证实为转移性前列腺癌的患者,在静脉注射后进行成像。在注射75 - 150MBq铟 - 111(二乙三胺五乙酸螯合)标记的1mg单克隆抗体片段后的几个时间点(0 - 180小时)对患者进行研究。对切除的组织进行放射性计数,并进行免疫组织化学(IHC)和组织学研究。抗PAP单克隆抗体标记效率高(87 - 99%),显示出良好的免疫反应性(90 - 95%)和对靶抗原的高亲和力。在切成12 - 18个小块的切除前列腺中,(通过免疫组织化学检测的)PAP含量与绝对放射性(每克前列腺中铟 - 111抗PAP的%ID)之间存在明显相关性。然而,放射性与切除前列腺组织内癌组织量(组织切片的%)之间没有相关性。在药代动力学研究中,前列腺内注射后3 - 5小时血清中活性达到最高;之后其动力学行为与静脉注射后相似。静脉注射后,药代动力学曲线可分为两个成分;平均分布和消除的半衰期分别为0.62小时和35.6小时。药代动力学曲线的平均分布半衰期以及曲线下面积与血清PAP显著相关(p < 0.05)。(摘要截短于250字)

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