111in标记单克隆抗前列腺酸性磷酸酶抗体在前列腺内和静脉注射后的体内行为。

K J Kairemo, S Rannikko, S Nordling, S Savalainen, A Ahonen, M J Taavitsainen, O S Alfthan
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引用次数: 0

摘要

111in标记的单克隆抗前列腺酸磷酸酶(PAP)单克隆抗体F(ab’)2片段用于两组不同患者的前列腺癌放射免疫检测:15例手术证实的T1-2前列腺癌患者在分期淋巴结切除术和全前列腺切除术前通过淋巴给药(前列腺内注射(ipr))进行影像学检查,15例确诊的转移性前列腺癌患者在静脉注射(i.v)后进行影像学检查。在注射了标有75-150 MBq111In (dtpa -螯合)标记的1mg MoAb片段后,对患者进行了多次(0-180小时)研究。用免疫组化(IHC)和组织学方法观察组织放射性。该抗pap MoAb标记效率高(87-99%),具有良好的免疫反应性(90-95%)和对靶抗原的高亲和力。在切除的前列腺中,切成12-18个小块,PAP含量(通过免疫组化检测)与绝对放射性(111In抗PAP/g前列腺的% ID)之间有明显的相关性。然而,放射性与切除前列腺组织内癌组织的数量(占组织学切片的百分比)之间没有相关性。在药代动力学研究中,血清活性在注射后3-5小时内达到最大值;注射后的动力学行为与静脉注射后相似。静脉注射后,两组分均可区分药动学曲线;平均分布和消除的半衰期分别为0.62和35.6小时。平均分布半衰期及药动学曲线AUC与血清PAP呈显著相关(p < 0.05)。(摘要删节250字)
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In vivo behavior of 111In-labeled monoclonal anti-prostatic acid phosphatase antibody after intraprostatic and intravenous injections.

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)

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