Clinical evaluation of two new bifunctional chelating agents for immunoscintigraphy (I.S.) with indium-111-anti-CEA monoclonal antibody
Journal Article
·
· Journal of Nuclear Medicine
OSTI ID:197894
- Brookhaven National Lab., Upton, NY (United States); and others
Previous animal studies have shown that chelates of In-111 with semi-rigid cyclohexyl EDTA (CDTA) derivatives produce improved in-vivo stability compared to non-rigid analogs. Two CDTA derivatives, CDTA-EN-SCN (dilithium salt of N-(methyl (2-isothiocyanato-ethyl) carbamide) trans-1,2-diaminocyclohexane N,N{prime},N{prime}-triacetic acid) and 4-ICE (4-isothiocyanato-trans-1,2-diaminocyclohexane-N,N,N {prime},N{prime}-tetraacetic acid), were synthesized, coupled to anti-CEA F(ab{prime}){sub 2} fragments and labeled with In-111 with a specific activity of 111MBq/mg. Five patients were injected with CDTA-EN-SCN and 4 with 4-ICE. IS was performed 3 days after injection. Mean blood activity, at the time of IS, expressed as the percentage of injected dose per ml, was 0.0038% with 4-ICE and 0.0071% with CDTA-EN-SCN. For comparative purposes, the mean value previously obtained with DTPA coupled to the same antibody was 0.0035%. Liver uptake was estimated from semi-quantitative calculations on scintigraphic images. Compared with the value obtained in a patient injected with 72.3 antibody coupled to DTFPA, a 2.5-fold reduction in liver uptake was observed. However, this reduction was sufficient to allow visualization of a large liver metastasis in one patient. With CDTA-EN-SCN, colon activity was moderate in 3 patients and intense in 1. With 4-ICE it was moderate in 2 patients and intense in 1, With CDTA-EN-SCN, true-positive IS results were observed in 2 patients (pelvis and mediastinum) and a false-negative result was observed in 1 patient (pelvis). In 3 patients, IS was negative and recurrence not yet confirmed despite high serum CEA level. With 4-FICE, true-positive IS results were observed in 3 patients (2 pelvis, 1 lung). A false-negative result was found in a patient with a confirmed liver metastasis.
- OSTI ID:
- 197894
- Report Number(s):
- CONF-940605--
- Journal Information:
- Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: Suppl.5 Vol. 35; ISSN JNMEAQ; ISSN 0161-5505
- Country of Publication:
- United States
- Language:
- English
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