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A Novel DOTA--Melanocyte–Stimulating Hormone Analog for Metastatic Melanoma Diagnosis

Laboratory of Endocrinology, Department of Research, University Hospital and University Children’s Hospital, Basel, Switzerland

View larger version (19K): [in a new window]   FIGURE 1. Structure of MSHoct, NDP-MSH, -MSH, and DOTA--MSH analog.

View larger version (38K): [in a new window]   FIGURE 2. Tumor-to-organ uptake ratios 4 h after injection. 111In-DOTA-MSHoct (white bars) or 111In-DOTA-NDP-MSH (black bars) was injected into melanoma-bearing mice, and tissues were collected 4 h after injection. Results are expressed as tumor-to-tissue uptake ratios (mean ± SEM, n = 4–8). P < 0.05 vs. 111In-DOTA-NDP-MSH. P < 0.01 vs. 111In-DOTA-NDP-MSH. P < 0.001 vs. 111In-DOTA-NDP-MSH. P < 0.0001 vs. 111In-DOTA-NDP-MSH.

View larger version (61K): [in a new window]   FIGURE 3. Autoradiographs of tissue sections from nonmalignant organs and primary melanoma: melanoma with surrounding skin tissue (A), liver (B), and transverse section of kidney (C). 111In-DOTA-MSHoct was injected into melanoma-bearing mice, and tissues of interest were collected 4 h after injection and immediately fixed. After sectioning, tissues were exposed to storage phosphor plate. Similar autoradiographs were obtained for 3 mice.

View larger version (67K): [in a new window]   FIGURE 4. Autoradiographs of tissue sections from lung and liver colonized by melanoma metastases: lung with melanotic melanoma metastases (A), lung with amelanotic melanoma metastases (B), liver with melanotic melanoma metastases (C). 111In-DOTA-MSHoct was injected into mice inoculated with B16F1 cells, and tissues showing macroscopic metastases were collected 4 h after injection and immediately fixed. After sectioning, tissues were exposed to storage phosphor plate (left) and later to scanner (right). Arrows indicate amelanotic/melanotic metastatic nodules.

View larger version (15K): [in a new window]   FIGURE 5. Radio-RP-HPLC analysis of urine samples 4 or 24 h after injection of 111In-DOTA-MSHoct. Urine samples were collected from melanoma-bearing mice (n = 4) and were analyzed by RP-HPLC after protein precipitation. Elution time of intact 111In-DOTA-MSHoct was 15.9 min.