Clinical Properties of Current Food and Drug Administration–Approved Molecular Tracers Targeting Cell Surface Protein Receptors
| Property | 18F-fluoroestradiol | 99mTc-tilmanocept | 68Ga-DOTATATE, 68Ga-DOTATOC, 177Lu-DOTATATE, 64Cu-DOTATATE, and 111In-pentetreotide | 90Y-ibritumomab tiuxetan |
|---|---|---|---|---|
| Indication | Detecting estrogen receptor–positive lesions as adjunct to biopsy in patients with recurrent or metastatic breast cancer | Mapping lymph nodes draining from primary tumor site and guiding sentinel lymph node biopsy with intraoperative γ-probe | 68Ga-DOTATATE or 68Ga-DOTATOC: locating SSTR-positive neuroendocrine tumors in adult and pediatric patients; 177Lu/64Cu-DOTATATE: treating SSTR-positive gastroenteropancreatic neuroendocrine tumors, including foregut, midgut, and hindgut neuroendocrine tumors in adults* | Evaluating relapsed or refractory, low-grade or follicular B-cell non-Hodgkin lymphoma |
| Administered dose for adults | 111–222 MBq (3–6 mCi) | 18.5 MBq (0.5 mCi) | 68Ga-DOTATATE: 2 MBq/kg (0.054 mCi/kg) up to 200 MBq (5.4 mCi); 68Ga-DOTATOC: adult—148 MBq (4 mCi); pediatric—1.59 MBq/kg (0.043 mCi/kg) with range of 11.1 MBq (0.3 mCi) to 111 MBq (3 mCi); 177Lu-DOTATATE: 7.4 GBq (200 mCi) every 8 wk for total of 4 doses; 64Cu-DOTATATE: 148 MBq (4 mCi); 111In-pentetreotide: 111--222 MBq (3--6 mCi) | 14.8 MBq per kg (0.4 mCi/kg); dose adjustment needed if platelet counts are low |
| Injection route | Intravenous | Subcutaneous, intradermal, subareolar, or peritumoral injection in 1 mL or less | Intravenous | Intravenous |
| Injection-to-imaging time | 80 min | 10–15 min | 68Ga-DOTATATE: 40–90 min; 68Ga-DOTATOC: 60 min† | Imaging not usually done |
| Normal biodistribution | Hepatobiliary system (excretion); intestines (excretion); heart, blood, uterus, kidney (excretion); and bladder (excretion) | Lymphatic channels draining injection site | Pituitary, thyroid, spleen, adrenals, kidney, pancreas, prostate, liver, and salivary glands | Significant marrow and splenic distribution without cold antibody pretreatment; pretreatment with rituximab cold anti-CD20 antibody blocks CD20 sites of normal circulating B-cells in spleen and bone marrow by binding to it, thereby allowing the following hot antibodies to reach tumor areas |
*111In-pentetreotide: detection of neuroendocrine tumors bearing somatostatin receptors.
†177Lu-DOTATATE: not imaged; 64Cu-DOTATATE: not imaged; 111In-pentetreotide: 24--48 h.