Table 3.
Characteristics of 177Lu-DOTATATE and competitor radiolabeled SSAs and somatostatin antagonists.
| Compound | Peptide | Radionuclide | Unique Characteristics |
|---|---|---|---|
| 177Lu-DOTATATE | Octreotate | 177Lu | Compared to 90Y-DOTATOC, it has greater tumor uptake and a reduced risk of toxicity due to the medium energy B-emitting character of 177Lu. This agent has randomized phase III data while no other radiolabeled SRA has such data yet. |
| 90Y-DOTATOC | Octreotide | 90Y | 90Y is a high energy B-emitter with a potential ability to be more effective than 177Lu for larger metastases. This was one of the first radiolabeled SSAs to be trialed in humans. |
| 111In-DOTATOC | Octreotide | 111In | 111In emits γ rays and conversion electrons. It was the initial radiolabeled SSA trialed in humans therapeutically after initially being used at lower doses for diagnostic purposes. |
| 177Lu-DOTA-EB-TATE | Octreotate | 177Lu | The Evans Blue modification of the somatostatin analog enables reversible binding to albumin which increases the circulating half-life of the radiolabeled SSA and increases its tumor exposure. |
| 177Lu-OPS201 | OPS201 | 177Lu | OPS201 is a somatostatin receptor 2 antagonist (which is not internalized) and may result in increased DNA damage than 177Lu-DOTATATE. |
Abbreviations: 177Lu, lutetium-177; 90Y, yttrium-90; SSA, 111In, indium-111; SSA, somatostatin receptor agonist