Examples of Clinical Evaluation of α-Therapy
| Radiopharmaceutical and dose | Target and study population | Features and outcome | Dose-limiting observations and toxicity | Study |
| 211At-ch81C6: 71–347 MBq | Tenascin: 18 patients with primary or metastatic brain tumor | Phase I and II feasibility, safety, and efficacy: overall survival of 54.1 vs. 23 wk for glioblastoma patients | No grade 3 or higher toxicity | (40) |
| 211At-MX35 F(ab′)2: 22.4–101 MBq/L | Sodium-dependent phosphate transport protein 2b: patients with complete clinical remission after second-line chemotherapy of recurrent ovarian cancer | Phase I pharmacokinetic and dosimetry: estimated absorbed dose to peritoneum, 15.6 ± 1.0 mGy/(MBq/L) | With 200 MBq/mL, effective dose of 2.6 Sv (lifelong lethal cancer risk of 10%) | (41,42) |
| 213Bi-DOTATOC: 1.0–4.0 GBq | Somatostatin receptors: patients with progressive neuroendocrine tumor | First-in-human: long-lasting tumor response, and remission of tumors refractory to β-radiation | Moderate acute hematologic and chronic kidney toxicities | (27) |
| 213Bi-HuM195: 10.36–37.0 MBq/kg | CD-33: patients with primary refractory or relapsed acute myeloid leukemia | Phase I dose escalation: reduction in peripheral blood leukemia cells and bone marrow blasts | Transient myelosuppression | (22) |
| 225Ac-HuM195: 18.5–148 kBq/kg | CD-33: patients with acute myeloid leukemia | Phase I dose escalation: MTD of 111 kBq/mL to bone marrow and peripheral blast reduction | Myelosuppression | (24) |
| 225Ac-PSMA-617: 100 kBq/kg | PSMA: patients with metastatic CRPC | First-in-human: complete response on PET imaging and PSA level below measurable levels | Xerostomia | (2) |
| 227Th-epratuzumab BAY1862864: 1.4 MBq* | CD-22: patients with relapsed or refractory CD-22–positive non-Hodgkin lymphoma | Phase I dose escalation and determination of MTD, currently recruiting (NCT02581878) | ||
| 223Ra-dichloride: 50 kBq/kg | Bone: patients with symptomatic CRPC | Phase III ALSYMPCA overall survival and time to disease progression: overall survival of 14.9 vs. 11.3 mo | (31,32) | |
| 212Pb-trastuzumab: 7.4–21.1 MBq/m2 | HER2: patients with progressive ovarian carcinoma after multiple therapies | Phase I safety and tolerability: few tumor volume decreases | (29) |
↵* Starting dose.