Table 2 |.
Radiopharmaceuticals approved for radionuclide therapy in oncology indications
| Agent | Approval (FDA, EMA) | Companion diagnostics | Indication | Efficacy data |
|---|---|---|---|---|
| [131I]sodium iodide | 1971a,118 | [131I]sodium iodide | Treatment of selected patients with differentiated thyroid carcinoma | Enables complete thyroid ablation in 92% of patients with low-risk thyroid cancer; 98% were free of disease at 5 years146; uptake observed in 59% of patients with metastatic thyroid cancer147,148 |
| 153Sm-EDTMP | 1997, 1998 |
99mTc-bisphosphonates, including 99mTc-medronate; 99mTc-oxidronate; 99mTc-pyrophosphate |
Palliation of bone pain in patients with multiple painful skeletal metastases | 62–72% had pain relief at 4 weeks following a single dose of 153Sm-EDTMP, including complete pain relief in 31%; pain relief persisted for up to 16 weeks in 43% of patients149; improvements in 4-week pain scores and opioid use vs controls26,149 |
| 90Y-ibritumomab tiuxetanb | 2002, 2004 | 111In-ibritumomab | R/R low-grade or follicular B cell NHL; previously untreated patients with follicular NHL who achieve a partial or complete response to first-line chemotherapy | ORR 80% vs 56%, P = 0.02 for rituximab alone (CR in 30% vs 16%); median DOR 14.2 vs 12.1 months (P = 0.64), durable responses ≥6 months. in 64% vs 47% (P = 0.03)17; clinical benefit was also seen in various combination settings150–154 |
| 131I-tositumomabc | 2003, 2003 | 131I-tositumomab | CD20+ R/R low-grade, follicular or transformed NHL following disease progression during or after rituximab | ORR 49–64%; median DOR 6.5–16 months in single-arm studies155,156 |
| 131I-iobenguane (or MIBG) | 2018a,157 | 123I-iobenguane | Noradrenaline-positive pheochromocytomas or paragangliomas | ORR 25%, DCR 92%; 53% of responders had tumour responses lasting ≥6 months, median OS 36.7 months158 |
| 223Ra-dichloride | 2013, 2013 | – | CRPC with symptomatic bone metastases and no known visceral metastases | Median OS 14.9 vs 11.3 months with placebo, HR 0.70, 95% CI 0.58–0.83, P < 0.001; time to first SSE 15.6 vs 9.8 months, HR 0.66, 95% CI 0.52–0.83, P < 0.001; increase in FACT-P QOL score ≥10 points in 25% vs 16% of patients, P = 0.02 (REFs24,159,160) |
| 177Lu-DOTATATE | 2018, 2017 |
68Ga-DOTATATE (USA); 64Cu-DOTATATE (USA); 68Ga-DOTATOC (EU) |
Somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours | Median OS 48.0 vs 36.3 monthsd, HR 0.84, 95% CI 0.60–1.17, P = 0.30; increase in QOL37 |
| 177Lu-PSMA-617 | 2022, pending | 68Ga-PSMA-11, FDA approved in 2021 and 2022 | Treatment of metastatic CRPC following disease progression on AR inhibitors and taxane-based chemotherapy | Median PFS 8.7 vs 3.4 months; median OS 15.3 vs 11.3 months in the 177Lu-PSMA-617 and control groups; time to first SSE 11.5 vs 6.8 months HR 0.50, 95% CI 0.40–0.62, P < 0.001 (REF.43) |
EMA nationally authorized medicinal product.
Discontinued in the USA in 2021.
Approval withdrawn and discontinued in 2014.
Improvement in median overall survival (OS) likely underestimated owing to 36% crossover from control arm. AR, androgen receptor; CI, confidence interval; CR, complete response; CRPC, castration-resistant prostate cancer; DCR, disease control rate; DOR, duration of response; DOTATATE, DOTA0, Tyr3-octreotate; EDTMP, ethylenediamine tetramethylene phosphonate; HR, hazard ratio; MIBG, meta-iodobenzylguanidine; NHL, non-Hodgkin lymphoma; OR, objective response; ORR, objective response rate; PFS, progression-free survival; PSMA, prostate-specific membrane antigen; QOL, quality of life; R/R, relapsed and/or refractory; SSE, symptomatic skeletal event.