TABLE 1

Key Reports of PSMA-Targeted Antibody and Small-Molecule Radioligand Therapy for mCRPC

First author	PMID	Report date	Agent	n	Key efficacy outcomes	Key safety outcomes
Bräuer	28624848	September 2017	¹⁷⁷Lu-PSMA-617	59	↓PSA in 91% of pts; ≥50% ↓PSA in 53%; median OS 32 wk; PSA decrease after 1 cycle and AP <220 U/L associated with longer OS	2 pts each with grade 3 leukopenia and thrombocytopenia; 12 with new-onset xerostomia
Ahmadzadehfar	28488028	August 2017	¹⁷⁷Lu-PSMA-617	52	After 1 cycle, ↓PSA in 81% of pts and ≥50% ↓PSA in 44%; 50% of cycle 1 NRs with no response to subsequent treatment; survival of cycle 1 Rs more than twice that of cycle 1 NRs (68 vs. 33 wk)	Not reported
Afshar-Oromieh	28280855	June 2017	¹³¹I-MIP-1095	34	≥50% ↓PSA in 70.6% of pts; first dose most effective; no association between applied activity and PSA response; median OS 17 mo	Measurable leukopenia and thrombocytopenia, significant xerostomia transient but worsening with increasing number of treatments
Kratochwil	28408529	April 2017	²²⁵Ac-PSMA-617	14	At 100 kBq/kg, duration of ↓PSA <4 mo; antitumor effects additive if therapy repeated every 2 mo	Severe xerostomia: dose-limiting toxicity at >100 kBq/kg
Rahbar	27765862	January 2017	¹⁷⁷Lu-PSMA-617	145	↓PSA in 60% of pts; ≥50% ↓PSA in 45%; elevated AP and visceral metastases negative predictors of response	10%, 4%, and 3% of pts with anemia, thrombocytopenia, and leukopenia, respectively; 8% with xerostomia
Fendler	27683041	January 2017	¹⁷⁷Lu-PSMA-617	15	2 cycles of 3.7 GBq (n = 5) or 6.0 GBq (n = 10); ↓PSA in 80% of pts; 67% with PR or SD; pain relief in 70% of symptomatic pts	3 pts with grade 3 events (nausea, leukopenia, anemia)
Kratochwil	26985056	August 2016	¹⁷⁷Lu-PSMA-617	30	↓PSA in 70% of pts; ≥50% ↓PSA in 43%; PSA response >24 wk in 8/11 pts receiving 3 cycles	9 pts with worsening of anemia; 8 with leukopenia; 6 with thrombocytopenia
Baum	26795286	January 2016	¹⁷⁷Lu-PSMA-I&T	56	↓PSA in 80.4% of pts; ≥50% ↓PSA in 58.9%; 72% PR or SD by CT; 64% PR or SD by ⁶⁸Ga-PSMA PET	2 pts with transient xerostomia; statistically significant/clinically insignificant decreases in leukocyte and erythrocyte counts
Tagawa	23714732	September 2013	¹⁷⁷Lu-huJ591 mAb	47	↓PSA in 59.6%; ≥50% ↓PSA in 10.6%	Grade 4 thrombocytopenia in 46.8%; grade 4 neutropenia in 25.5%
Milowsky	15173215	July 2004	⁹⁰Y-huJ591 mAb	29	↓PSA of 85% and 70% in 2 pts; 6 pts with SD	2 pts with thrombocytopenia and non–life-threatening bleeding

pts = patients; AP = alkaline phosphatase; NRs = nonresponders; Rs = responders; mAb = monoclonal antibody; PMID = PubMed identification number; OS = overall survival; PR = partial response; SD = stable disease.