Background: 177Lutetium-prostate-specific membrane antigen (177Lu-PSMA) is an effective treatment for metastatic castration-resistant prostate cancer (mCRPC) which is generally well-tolerated. Clinically significant hypocalcaemia has not been reported during 177Lu-PSMA treatment.
Methods: A clinical dataset of men with progressive mCRPC (n = 127) receiving a minimum of two doses of 177Lu-PSMA-I&T at 6-week intervals was evaluated to estimate the incidence, severity and clinical associations with hypocalcaemia. A median of 8 GBq was administered at each dose with blood collected at baseline and 3-week intervals including corrected calcium, alkaline phosphatase (ALP) and prostate specific antigen (PSA) concentrations.
Results: Forty-one of the 127 men (32%) experienced a reduction in serum calcium and 6/127 (5%) developed laboratory-defined hypocalcaemia within 12-weeks of commencing 177Lu-PSMA. Baseline SPECT total tumour volume was significantly higher in those who developed hypocalcaemia (median 3,249 cm3 [interquartile range 1,856-3,852] vs 465 [interquartile range 135-1,172]; p = 0.002). The mean PSA response was 78% ± 24% in those who developed hypocalcaemia and some developed marked osteosclerosis. Two patients experienced severe hypocalcaemia (1.54 mmol/L, 1.68 mmol/L) with appropriately elevated parathyroid hormone (PTH) concentrations despite prior cessation of denosumab and required treatment with ≥50mg daily prednisone. Hypocalcaemia was associated with elevated ALP (2,049 U/L, normal-range 35-110) and P1NP (744 ug/L, normal-range 15-115) concentrations in one patient.
Conclusion: Clinically significant hypocalcaemia and osteosclerosis are rare but important side effects of 177Lu-PSMA in men with high-volume osseous metastatic disease and significant treatment response. Given markedly elevated bone formation markers and response to high-dose glucocorticoids in the most severe case, we hypothesise Lu-PSMA triggered an exaggerated osteoblastic response resulting in depletion of circulating calcium stores and subsequent hypocalcaemia. Prospective evaluation of 177Lu-PSMA-induced hypocalcaemia and histopathological examination of the tumour microenvironment is required to better understand the underlying mechanisms, optimal treatment, and consequences of any associated osteosclerotic response.