177Lu-rhPSMA-10.1 Induces Tumor Response in a Patient With mCRPC After PSMA-Directed Radioligand Therapy With 177Lu-PSMA-I&T : Clinical Nuclear Medicine

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177Lu-rhPSMA-10.1 Induces Tumor Response in a Patient With mCRPC After PSMA-Directed Radioligand Therapy With 177Lu-PSMA-I&T

Bundschuh, Ralph A. MD, PhD; Pfob, Christian H. MD; Wienand, Georgine; Dierks, Alexander MD; Kircher, Malte MD; Lapa, Constantin MD

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Clinical Nuclear Medicine 48(4):p 337-338, April 2023. | DOI: 10.1097/RLU.0000000000004573
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An 86-year-old man with metastastic castrate-resistant prostate cancer (mCRPC) and biochemical progression was referred for further theranostic workup. Previously, he had undergone androgen deprivation therapy including LHRH agonists (buserelin) and novel androgen axis drugs (enzalutamide) as well as taxane-based chemotherapy (docetaxel and cabazitaxel). PET/CT using 68Ga-PSMA-I&T1,2 revealed local recurrence as well as multiple (pelvic, retroperitoneal, supraclavicular) lymph node and bone (eg, left femur, arrows) metastases (A). Subsequently, PSMA-directed radioligand therapy was recommended according to recent practice3,4 and the decision of the institutional interdisciplinary tumor conference. After 4 cycles with 177Lu-PSMA-I&T (B), a biochemical as well as radiologic partial response was noted. Treatment was continued for another 2 cycles. At restaging, in contrast to the continued response in the local as well as the lymphonodal tumor manifestations, increasing PSMA expression of metastases in the left femur (arrows) and left iliac wing (stars) as well as a new lesion in lumbar vertebra 5 was recorded, consistent with rising PSA serum values (C). Given the lack of further therapeutic options, 2 additional cycles of radioligand therapy with 177Lu-rhPSMA-10.1 were offered on a compassionate use basis resulting in a renewed tumor response (D). Radiohybrid prostate-specific membrane antigen (rhPSMA) ligands are a new class of radiopharmaceuticals in prostate cancer theranostics.5–7 Pretherapeutic dosimetry with one agent from this class (177Lu-rhPSMA-7.3C) has recently shown (on an intrapatient basis) tumor uptake to be approximately 2.5 times higher than with 177Lu-PSMA-I&T.8 Building on this observation, 177Lu-rhPSMA-7.3C has been optimized in terms of pharmacological and pharmacokinetic properties yielding 177Lu-rhPSMA-10.1 that is now being investigated in clinical trials (NCT05413850).


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theranostics; 177Lu-rhPSMA-10.1; prostate cancer; radiologand therapy

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