A new radioligand therapy, 177Lu-JH020002, is demonstrating encouraging results in an ongoing phase 1/2 clinical trial. This innovative therapy, designed to target prostate-specific membrane antigen (PSMA)-expressing tumor cells with precision radiation, is offering hope to patients with advanced prostate cancer who have exhausted standard treatment options. Preliminary data from the JH020002-01C study, reveal a favorable safety profile and robust antitumor activity, positioning ¹⁷⁷Lu-JH020002 as a potential game-changer in the fight against this aggressive disease.

The JH020002-01C trial, a multicenter, open-label study (NCT06139575), is evaluating the safety, tolerability, pharmacokinetics, dosimetry, and preliminary efficacy of 177Lu-JH020002 in men with mCRPC who have progressed after at least one androgen receptor pathway inhibitor (ARPI) and chemotherapy. As of January 22, 2025, 12 heavily pre-treated patients, most with bone metastases (91.7%) and all having received prior ARPI therapy, were administered a median cumulative dose of 18.06 GBq across up to six 6-week cycles.

The safety data are particularly encouraging. No dose-limiting toxicities or severe (grade 4/5) adverse events were reported, and the MTD was not reached, suggesting that ¹⁷⁷Lu-JH020002 is well-tolerated even in patients with significant prior treatment exposure. The most common side effects were mild to moderate hematologic issues, including decreased lymphocyte count (91.7%), anemia (66.7%), platelet count decreased (50%), and white blood cell count decreased (16.7%).

Efficacy results are equally promising. Among 11 patients in higher-dose cohorts (≥3.70 GBq), 63.6% experienced a significant prostate-specific antigen (PSA) decline of at least 50%, with 27.3% achieving a remarkable 90% or greater PSA reduction—a key indicator of antitumor activity.

Of the seven patients evaluated using Prostate Cancer Working Group 3 (PCWG3) criteria, none showed disease progression, and all remained under treatment follow-up. One patient with measurable disease achieved a partial response, underscoring the therapy’s potential to control advanced cancer. These outcomes are particularly striking given the patient population’s extensive prior treatments, including chemotherapy (50%), radium-223 (16.7%), and PARP inhibitors (33.3%).

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