To review pharmacology, pharmacokinetics, therapeutic use, product safety/description and perspectives on use of lutetium Lu 177 vipivotide tetraxetan in patients with metastatic castration-resistant prostate cancer (mCRPC). Data sources: A literature search was conducted using PubMed/Dynamed (October 2013-May 2025), limited to English language, humans, clinical trials, case reports, and guidelines. Data summary: Lutetium Lu 177 vipivotide tetraxetan is comprised of the beta-emitting radioisotope lutetium Lu-177 linked to a peptide, vipivotide tetraxetan, which binds to cells expressing prostate-specific membrane antigen (PSMA), resulting in cell death from the radiation. Kidney excretion may result in increased renal toxicity in patients with reduced renal function. Based on 2 phase III clinical trials, lutetium Lu 177 vipivotide tetraxetan 7.4 GBq administered intravenously every 6 weeks for up to 6 doses is effective in patients with mCRPC and PSMA-positive metastases after progressing on an androgen receptor pathway inhibitor and docetaxel therapy or an androgen receptor pathway inhibitor alone, by significantly improving radiographic progression-free survival. It is generally well tolerated, with asthenia/fatigue, dry mouth, mild nausea and low-grade anemia most commonly occurring. Severe adverse drug reactions are uncommon. It should only be administered by trained personnel in a designated clinical setting with existing radiation safety protocols. Patients must limit close contact, use precautions with using the bathroom and other daily activities in days following treatment. Patient education is necessary to ensure safe daily practices. Several ongoing trials are evaluating lutetium Lu 177 vipivotide tetraxetan in combination with other anticancer agents for treatment of mCRPC, using different dosing strategies, or in other settings (metastatic castration-sensitive prostate cancer and early-stage prostate cancer). Conclusion: Lutetium Lu 177 vipivotide tetraxetan is an effective and well tolerated treatment for patients with mCRPC, PSMA-positive metastases after progressing on an androgen receptor pathway inhibitor ± docetaxel. Ongoing studies evaluating its use in earlier disease stages and with different dosing strategies, will better define the role of this therapy in the treatment of prostate cancer.
