177Lu-PSMA-617 (Pluvicto)
Overview
177Lu-PSMA-617 is a radioligand therapeutic consisting of a small peptide-based ligand targeting prostate-specific membrane antigen (PSMA) conjugated to the beta-emitting radioisotope lutetium-177. The peptide component binds selectively to PSMA, a transmembrane protein highly expressed on prostate cancer cells, enabling targeted delivery of cytotoxic radiation to tumor sites while sparing normal tissues. It is indicated for treatment of metastatic castration-resistant prostate cancer in patients previously treated with androgen receptor pathway inhibition and taxane-based chemotherapy. The targeting moiety is derived from a urea-based peptidomimetic scaffold optimized for PSMA affinity.
Key Research Findings
177Lu-PSMA-617 received FDA approval in March 2022 based on the VISION trial (NEJM 2021), a randomized phase 3 study demonstrating significant improvements in overall survival (median 15.3 vs 11.3 months) and radiographic progression-free survival compared to standard of care alone. The trial enrolled 831 patients with PSMA-positive metastatic castration-resistant prostate cancer. Treatment-related adverse events included myelosuppression and dry mouth, with the majority of events being grade 1 or 2.
Intravenous
FDA Approved
Interested in 177Lu-PSMA-617 (Pluvicto)?
Find a verified provider experienced with 177Lu-PSMA-617 (Pluvicto) protocols in your area. All providers are credentialed and use compliant sourcing.
Find a 177Lu-PSMA-617 (Pluvicto) ProviderRelated Peptides
Carfilzomib (Kyprolis)
FDA ApprovedA tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds the chymotrypsin-like (beta5) subunit of the 20S proteasome. By blocking proteasomal degradation of ubiquitinated proteins, carfilzomib causes accumulation of misfolded proteins, endoplasmic reticulum stress, and activation of the unfolded protein response, leading to apoptosis preferentially in malignant plasma cells. Its irreversible binding confers greater proteasome inhibition than bortezomib.
Bortezomib (Velcade)
FDA ApprovedA modified dipeptidyl boronic acid that reversibly inhibits the chymotrypsin-like activity of the 26S proteasome. Bortezomib disrupts the ubiquitin-proteasome pathway, stabilizing pro-apoptotic factors and inhibiting NF-kB activation, which is constitutively active in many hematologic malignancies. It was the first proteasome inhibitor approved for cancer treatment and fundamentally changed the treatment landscape of multiple myeloma.
Lutetium-177 dotatate (Lutathera)
FDA ApprovedA radiolabeled somatostatin analog consisting of the peptide DOTA-Tyr3-octreotate chelated to the beta-emitting radioisotope lutetium-177. Lutathera binds with high affinity to somatostatin receptor subtype 2 (SSTR2), which is overexpressed on neuroendocrine tumor cells, delivering targeted radiation therapy directly to tumor cells while sparing surrounding normal tissue. This peptide receptor radionuclide therapy (PRRT) approach combines receptor-targeted delivery with cytotoxic radiation.
Leuprolide (Lupron) - Oncology
FDA ApprovedA GnRH agonist used in oncology for androgen deprivation therapy (ADT) in prostate cancer and hormone suppression in premenopausal breast cancer. Chronic administration produces sustained downregulation of pituitary GnRH receptors, achieving medical castration with testosterone levels below 50 ng/dL. The initial testosterone flare can be mitigated by co-administration of an antiandrogen. Depot formulations provide sustained release for up to 6 months.