First-in-Human Experience of CXCR4-Directed Endoradiotherapy with 177Lu- and 90Y-Labeled Pentixather in Advanced-Stage Multiple Myeloma with Extensive Intra- and Extramedullary Disease

J Nucl Med. 2016 Feb;57(2):248-51. doi: 10.2967/jnumed.115.167361. Epub 2015 Nov 12.

Abstract

Chemokine receptor 4 (CXCR4) is a key factor for tumor growth and metastasis in several types of human cancer. Based on promising experiences with a radiolabeled CXCR4 ligand ((68)Ga-pentixafor) for diagnostic receptor targeting, (177)Lu- and (90)Y-pentixather were recently developed as endoradiotherapeutic vectors. Here, we summarize the first-in-human experience in 3 heavily pretreated patients with intramedullary and extensive extramedullary manifestations of multiple myeloma undergoing CXCR4-directed endoradiotherapy.

Methods: CXCR4 target expression was demonstrated by baseline (68)Ga-pentixafor PET. Each treatment was approved by the clinical ethics committee. Pretherapeutic (177)Lu-pentixather dosimetry was performed before (177)Lu-pentixather or (90)Y-pentixather treatment. Subsequently, patients underwent additional chemotherapy and autologous stem cell transplantation for bone marrow rescue.

Results: A remarkable therapeutic effect was visualized in 2 patients, who showed a significant reduction in (18)F-FDG uptake.

Conclusion: CXCR4-targeted radiotherapy with pentixather appears to be a promising novel treatment option in combination with cytotoxic chemotherapy and autologous stem cell transplantation, especially for patients with advanced multiple myeloma.

Keywords: CXCR4; endoradiotherapy; multiple myeloma; pentixather.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Antineoplastic Agents / therapeutic use
  • Bone Marrow Transplantation
  • Combined Modality Therapy
  • Female
  • Fluorodeoxyglucose F18 / pharmacokinetics
  • Humans
  • Male
  • Middle Aged
  • Multiple Myeloma / diagnostic imaging
  • Multiple Myeloma / radiotherapy*
  • Neoplasm Metastasis
  • Peptides / therapeutic use*
  • Radiometry
  • Radionuclide Imaging
  • Radiopharmaceuticals / therapeutic use*
  • Receptors, CXCR4 / drug effects*
  • Treatment Outcome

Substances

  • 177Lu-pentixather
  • 90Y-pentixather
  • Antineoplastic Agents
  • Peptides
  • Radiopharmaceuticals
  • Receptors, CXCR4
  • Fluorodeoxyglucose F18