Alkylphosphocholine analogs for broad-spectrum cancer imaging and therapy

Jamey P. Weichert*, Paul A. Clark, Irawati K. Kandela, Abram M. Vaccaro, William Clarke, Marc A. Longino, Anatoly N. Pinchuk, Mohammed Farhoud, Kyle I. Swanson, John M. Floberg, Joseph Grudzinski, Benjamin Titz, Anne M. Traynor, Hong En Chen, Lance T. Hall, Christopher J. Pazoles, Perry J. Pickhardt, John S. Kuo

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

54 Scopus citations


Many solid tumors contain an overabundance of phospholipid ethers relative to normal cells. Capitalizing on this difference, we created cancer-targeted alkylphosphocholine (APC) analogs through structure-activity analyses. Depending on the iodine isotope used, radioiodinated APC analog CLR1404 was used as either a positron emission tomography (PET) imaging (124I) or molecular radiotherapeutic (131I) agent. CLR1404 analogs displayed prolonged tumor-selective retention in 55 in vivo rodent and human cancer and cancer stem cell models. 131I-CLR1404 also displayed efficacy (tumor growth suppression and survival extension) in a wide range of human tumor xenograft models. Human PET/CT (computed tomography) and SPECT (single-photon emission computed tomography)/CT imaging in advanced-cancer patients with 124I-CLR1404 or 131I-CLR1404, respectively, demonstrated selective uptake and prolonged retention in both primary and metastatic malignant tumors. Combined application of these chemically identical APC-based radioisosteres will enable personalized dual modality cancer therapy of using molecular 124I-CLR1404 tumor imaging for planning 131I-CLR1404 therapy.

Original languageEnglish (US)
Article number240ra75
JournalScience translational medicine
Issue number240
StatePublished - Jun 11 2014

ASJC Scopus subject areas

  • Medicine(all)

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