Diapeutic cancer-targeting alkylphosphocholine analogs may advance management of brain malignancies

Written by Zhang RR, Swanson KI, Hall LT, Weichert JP, Kuo JS

The following is a special report on alkylphosphocholine analogs as targeted imaging and therapy agents for cancer, and their potential role in diagnosis and treatment in glioblastoma and brain metastases. These novel cancer-targeting agents display impressive tumor avidity with low background in the normal brain, and multimodal diagnostic imaging and therapy capabilities. The use of these agents may significantly improve diagnosis, treatment and post-treatment follow-up in patients with brain malignancies.
‘Theranostics’ are defined as diagnostic tests that inform treatment choice and clinical outcome. To improve patient outcomes, theranostics would ideally be used in therapy decision-making to predict treatment efficacy and response, and change clinical management by avoiding unnecessary risks and associated costs of ineffective care [1,2]. Optimizing therapeutic efficacy and safety is especially warranted in treating primary brain tumors or brain metastases, where tumor cells are infiltrating or adjacent to vital functional brain tissue, and deleterious side effects carry significant morbidity and mortality. Therefore, theranostics can have transformative implications in managing brain tumor patients. In this report, we highlight alkylphosphocholine (APC) analogs as a special theranostics type: the ‘diapeutic’ (diagnostic imaging and therapy) agent. APC analogs have a cancer-selective retention mechanism mediated by an identical cancer-targeting chemical backbone, exhibit broad specificity for tumor cells in multimodal imaging and therapy, and could predict, inform and monitor therapy outcomes. We discuss how this versatility may ultimately transform clinical management of primary and metastatic brain tumors.

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