Key trends driving the emergence of targeted radiotherapeutics as an oncology therapeutic pillar

Research Contributors: Andris Ortmanis, Sr. Director & Anita Zutshi, Associate Director

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Targeted radiopharmaceuticals are transforming cancer treatment by enabling systemically delivered radiotherapy to be integrated into diagnostic workup algorithms and personalized medicine treatment strategies across a range of tumors.

The FDA and EMA have approved two radioligand therapies for the treatment of cancer, LUTATHERA (GEP-NETs) and PLUVICTO (mCRPC). Both agents were acquired by market leader Novartis while in pivotal development and delivered global revenue of $1.8B in 2023. Novartis projects PLUVICTO alone has >$3B global market potential, which underscores the commercial and therapeutic impact of the expanding pipeline of radioligand therapeutics.

Targeted radiopharmaceuticals may become the ultimate focal therapy by enabling the delivery of lethal radiation to malignant tissue – with minimal healthy tissue involvement. The specific structure of a radiopharmaceutical depends on the intended application but consists of a radioisotope payload associated with a small molecule ligand or monoclonal antibody to target malignant tissue.

Figure 1: Therapeutic RLTs and their companion diagnostic counterparts generally only differ in their associated radioisotopes, with either beta (e.g. 177-Lu, 67-Cu, 131-I) or alpha (e.g. 225-Ac, 227-Th) emitters used therapeutically, and positron-emitting radioisotopes (e.g. 68-Ga, 18-F) used for diagnostic purposes. This enables the personalized radiotherapy to be delivered with the same construct that was used to visualize and characterize the tumor diagnostically.

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