Novartis expands targeted radioligand therapy pipeline with in-license for compounds targeting Fibroblast Activation Protein (FAP)

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Algemeen advies 30/03/2021 13:26
- Expands Novartis Oncology radioligand pipeline with exclusive worldwide rights to develop and commercialize therapeutic applications for a library of FAP assets including FAPI-46 and FAPI-74

- Broad expression of FAP demonstrated in tumors or in tumor stroma across many solid tumors1,2,3

- Novartis Oncology continues to reimagine cancer care through development of robust radioligand therapy portfolio

Basel, March 30, 2021 — Novartis has obtained exclusive worldwide rights to develop and commercialize therapeutic applications for a library of Fibroblast Activation Protein (FAP) targeting agents including FAPI-46 and FAPI-74, through an assignment agreement with iTheranostics, Inc., an affiliate of SOFIE Biosciences, Inc. The FAP assets were originally developed at the University of Heidelberg. The agreement also includes co-exclusive rights for Novartis to develop imaging applications for these assets.

Fibroblast activation protein (FAP) is a cell-surface protein expressed at low levels in most normal adult tissues, but over-expressed in common cancers, particularly on cancer-associated fibroblasts that form the tumor stroma, which is essential for growth1,2,3,4. High FAP expression on cancer-associated fibroblasts is generally associated with worse prognosis in solid tumors due to promotion of tumorigenesis and progression4,5,6,7.

“We continue to invest in radioligand therapy as one of the four unique platforms of Novartis Oncology. We believe working across multiple approaches is the key to reimagining cancer care,” said Susanne Schaffert, PhD, President, Novartis Oncology. “FAP is an exciting target and these agents are a great fit with our radioligand therapy pipeline, which we are actively investigating across multiple tumor types. We believe this technology has the potential to transform many patients’ lives.”

Targeted radioligand therapy is a type of precision medicine combining two key elements: a targeting compound, or ligand, and a radioactive isotope, causing DNA damage that inhibits tumor growth and replication. These targeted drugs bind to markers or proteins over-expressed by certain tumors, or tumor-associated tissue, such as stroma. Due to the high-affinity of these agents for specific tumor cells or associated tumor tissue, surrounding healthy tissue is less affected.

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Park JE, Lenter MC, Zimmermann RN, Garin-Chesa P, Old LJ, Rettig WJ. Fibroblast activation protein, a dual specificity serine protease expressed in reactive human tumor stromal fibroblasts. J Biol Chem. 1999;274(51):36505-12.
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Saigusa S, Toiyama Y, Tanaka K, et al. Cancer-associated fibroblasts correlate with poor prognosis in rectal cancer after chemoradiotherapy. Int J Oncol 2011;38: 655-663. doi: 10.3892/ijo.2011.906.

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