• Novel small molecule FF-10158 targets integrin alphavbeta3 (avβ3) and alphavbeta5 (avβ5) receptors
  • Expands theragnostic pipeline 
  • Potential broad application in the detection and treatment of highly vascularized tumors and metastases

SAINT-GENIS-POUILLY, France I December 03, 2018 I Advanced Accelerator Applications S.A. (AAA), a Novartis company and leader in nuclear medicine theragnostics, today announced that it has entered into an exclusive option and license agreement with FUJIFILM Toyama Chemical, a leading radiopharmaceutical company in Japan, to develop and commercialize radiolabeled FF-10158 for oncology indications. Under the terms of the agreement, AAA is granted worldwide rights to FF-10158, with the exception of Japan, in exchange for an upfront payment and future milestones and royalties.

FF-10158 is a pre-clinical small molecule antagonist with high affinity for integrin alphavbeta3 (avβ3) and alphavbeta5 (avβ5) receptors. Integrins are cell surface receptors that are embedded in the cell membrane. Integrin alphavbeta3/5 subtypes are over expressed on many types of cancer cells and the blocking of integrin signalling has been shown to inhibit tumor growth, angiogenesis (formation of blood vessels) and metastasis1,2,3. AAA plans to develop a theragnostic pairing of compounds based on FF-10158, including a gallium 68-labeled drug for diagnosis and a lutetium 177-labeled drug for therapy.

“Our goal is to develop radiopharmaceuticals that transform oncology treatment,” said Susanne Schaffert, Ph.D., President, Advanced Accelerator Applications. “The in-licensing of FF-10158 expands our oncology theragnostic pipeline and we believe that this approach to integrating diagnostics and therapeutics has the potential to change patient management.”

Among the first potential indications planned for investigation is glioblastoma, an orphan disease with high unmet medical need. Increased alphavbeta3 expression on glioblastoma is associated with invasive growth and poor survival4,5. Integrin-targeted delivery of radionuclides has been explored in pre-clinical models of glioblastoma6.

FUJIFILM Toyama Chemical contributes to healthcare through the research and development, manufacturing and distribution of radiopharmaceuticals as well as other kinds of therapeutic drugs in Japan. The company is responsible for core elements of the healthcare business of FUJIFILM Corporation, that seeks to expand its business in the areas of disease prevention, diagnosis, and treatment. Currently, FUJIFILM Toyama Chemical offers Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET) diagnostics, therapeutic radiopharmaceuticals and small molecule pharmaceutical products.

About Advanced Accelerator Applications S.A.

Advanced Accelerator Applications, a Novartis company, is an innovative radiopharmaceutical company developing, producing and commercializing radioligand theragnostics (pairings of therapeutic and diagnostic drugs based on the same targeting molecule) for oncology. AAA is an established leader in radiopharmaceuticals for Positron Emission tomography (PET) and Single-Photon Emission Computed Tomography (SPECT) diagnostic imaging, mainly used in clinical oncology, cardiology and neurology. For more information, please visit: https://www.adacap.com/.

References

  1. Liu Z, Wang F, Chen X. Integrin αvβ3-Targeted Cancer Therapy. Drug Dev Res. 2008; 69(6): 329–339.
  2. Sun C, Qu X, Gao Z. Integrins: players in cancer progression and targets in cancer therapy. Anti-Cancer Drugs. 2014; 25:1107–1121.
  3. Raab-Westphal S, Marchall JF, Goodman SL. Integrins as therapeutic Targets: Successes and Cancers. Cancers 2017; Sep; 9(9): 110.
  4. Albeda SM, Mette SA, Elder D.E., Stewart R, Damjanovich L, Herlyn M, Buck CA. Integrin distribution in malignant melanoma: Association of the beta 3 subunit with tumor progression. Cancer Res. 1990; 50, 6757–6764.
  5. Gladson CL, Cheresh DA. Glioblastoma expression of vitronectin and the alpha v beta 3 integrin. Adhesion mechanism for transformed glial cells. J. Clin. Investig. 1991; 88, 1924–1932.
  6. Veeravagu A, Liu Z, Niu G, Chen K, Jia B, Cai W, Jin C, Hsu AR, Connolly AJ, Tse V, Wang IF, Chen X. Integrin alphavbeta3-targeted radioimmunotherapy of glioblastoma multiforme. Clin Cancer Res. 2008 (in press).

SOURCE: Advanced Accelerator Applications