Pipeline

We are developing a pipeline of theragnostic pairings for oncology indications. AAA’s theragnostic platform involves radiolabeling a targeting molecule with either gallium Ga 68 for diagnostic use, or lutetium Lu 177 for therapy.

Investigational Candidates in Clinical Development:

Disease

Preclinical

Phase I

Phase II

Phase III

Prostate cancer
Phase I

177LuPSMA-R2

Therapeutic
Prostate cancer
Phase I

68GaPSMA-R2

PET Diagnostic
Prostate cancer
Phase I

CTT1057

18F PET Diagnostic
Gastrointestinal stromal tumors, Prostate cancer, Breast cancer
Preclinical

177LuNeoBOMB1

Therapeutic
Gastrointestinal stromal tumors, Prostate cancer, Breast cancer
Phase I

68GaNeoBOMB1

PET Diagnostic
Glioblastoma, others
Preclinical

177LuFF-10158

Therapeutic
Glioblastoma, others
Preclinical

68GaFF-10158

PET Diagnostic
Apoptosis and necrosis
Phase II

99MTc-rhAnnexin V-128

SPECT Diagnostic

177LuPSMA-R2 and 68GaPSMA-R2. 177LuPSMAR2 and 68GaPSMA-R2 are in development to treat, image, monitor and stage prostate cancer. PSMA-R2 is a ligand of Prostate-Specific Membrane Antigen (PSMA), expressed on the majority of prostate tumor cells. 177LuPSMA-R2 is being developed to treat prostate cancer and 68GaPSMA-R2 is under development as its complementary diagnostic. AAA has signed an exclusive license agreement with Johns Hopkins University in Baltimore, Maryland to develop and market PSMA-R2 for prostate cancer. Phase I/II studies for 177LuPSMA-R2 and 68GaPSMA-R2 were initiated in 2018.

CTT1057. CTT1057 is an 18F-labeled investigational diagnostic candidate in development for PET imaging of prostate cancer. CTT1057 is a phosphoramidate-based peptide, which specifically binds to Prostate-Specific Membrane Antigen (PSMA), expressed on the majority of prostate tumor cells. AAA has signed an exclusive worldwide license agreement with Cancer Targeted Technology, LLC (CTT) to develop CTT1057 for PET imaging of prostate cancer. A Phase 1 study evaluating the safety, biodistribution and dosimetry of CTT1057 was completed by the University of California, San Francisco.

177LuNeoBOMB1 and 68GaNeoBOMB1. 177LuNeoBOMB1 and 68GaNeoBOMB1 are new generation antagonist bombesin analogs in development to treat, image, monitor and stage gastrin-releasing peptide receptor (GRPR)-expressing malignancies, such as such as gastrointestinal stromal tumors (GIST), prostate cancer and breast cancer. 177LuNeoBOMB1 is a therapeutic candidate and 68GaNeoBOMB1 is its complementary diagnostic candidate. AAA has signed an exclusive license agreement with Erasmus University Medical Center (UMC) and Demokritos National Center for Scientific Research to develop NeoBOMB1. A Phase I/IIa study of 68GaNeoBOMB1 for diagnostic use in GIST is ongoing, and a Phase II study in other GRPR-expressing tumors was initiated in mid-2018.

177LuFF-10158 and 68GaFF-10158. 177LuFF-10158 and 68GaFF-10158 are preclinical small molecule antagonists with high affinity for integrin alphavbeta3 (⍺vβ3) and alphavbeta5 (⍺vβ5) 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, including particularly highly vascularized tumors and metastases. In preclinical studies, blocking integrin signaling has been shown to inhibit tumor growth, angiogenesis (formation of blood vessels) and metastasis. AAA has signed an exclusive option and license agreement with FUJIFILM Toyama Chemical Co,. LTD to develop and commercialize radiolabeled FF-10158 for oncology indications. Among the first potential indications planned for investigation is glioblastoma, an orphan disease with high unmet medical need.

99MTc-rhAnnexin V-128. 99MTc-rhAnnexin V-128 is a Single Photon Emission Computed Tomography (SPECT) investigational candidate for the diagnosis and assessment of apoptotic and necrotic processes, which are present in a number of pathological conditions in oncology and cardiovascular disease, as well as in autoimmune disorders. A Phase I trial of Annexin V-128 was conducted at the University of Ottawa Heart Institute in Canada to assess its safety, tolerability, biodistribution and dosimetry. 99MTc-rhAnnexin V-128 is currently in a Phase I/II trial for the diagnosis of rheumatoid arthritis and ankylosing spondylitis, as well as several Phase II studies in cardiovascular, cardio-oncology, and pulmonary indications.