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

Filing

Approved

Marketed

Neuroendocrine tumors
Marketed

*LUTATHERA® (USAN: lutetium Lu 177 dotatate/INN: lutetium (177Lu) oxodotreotide)

Therapeutic
Neuroendocrine tumors
Marketed

*NETSPOT® (gallium Ga 68 dotatate)

PET Diagnostic
Neuroendocrine tumors
Marketed

*SOMAKIT TOC® (gallium (Ga 68) edotreotide)

PET Diagnostic
Apoptosis and necrosis
Phase II

99MTc-rhAnnexin V-128

SPECT Diagnostic
Prostate cancer
Phase I

177LuPSMA-R2

Therapeutic
Prostate cancer
Phase I

68GaPSMA-R2

PET Diagnostic
Prostate cancer
Phase I

CTT1057

18F PET Diagnostic
GI, Prostate, Breast, Lung cancers
Preclinical

177LuNeoBOMB1

Therapeutic
GI, Prostate, Breast, Lung cancers
Phase I

68GaNeoBOMB1

PET Diagnostic

LUTATHERA® (USAN: Lutetium Lu 177 dotatate/INN: Lutetium (177Lu) oxodotreotide). LUTATHERA® is a Lu-177-labeled somatostatin analogue peptide. LUTATHERA® was approved by the FDA in January 2018, and by the European Commission in September 2017. LUTATHERA® also received orphan drug designation from the FDA and EMA.

NETSPOT® (gallium Ga 68 dotatate) and SOMAKIT TOC® (gallium (Ga 68) edotreotide). NETSPOT® was approved by the FDA in June 2016, and SOMAKIT TOC® was approved by the European Commission in December 2016. These products have received orphan drug designation from the FDA and EMA.

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.

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 in metastatic prostate cancer are ongoing.

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 conducted at 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. A Phase I study of 177LuNeoBOMB1 was initiated in mid-2018.

*See full Prescribing Information for approved indications and important safety information.