Sartate (67Cu MeCOSar octreotate)

P1/2, N=21, Terminated, Clarity Pharmaceuticals Ltd | Trial primary completion date: Oct 2024 --> Jan 2025

P1/2, N=21, Terminated, Clarity Pharmaceuticals Ltd | N=34 --> 21 | Trial completion date: Dec 2028 --> Mar 2025 | Recruiting --> Terminated | Trial primary completion date: Dec 2028 --> Oct 2024; Sponsor decision

Therefore, in this work, we carefully analyzed the key dynamical features and detailed molecular interactions of SSTR2 in complex with six radiopharmaceutical compounds selected among the few already in use (Cu/Ga-DOTATATE, Ga-DOTATOC, Cu-SARTATE) and some in clinical development (Ga-DOTANOC, Cu-TETATATE)...We thus unveiled detailed molecular interactions crucial for the recognition of this class of radiopharmaceuticals. The microscopically well-founded analysis presented in this study provides guidelines for the design of new potent ligands targeting SSTR2.

Further clinical studies will be required to examine the therapeutic dose required for [Cu]Cu-SARTATE for various indications. In addition, the ability to use predictive copper-64 based dosimetry for treatment planning with copper-67 should be further explored.

In recent years, however, several new tracers were designed exploiting the many potential targets of the neuroendocrine cell and were employed in clinical trials for both imaging and therapy. Currently, the real-life clinical impact of these tracers is still mostly not known; however, the favourable biodistribution (e.g. [68Ga]Ga-FAPI, SSTR antagonists) and the possibility to use new theranostic pairs may provide novel diagnostic as well as therapeutic options (e.g. [68Ga]Ga-PSMA, [64Cu]Cu-SARTATE, [68Ga]Ga-CXCR4) for NEN patients.

MRD may be detected by [Cu]Cu-SARTATE and subsequently treated by [Cu]Cu-SARTATE. Since therapeutic dosimetry estimation of the latter agent from the uptake of the former one in the initial diagnostic scan was not addressed, the present theoretical commentary proposes the derivation of an abbreviated therapy-dosimetric equation for the companion diagnostic/therapeutic [/Cu]Cu-SARTATE that might be of interest for future clinical theranostic practice.