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Onzigolide (TBR-760) is a first-in-class chimeric molecule, often referred to as a "dopastatin," developed by Tiburio Therapeutics (a PureTech Health company) for the treatment of non-functioning pituitary adenomas (NFPA). It is engineered to simultaneously target and activate the dopamine D2 receptor (DRD2) and somatostatin receptor subtypes 2 and 5 (SSTR2 and SSTR5). These receptors are frequently co-expressed on the surface of pituitary tumor cells, and their dual activation is hypothesized to exert synergistic inhibitory effects on tumor cell proliferation and hormone secretion. Onzigolide reached Phase 2 clinical development (NCT04393792) for patients with NFPA where surgical intervention was insufficient or not an option. However, the program was terminated in 2021 for strategic business reasons rather than safety or efficacy concerns.
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