Tarveda’s lead Pentarin®, PEN-221, is based on the company’s know-how and intellectual property from our Pentarin platform. PEN-221 is a miniature drug conjugate containing a peptide ligand that is highly selective in targeting, and dependent on, the somatostatin receptor SSTR2. This somatostatin receptor is overexpressed on the surface of cancer cells in a variety of neuroendocrine cancers, including small cell lung cancer. Our team rapidly engineered PEN-221 with its modified peptide ligand, which is chemically linked in a unique and optimized fashion to the potent cell-killing payload DM1, to achieve the desired efficacy and pharmacokinetic and biodistribution attributes.

PEN-221 exemplifies the implementation of the Pentarin platform and was optimized through a deep understanding of target biology, ligands to receptors, linker chemistries, and payloads. In preclinical studies, PEN-221 has demonstrated deep tumor penetration with complete tumor regressions in multiple, hard to treat xenograft cancer models and has demonstrated superiority to the clinical standard of care, while a mixture of the unconjugated payload with a targeting peptide shows no efficacy. PEN-221 is in a Phase 1/2a clinical trial.