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WATERTOWN, MA — January 4, 2017 — Tarveda Therapeutics, Inc., a biopharmaceutical company discovering and developing Pentarins™ as a new class of potent and selective anti-cancer medicines, today announced that a Phase 1/2a clinical trial evaluating PEN-221 in patients with advanced neuroendocrine tumors and small cell lung cancer expressing the somatostatin receptor 2 (SSTR2) is underway, with patients enrolled and treated. The somatostatin receptor is highly expressed in neuroendocrine cancers. PEN-221 is a novel, miniaturized drug conjugate designed to selectively target SSTR2 and then internalize and release its potent DM1 payload in the tumor cell.

“Pentarins are engineered to rapidly penetrate and kill solid tumors that have proven challenging for treatment modalities such as antibody drug conjugates and chemotherapeutics,” said Gordon B. Mills, M.D., Ph.D., Professor and Chair, Department of Systems Biology, at The University of Texas MD Anderson Cancer Center, Houston, TX. “The miniaturized size, unique design and potent payloads of Pentarins allow for sustained payload release in solid tumors to drive potential efficacy while sparing normal tissue.

“PEN-221 has high affinity for the SSTR2 on the surface of neuroendocrine and small cell lung cancer cells, which facilitates internalization followed by release of its potent cell-killing payload, DM1. Pentarins offer a new treatment approach to address the deficits of current treatments, and PEN-221 has the potential to address the urgent and significant medical need of patients with neuroendocrine and small cell lung cancers. Having an imaging approach to identify neuroendocrine and small cell lung cancers expressing the somatostatin receptor 2 makes the PEN-221 trial an exciting proof-of-concept as well as an opportunity for patients with these challenging tumors,” concluded Mills.

The Phase 1/2a first-in-human study is an open-label, multicenter trial to assess the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of PEN-221 in patients with SSTR2-expressing advanced neuroendocrine cancers, including a range of neuroendocrine tumors and small cell lung cancer. Utilizing FDA-approved imaging diagnostics, the study employs a seamless, Phase 1/2a design that identifies and selects advanced cancer patients with SSTR2 expressing tumors. These patients are believed to be the most likely to benefit from treatment with PEN-221. For additional information on this clinical trial, please visit, identifier number NCT02936323.

“The initiation of this Phase 1/2a clinical trial of PEN-221 in patients with neuroendocrine tumors and small cell lung cancer marks an important milestone in the development of this product candidate and our Pentarin drug conjugates,” said Leila Alland, M.D., Chief Medical Officer of Tarveda. “PEN-221 consistently demonstrated complete and durable regressions in hard-to-treat xenograft cancer models. We and our industry leading clinical investigators are excited to advance this therapy into the clinic.”

About Pentarins™

Tarveda is developing Pentarins, potent and selective miniaturized drug conjugates with high affinity for specific cell surface and intracellular targets. Pentarins are engineered to bind to their tumor cell targets and provide sustained release of their potent therapeutic payloads deep into solid tumor tissue. Comprised of a targeting ligand conjugated to a potent cell-killing agent through a chemical linker, Pentarins are designed to overcome the deficits of both larger antibody drug conjugates and small molecules that limit their therapeutic effectiveness against solid tumors. Together, the components of Tarveda’s Pentarins have distinct, yet synergistic, anticancer attributes: the small size of Pentarins allows for effective penetration and distribution into the tumor tissue, the ligand’s targeting ability allows for specific binding and retention in tumor cells, and the chemical linker is tuned to optimize the release of the potent, cell-killing payload inside the cancer cells for efficacy.

About Tarveda Therapeutics

Tarveda Therapeutics, Inc. discovers and develops Pentarins™, a new class of potent and selective miniaturized drug conjugates with enhanced targeting capabilities for the treatment of solid cancer tumors. Tarveda’s lead Pentarin drug candidate, PEN-221, is a miniaturized drug conjugate that targets the somatostatin receptor 2 (SSTR2) for treatment of patients with neuroendocrine and small cell lung cancers. PEN-221 comprises a highly selective peptide that targets SSTR2 linked to the potent cytotoxic DM1 through a cleavable linker. Tarveda is also advancing its HSP90 drug conjugate platform with lead drug candidate PEN-866, which is a miniaturized drug conjugate that comprises a small molecule HSP90 targeting ligand conjugated to SN-38, the highly-potent, active metabolite of irinotecan. Tarveda’s strategy includes developing its own proprietary Pentarins as well as applying the Pentarin platform to enhance the effectiveness of the targeting moieties and novel payloads of its pharmaceutical collaborators.