Tarveda Therapeutics Provides Year-End Update and Outlines Milestones for 2017

• Raised $38 Million Series C to Fund Clinical and Discovery Pipeline of Pentarin Miniaturized Drug Conjugates
• Phase 1/2a Trial of PEN-221 in Neuroendocrine and Small Cell Lung Cancer Patients Initiated in 2016
• Phase 1/2a Trial of PEN-866 in Topo-1 Inhibitor Sensitive Cancer Patients to Begin in 2017

WATERTOWN, MA — January 4, 2017 — Tarveda Therapeutics, Inc., a clinical stage biopharmaceutical company discovering and developing Pentarins™ as a new class of potent and selective anti-cancer medicines, today provided highlights from 2016 and outlined expected milestones for 2017.

"2016 was a year of transformative progress for Tarveda’s Pentarin platform and acceleration in the development of our novel treatments to improve the effectiveness of cancer therapies for patients with solid tumors. The company raised substantial capital and strengthened its premier venture capital syndicate, completed the in-licensing of PEN-866, which will be in a Phase I clinical trial in 2017, and embarked on our first-in-human trial for our lead drug candidate PEN-221," said Drew Fromkin, President and Chief Executive Officer of Tarveda. "We have constructed an attractive pipeline of novel, anti-cancer medicines, built a solid foundation on which to create true value for patients and our Company’s stakeholders, and look forward to achieving additional, validating milestones in 2017.”

Key 2016 Accomplishments

• Secured $38 million in Series C financing co-led by Novo A/S and New Enterprise Associates (NEA) with Flagship Pioneering, NanoDimension and Eminent Venture Capital also participating
• Concentrated the Company’s development and discovery resources on Tarveda’s Pentarin Platform through the spin-off of BTP-114 to Placon Therapeutics. BTP-114 is a next-generation, platinum-based chemotherapy that is now in a Phase I clinical trial in collaboration with a domestic pharmaceutical partner
• Expanded clinical program and R&D expertise with the appointment of Leila Alland, M.D. to Chief Medical Officer. Dr. Alland brings more than 15 years of pharmaceutical drug development experience including her most recent leadership roles in oncology clinical development at AstraZeneca and Bristol-Myers Squibb
• In-licensed the broad Heat Shock Protein 90 (HSP90) targeting conjugate platform, including lead drug PEN-866, from Madrigal Pharmaceuticals
  • Miniaturized HSP90 targeting drug conjugates are designed to have high affinity for the well-characterized intracellular target, HSP90, and increase the killing of cancer cells while reducing collateral damage to normal cells
  • PEN-866 accumulates and is retained in xenograft tumors, releasing over time the potent tumor-killing payload SN-38, the active component of the approved anticancer medicine, irinotecan
  • PEN-866 has shown efficacy and durability of response in multiple preclinical tumor models including small cell lung, pancreatic, and ovarian cancers, sarcoma and patient derived tumor models
• Presented preclinical data for PEN-221 demonstrating complete and sustained tumor regressions in hard-to-treat, somatostatin receptor 2 (SSTR2) positive cancer models
  • Miniaturized size and unique design of Pentarins such as PEN-221 allow for rapid penetration deep into solid tumors to drive efficacy
  • PEN-221 binds with high affinity to the cell surface target, SSTR2, internalizes into the tumor cell and releases its DM1 payload, which is retained in the tumor cell long after PEN-221 is cleared from circulation
• Initiated a first-in-human Phase 1/2a trial of PEN-221 at multiple, premier clinical sites in the United States
  • The Phase 1/2a study of PEN-221 selects patients most likely to respond to PEN-221 by using FDA approved imaging diagnostics to identify those with tumors expressing SSTR2

Expected Key 2017 Milestones

• Complete PEN-221 Phase 1 dose escalation and identify the recommended Phase 2 dose of PEN-221 in patients with SSTR2 expressing neuroendocrine tumors and small cell lung cancer in 2017
• Initiate the first-in-human trial of PEN-866 in 2017, a Phase 1/2a dose escalation/expansion study evaluating safety and efficacy of PEN-866 in advanced, topoisomerase-1 sensitive cancer patients
• Report preclinical data in 2017 on new Pentarins™ that bind to intracellular and cell-surface targets and drive anti-tumor activity
• Announce the Tarveda Scientific Advisory Board in the first quarter of 2017

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 HSP90 targeting 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. www.tarveda.com