Tarveda Therapeutics to Present Preclinical Data on PEN-866 in Combination with PARP Inhibitors at the 2018 AACR Annual Meeting
Published: Apr 17, 2018
|Combination of the miniature drug conjugate PEN-866 with PARP inhibitors as a rational approach to overcoming limitations of PARP inhibitor monotherapy|
|April 18, 2018|
|8:00 AM – 12:00 PM CT|
|Section 37, McCormick Place North/South, Chicago, IL|
PEN-866 exploits the activation of Heat Shock Protein 90 (HSP90) in tumors to accumulate and release its potent anti-cancer payload, SN-38. PEN-866 is a miniature conjugate that comprises a small molecule, HSP90-targeting ligand linked to SN-38, the active metabolite of irinotecan. The conjugate accumulates and is retained in tumors, and by way of a sustained release of SN-38, causes prolonged DNA damage and tumor regressions in multiple patient-derived and other xenograft tumor models.
Tarveda is developing Pentarins™, potent and selective miniature 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 cancer cell killing agent through a tuned 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 rapid and deep penetration 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, Inc.
Tarveda Therapeutics, Inc. discovers and develops Pentarins™, a new class of potent and selective miniature drug conjugates with enhanced targeting capabilities for the treatment of a wide range of solid tumor cancers. Tarveda’s lead Pentarin drug candidate, PEN-221, is a miniature drug conjugate that targets the somatostatin receptor 2 (SSTR2) for treatment of patients with neuroendocrine, prostate, small cell lung and other cancers that express SSTR2. PEN-221 comprises a highly selective peptide for SSTR2 conjugated to the potent cytotoxic payload, DM1, through a tuned cleavable linker. Tarveda is also advancing its Pentarin HSP90 drug conjugate platform with lead drug candidate PEN-866, which is a miniature drug conjugate that selectively binds to the intracellular target, Heat Shock Protein 90 (HSP90), and is linked to the payload 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 pharmaceutical collaborators. www.tarveda.com
MacDougall Biomedical Communications
George E. MacDougall, 781-235-3060
Source: Tarveda Therapeutics, Inc.