On April 24, 2018 Tarveda Therapeutics, Inc., a clinical stage biopharmaceutical company discovering and developing Pentarins as a new class of potent and selective cancer medicines, reported that it has dosed the first patient in a Phase 1/2a study evaluating PEN-866 in patients with advanced solid tumors (Press release, Tarveda Therapeutics, APR 24, 2018, View Source [SID1234525654]). miniature drug conjugate that selectively binds to the intracellular target Heat Shock Protein 90 (HSP90) and is linked to SN-38, a known and potent anti-cancer payload. The multi-center, dose escalation and expansion study will assess safety and efficacy across a range of tumor types including those previously shown to be sensitive to topoisomerase 1 inhibitors. This includes but is not limited to small cell lung, pancreatic, triple negative breast, colon and ovarian cancers and sarcomas.
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"This innovative approach of a drug conjugate which uses an HSP90 inhibitor to facilitate intracellular, tumor-targeted delivery of the topoisomerase 1 inhibitor SN-38 is a promising treatment for patients with cancer," said Anish Thomas, MBBS, M.D., Lasker Clinical Research Scholar and Principal Investigator, Developmental Therapeutics Branch, Center for Cancer Research, at the National Cancer Institute (NCI), part of the National Institutes of Health (NIH). "Preclinical studies of PEN-866 by a number of groups, including NCI researchers, have demonstrated efficacy and durability of response in multiple preclinical patient-derived and xenograft tumor models in a wide range of tumor types. Patients with these cancers are very much in need of effective new treatment options." Dr. Thomas and Dr. Yves Pommier, NCI’s Developmental Therapeutics Branch, are collaborating with Tarveda through a Cooperative Research and Development Agreement (CRADA).
Drew Fromkin, President and Chief Executive Officer of Tarveda commented, "There exists a large body of evidence demonstrating that HSP90 is upregulated and activated in tumors. This results in a change in HSP90’s binding conformation allowing for the extended retention and accumulation of cancer cell killing payloads in diverse, difficult-to-treat tumor types versus normal tissue. The dosing of our first patient with PEN-866 is a major accomplishment for our Company and demonstrates our commitment to linking potent, anti-cancer payloads to HSP90 small molecule targeting ligands."
Earlier this year, Tarveda announced plans to initiate the Phase 2a portion of the Phase 1/2a clinical trial for PEN-221, a Pentarin miniature conjugate designed to selectively bind to solid tumors expressing somatostatin receptor 2 (SSTR2). The Phase 2a portion of the trial has now been initiated and enrollment has begun in patients with small cell lung cancer as well as GI-midgut and pancreatic neuroendocrine tumors that express SSTR2.
The company is actively advancing its two clinical stage programs, PEN-221 and PEN-866, and other novel pre-clinical miniature conjugates.
Additional information on clinical trials being conducted by Tarveda is available at clinicaltrials.gov, through identifier number NCT03221400 for PEN-866 and NCT02936323 for PEN-221. Patients interested in enrolling in the PEN-866 clinical trial can contact Tarveda at [email protected] or call the National Cancer Institute’s toll-free number 1-800-4-Cancer (1-800-422-6237) (TTY: 1-800-332-8615).
About PEN-866
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.
About Pentarins
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.