Tarveda Therapeutics, Inc., a clinical stage biopharmaceutical company discovering and developing Pentarins as a new class of potent and selective cancer medicines, announced on 4/24/18 that it has dosed the first patient in a Phase 1/2a study evaluating PEN-866 in patients with advanced solid tumors. PEN-866 is a 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.

“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).

Tarveda’s proprietary Pentarins are miniature drug conjugates, a class of cancer therapeutics uniquely designed to target, penetrate and treat solid tumors. Pentarins are designed to maintain their miniature size and overcome biological barriers in solid tumors through two distinct capabilities as highlighted in the name “PENTARIN”. On Tarveda's website they note the origins of the name:

• Effective penetration:  The PEN in Pentarin represents the penetration into solid tumors.
• Tumor cell targeting:  The TAR in Pentarin represents the selective tumor cell targeting.

They describe the benefits of the Pentarin approach as including:

• Penetration deep into the tumor
• Targeting Ligands
• Accumulation deep into the tumor
• Linker Chemistry tuned for sustained release inside the tumor while limiting release outside the tumor
• Selected payloads
• Tuned pharmacokinetics to enhance tumor uptake while limiting duration of circulation in the bloodstream.

The company's Pentarin platform allows for the rapid development of drug candidates to target solid tumors.