Tarveda Therapeutics has dosed the first patient in a Phase I/IIa trial designed to evaluate PEN-866 to treat patients with advanced solid tumours.

The multi-centre dose escalation and expansion trial will investigate the safety and efficacy across a range of tumour types including those previously reported to be sensitive to topoisomerase 1 inhibitors.

The Phase IIa portion of the trial, which has started enrolling patients, will include patients with small cell lung cancer as well as GI-midgut and pancreatic neuroendocrine tumours that express somatostatin receptor 2 (SSTR2).

"This innovative approach of a drug conjugate which uses an HSP90 inhibitor is a promising treatment for patients with cancer."

PEN-866 is a miniature conjugate that selectively binds to the intracellular target Heat Shock Protein 90 (HSP90) and is associated with SN-38, a known and potent anti-cancer payload.

The trial principal investigator Anish Thomas said: “This innovative approach of a drug conjugate which uses an HSP90 inhibitor to facilitate intracellular, tumour-targeted delivery of the topoisomerase 1 inhibitor SN-38 is a promising treatment for patients with cancer.

“Preclinical studies of PEN-866 by a number of groups, including National Cancer Institute (NCI) researchers, have demonstrated efficacy and durability of response in multiple preclinical patient-derived and xenograft tumor models in a wide range of tumour types.

“Patients with these cancers are very much in need of effective new treatment options.”

Tarveda Therapeutics president and CEO Drew Fromkin noted that several evidences are currently available to demonstrate that HSP90 is upregulated and activated in tumours.

Fromkin said: “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 tumour types versus normal tissue.”