Clinical-stage pharmaceutical company Karyopharm Therapeutics has started its Phase Ib trial of oral SINE Selinexor, KPT-330, in patients with advanced soft tissue or bone sarcomas.

By specifically and irreversibly inhibiting the nuclear export protein Exportin 1 (XPO1 or CRM1), SINE compounds force the nuclear localisation and activation of multiple tumour suppressor proteins leading to selective killing of tumour cells.

Selinexor becomes the first oral SINE XPO1 antagonist to enter human clinical trials.

Karyopharm founder and research and development president Dr Sharon Shacham said the initiation of Phase Ib trial of Selinexor was an important step forward in the clinical development of the drug candidate.

"It is crucial with oral drugs to determine the effect of food on absorption," Shacham said.

"It is crucial with oral drugs to determine the effect of food on absorption."

"In addition, we anticipate that Selinexor tablets may be the formulation used in future studies so we look forward to data on that formulation."

The open-label study is designed to assess the effects of food and formulations like capsules and tablets on the absorption of oral Selinexor and to determine its anti-tumour activity in sarcoma patients with progressed disease on existing therapies.

A total of 20 patients will be enrolled in the US and Canada in the study, which is being initiated based on the observations of preliminary evidence of anti-cancer activity of Selinexor in clinical trials.

NPM Pharma is managing the trial on behalf of Karyopharm in Toronto, Canada, and the US.

Image: Optical Coherence Tomography (OCT) image of a sarcoma. Photo: courtesy of Dr Stephen Boppart, Biophotonics Imaging Laboratory, University of Illinois at Urbana-Champaign. EB 005221.