LSK BioPharma (LSKB), a privately-held biopharmaceutical company, and the University of Utah’s Huntsman Cancer Institute (HCI), one of the world’s top academic research and cancer treatment centres, have entered into an exclusive license agreement to develop and commercialise HCI-1401, an orally bioavailable, small molecule, irreversible inhibitor of Bruton’s tyrosine kinase (BTK).

Under the terms of the agreement, HCI awarded LSKB global rights in all therapeutic indications of HCI-1401. Financial terms of the deal have not been disclosed.

“BTK inhibitors are an exciting class of drugs not only because of their proven efficacy in B-cell cancers but because of their potential in other disease areas as well. With recent clinical findings highlighting the emergence of resistance mutations against the BTK inhibitor ibrutinib, there is an acute need for new compounds that maintain their activity in cancers that acquire these mutations,” said Sunil Sharma, M.D., HCI’s senior director of clinical research and division chief of oncology.

HCI-1401 was developed by HCI’s Center for Investigational Therapeutics and was selectively designed to have excellent oral bioavailability while inhibiting the BTK enzyme, a mediator of several pro-survival mechanisms in B-cell cancers. In addition to showing high potency inhibiting normal BTK, HCI-1401 was designed to maintain its activity against the commonly mutated form of BTK that gives resistance to other BTK inhibitors such as ibrutinib.

Preclinical in vitro data shows that HCI-1401 is several times more potent in inhibiting BTK than other competitive inhibitors. LSKB and HCI expect HCI-1401 to enter into clinical trials next year and to have clinical utility in fighting certain B-cell mediated malignancies as well as in autoimmune and inflammatory diseases such as rheumatoid arthritis and systemic lupus erythematosus.

“Huntsman Cancer Institute has made significant progress in the research and development of HCI-1401, and we look forward to bringing this molecule closer to application in cancer and autoimmune disorders,” said LSKB president, Dr. Sung Chul Kim.