Israel’s Kitov Pharmaceuticals Holdings is taking a majority equity stake in cancer immunotherapeutics firm TyrNovo to expand its own noncancer pipeline with TyrNovo’s preclinical-stage small-molecule candidate NT219. The IRS1/2 (insulin receptor substrates 1 and 2) and STAT3 (signal transducer and activator of transcription 3) inhibitor is designed to prevent acquired drug resistance and is in preclinical development against multiple tumor types. Kitov will initially acquire a 56% stake in TyrNovo from the latter’s major shareholder for $2 million in cash and $1.8 million in Kitov shares. The firm said it may subsequently increase its stake through the acquisition of additional equity from all or part of TyrNovo’s additional minority shareholders. TyrNovo is developing NT219 under an exclusive license from Yissum, the research development company of the Hebrew University of Jerusalem.

“The TyrNovo acquisition represents a major milestone in Kitov's strategic vision of establishing a diverse pipeline that we believe will secure long-term value creation for its shareholders,” stated Dr. Paul Waymack, M.D., Sc.D., Kitov's chairman and chief medical officer. “NT219 can be developed as a platform combination drug for overcoming multidrug resistance often observed in various tumors. It has the potential to be developed as a combination therapy with several approved oncology drugs for multiple types of tumors.”

NT219 is designed to degrade the checkpoint inhibitor IRS1/2 and block STAT3, both to prevent tumors from developing drug resistance and reduce multidrug resistance in tumors that have already become refractive to treatment. Kitov says preclinical studies have demonstrated that combining NT219 with approved anticancer drugs results in potent antitumor effects and increases survival in models of sarcoma, melanoma, pancreatic, lung, ovarian, head and neck, prostate, and colon cancers.

Kitov also confirmed that it aims to file an NDA for its own lead product KIT-302 during Q1 2017. KIT-302 is a patented combination of celecoxib and amlopidine besylate, which has been developed as a dual therapy for the simultaneous treatment of osteoarthritis pain and hypertension. A second combination therapy, KIT-301, which includes naproxen, is also in development for the same indication.

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