On April 13, 2021 Theseus Pharmaceuticals, a biotechnology company shaping the future of targeted oncology by developing best-in-class, pan-variant kinase inhibitors, emerged from stealth reported the close of a $100 million Series B financing led by Foresite Capital (Press release, Theseus Pharmaceuticals, APR 13, 2021, View Source [SID1234577973]). Theseus also announced data from a poster presentation at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) 2021 Annual Meeting, which demonstrated that the Company’s lead product candidate, THE-630, has potent activity against all major classes of activating and resistance mutations observed in patients with KIT-mutant gastrointestinal stromal tumors (GIST).
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OrbiMed incubated Theseus to develop therapies designed to outsmart treatment-resistant cancer mutations, funding the Company’s Series A in 2018. In addition to Foresite Capital, the Series B raise was supported by a syndicate of other new investors, including Adage Capital Management, Boxer Capital, Farallon Capital Management, Longitude Capital, Nextech Ventures, Omega Funds, Pontifax Venture Capital, Rock Springs Capital, and T. Rowe Price, as well as OrbiMed. In conjunction with the financing, Michael Rome, Ph.D., Managing Director of Foresite Capital, has joined the Theseus Board of Directors, which also includes Carl Gordon, General Partner at OrbiMed.
"We are thrilled by the validation of this discerning group of investors and welcome Michael to Theseus’ board of directors," said William C. Shakespeare, Ph.D., Co-founder and President of Research and Development at Theseus Pharmaceuticals. "For many driver-oncogene targets, current standard-of-care kinase inhibitors have insufficient activity to cover the broad array of variants that could lead to resistance, so they are limited by constantly mutating cancer. At Theseus, we take a pan-variant approach to targeting oncogenes with kinase inhibitors specifically designed to retain their effectiveness even as cancer mutates. Using sophisticated assays, we can predict how cancers will change, enabling new therapies to stay ahead of future mutations and overcome the demonstrated burden of treatment resistance."
Theseus is developing a pipeline of pan-variant tyrosine kinase inhibitors (TKIs) that can anticipate and inhibit new cancer mutations. The Company’s lead candidate, THE-630, is a next-generation pan-variant KIT inhibitor in development for the treatment of refractory GIST. The Company expects to file an IND before the end of the year. Theseus’ pipeline also includes a selective EGFR inhibitor to overcome C797S-mediated resistance to first- or later-line osimertinib treatment for patients with non-small cell lung cancer, and a third kinase target candidate for an undisclosed indication.
Iain Dukes, D. Phil., Co-founder and Interim CEO of Theseus Pharmaceuticals, and Venture Partner of OrbiMed, commented, "The scientific co-founders of Theseus are a team of distinguished drug discovery and development leaders who have pioneered the development of pan-variant kinase inhibitors. Together at ARIAD Pharmaceuticals, they discovered and developed multiple kinase inhibitors in areas of high clinical need, two of which they brought to market, ponatinib and brigatinib, and a third, mobocertinib, that is now in late-stage clinical development. With this foundation of expertise, combined with the backing of a top-tier syndicate of investors, Theseus is well positioned to develop best-in-class, pan-variant TKIs that provide durable benefit for people living with cancer."
At the AACR (Free AACR Whitepaper) meeting, Theseus presented preclinical data demonstrating that THE-630 has potent activity against all classes of activating and resistance mutations observed in KIT-mutated GIST. These data showed that THE-630 was highly efficacious in tumor models containing mutations that confer resistance to approved TKIs. These data highlight the potential for a pan-variant inhibitor such as THE-630 to deliver meaningful clinical benefit for patients with refractory GIST. The presentation can be found on Theseus’ website.