Exelixis In-Licenses Iconic Therapeutics’ Tissue Factor-Targeting Antibody-Drug Conjugate Ahead of Planned Investigational New Drug Application

On December 2, 2020 Exelixis, Inc. (Nasdaq: EXEL), Iconic Therapeutics, Inc. (Iconic) and Zymeworks Inc. (NYSE:ZYME) reported that Exelixis has exercised its exclusive option for Iconic’s lead oncology antibody-drug conjugate (ADC) program under the companies’ May 2019 agreement (Press release, Exelixis, DEC 2, 2020, View Source [SID1234572090]). As a result, Exelixis now has responsibility for the future clinical development, commercialization, and manufacturing of the Tissue Factor (TF)-targeting ADC now known as XB002 (formerly ICON-2). A rationally designed next-generation ADC, XB002 comprises a Tissue Factor-targeting antibody with Zymeworks’ proprietary ZymeLink linker-payload, creating the potential for an improved therapeutic index and favorable safety profile as compared to earlier-generation, TF-targeting ADCs. Exelixis plans to file an Investigational New Drug application (IND) with the U.S. Food and Drug Administration (FDA) for XB002 in the near-term and, pending the FDA’s acceptance of the IND, initiate a phase 1 clinical trial of XB002 in early 2021.

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"XB002 is an important addition to the Exelixis pipeline given its potential differentiation from other Tissue Factor-targeting antibody-drug conjugates and its status as the first program in our growing biologics portfolio to reach IND filing stage," said Peter Lamb, Ph.D., Executive Vice President and Chief Scientific Officer of Exelixis. "Iconic designed a highly promising molecule and advanced it through a rigorous preclinical evaluation, setting the stage for Exelixis to complete our planned IND filing in the coming weeks. We are grateful for Iconic’s partnership over the past 18 months and look forward to fully evaluating the potential of XB002 to help patients with cancer."

Under the terms of the May 2019 agreement between Exelixis and Iconic, Exelixis gained an exclusive option to license XB002 (then ICON-2) in exchange for an upfront payment to Iconic of $7.5 million and a commitment of preclinical development funding. In exercising its exclusive option, Exelixis has made an additional option exercise payment of $20 million to Iconic. Iconic is now also eligible for future development, regulatory and commercialization milestone payments, as well as royalties on potential sales. The ZymeLink ADC technology in XB002 was originally licensed to Iconic from Zymeworks. Under the terms of their 2019 agreement, Zymeworks will receive a share of the $20 million option fee and is eligible to receive a share of all future revenue received by Iconic, as well as tiered royalties on worldwide sales.

"Exelixis’ decision to in-license our lead oncology program provides important validation of Iconic’s discovery and development capabilities, our platform of proprietary anti-Tissue Factor molecules designed to efficiently but safely bind Tissue Factor, and the potential of Tissue Factor as an oncology antibody-drug conjugate target," said William L. Greene, M.D., Chief Executive Officer of Iconic Therapeutics. "Preclinical data presented earlier this year demonstrate that XB002 binds Tissue Factor without affecting the coagulation cascade, which has hindered prior development of Tissue Factor-targeting molecules, has activity in multiple solid tumor cancer models and has improved tolerability compared to other Tissue Factor-targeting ADCs. We are excited to see XB002 make further progress as part of Exelixis’ highly-regarded clinical development organization."

"We are excited to see this promising molecule take an important step towards clinical trials backed by the experienced clinical team at Exelixis," said Tony Polverino, Ph.D., Executive Vice President, Early Development and Chief Scientific Officer of Zymeworks. "This would mark the second ZymeLink-based therapeutic to enter the clinic in addition to our bispecific HER2 antibody-drug conjugate, ZW49, further highlighting the differentiative potential of our novel antibody-drug conjugate platform."

Pending the completion of Exelixis’ planned IND and the FDA’s acceptance of the filing, Exelixis intends to initiate a phase 1 dose escalation and expansion study of XB002 in subjects with inoperable locally advanced or metastatic solid tumors early in 2021.