On August 5, 2020 ARC Therapeutics, a development-stage pharmaceutical company developing small molecule inhibitors of cyclin-dependent kinases (CDKs) for the treatment of advanced and resistant cancers,reported that launched with a $6 million financing led by founding investor Eshelman Ventures LLC (Press release, ARC Therapeutics, AUG 5, 2020, View Source [SID1234562961]). With this financing, ARC Therapeutics has executed an exclusive license agreement with G1 Therapeutics for its preclinical CDK2 inhibitor program and will utilize remaining proceeds to advance this program into the clinic.
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Uncontrolled cellular proliferation is a hallmark of cancer and is commonly driven by dysregulated kinase activity of specific CDK family members. Recent advances in cancer treatment using CDK inhibition have focused on targeting CDK4/6, key mediators of cell cycle progression. While this therapeutic approach has provided significant clinical benefit to patients with ER+/HER2- metastatic breast cancer, many tumors activate other CDK family members to drive uncontrolled proliferation. As a result, primary resistance has limited the broad clinical utility of CDK4/6 inhibitors. Those that do respond inevitably develop acquired resistance, resulting in tumor progression and limiting the drug’s effectiveness.
"The clinical success of CDK4/6 inhibitors demonstrates the practice-changing outcomes that can be achieved by therapeutically targeting specific CDK family members," said Patrick Roberts, Ph.D., Pharm.D., Chief Executive Officer and Co-Founder of ARC Therapeutics. "CDK2 is a known driver of abnormal cancer cell proliferation and is an important therapeutic target of unmet need. Our team is excited to apply its knowledge and expertise in developing potent and selective CDK inhibitors toward the development of a CDK2 inhibitor that has significant promise to advance the current standard of care for people living with cancer."
Scientific Approach
With an initial focus on developing a novel, potent, and selective inhibitor of CDK2 to treat patients whose tumors are insensitive to CDK4/6 inhibition, the founding scientific team at ARC Therapeutic is applying rational design and stringent screening criteria to select a candidate CDK2 inhibitor.
"Historical efforts to target CDK2 have been unsuccessful due to an inability to design or identify potent and selective CDK2 inhibitors," said Jay Strum, Ph.D., Chief Scientific Officer and Co-Founder of ARC Therapeutics. "The rational design approach we used to develop inhibitors selective for CDK4/6 versus CDK2 at G1 Therapeutics led to a keen understanding of key structural features within the CDK2 binding pocket that can be exploited to develop a potent and selective CDK2 inhibitor. At ARC Therapeutics, we now have an incredible opportunity to effectively treat patients with advanced and resistant cancers."
ARC Therapeutics entered into an exclusive license for the IP covering G1 Therapeutics’ preclinical CDK2 inhibitor program. Under the terms of the agreement, G1 Therapeutics received an upfront payment and equity in ARC Therapeutics.
Founding Team
ARC Therapeutics was founded by a group of experts with robust drug design, discovery, and development experience. As senior members of the scientific team that successfully identified and advanced three oncology compounds into the clinic at G1 Therapeutics, including a first-in-class myelopreservation therapy, a potential best-in-class differentiated oral CDK4/6 inhibitor and an oral selective estrogen receptor degrader (SERD), the team will apply its unique, multidisciplinary expertise and knowledge to pursue novel cancer treatments and drive programs in an expeditious manner.
"This team has an ideal combination of complementary experience and expertise to select the best compounds and bring them to the clinic," said Fred Eshelman, Pharm.D., co-founder and chairman of ARC Therapeutics and founder of Eshelman Ventures LLC. "I am confident in this team’s ability to successfully discover and develop inhibitors of CDK proteins and realize the company’s mission of improving the lives of patients with advanced and resistant cancers."