Enzymes that drive cancer growth are already addressed by several drugs, but there’s still room to improve and expand this approach. BeiGene sees opportunity in the lead program of Ensem Therapeutics and it’s licensing global rights to a small molecule ready to start its first test in humans.
Per deal terms announced Tuesday, BeiGene is committing up to $1.33 billion, a sum that includes an unspecified upfront payment as well as potential milestone payments.
The three FDA-approved cyclin-dependent kinase (CDK) inhibitors block the enzymes CDK 4 and 6. These products—Ibrance from Pfizer, Kisqali from Novartis, and Eli Lilly’s Verenzio—are all blockbuster sellers as treatments for breast cancer. Ensem’s lead program, ETX-197, blocks the CDK2 enzyme, which is hyperactivated in certain cancers. Ensem has said its drug could help patients whose cancers have acquired resistance due to CDK2 dysregulation. BeiGene views this molecule as complementary to its own cancer pipeline.
“We are committed to developing novel molecules with the potential to transform the therapeutic landscape for cancer patients, and this partnership fits well with our strategic focus on breast cancer as an area with tremendous unmet need for innovative treatment options,” Lai Wang, BeiGene’s Global Head of R&D, said in a prepared statement. “This CDK2 inhibitor from Ensem complements our internally discovered Phase 1 CDK4 inhibitor, which has the potential to improve upon current CDK4/6 inhibitors in some breast cancer patients, and strengthens our early development pipeline in breast cancer and other solid tumors.”
Ensem discovers drugs with Kinetic Ensemble, a platform technology that employs molecular simulation and artificial intelligence to identify “cryptic pockets,” non-obvious binding locations for its small molecules. The startup was incubated by CBC Group, a Singapore-based healthcare investment firm.
Last year, Ensem announced it had raised $67 million in Series A financing to support its work researching new small molecules for difficult-to-drug cancer targets. At the time, the startup did not say which targets it was pursuing.
Ensem’s remaining pipeline includes potential drugs addressing mutant versions of the PI3K alpha enzyme, whose overactivation contributes to cancer metastasis. FDA scrutiny on the safety of PI3K inhibitors has led several companies to withdraw their products from the market. On its website, Ensem says believes its PI3K alpha inhibitor will be both more potent and selective to its target. The company has additional discovery-stage programs in development for cancer.
Public domain image by Stuart S. Martin via the National Cancer Institute