BeiGene stakes out space in hot cancer niche, offering up $1.3B in biobucks for preclinical prospect

BeiGene is buying its way into a cancer niche targeted by Bayer, Blueprint Medicines, Incyte and Pfizer, striking a backloaded, $1.33 billion deal for a global license to Ensem Therapeutics’ CDK2 inhibitor.

CDK2, a kinase, is implicated in cancers of the breast, ovaries, uterus, stomach and esophagus. Notably, research suggests the cell cycle regulator is involved in the changes that render breast cancers resistant to CDK4/6 inhibitors such as Pfizer’s Ibrance, Novartis’ Kisqali and Eli Lilly’s Verzenio. Inhibiting the target may therefore unlock a range of opportunities in solid tumors, although toxicity is a challenge.

Ensem, a biotech that emerged last year with a $67 million series A round, identified the challenge as a good fit for its Kinetic Ensemble platform. The platform combines computational approaches, such as AI models for predicting pockets, and experimental technologies to identify non-obvious binding sites. 

Applying the capabilities to CDK2 has yielded ETX-197, an oral kinase inhibitor that Ensem is pitching as a best-in-class candidate. Ensem sees a role for the molecule in the treatment of cancer patients who have acquired resistance to standard of care because of the dysregulation of CDK2 activity.

BeiGene is a believer. The Chinese-American biotech has struck a deal for ETX-197. In return for an upfront fee of undisclosed size, plus milestones that could swell the value of the deal to $1.33 billion, BeiGene has secured global rights to a candidate that is ready for regulatory filings to study in humans. 

“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,” said Lai Wang, Ph.D., global head of R&D at BeiGene. “We are excited to work with Ensem to bring this molecule into the clinic in the near future.” 

As a preclinical prospect, ETX-197 is toward the back of the CDK2 race. Pfizer shared phase 1 data on its candidate earlier this year and is three years into a study that is testing the molecule in multiple tumor types and in combination with a clutch of other therapies. Incyte’s INCB123667 and Blueprint’s BLU-222 are in the clinic, too, while Bayer disclosed a CDK2 deal with the now-shuttered Cedilla Therapeutics in June.