Exelixis, Cybrexa Pen $700 Million Deal Over Peptide-Drug Conjugate

Oncology-focused Exelixis is making a move to claim Cybrexa’s clinical-stage peptide-drug conjugate (PDC), CBX-12, agreeing on a deal that could net Cybrexa over $700 million. The new agreement highlights Exelixis’ push to expand its clinical pipeline of targeted drug therapy. 

Under the terms of the deal outlined in Exelixis’ filing to the SEC, Exelixis will pay $60 million upfront for the right to acquire CBX-12, which is in Phase 1. The company will foot the bill for the clinical advancement and manufacturing of CBX-12 under an agreed development plan, while Cybrexa could receive up to $65 million in development milestones. Provided that CBX-12 meets pre-specified goals in Phase 1, Exelixis will exercise its right to buy the drug for $300 million. If everything goes smoothly, Cybrexa could expect $277.5 million in milestone payments regarding CBX-12. 

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Enhancing Delivery While Minimizing Toxicity 

CBX-12 utilizes Cybrexa’s alphalex technology that enhances the delivery of anti-cancer compounds to the site of the tumor, thereby reducing systemic exposure and toxicity. It is composed of a pH-Low Insertion Peptide (pHLIP), a linker, and exatecan. pHLIP selectively activates in the low pH environment of the tumor, forming an alpha-helical structure that inserts into and across the tumor membrane. The linker is cleaved within the cell to release the payload, which in this case is exatecan, a topoisomerase I inhibitor. 

The antigen-independent approach may be suitable for patients who are not suitable for antigen-targeting therapies such as monoclonal antibodies and antibody-drug conjugates (ADCs). CBX-12 has the potential as a component in combination therapies and immunotherapies and could also be a complement to ADCs, Cybrexa said. 

Results from the ongoing Phase 1 of CBX-12 in metastatic solid tumor showed anti-tumor activity in the heavily-pretreated patient population. This included a complete response in a patient with ovarian cancer, Cybrexa said. 

“Robust preclinical data and initial clinical data from the ongoing phase 1 trial suggest that CBX-12 may provide differentiated clinical benefit in several solid tumors. said Michael Morrissey, Ph.D., President and CEO of Exelixis. 

“Similar to our interest in antibody-drug conjugates, we believe this novel peptide-drug conjugate has transformative clinical potential, and this collaboration affords us the opportunity to expand our clinical pipeline with a best-in-class exatecan therapy if additional CBX-12 clinical data demonstrate enhanced safety and efficacy,” he said. 

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Joy Lin

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