Mercator and Pepscan Collaborate to Fine-Tune Peptide-Based Anticancer Agents

Pepscan’s CLIPS platform will be used to optimize Mercator’s homing peptides.

Mercator Therapeutics and Pepscan Therapeutics have entered a multiprogram research collaboration through which Mercator’s homing peptides will be optimized using Pepscan’s CLIPS technology.

The homing peptides are discovered through an in vivo screening process that includes screening in consenting end-stage cancer patients. These peptides have been demonstrated in vivo to bind to receptors that are highly expressed on human tumors and induce internalization of both the peptide and the receptor.

Pepscan’s CLIPS technology will be applied to improve the potency and stability of peptides by locking the peptides into the biologically active conformation. “Pepscan’s approach to peptide optimization is unique, systematic, fast, and efficient, and it provides Mercator with an opportunity to rapidly move its peptide-drug conjugates (PDCs) into development,” remarks Roy Lobb, D.Phil., chairman and CSO of Mercator.

Under the terms of the research and license agreement, Pepscan will license to Mercator the associated intellectual property rights. Mercator will pay Pepscan research funding, milestones, and royalties in connection with the development of optimized homing peptides and the development and commercialization of PDC products that couple optimized homing peptides with tumor-killing payloads.

Mercator Therapeutics was founded to translate the research of Renata Pasqualini, Ph.D., and Wadih Arap, M.D., Ph.D., into effective cancer therapeutics. Drs. Pasqualini and Arap are using in vivo phage display to identify peptides that are believed to selectively deliver tumor-killing payloads without damaging surrounding tissue.

They are targeting drugs selectively to tumors by directly injecting peptide-expressing phage libraries in vivo—most recently in end-stage cancer patients under strict ethical guidelines—and identifying a suite of peptides responsible for tumor targeting.

Pepscan Therapeutics is a privately held company based in Lelystad, The Netherlands. Its CLIPS protein mimicking technology (chemical linkage of peptides onto scaffolds) presents one or more peptides in a structurally constrained configuration. These molecules behave as functional mimics of complex protein domains. Pepscan has used this platform to develop anti-GPCR mAb products and has various collaborations with pharmaceutical and biotech companies to develop therapeutics based on the CLIPS technology.