Immune checkpoint inhibitors: Interaction between PD-1 and PD-L1  blocked by therapeutic antibodies
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Yesterday, Boehringer Ingelheim announced it is acquiring Nerio Therapeutics, which has novel checkpoint inhibitors, for up to $1.3 billion. The pharma company aims to develop this program as a “potential key centerpiece component for its immuno-oncology portfolio,” according to a release. Nerio’s small molecules inhibit the proteins tyrosine phosphatases N1 and N2 (PTPN1 and PTPN2), which act as immune checkpoints and can activate the immune system to fight cancer cells. 

The checkpoint inhibitor market is one of the world’s fastest growing and most lucrative. Almost a dozen such drugs have been approved in the last ten years. The global market was estimated to be worth over $40B in 2022 and is projected to reach almost $190B by 2032.

“Securing the rights to Nerio Therapeutics’ novel checkpoint inhibitors creates a broad panel of exciting new cancer treatment combination opportunities,” said Paola Casarosa, member of the board of managing directors at Boehringer Ingelheim with responsibility for the Innovation Unit.

Checkpoint inhibitors have transformed the cancer treatment landscape. However, while they work very well in some, they not work for all. Only half of patients are eligible, and it’s estimated that only between 15% and 30% of those treated will respond. 

Tremendous research is ongoing to improve the outcomes with current checkpoint inhibitors. New targets are also being explored. PD-(L)1, CTLA-4 and LAG-3 are well established, novel targets include ICOS, VISTA, TIGIT, CD112R, BTLA, TIM-3, GITR, NKG2A.

Boehringer Ingelheim aims to extend the benefits of immuno-oncology to more cancer patients. The pharma currently focuses on four key areas of cancer research: T cell engagers, cancer vaccines, oncolytic viruses and immune & stromal modulation.The company says Nerio’s small molecule inhibitors will be an important addition to the pharma’s portfolio with the potential to act as a single agent therapy and, importantly, in combination with many cancer therapies already being developed in-house.

Sanford Madigan, partner at Avalon BioVentures, L.P. and co-founder and CEO of Nerio Therapeutics, said, “We believe Nerio’s small molecule PTPN1/N2 inhibitors have superior drug-like properties and provide a first-in-class opportunity. We are excited to expand Boehringer Ingelheim’s pipeline and commend their commitment to unlock the full potential of our compounds and their mechanistically unique approach to fighting cancer.” 

Nerio Therapeutics  is focused on phosphatases, a hard-to-drug class. The company’s selective PTPN2/N1 inhibitors novel, potent, and highly with drug-like properties. These checkpoint inhibitors are novel, first-in-class, and enhance immune function and sensitize tumors to pro-inflammatory signals, promoting anti-tumor activity. 

Nerio was founded by Avalon Ventures and had additional financial support from a syndicate including Bregua Corporation, Correlation Ventures, Alexandria Venture Investments and Viva BioInnovator. The company was developed in the Avalon BioVentures accelerator.

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