Proteolysis-targeting chimeras (PROTACs)

Arvinas Inc., Astrazeneca and Pfizer are among the companies working on PROTACs, alongside research groups such as Chinese Academy of Sciences CAS and Fudan University. Arvinas’ pipeline includes degraders targeting estrogen and androgen receptors, while Pfizer partners on vepdegestrant. Patent and research activity also points to companies including Paq Therapeutics and Dark Blue Therapeutics.

Chinese Academy of Sciences CAS has 161 recent-window documents, China Pharmaceutical University has 97, and the University of Chinese Academy of Sciences has 83. These organizations are active in degrader discovery and related research. Zhejiang University also has 82 recent-window documents, including work on BRD9 and androgen-receptor degraders.

The funding data records $38,344,896 in grants across 99 awards since 2020. This is grant support associated with the topic, not a complete measure of company financing or all investment in targeted protein degradation. The listed funding rounds include activity across many fields, so they should not be treated as PROTAC-specific totals.

Astrazeneca leads the listed patent holders with 7 patents, followed by Dana-Farber Cancer Institute and Shenzhen Zhongge Biological Technology Co. with 6 each. Tsinghua University, Hangzhou Zhongmei Huadong Pharmaceutical Co., Gan & Lee Pharmaceutical, Hinova Pharmaceuticals Inc and The Brigham And Womens Hospital each have 5.

No: patent activity declined 33.3% in the latest 12-month period compared with the previous 12 months, with 270 patents in the 24-month window. Publication activity moved in the opposite direction, growing 32.8% to 1,591 publications last year. This contrast suggests research is expanding faster than recent patent filings.

PROTACs have reached clinical validation: vepdegestrant received FDA approval in May 2026, and the topic records 19 clinical-trial documents overall. That milestone does not remove development challenges. Drug-like exposure, selectivity, delivery and the quality of target degradation remain important considerations as the modality moves into broader clinical use.

Recent developments include vepdegestrant’s FDA approval in May 2026 and RP04340, an orally active pan-KRAS degrader reported by Fudan University and Risen Pharma in September 2026. Other recent work examines predictive PROTAC design, linker effects on CDK degradation selectivity, and KLHL12 as a potentially tumor-selective E3 ligase.

CRBN-recruiting PROTACs are the largest listed approach, with 669 documents; VHL-recruiting has 241, and MDM2-recruiting has 105. The approaches differ in the E3 ligase they bring to the target. Ligase choice affects the chance of forming a productive degradation complex, while expression patterns and biology can influence selectivity and safety.

Oncology is the largest listed application, with 1,114 documents and 102 patents in the window. Other areas include neurodegenerative disease, infectious disease, metabolic disease, and autoimmune and inflammatory disease. Recent work on viral proteins and inflammatory targets illustrates efforts to extend degradation beyond cancer, though each use case has distinct delivery and target-selection challenges.

China leads the listed activity with 3,815 documents, followed by the United States with 3,707 and the United Kingdom with 1,266. China accounts for 37.4% of the documented activity and the United States 36.4%. The figures show substantial research activity in both China and the United States, with contributions from Europe and other regions.