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Following is a market landscape on targeted protein degradation (TPD) covering leading organizations, technologies, and experts based on ResoluteAI’s systematic review from the following ResoluteAI datasets: patents, clinical trials, grants, news, publications, and tech transfer. This review provides insight into:
- Research and investment trends
- Leading companies, universities, inventors, and researchers
- Technologies available for licensing
- PROTACs and emerging TPD strategies
- Scatter analysis by therapeutic area
All tables, graphs and heat maps were generated using ResoluteAI’s discovery engine, Foundation.
Patent analysis
Let’s begin by exploring the last 20 years of TPD patent activity with results from USPTO, EPO, and WIPO. Where we see a 10x increase in published patents in application, and granted, status since 2002:
TPD patent applications and grants over the last 20 years
Search String Used: (targeted protein degradation)
By narrowing our patent search to the last 10 years and filtering to patent families that have been cited 10+ times, we can identify the organizations with the largest TPD patent portfolios:
Protein degradation patents by assignee name and family size
Search String Used:(("protein degradation"~2) AND (target))
Respectively, leading inventors using the same search parameters as outlined above include many names found on the 4th Annual Targeted Protein Degradation Summit's attendee list and are highlighted below:
Protein degradation patents by inventor name, assignee name, and family size
Search String Used:(("protein degradation"~2) AND (target))
By using the same search parameters as above and changing our view to a Graph-based search instead of a Heatmap, we identify groups of diseases and disorders that TPD patented technology aim to treat:
Diseases and disorders that TPD patented technology aim to treatSearch String Used:(("protein degradation"~2) AND (target))
Among some of the major “undruggable” subgroups found in ResoluteAI’s patent search include:
- Alzheimer’s Disease
Leading Patent Assignee: Arvinas - Amyotrophic Lateral Sclerosis (ALS)
Leading Patent Assignee: Arvinas - Angelman Syndrome
Leading Patent Assignee: Arvinas - SARS-CoV-2
Leading Patent Assignee: Neutrolis - Lysosomal Storage Disease
Leading Patent Assignee: Global Bio Therapeutics - Multiple Sclerosis
Leading Patent Assignee: Arvinas - Parkinson’s Disease
Leading Patent Assignee: Arvinas - Various Cancers
Leading Patent Assignee: Arvinas
Publication analysis
When searching for TPD-related publications from PubMed, Crossref, arXiv, bioRxiv, and medRxiv; we notice the annual growth rate for new publications follows the same trajectory as published patents.
TPD publications over the last 20 years
Search String Used: (targeted protein degradation)
The 30 Most Frequently published organizations researching TPD since 2011 include:
The 30 most frequently published organizations researching TPD since 2011Search String Used: (targeted protein degradation)
The 10 Most Frequently published authors in the last 10 years and their 10 most frequently used MeSH Qualifiers are connected below via a Sankey Diagram:
The 10 most frequently published authors on TPD and their 10 most frequently used MeSH qualifiers since 2011
Search String Used:(("targeted protein degradation"~2) OR (PROTAC) OR (LYTAC) OR (PHOTAC) OR (MADTAC))
Alessio Ciulli (Amphista & University of Dundee) and Craig Crews (Arvinas & Yale) are two leading TPD Authors. By using ResoluteAI’s Network Graph, we can identify their network of co-authors and institutional affiliations:
Alessio Ciulli and Craig M Crews co-authors and institutional affiliations
You can find some of their recent publications here:
- Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
- Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins.
- Recent Developments in PROTAC-Mediated Protein Degradation: From Bench to Clinic.
- Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation.
We’ve identified 30 topics emerging in popularity when searching TPD publications from the last 10 years by using ResoluteAI’s proprietary tagging engine to capture significant and frequent terms discovered from publication abstracts then mapped the topics to their Medical Subject Heading (MeSH) Qualifiers provided by peer-reviewed authors:
30 popular targets in TPD publications by ResoluteAI tags and MeSH qualifier
Search String Used:("targeted protein degradation"~2)
A few of the “hot spots” on the above below include Cereblon, BRD4, N-End Rule, Ubiquitin Ligase, Von Hippel-Lindau Tumor Suppressor, and Lenalidomide.
Cereblon (CRBN; a member of the ATP-dependent Lon protease) is an enzyme implicated in memory and learning. But when selecting Cereblon’s tag in a Graph view, we discover CBRN has primary and tertiary connections to BRD4, which is a transcriptional and epigenetic regulator that plays a pivotal role during embryogenesis and cancer development.
Network graph view of Cereblon showing primary and tertiary connections to BRD4
The connections in the above Graph were generated from research captured in the below 5 publications released in 2021:
- Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.
- BRD4 PROTAC degrader ARV-825 inhibits T-cell acute lymphoblastic leukemia by targeting 'Undruggable' Myc-pathway genes
- Traceless Staudinger ligation enabled parallel synthesis of proteolysis targeting chimera linker variants
- USP15 antagonizes CRL4CRBN-mediated ubiquitylation of glutamine synthetase and neosubstrates
- A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination
Search String Used: (("targeted protein degradation"~2) OR (PROTAC OR PHOTAC OR MADTAC OR LYTAC))
Grant analysis
Total funding for TPD Grant Research has exceeded $886,209,035 since 2011. Organizations who received Grant funding most frequently include University of California and University of Pittsburgh. The below Sankey Diagram highlights the Top 5 Grant Recipients and the Agencies funding some of their projects:
Top 5 TPD grant recipients and agencies funding some of their projects
Search String Used: (targeted protein degradation) w/ Award Notice Date & Award Start Date Filter Jan 1, 2011 - Present
Most frequently funded TPD Principal Investigators (PI) from the US and EU include:
Most frequently funded TPD PI's from the US and US by PI name and organizationSearch String Used: (targeted protein degradation) w/ Award Notice Date & Award Start Date Filter Jan 1, 2011 - Present
Among the Awarded Grants discovered in our search include active projects with connections between BRD4 and CBRN both funded by the National Cancer Institute.
- BET protein antagonist-based targeted therapy of Mantle Cell Lymphoma
- Total Funding: $390,134
- Organization: University of Texas MD Anderson
- PI: Kapil Bhalla
- Developing Tumor-specific PROTACs
- Total Funding: $382,245
- Organization: Yale University
- PI: Craig M Crews
Clinical trial analysis
Attending the 2021 TPD Summit are incredible companies like Arvinas, BioTeryX, Foghorn Therapeutics, Kymera Therapeutics, and Nurix Therapeutics who are all actively recruiting for clinical trials.
Companies actively recruiting for TPD clinical trials by sponsor name, intervention name, and start date
Kymera recently completed one of their trials in Canada using York Dermatology Clinic and Research Centre as their Facility location. The other 8 actively recruiting trials discovered in the previous search can be found in the USA, with California being the favorite state for site selection amongst the group of 5 Sponsors:
Locations of actively recruiting clinical trials for TPD by location name, U.S. state, and phaseSearch String Used: sponsors.name:((arvinas) OR (bioteryx) OR (foghorn) OR (kymera) OR (nurix))
Technology transfer analysis
By using ResoluteAI to search active licensing opportunities from over 300 global Tech Transfer Offices (TTO), we’re able to source 114 assets available for tech transfer listed since 2011 and still active. The top 15 TTOs are highlighted below:
Top 15 TPD tech transfer opportunities active by organization name and submitted date Search String Used: ((targeted protein degradation) OR (PROTAC) OR (LYTAC) OR (MADTAC) OR (PHOTAC))
Some of the active opportunities listed in 2021 include the following:
- Stanford: Polyspecific integrin-binding peptide (PIP)-LYTAC for degradation of integrins
- SUNY: High-yield, high-stability overexpression tag for bacterial protein production
- Rutgers: Novel Inhibitors of Keap1-Nrf2 Protein-Protein Interaction
- Stanford: Methods for Treating Protein Aggregation-Associated Diseases
- Medical College of Georgia: Bivalent aptamer-dual siRNA chimera effectively suppresses prostate cancer
- Johns Hopkins: Novel Bis-benzylidine Piperidone-based Proteasome Inhibitors with Anticancer Activity
- Emory: Combination Therapy to Overcome Resistance to Platinum-Based Chemotherapy
- Medical College of Georgia: Novel TREM1 inhibitor for pathological inflammatory response
News analysis
By using ResoluteAI to review the last 2 years of Global News, we can easily understand the most frequently mentioned companies Quarter-over-Quarter:
Companies most frequently mentioned in the news involving TPD for the last two yearsSearch String Used: ((targeted protein degradation) OR (PROTAC) OR (LYTAC) OR (MADTAC) OR (PHOTAC))
Among the news sources that mention these companies and actively cover various topics in TPD include:
News sources that actively cover various TPD topics by source and published date
Search String Used: ((targeted protein degradation) OR (PROTAC) OR (LYTAC) OR (MADTAC) OR (PHOTAC))
Resolute’s Recent News Round-up. Significant Headlines since August 2021:
- Monte Rosa Therapeutics lists on New York Stock Exchange
- Amphista Therapeutics Appoints New Chairman, Joshua T. Brumm
- Kymera’s Protein Degraders are Expanding the Druggable Universe
- Nurix Therapeutics Highlights New Risk Factors as Clinical Programs Expand
- German drug giant Bayer plants flag in San Diego with $2B biotech acquisition
- Lilly licenses Lycia’s LYTAC protein degrader platform
- Lilly Says Carolyn Bertozzi Resigns From Board
- Promega Corporation and the University of Dundee show a “three-headed hydra” significantly improves efficacy in targeted protein degradation.
- Insilico Medicine Announces an AI-driven PROTAC R&D Collaboration with Arvinas
- PAQ Therapeutics Announces Collaboration with Insilico Medicine to Develop Novel Therapies through Autophagy-Dependent Degradation
Startup analysis
Since 2016, 10 targeted protein degradation startups have been founded and are still in operation. Those companies include Venquis Therapeutics, Ligature Therapeutics, FIMECS, Oerth Bio, Celeris Therapeutics, Neomorph, Cullgen, PAQ Therapeutics, Ranok Therapeutics, and Caraway Therapeutics which are headquartered in the following countries:
10 protein degradation startups by country and name
Collectively, these 10 companies have accumulated more than $330MM in total funding. Venture funds who have made investments $10MM+ in these startups include 3E Bioventures, AbbVie Biotech Ventures, Deerfield, GNI Group, Highlight Capital, Lapam Capital, MRL Ventures Fund, Sequoia Capital China, Shanghai Healthcare Capital, and Sherpa Venture Capital.
In the last 2 years alone, these 10 startups have been mentioned in the news over 200 times in the following 20 countries most frequently:
The 10 protein degradation startups by mentions in the news by country
There's a TAC for that
What are commonly referenced diseases and disorders that appear alongside PROTACs and emerging TPD strategies (i.e. LYTAC, AUTAC, ATTEC), where do they appear, and how frequently do they appear?
Commonly referenced diseases and disorders that appear alongside PROTACsSearch String Used: ((PROTAC) AND (INSERT DISEASE OR DISORDER))
Search String Used:((AUTAC OR ATTEC OR LYTAC) AND (INSERT DISEASE OR DISORDER))
Recently published LYTAC, AUTAC, and ATTEC peer-reviewed literature:
- Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs.
- Redefining the Scope of Targeted Protein Degradation: Translational Opportunities in Hijacking the Autophagy-Lysosome Pathway.
- Targeting lipid droplets for autophagic degradation by ATTEC.
- LYTACs Target Extracellular and Membrane Proteins for Degradation.
- Beyond targeted protein degradation: LD·ATTECs clear cellular lipid droplets.
- LYTACs: An Emerging Tool for the Degradation of Non‐Cytosolic Proteins.
Data Provided by ResoluteAI:
All tables, graphs and heat maps were generated using ResoluteAI’s discovery engine, Foundation.
ResoluteAI’s external search function ("Foundation") enables exploration, search, analytics, and alerts on over a dozen science-focused databases, including PubMed, Clinical Trials, Patents, Grants, FDA, Tech Transfer, News, and more.
ResoluteAI’s Nebula platform is commercializing AI & ML-assisted enterprise search tools that cater to pharmaceutical, biotechnology, and medical device companies. ResoluteAI indexes, analyzes, tags, and connects disparate silos of both internal and external data without the need for dedicated engineers on the customer side. ResoluteAI’s powerful enterprise search platform has been trained on over 1MM scientific documents, can handle nearly any file type, and generate large time savings and direct cost savings.
ResoluteAI provides your team of scientific professionals convenient, secure, and anonymous access to information that has more context, detail, truth, and semantics by capturing real world and internal information more precisely and more comprehensively.
ResoluteAI proudly supports clients like SCIEX, Thermo Fisher, and MilliporeSigma; who are all sponsors for the 4th Annual TPD Summit.
For more information on any of the data and visualizations presented here, please email us at info@resolute.ai
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