Expert Opinion On Therapeutic Patents[JOURNAL]
Sun
200 papers
Insights and trends in development of TEAD-YAP/TAZ inhibitors: a review of PCT patents (2022 to June 2025).
Fan T, Yu Z, Xiao A … +2 more , Zhang Y, Xiang F
Expert Opin Ther Pat · 2025 Dec · PMID 41082257 · Publisher ↗
INTRODUCTION: The transcription enhancer associated domain (TEAD) family has been well documented for its roles in modulating cancer development, primarily through interactions with its two co-activators: yes-associated...
INTRODUCTION: The transcription enhancer associated domain (TEAD) family has been well documented for its roles in modulating cancer development, primarily through interactions with its two co-activators: yes-associated protein (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ). Although TEAD was first reported more than two decades ago, no therapeutic compounds directly targeting this protein or its interaction with YAP/TAZ are currently available or in late-phase clinical development. This underscores the need for continued exploration of novel strategies for the molecular design of targeted therapies, to which updated patent reviews are expected to make a considerable contribution. AREAS COVERED: This review evaluated the Patent Cooperation Treaty (PCT) patents claiming TEAD - YAP/TAZ inhibitors published between 1 January 2022 and 30 June 2025, and provides opinions on strategies for the development of TEAD - YAP/TAZ inhibitors. EXPERT OPINION: Over the past 3 years, there has been a marked increase in the number of PCT patents claiming structurally diverse TEAD - YAP/TAZ inhibitors, including filings by potentially new players. This trend highlights the growing recognition of the TEAD - YAP/TAZ axis as an attractive strategy for the development of new drugs, particularly for anti-cancer therapeutics.
An updated patent review of small molecule glucagon receptor antagonists (2020-2024).
Wang C, Lyu L, Liu D … +1 more , Hu Y
Expert Opin Ther Pat · 2025 Nov · PMID 40968011 · Publisher ↗
INTRODUCTION: The glucagon receptor (GCGR) plays a pivotal role in diabetes management. While small molecule GCGR antagonists (GCGRAs) offer several advantages, including glycemic control, oral bioavailability, and cost-...
INTRODUCTION: The glucagon receptor (GCGR) plays a pivotal role in diabetes management. While small molecule GCGR antagonists (GCGRAs) offer several advantages, including glycemic control, oral bioavailability, and cost-effectiveness, their clinical development is hampered by safety concerns. Recent structural and mechanistic insights have elucidated ligand binding and biased signaling and informed the rational design of GCGRAs. AREAS COVERED: This review presents an overview of small molecule GCGRAs between 2020 and 2024, drawing information from existing patents, peer-reviewed literature, and clinical data retrieved from the PubMed, Web of Science, SciFinder, and Derwent Innovation databases. EXPERT OPINION: In this observation period, innovation ownership shifted from pharmaceutical companies to academic institutions, which are emerging as key applicants for novel chemotypes. Such a significant shift reflects a broader divergence in innovation strategies, with academia increasingly exploring new chemotypes supported by deep learning and virtual screening, while companies focus on maintaining and optimizing established scaffolds. Furthermore, advances in structural and mechanistic studies have clarified ligand binding and biased signaling, informing the rational design of high-specificity, high-affinity GCGRAs. However, clinical investigations are warranted to assess whether these compounds can overcome current developmental bottlenecks, restore glucose homeostasis, and address safety concerns.
A patent review of MLKL modulators (2023 - present).
Wan BW, Jiang CS, Zhuang C
Expert Opin Ther Pat · 2025 Nov · PMID 40963226 · Publisher ↗
INTRODUCTION: Mixed-spectrum kinase structural domain-like protein (MLKL), which emerged as a pivotal regulator in biomedical research, plays a critical role in necroptotic pathways. Recent advancements have underscored...
INTRODUCTION: Mixed-spectrum kinase structural domain-like protein (MLKL), which emerged as a pivotal regulator in biomedical research, plays a critical role in necroptotic pathways. Recent advancements have underscored the therapeutic potential of MLKL modulators. AREAS COVERED: This review focuses on the patent literature covering MLKL-targeted molecules published from 2023 to July 2025. Patent and literature searching were performed using SciFinder, Espacenet, and PubMed databases. EXPERT OPINION: Research on MLKL modulators has seen significant progress in recent years, with many preclinical studies documenting various modulators, but the development of MLKL modulators, particularly activators, remains in its early stages due to challenges in specificity, efficacy, and bioavailability. Advancing therapeutic strategies will require a deeper understanding of MLKL-driven pathologies, optimizing existing modulators, and discovering new ones. The notable increase in natural product-derived MLKL inhibitors highlights the potential of identifying and modifying natural products as an effective approach for developing novel inhibitors.
Topoisomerase II inhibitors in oncology: an updated patent review (2016-present).
Turrini E, Maffei F, Milelli A … +1 more , Fimognari C
Expert Opin Ther Pat · 2025 Nov · PMID 40914847 · Publisher ↗
INTRODUCTION: Topoisomerase (topo) II inhibitors continue to represent a promising approach in anticancer therapy, although their clinical application is hampered by drug resistance and dose limiting toxicities. AREA COV...
INTRODUCTION: Topoisomerase (topo) II inhibitors continue to represent a promising approach in anticancer therapy, although their clinical application is hampered by drug resistance and dose limiting toxicities. AREA COVERED: We performed a critical analysis of patent literature from January 2016 to January 2025 on topo II inhibitors in oncology using the online databases Espacenet, Wipo, and Google patent. EXPERT OPINION: Substantial progress in the development of novel topo II inhibitors through synthetic chemistry, natural product isolation, molecular modification, and screening was recorded. These compounds belong to different chemical classes and mainly exhibit in vitro cytotoxicity in a low micromolar range, comparable to or greater than that induced by clinically established topo II inhibitors such as doxorubicin and etoposide. Some patented compounds showed catalytic inhibition of topo II enzyme, offering a safer and more effective alternative to topo II poisons. Despite encouraging data, only a few patents provide data or mechanistic insights, and none have progressed to clinical trials, highlighting a gap between preclinical innovation and clinical translation. Future research needs advancing in clinical development to fully realize the therapeutic potential of next-generation topo II inhibitors.
Toll-like receptor agonists as cancer therapeutics: a patent review (2014-2024).
Kumar P, Zargar ZB, Chopra K … +2 more , Pawar SV, Salunke DB
Expert Opin Ther Pat · 2025 Nov · PMID 40911336 · Publisher ↗
INTRODUCTION: Toll-like receptors (TLRs) play a key role in cancer immunotherapy by harnessing the immune system's natural response to target and fight tumors. Among the various TLRs, mainly TLR3, TLR4, TLR7, TLR8, and T...
INTRODUCTION: Toll-like receptors (TLRs) play a key role in cancer immunotherapy by harnessing the immune system's natural response to target and fight tumors. Among the various TLRs, mainly TLR3, TLR4, TLR7, TLR8, and TLR9, have been investigated for their ability to modulate immune responses, improve tumor recognition, and enhance the efficacy of conventional treatments like chemotherapy and radiotherapy. AREAS COVERED: This review provides an in-depth analysis of patents filed from 2014 to 2024 that explored TLR-targeting strategies in cancer therapy. TLRs trigger the release of pro-inflammatory cytokines such as IFN-γ, TNF-α, IL-12, and IL-6, which promote anti-tumor immunity by enhancing T-cell activation and dendritic cell maturation. TLR-based therapies have shown promise by stimulating innate and adaptive immunity, leading to increased tumor cell death. EXPERT OPINION: TLR agonists have been shown to, reduce treatment-related side effects, and inhibit tumor growth. However, challenges such as immune-related adverse events, including cytokine storms, and limited efficacy in specific tumor types persist. Advances in delivery systems, such as nanoparticles, liposomes, and conjugates, further enhance the targeting and effectiveness of TLR-based therapies while minimizing toxicity. The ongoing exploration of TLR agonists and their integration into combination therapies holds significant promise for improving cancer immunotherapy and patient outcomes.
Bruton's tyrosine kinase (BTK) inhibitors: an updated patent review (2019-2024).
Cui ZX, Yao SX, Zhang YX … +3 more , Lu HY, Sun LP, Shi L
Expert Opin Ther Pat · 2025 Oct · PMID 40878081 · Publisher ↗
INTRODUCTION: Bruton's tyrosine kinase (BTK) is a critical regulator in the pathogenesis of B-cell malignancies, inflammatory diseases, and autoimmune diseases. In recent years, BTK inhibitors have been a hot topic in dr...
INTRODUCTION: Bruton's tyrosine kinase (BTK) is a critical regulator in the pathogenesis of B-cell malignancies, inflammatory diseases, and autoimmune diseases. In recent years, BTK inhibitors have been a hot topic in drug development, with promising therapeutic prospects. Six BTK inhibitors have been approved, and several (including PROTAC) are undergoing clinical research. AREAS COVERED: This review provides a comprehensive analysis of BTK inhibitor mechanisms and synthesizes recent advancements documented in patent literature (2019-2024), with particular emphasis on structural innovations and therapeutic applications. Web of Science, PubMed, SciFinder, WIPO, EPO, USPTO and CNIPA databases were used for searching the literature and patents for BTK inhibitors. EXPERT OPINION: In recent years, many new drug development strategies proposed by medicinal chemists, such as multi-target inhibition, deuterium substitution, macrocyclization, and targeted protein degradation strategy (such as PROTAC), may provide guidance for the development of novel BTK inhibitors and overcome the problems of existing BTK inhibitors. Despite many challenges, BTK inhibitors have great potential in treating cancer and other diseases. With the application of new drug development strategies, the development of the next generation of BTK inhibitors may be promising.
Implementation and outcomes of China's drug patent linkage system: lessons from international experience.
Chen Y, Liu X, Li S … +1 more , Xu Z
Expert Opin Ther Pat · 2025 Oct · PMID 40836589 · Publisher ↗
INTRODUCTION: The drug patent linkage system plays a crucial role in achieving a balance between protecting drug innovation and ensuring the accessibility of generic drugs. Currently, this system has been implemented in...
INTRODUCTION: The drug patent linkage system plays a crucial role in achieving a balance between protecting drug innovation and ensuring the accessibility of generic drugs. Currently, this system has been implemented in many countries. This review aims to provide policy guidance and a reference basis for relevant stakeholders, while also offering valuable insights to other countries considering the implementation of the patent linkage system globally. AREAS COVERED: This review provides a comprehensive summary and comparative analysis of the patent linkage systems in the United States, Canada, South Korea, Singapore, and China, with a focus on China's recently implemented system and its outcomes. The data presented are derived from the official websites of the China NIPA, the IPC, and the NMPA's Drug Patent Information Registration Platform. EXPERT OPINION: This main goal of this system is to balance the interests of both parties through an efficient dispute resolution mechanism, while policy formulation is only the initial stage of the reform process and requires continuous improvement throughout the implementation phase. The author employed descriptive statistical methods to systematically analyze relevant data, providing valuable insights to colleagues in the field both domestically and internationally.
Evaluation of the patent portfolio for helicase-primase inhibitor ABI-5366 of Assembly Biosciences Inc.
Gege C, Kleymann G
Expert Opin Ther Pat · 2025 Oct · PMID 40830081 · Publisher ↗
BACKGROUND: Helicase-primase is an interesting target for small-molecule therapy of herpes simplex virus (HSV) infections. With amenamevir already approved for varicella-zoster virus and herpes simplex in Japan and with...
BACKGROUND: Helicase-primase is an interesting target for small-molecule therapy of herpes simplex virus (HSV) infections. With amenamevir already approved for varicella-zoster virus and herpes simplex in Japan and with pritelivir's granted breakthrough therapy designation for the treatment of acyclovir-resistant HSV infections in immunocompromised patients, the target has sparked interest in helicase-primase inhibitors. AREAS COVERED: Here, we analyze the series of patent applications from Assembly Biosciences (published between 03/2024 and 03/2025) covering their drug candidate ABI-5366 together with additional data from poster presentations, press releases and company updates. This me-too approach on the old Bayer urea series is currently in clinical phase I (NCT06385327) and the modification is the bridging of the two urea nitrogens via an alkylene linkage. EXPERT OPINION: The chemical structure for 1,3-disubstituted tetrahydropyrimidin-2(1)-one derivative ABI-5366 is presented and its potential opportunities and limitations as a long-acting oral administration or injectable depot drug compared to other HPIs are discussed.
A patent review of CHK1 inhibitors (2019 - present).
Liu T, Su M, Wang Y … +4 more , Gao A, Jiang K, Xu L, Li J
Expert Opin Ther Pat · 2025 Sep · PMID 40820497 · Publisher ↗
INTRODUCTION: Checkpoint kinase 1 (CHK1), a serine/threonine kinase, plays an important role in the DNA damage response (DDR), such as cell cycle checkpoints, DNA repair, transcriptional regulation, and apoptosis inhibit...
INTRODUCTION: Checkpoint kinase 1 (CHK1), a serine/threonine kinase, plays an important role in the DNA damage response (DDR), such as cell cycle checkpoints, DNA repair, transcriptional regulation, and apoptosis inhibition. CHK1 has emerged as a promising therapeutic target for cancer treatment. To date, over 15 CHK1 inhibitors have advanced into clinical trials, yet none have been approved for marketing. AREAS COVERED: A comprehensive patent review of literature from January 2019 to December 2024 on CHK1 inhibitors in oncology, their combination products, and structural insights have been reviewed through searching relevant information in Scopus, Espacenet, Web of Science, World Intellectual Property Organization, Google Patent databases, Cortellis Drug Discovery Intelligence, and United States Patent and Trademark Office. EXPERT OPINION: Considering the current advancements and the state of the field, the development of potent and selective CHK1 inhibitors with novel skeleton, either as monotherapies or in combination therapies, is of paramount importance. Ongoing research focuses on rational drug design, synergistic treatment integration, and predictive biomarkers identification. These advancements, along with future progress in the realm of CHK1 inhibitors, offer great promise as a pivotal strategy in biomarker-guided cancer therapeutics.
Traf2- and Nck-interacting kinase inhibitors: a patent review (2008-2024).
Qin L, Aladinskiy V, Gennert D … +5 more , Cheng X, Liu J, Liu T, Ren F, Zhavoronkov A
Expert Opin Ther Pat · 2025 Oct · PMID 40820280 · Publisher ↗
INTRODUCTION: Traf2- and Nck-interacting kinase (TNIK) is a crucial player in various intracellular signaling pathways, including Wnt/β-catenin, cytoskeleton organization, and immune activation. It phosphorylates several...
INTRODUCTION: Traf2- and Nck-interacting kinase (TNIK) is a crucial player in various intracellular signaling pathways, including Wnt/β-catenin, cytoskeleton organization, and immune activation. It phosphorylates several key target genes and is widely expressed in different organ systems, such as neural, gastrointestinal, lung, liver, and kidney tissues. TNIK has been implicated in multiple different disease areas, including oncology, neurological diseases, and fibrosis. AREA COVERED: This review provides an update of small molecule TNIK inhibitors in patents published from 2008 to 2024. EXPERT OPINION: Despite over 10 patents disclosing multiple scaffolds since 2008, only one inhibitor, INS018_055, has advanced to clinical trials to treat idiopathic pulmonary fibrosis. For the oncology indications, this is largely due to complexities in the relationship between TNIK and oncogenic pathways. Additionally, key characteristics of the molecules, such as kinase selectivity, physicochemical properties, and pharmacokinetic profiles, have played significant roles in determining whether the molecules are drug-like enough to advance to clinical trials.
An updated patent review on rational combinations of HDAC inhibitors for cancer chemotherapy (2020 - present): part 1-patent granted.
Shukla YK, Vandana, Mandal V … +3 more , Asati V, Keservani RK, Bharti SK
Expert Opin Ther Pat · 2025 Sep · PMID 40792589 · Publisher ↗
INTRODUCTION: Tumor cell heterogeneity poses a challenge to monotherapy, as a single drug cannot kill all heterogeneous cancer cells of a tumor. The surviving cells may develop resistance, potentially leading to tumor re...
INTRODUCTION: Tumor cell heterogeneity poses a challenge to monotherapy, as a single drug cannot kill all heterogeneous cancer cells of a tumor. The surviving cells may develop resistance, potentially leading to tumor recurrence. The combination therapy targets the disease through multiple mechanisms. Combinations of histone deacetylase (HDAC) inhibitor(s) with other inhibitor(s) have represented promising cancer chemotherapeutics by altering the epigenetic landscape of cancer cells by restoring acetylation and reactivating tumor suppressor genes, leading to cell cycle arrest, promoting apoptosis, and thus inhibiting cancer cell proliferation. AREAS COVERED: The patent literature (2020-present) on rational combinations of HDAC inhibitor(s) for cancer chemotherapy has been searched and reviewed from Google Patents, Patentscope, Espacenet, WIPO, and USPTO to provide an expert opinion on rational combinations for improved, optimized, and precise cancer therapy. This first part of a two-part review highlights the patent granted for the combination. EXPERT OPINION: The combination of HDAC inhibitors with other inhibitors, including Janus kinase (JAK), aurora kinase, tubulin, Sirtuin 2, and/or topoisomerase inhibitors, demonstrated a synergistic anti-cancer effect. Dual and multi-target inhibitors showed enhanced therapeutic efficacy in relapsed and refractory cases characterized by epigenetic dysregulation via histone modifications and alterations that contribute to disease progression.
GPR120 agonists for the treatment of type 2 diabetes: an updated patent review (2020-present).
Ilyas K, Nawaz I, Rehman K … +1 more , Iqbal J
Expert Opin Ther Pat · 2025 Sep · PMID 40789269 · Publisher ↗
INTRODUCTION: Type 2 diabetes mellitus (T2DM) affects over 530 million individuals globally, and is projected to reach 783 million by 2045, necessitating novel therapeutic strategies beyond current options. G-protein-cou...
INTRODUCTION: Type 2 diabetes mellitus (T2DM) affects over 530 million individuals globally, and is projected to reach 783 million by 2045, necessitating novel therapeutic strategies beyond current options. G-protein-coupled receptor 120 (GPR120), a lipid sensor regulating insulin sensitivity and inflammation, has gained attention as a promising target. AREAS COVERED: This review evaluates 25 patents and peer-reviewed studies (2020-2025) on GPR120 agonists. It highlights potent thiophene derivatives (EC₅₀ < 50 nM), sulfonamides, and stable fatty acid mimetics. Special attention is given to β-arrestin-biased agonists that improve glucose control (25% AUC reduction), improve insulin sensitivity (30% glucose drop), and reduce inflammation (40% TNFα inhibition). These compounds enhance GLP-1 secretion (a 2-fold increase), offering triple therapeutic benefits for diabetes. Sources were identified through a structured search of recent scientific literature and databases. EXPERT OPINION: GPR120 agonists, particularly β-arrestin-biased ligands, hold significant potential for T2DM treatment by modulating glucose homeostasis and inflammation. However, challenges like receptor desensitization and translational barriers such as species-specific receptor expression, off-target activity, and suboptimal pharmacokinetics must be addressed. Future research should optimize drug design to enhance efficacy and safety, paving the way for novel metabolic disorder therapies.
The potential of bacteriophages in treating multidrug-resistant ESKAPE pathogen infections.
Faccin ID, Hellen de Almeida de Souza G, Vicente JCP … +5 more , da Silva Damaceno N, Vitória de Oliveira Perez E, Martins W, Gales AC, Simionatto S
Expert Opin Ther Pat · 2025 Sep · PMID 40781777 · Publisher ↗
INTRODUCTION: Antimicrobial resistance (AMR) and the emergence of multidrug-resistant bacteria, including and spp. (ESKAPE) pathogens, have significantly reduced the effectiveness of antibiotics. In this context, bacte...
INTRODUCTION: Antimicrobial resistance (AMR) and the emergence of multidrug-resistant bacteria, including and spp. (ESKAPE) pathogens, have significantly reduced the effectiveness of antibiotics. In this context, bacteriophage therapy offers a promising alternative, targeting specific bacterial strains, disrupting biofilms, minimizing side effects, and preserve beneficial microbiota. AREAS RECOVERED: This review focuses on patent applications and patents granted up to 18 October 2024, related to the application of bacteriophages or their derivatives in treating infections caused by ESKAPE pathogens, as well as the methods for selecting bacteriophages. EXPERT OPINION: Phage-based strategies to overcome AMR have piqued the interest of the scientific community owing to the limited efficacy of new antimicrobial agents. Bacteriophages, co-evolved with antimicrobial-resistant bacteria, offer a diverse and cost-effective arsenal, especially beneficial for low- to middle-income countries. This review examines various patents on phage applications, including those on computational methods used for improving phage cocktail design, classical phages or phage-derived proteins, and potential combinations of antimicrobial agents and phages. The increasing number of phage-related patents, especially in China and the United States, suggests that the antimicrobial activity of bacteriophages is a research hotspot.
Glycogen synthase kinase 3β (GSK-3β) inhibitors - a patent update (2019-2024).
Joshi SV, Soujanya D, Sai Supriya M … +2 more , Yaddanapudi VM, Nanduri S
Expert Opin Ther Pat · 2025 Sep · PMID 40693819 · Publisher ↗
INTRODUCTION: Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine/threonine kinase identified over 40 years ago. It is the key enzyme involved in glycogen biosynthesis and is expressed in all human tissues....
INTRODUCTION: Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine/threonine kinase identified over 40 years ago. It is the key enzyme involved in glycogen biosynthesis and is expressed in all human tissues. Overexpression of GSK-3β is linked to several diseases, including diabetes mellitus, neurodegenerative disorders such as Alzheimer's disease, and cancer. Owing to its critical role in the pathophysiology of these diseases, GSK-3β has emerged as a validated and potential target for therapeutic intervention. In recent years, significant progress has been made in developing novel GSK-3 inhibitors. Some of these new inhibitors have shown promising results in treating some of these diseases. AREAS COVERED: This review covers patent literature on various GSK-3β inhibitors published between 2019 and 2024. This review also discusses the recent clinical developmental status of some of the promising GSK-3 inhibitors. EXPERT OPINION: Although many heterocyclic compounds from natural as well as synthetic origin have shown promising inhibitory effects against GSK-3β, most of them have not yet progressed to the development stage. However, a critical review of their structures and biological profiles reveals significant potential for further development.
Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024).
Nagpure NR, Patel HM
Expert Opin Ther Pat · 2025 Sep · PMID 40667612 · Publisher ↗
INTRODUCTION: Non-small cell lung cancer (NSCLC) remains a leading cause of cancer mortality, with epidermal growth factor receptor (EGFR) mutations being the primary driver of tumor progression. This review highlights t...
INTRODUCTION: Non-small cell lung cancer (NSCLC) remains a leading cause of cancer mortality, with epidermal growth factor receptor (EGFR) mutations being the primary driver of tumor progression. This review highlights the significance of fourth-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs) in addressing acquired resistance mechanisms, such as the C797S mutation, which compromises the efficacy of third-generation inhibitors like Osimertinib and explores their potential to revolutionize NSCLC treatment through enhanced molecular specificity. AREAS COVERED: This review covers the latest progress in patented fourth-generation EGFR-TKIs and their clinical trial status for the treatment of NSCLC from 2017 to the present. EXPERT OPINION: Osimertinib, a third-generation EGFR inhibitor, revolutionized treatment for T790M mutations but is limited by resistance from C797S mutations. Fourth-generation EGFR inhibitors, incorporating scaffolds like aminopyrimidine and quinazoline, are designed to selectively target resistant EGFR variants, including L858R/T790M/C797S. Preclinical trials highlight the potential of sulfonyl and phosphine oxide-based compounds for their potency, selectivity, and favorable pharmacokinetics. Promising clinical trials with inhibitors like BDTX-1535, JIN-A02, and HS-10504 could redefine NSCLC treatment, with future success likely relying on innovative strategies, such as combination therapies, to combat resistance and enhance efficacy.
Recent advances in tropomyosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review.
Le M, Timakova E, Schirrmacher R … +1 more , Bailey JJ
Expert Opin Ther Pat · 2025 Aug · PMID 40616417 · Publisher ↗
INTRODUCTION: The rise of tissue-agnostic therapies has revolutionized cancer treatment, with therapies targeting fusions leading the way. TRK inhibitors like larotrectinib and entrectinib marked a paradigm shift - prio...
INTRODUCTION: The rise of tissue-agnostic therapies has revolutionized cancer treatment, with therapies targeting fusions leading the way. TRK inhibitors like larotrectinib and entrectinib marked a paradigm shift - prioritizing molecular alterations over the tumor's anatomical location. Acquired resistance remains a significant challenge, with next-generation inhibitors and combination strategies at the forefront of efforts to enhance the clinical efficacy of TRK-targeted therapies. AREAS COVERED: This review discusses patents published in 2023 and 2024 covering inhibitors of the TRK family, extending our ongoing review series on TRK inhibitors. Patent searches were conducted using the key word 'TRK*' and 'inhibitor' in Google Patents database to identify novel TRK-targeting inhibitors and therapeutic strategies. EXPERT OPINION: Ongoing advancements in TRK inhibitor development, combination therapies, and precision diagnostics continue to elevate the potential of treatment outcomes. Recent patent filings reflect the expanding promise of TRK inhibitors for fusion-driven cancers. However, widespread adoption of high-throughput screening remains crucial unlocking their full therapeutic value and delivering truly precision-guided care. Combination therapies with TRK inhibitors are emerging as a key strategy to enhance efficacy and overcome resistance. The FDA's recent approval of repotrectinib underscores progress in the TRK inhibitor landscape, while highlighting the continued need for innovation.
Rho kinase inhibitors: a patent review (2017-2023).
de Oliveira DR, Tolomeu HV, Manssour Fraga CA … +1 more , Moreira Lima L
Expert Opin Ther Pat · 2025 Aug · PMID 40552832 · Publisher ↗
INTRODUCTION: Rho-associated protein kinases (ROCK) play a crucial role in various biological processes, making them a valuable therapeutic target. Recent FDA approvals of ROCK-targeting drugs have brought renewed focus...
INTRODUCTION: Rho-associated protein kinases (ROCK) play a crucial role in various biological processes, making them a valuable therapeutic target. Recent FDA approvals of ROCK-targeting drugs have brought renewed focus to this area, which this review aims to explore. AREAS COVERED: This review examines patents published from 2017 to 2023, highlighting novel ROCK inhibitors, progress on previously studied compounds, and new therapeutic applications. A thorough literature search was conducted using patent databases and relevant publications. EXPERT OPINION: Fasudil, ripasudil, netarsudil, and belumosudil are the primary ROCK inhibitors approved for human use. Despite some pharmacokinetic challenges, research in this field continues to advance, with significant potential for further clinical development.
An updated patent review of TEAD modulators (2022-present).
Xu D, Zhong J, Zeng Y … +4 more , Zhang X, Wang C, Luo C, Xiong H
Expert Opin Ther Pat · 2025 Jun · PMID 40536362 · Publisher ↗
INTRODUCTION: The Transcriptional Enhanced Associated Domain (TEAD) family has attracted increasing attention due to its crucial role in the Hippo signaling pathway, which regulates cell growth, division, survival, diffe...
INTRODUCTION: The Transcriptional Enhanced Associated Domain (TEAD) family has attracted increasing attention due to its crucial role in the Hippo signaling pathway, which regulates cell growth, division, survival, differentiation, and tissue homeostasis in multicellular organisms. Inhibition of TEADs with small molecules has been shown to be an effective strategy for the treatment of tumors, and several compounds have entered clinical trials as monotherapy and/or combination therapy. AREAS COVERED: Due to the explosion of patent disclosures on TEAD modulators (inhibitors or degraders) in the last two years, this review focuses on the published patent literature on small molecule inhibitors or degraders of TEAD and their applications from June 2022 to present（March 2025）, as a complementary update to the previous patent review (2018-2022). EXPERT OPINION: The reported TEAD modulators can be categorized into 4 types: non-covalent inhibitors, covalent inhibitors, protein-protein interaction inhibitors and degraders. Meanwhile, the combination therapy with TEAD inhibitors and other kinases or mutated gene inhibitors has shown promising therapeutic effects in patients with various types of cancer, which has greatly expanded the application field of TEAD inhibitors in disease treatment.
An updated patent review of rearranged during transfection (RET) kinase inhibitors (2022-present).
Armstrong D, Hanafi M, Frett B
Expert Opin Ther Pat · 2025 Aug · PMID 40501177 · Publisher ↗
INTRODUCTION: Rearranged during transfection (RET) is a receptor tyrosine kinase essential for cell signaling processes such as proliferation, differentiation, and migration. RET alterations, including point mutations an...
INTRODUCTION: Rearranged during transfection (RET) is a receptor tyrosine kinase essential for cell signaling processes such as proliferation, differentiation, and migration. RET alterations, including point mutations and gene fusions, contribute to oncogenesis. Recent advances in precision oncology have led to the development of selective RET inhibitors with improved safety and efficacy profiles. AREAS COVERED: This review discusses recent innovations in RET inhibitor development, with a focus on small-molecule patents published from 2022 to 2024. A comprehensive literature search was conducted using SciFinder and PatentScope with the keywords 'RET' and 'RET inhibitor.' The review summarizes the structural classes, target profiles, and potential advantages of newly patented compounds, particularly those designed to overcome known resistance mechanisms. EXPERT OPINION: While selective RET inhibitors such as selpercatinib have shown clinical success and expanded indications, their use is limited by adverse events and emerging resistance mechanisms. Next-generation RET inhibitors that address these limitations represent a critical frontier in drug development.
Nurr1 modulators - a patent review (2019-present).
Egner M, Merk D
Expert Opin Ther Pat · 2025 Aug · PMID 40481732 · Publisher ↗
BACKGROUND: Nuclear receptor related 1 (Nurr1) is a ligand-activated transcription factor and considered as neuroprotective and anti-neuroinflammatory target. Several lines of evidence support potential of Nurr1 modulati...
BACKGROUND: Nuclear receptor related 1 (Nurr1) is a ligand-activated transcription factor and considered as neuroprotective and anti-neuroinflammatory target. Several lines of evidence support potential of Nurr1 modulation in treating neurodegenerative diseases as well as in certain cancers, but potent and selective Nurr1 modulators are rare. AREAS COVERED: Development of small molecule Nurr1 modulators is gaining momentum which is also reflected in recent patent applications (published between 01/2019 and 09/2024, available on Google Patents). The claimed Nurr1 ligands are derived from the natural ligands prostaglandin A and dihydroxyindole as well as synthetic scaffolds. Their proposed use mainly refers to neurodegenerative disease and cancer treatment. EXPERT OPINION: Nurr1 modulation is emerging as new therapeutic concept in neurodegeneration and beyond and considerable progress has been made in Nurr1 ligand discovery with several promising compounds covered by patent applications. However, some reported and claimed ligands seem to lack validation and some claims appear very broad without presenting respective examples.
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