Cathepsin 

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  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Clinical, Review, Journal:  Expanding the Role of Heparin Derivatives in Oncology: From Anticoagulation to Antitumor Activity. (Pubmed Central) -  Mar 27, 2025   
    Significant challenges remain in manufacturing scale-up, analytical validation, and long-term safety assessment. Future studies must address dose optimization, combination strategies, and controlled clinical trials to determine the full therapeutic potential of these compounds in clinical oncology.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  Cathepsin K cleavage of Angiopoietin-2 creates detrimental Tie2 antagonist fragments in sepsis. (Pubmed Central) -  Mar 3, 2025   
    Cathepsin K inhibition with the Phase-3 small molecule inhibitor odanacatib improved survival in distinct murine sepsis models...Septic humans accumulated circulating Angiopoietin-2 fragments, which were associated with adverse outcomes. These results identify cathepsin K as a candidate marker of sepsis and a proteolytic mechanism for the conversion of Angiopoietin-2 from Tie2 agonist to antagonist with therapeutic implications for inflammatory conditions associated with Angiopoietin-2 induction.
  • ||||||||||  Review, Journal:  Advances and Challenges in the Pursuit of Disease-Modifying Osteoarthritis Drugs: A Review of 2010-2024 Clinical Trials. (Pubmed Central) -  Feb 26, 2025   
    Eleven DMOAD candidates are reviewed and critically analyzed for their potential benefit in OA treatment-Lorecivivint (SM04690), TissueGene-C, Cindunistat (SD-6010), Sprifermin, UBX0101, TPX-100, GLPG1972/S201086, Lutikizumab (ABT-981), SAR113945, MIV-711, and LNA043-and relevant challenges to their development are discussed. Six DMOADs have demonstrated statistically significant evidence of a structural or symptomatic benefit without major safety concerns in phase II and III randomized controlled trials post-2010.
  • ||||||||||  Prolia (denosumab) / Amgen, Evenity (romosozumab-aqqg) / Astellas, Amgen, UCB, odanacatib (MK-0822) / Merck (MSD)
    Review, Journal:  The Management of Osteoporosis in Chronic Kidney Disease: A Review of Diagnostic and Therapeutic Approaches. (Pubmed Central) -  Dec 19, 2024   
    While traditional osteoporosis treatments such as bisphosphonates, denosumab, and teriparatide have been adapted for CKD patients, recent innovations have introduced agents aimed at enhancing bone mass and reducing fracture incidence...Osteoporosis management in CKD patients necessitates a personalized approach guided by the disease's stage and individual profile. This review underscores the potential of emerging therapies and emphasizes the need for further research to refine treatment protocols, aiming to enhance patient outcomes in this complex population.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  Impact of cathepsin K-induced proteoglycans degradation on dentin collagen. (Pubmed Central) -  Dec 1, 2024   
    axis. CatK-mediated degradation of PGs negatively impacted the stability of collagen fibers, promoted gaps, led to a less organized arrangement of dentin collagen fibers, ultimately increasing collagen degradation.
  • ||||||||||  MIV-711 / Medivir
    Journal:  Synthesis and Biological Evaluation of Novel Piperidine-3-Carboxamide Derivatives as Anti-Osteoporosis Agents Targeting Cathepsin K. (Pubmed Central) -  Sep 14, 2024   
    Molecular docking studies revealed that H-9 formed several hydrogen bonds and hydrophobic interactions with key active-site residues of cathepsin K. In vitro, H-9 demonstrated anti-bone resorption effects that were comparable to those of MIV-711, a cathepsin K inhibitor currently in phase 2a clinical trials for the treatment of bone metabolic disease...Moreover, in vivo experiments showed that H-9 increased the bone mineral density of OVX-induced osteoporosis mice. These results suggest that H-9 is a potent anti-bone resorption agent targeting cathepsin K and warrants further investigation for its potential anti-osteoporosis values.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Journal:  Anti-Ceramide ScFv Prophylaxis for First Responders to a Limited Nuclear Attack. (Pubmed Central) -  Aug 22, 2024   
    Unclear links between ODN and cardiovascular AEs require further research to clarify. While CX-01 prevents GI-ARS lethality, structural modification to extend half-life may be necessary to optimize first responder prophylaxis.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Trial termination, Combination therapy:  Dociparstat in Combination With Standard Chemotherapy for the Treatment of Acute Myeloid Leukemia (clinicaltrials.gov) -  Apr 15, 2024   
    P3,  N=9, Terminated, 
    We conclude that the treatment-related difference in THBMD change would predict fracture reduction equally well for drugs with different mechanisms of action. Active, not recruiting --> Terminated; Study enrollment was terminated on 16 May 2022 due to slow recruitment.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  Real-time analysis of osteoclast resorption and fusion dynamics in response to bone resorption inhibitors. (Pubmed Central) -  Apr 2, 2024   
    Using live-cell imaging, we monitored the bone resorptive behaviour of OCs during dose-dependent inhibition of CatK by an ectosteric (Tanshinone IIA sulfonate) and an active site inhibitor (odanacatib)...Using an activity-based probe, we demonstrated the presence of active CatK at the resorbing front in pits and trenches. In conclusion, our data document how OCs respond to CatK-inhibition with respect to movement, bone resorption activity, and their attempt to compensate for inhibition by activating fusion.
  • ||||||||||  balicatib (AAE581) / Novartis
    Journal:  Electrochemical Synthesis of Unnatural Amino Acids via Anodic Decarboxylation of N-Acetylamino Malonic Acid Derivatives. (Pubmed Central) -  Nov 13, 2023   
    The decarboxylative cyclization proceeds under constant current conditions in an undivided cell in an aqueous medium without any added base. A successful bioisosteric replacement of the 1-aminocyclohexane-1-carboxylic acid subunit by the THP-containing amino acid scaffold in cathepsin K inhibitor balicatib helped to reduce lipophilicity while retaining low nanomolar enzyme inhibitory potency and comparable microsomal stability.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Journal:  Platform-agnostic electrochemical sensing app and companion potentiostat. (Pubmed Central) -  Aug 25, 2023   
    The versatility of PocketEC, developed with an assay developer mindset, was demonstrated by interfacing it, via Bluetooth, to the ADuCM355 evaluation board, the open-source DStat potentiostat and the Voyager board, a custom-built, small footprint potentiostat based around the LMP91000 chip...Importantly, the versatility of the app makes it a candidate of choice for the development of future portable potentiostats. Finally, the app is available to download on the Google Play store and the source codes and design files for the PocketEC app and the Voyager board are shared via Creative Commons license (CC BY-NC 3.0) to promote the development of novel portable or wearable applications based on electrochemical sensing.
  • ||||||||||  relacatib (GSK-462795) / GSK
    Journal:  Unravelling the Relacatib activity against the CTSK proteins causing pycnodysostosis: a molecular docking and dynamics approach. (Pubmed Central) -  May 31, 2023   
    Finally, Molecular dynamics simulations were done in duplicates to recognize the variant (Y283C) activity of the protein structure against Relacatib for 100?ns. This study assists in comprehending the most pathogenic amino-acid variant, the ligand interaction with the protein structure, and paves the way for understanding the steadiness of the ligand with the native and selected significant amino-acid variant.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  An approach combining deep learning and molecule docking for drug discovery of cathepsin L. (Pubmed Central) -  Mar 1, 2023   
    Notably, two of these molecules, ZINC-35287427 and ZINC-1857528743, showed better docking results with CTSL compared to other cathepsins. Our approach enables drug discovery from large-scale databases with little computational consumption, which will save the cost and time required for drug discovery.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  A multifunctional drug consisting of tetracycline conjugated with odanacatib for efficient periodontitis therapy. (Pubmed Central) -  Nov 18, 2022   
    Importantly, periodontal administration of TC-ODN could successfully promote bone healing in periodontitis rats with alveolar bone loss. The findings in our study uncovered the excellent biocompatibility and multifunction of TC-ODN, including bone-targeted accumulation, immunoregulation, anti-inflammatory activity and promotion of bone healing, which might contribute to the clinical treatment of periodontitis.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Review, Journal:  The impact of medication on osseointegration and implant anchorage in bone determined using removal torque-A review. (Pubmed Central) -  Oct 25, 2022   
    On the contrary, several substances (e.g., prednisolone, cyclosporin A, cisplatin, and enamel matrix derivative) tend to adversely impact RTQ...This further confirms that factors such as bone quality underpin biomechanical anchorage of metal implants. Several fundamental questions on drug metabolism and bioavailability, drug dosage, animal-to-human translation, and the consequences of treatment interruption remain yet unanswered.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Journal:  Varied Bulk Powder Properties of Micro-Sized API within Size Specifications as a Result of Particle Engineering Methods. (Pubmed Central) -  Sep 24, 2022   
    In this work, we systematically investigated key bulk properties of 10 different batches of Odanacatib prepared through either jet milling or fast precipitation, all of which meet the particle size specification established to ensure equivalent biopharmaceutical performance...Among the 10 batches, a directly precipitated sample exhibited overall best performance, considering tabletability, dissolution, and CU. This work highlights the measurable impact of processing route on API properties and the importance of selecting a suitable processing route for preparing fine particles with optimal properties and performance.
  • ||||||||||  Prolia (denosumab) / Amgen, Daiichi Sankyo, odanacatib (MK-0822) / Merck (MSD)
    Journal:  Diabetes mellitus and the benefit of antiresorptive therapy on fracture risk. (Pubmed Central) -  Sep 7, 2022   
    However, when we considered trials individually, we found a few interactions within individual studies between diabetes status and the effects of denosumab and odanacatib on fracture risk, change in BMD or BTM. In sum, these results provide strong evidence that bisphosphonates and most licensed antiresorptive drugs are effective at reducing fracture risk and increasing BMD irrespective of diabetes status.
  • ||||||||||  dociparstat sodium (CX-01) / Chimerix
    Journal:  WHITE-COAT HYPERTENSION WITHOUT ORGAN DAMAGE: IMPACT OF LONG-TERM MORTALITY, NEW HYPERTENSION AND NEW ORGAN DAMAGE. (Pubmed Central) -  Aug 27, 2022   
    In sum, these results provide strong evidence that bisphosphonates and most licensed antiresorptive drugs are effective at reducing fracture risk and increasing BMD irrespective of diabetes status. The present study provides the first evidence that WCH with no cardiac and renal OD is accompanied by an increased long-term risk of mortality, new hypertension and new OD, thereby not representing a clinically innocent condition.
  • ||||||||||  dociparstat sodium (CX-01) / Chimerix
    Journal:  Forecasting Bitcoin Price Using Interval Graph and ANN Model: A Novel Approach. (Pubmed Central) -  Aug 9, 2022   
    The empirical study has clearly demonstrated the encouraging performance and effectiveness of the IG-ANN. The performance is compared with traditional ANN techniques on bitcoin time-series data spanning 2013-2019 and found that IG-ANN is outperforming all.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Enrollment closed, Enrollment change, Trial completion date, Trial primary completion date, Combination therapy:  Dociparstat in Combination With Standard Chemotherapy for the Treatment of Acute Myeloid Leukemia (clinicaltrials.gov) -  Jun 16, 2022   
    P3,  N=9, Active, not recruiting, 
    The performance is compared with traditional ANN techniques on bitcoin time-series data spanning 2013-2019 and found that IG-ANN is outperforming all. Recruiting --> Active, not recruiting | N=570 --> 9 | Trial completion date: Feb 2026 --> Dec 2022 | Trial primary completion date: May 2024 --> Dec 2022
  • ||||||||||  balicatib (AAE581) / Novartis
    Morphea after covid 19 vaccine : A new case report (e-Poster Hall) -  Jun 13, 2022 - Abstract #EADVSp2022EADV_Sp_203;    
    Treatment is based on clinical subtype and extent of involvement. Our patient was put on oral corticosteroids and methotrexate with a good clinical evolution.