Cathepsin 

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  • ||||||||||  fondaparinux / Generic mfg.
    Journal:  Glycosaminoglycans as Tools to Decipher the Platelet Tumor Cell Interaction: A Focus on P-Selectin. (Pubmed Central) -  Dec 17, 2020   
    Light transmission aggregometry and ATP release assays confirmed that only those heparin derivatives with P-selectin blocking capacities were able to attenuate breast cancer cell-induced platelet activation, while pentasaccharide fondaparinux was without effects...In this study, we demonstrate that heparin blocks tumor cell-induced coagulation. Moreover, we identify platelet P-selectin, which obviously acts as molecular switch and controls aggregation and secretion of procoagulant platelets.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Preclinical, Journal:  Exploration of effect of Odanacatib on inhibiting orthodontic recurrence in rats and on CatK and IGF-1 mRNA. (Pubmed Central) -  Sep 5, 2020   
    More importantly, we illustrated a CTSK-mediated-positive feedback loop between CRC cells and TAMs during metastasis, prompting CTSK as a novel predictive biomarker and feasible therapeutic target for CRC. By promoting the IGF-1 mRNA expression and increasing the BMD and BVF of the alveolar bone, Odanacatib inhibits orthodontic recurrence and has no effect on osteoclast activity.
  • ||||||||||  dociparstat sodium (CX-01) / Chimerix
    Review, Journal:  Glycosaminoglycans as Multifunctional Anti-Elastase and Anti-Inflammatory Drugs in Cystic Fibrosis Lung Disease. (Pubmed Central) -  Aug 1, 2020   
    The modified heparin, 2-O, 3-O desulfated heparin (ODSH), maintains anti-elastase and anti-inflammatory activities in vitro and in vivo, and has little residual anticoagulant activity...Finally, nonsaccharide glycosaminoglycan mimetics with specific sulfate modifications can be designed to inhibit NE activity. Altogether, these novel GAGs or GAG mimetics hold significant promise to address the unmet need for inhaled anti-elastase and anti-inflammatory therapy for patients with CF.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Review, Journal:  Cathepsin K: The Action in and Beyond Bone. (Pubmed Central) -  Jun 27, 2020   
    Many studies have also demonstrated the involvement of CatK in various diseases beyond the musculoskeletal system. This review not only summarized the functional roles of CatK in bone and beyond bone, but also discussed the potential relevance of the CatK action beyond bone to the adverse effects of inhibiting CatK in non-bone sites.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Enrollment open:  Dociparstat for the Treatment of Severe COVID-19 in Adults at High Risk of Respiratory Failure (clinicaltrials.gov) -  Jun 3, 2020   
    P2/3,  N=524, Recruiting, 
    This review not only summarized the functional roles of CatK in bone and beyond bone, but also discussed the potential relevance of the CatK action beyond bone to the adverse effects of inhibiting CatK in non-bone sites. Not yet recruiting --> Recruiting
  • ||||||||||  dociparstat sodium (CX-01) / Chimerix
    [VIRTUAL] Anti-complement Effect of Heparin in Stimulated Whole Blood (Virtual Meeting Room 6) -  May 14, 2020 - Abstract #ISTH2020ISTH_1674;    
    This effect was charge dependent as both fully desulfated (N-acetyl-O-desulfated heparin with complete loss of negative-charge) and N-desulfated (which exposes positively charged amine groups) heparins had no effect, whilst selective desulfation retained some of heparin's activity. There was a molecular weight dependence, with a threshold of fractions ˃ Mw3450 g/mole (~10 saccharides) showing no further decrease in C3a levels induced by histones.
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Preclinical, Journal:  A Mild Inhibition of Cathepsin K Paradoxically Stimulates the Resorptive Activity of Osteoclasts in Culture. (Pubmed Central) -  May 13, 2020   
    In conclusion, the low-dose-induced stimulation of resorption observed in the clinical study can be reproduced in osteoclasts cultured in the absence of any other cell. Our data support an osteoclast-intrinsic mechanism where a mild inhibition of CatK results in increased levels of other proteinases contributing to the collagen degradation process.
  • ||||||||||  balicatib (AAE581) / Novartis, odanacatib (MK-0822) / Merck (MSD)
    Clinical, Review, Journal:  Clinical and translational pharmacology of the cathepsin K inhibitor odanacatib studied for osteoporosis. (Pubmed Central) -  Apr 14, 2020   
    The extensive clinical program for odanacatib, together with more limited clinical experience with other CatK inhibitors (balicatib and ONO-5334), provides important insights into the clinical pharmacology of CatK inhibition and the potential role of CatK in bone turnover and mineral homeostasis. Key findings include the ability of this mechanism to: 1) provide sustained reductions in resorption markers, increases in BMD, and demonstrated fracture risk reduction; 2) be associated with relative formation-sparing effects such that sustained resorption reduction is achieved without accompanying meaningful reductions in bone formation; and 3) lead to increases in osteoclast number as well as other osteoclast activity (including build-up of CatK enzyme) which may yield transient increases in resorption following treatment discontinuation and the potential for non-monotonic responses at sub-therapeutic doses.
  • ||||||||||  para-toluenesulfonamide (PTS100) / Gongwin Biopharm
    Trial completion date, Trial primary completion date:  OASES: A Study of PTS100 in Primary HCC Patients (clinicaltrials.gov) -  Feb 5, 2020   
    P2,  N=33, Recruiting, 
    Key findings include the ability of this mechanism to: 1) provide sustained reductions in resorption markers, increases in BMD, and demonstrated fracture risk reduction; 2) be associated with relative formation-sparing effects such that sustained resorption reduction is achieved without accompanying meaningful reductions in bone formation; and 3) lead to increases in osteoclast number as well as other osteoclast activity (including build-up of CatK enzyme) which may yield transient increases in resorption following treatment discontinuation and the potential for non-monotonic responses at sub-therapeutic doses. Trial completion date: Apr 2022 --> Dec 2023 | Trial primary completion date: Jul 2019 --> Dec 2021
  • ||||||||||  odanacatib (MK-0822) / Merck (MSD)
    Clinical, PK/PD data, Journal:  Odanacatib Pharmacokinetics Comparison Between Chinese and Non-Chinese Postmenopausal Women. (Pubmed Central) -  Oct 10, 2019   
    All adverse events were mild, none were serious, and none led to discontinuation. Single- and multiple-dose PKs of ODN 50 mg in Chinese postmenopausal women were generally similar to those previously reported in non-Chinese postmenopausal women.
  • ||||||||||  Prolia (denosumab) / Amgen, Daiichi Sankyo, GSK, odanacatib (MK-0822) / Merck (MSD)
    Clinical, Retrospective data, Journal:  Vertebral fractures cascade: potential causes and risk factors. (Pubmed Central) -  Aug 21, 2019   
    The results of this retrospective study showed that only half of VFC occurred in patients with a secondary cause of osteoporosis. Prospective studies are needed to further explore the determinants of this severe complication of osteoporosis.
  • ||||||||||  O-desulfated heparin (PGX-100) / Cantex
    Journal:  The Use of Myelinating Cultures as a Screen of Glycomolecules for CNS Repair. (Pubmed Central) -  Jul 3, 2019   
    Moreover, neither highly sulphated ulvans nor fucoidans had any effect on remyelination but CX-01, a low sulphated porcine intestinal heparin, promoted remyelination in vitro. These data illustrate the use of myelinating cultures as a screen and demonstrate the potential of heparin mimetics as CNS therapeutics.
  • ||||||||||  dociparstat sodium (CX-01) / Cantex Pharma, Chimerix
    Enrollment closed, Trial completion date, Trial primary completion date:  Dociparstat Sodium (CX-01) Combined With Standard Induction Therapy for Newly Diagnosed Acute Myeloid Leukemia (clinicaltrials.gov) -  Jan 30, 2019   
    P2,  N=76, Active, not recruiting, 
    CX-01 is well tolerated when combined with intensive therapy for AML and appears associated with enhanced count recovery and treatment efficacy. Recruiting --> Active, not recruiting | Trial completion date: Nov 2018 --> Apr 2019 | Trial primary completion date: Sep 2018 --> Mar 2019