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DRUG:

nafamostat

i
Other names: FUT-175, CKD-314
Company:
Generic mfg.
Drug class:
TMPRSS2 inhibitor, Serine protease inhibitor
1m
Nafamostat mesylate sensitizes ovarian cancer cells to carboplatin by promoting the ZNF24-mediated inhibition of WNT2B. (PubMed, J Toxicol Sci)
Taken together, NM enhanced the CBP sensitivity of ovarian cancer cells by promoting the ZNF24-mediated inactivation of the WNT2B/Wnt/β-catenin axis. These findings suggest a viable treatment approach for improving CBP resistance in ovarian cancer.
Journal
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WNT2 (Wnt Family Member 2)
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carboplatin • nafamostat
4ms
Nafamostat Efficacy in Phase 3 Registrational CRRT Study (clinicaltrials.gov)
P=N/A, N=166, Recruiting, Talphera, Inc | Not yet recruiting --> Recruiting | Trial completion date: Aug 2024 --> Dec 2024 | Initiation date: Mar 2024 --> Aug 2024 | Trial primary completion date: Aug 2024 --> Dec 2024
Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date
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nafamostat
5ms
The Safety of Nafamostat Mesylate for Patients With High Risk Bleeding Undergoing Hemodialysis: A Pilot Study (clinicaltrials.gov)
P=N/A, N=100, Recruiting, Wonju Severance Christian Hospital | Enrolling by invitation --> Recruiting | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Dec 2023 --> Dec 2025
Enrollment status • Trial completion date • Trial primary completion date
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nafamostat
6ms
SEN-CoV-Fadj: Efficacy and Safety Evaluation of Treatment Regimens in Adult COVID-19 Patients in Senegal (clinicaltrials.gov)
P3, N=59, Terminated, Institut Pasteur de Dakar | N=186 --> 59 | Recruiting --> Terminated; In conclusion, the results of the SEN-CoV Fadj trial to date do not meet the objectives of the clinical trial and the sample size required to meet them is clearly too large to be achieved within a reasonable time.
Enrollment change • Trial termination
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nafamostat
7ms
Australasian COVID-19 Trial (ASCOT) ADAptive Platform Trial (clinicaltrials.gov)
P3, N=2200, Active, not recruiting, University of Melbourne | Recruiting --> Active, not recruiting | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Jul 2025
Enrollment closed • Trial completion date • Trial primary completion date
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nafamostat • Fragmin (dalteparin sodium) • enoxaparin sodium
1year
DEFINE - Evaluating Therapies for COVID-19 (clinicaltrials.gov)
P1/2, N=200, Recruiting, University of Edinburgh | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Dec 2024
Trial completion date • Trial primary completion date
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nafamostat
1year
Efficacy of Nafamostat in Covid-19 Patients (RACONA Study) (clinicaltrials.gov)
P2/3, N=256, Recruiting, University Hospital Padova | Trial completion date: Dec 2021 --> Dec 2024 | Trial primary completion date: Dec 2021 --> Dec 2024
Trial completion date • Trial primary completion date
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nafamostat
1year
New P4 trial
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nafamostat
over1year
Identification of potential Indonesian marine invertebrate bioactive compounds as TMPRSS2 and SARS-CoV-2 Omicron spike protein inhibitors through computational screening. (PubMed, Arab J Chem)
Camostat and nafamostat (co-crystal) were utilized as reference ligands against TMPRSS2, whereas mefloquine was used as a reference ligand against spike protein. Furthermore, slight variances in the MD simulation demonstrated consistent binding to TMPRSS2 and spike protein after the initial 50 ns. These results are highly valuable in the search for a treatment for SARS-CoV-2 infection.
Journal
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nafamostat
over2years
Discovery of diminazene as a dual inhibitor of SARS-CoV-2 human host proteases TMPRSS2 and furin using cell-based assays. (PubMed, Curr Res Chem Biol)
Evaluation of camostat, nafamostat, and gabexate in these cell-based assays confirmed their known TMPRSS2 inhibitory activities. Diminazene, a veterinary medicinal agent and a known furin inhibitor was found to inhibit both TMPRSS2 and furin with ICs of 1.35 and 13.2 μM, respectively. Establishment and the use of cell-based assays for evaluation TMPRSS2 and furin inhibitory activity and implications of dual activity of diminazene vs TMPRSS2 and furin are presented.
Journal
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TMPRSS2 (Transmembrane serine protease 2)
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nafamostat
3years
Nafamostat mesylate overcomes endocrine resistance of breast cancer through epigenetic regulation of CDK4 and CDK6 expression. (PubMed, Transl Oncol)
Tamoxifen and fulvestrant are drugs currently used for endocrinal therapy. A combination of nafamostat mesylate and CDK4/6 inhibitor synergistically overcame endocrine resistance in ERPBC. Nafamostat mesylate might be an essential adjuvant or alternative drug for the treatment of endocrine-resistant ERPBC due to the low cost-efficiency of the CDK4/6 inhibitor.
Journal
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ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4) • CDK6 (Cyclin-dependent kinase 6)
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ER positive • CDK6 expression
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tamoxifen • fulvestrant • nafamostat
over4years
Sex Hormones and Hormone Therapy during COVID-19 Pandemic: Implications for Patients with Cancer. (PubMed, Cancers (Basel))
Clinical studies on TMPRSS2 inhibitors, such as camostat, nafamostat, and bromhexine, are ongoing. Antiandrogens, such as bicalutamide and enzalutamide, are also under investigation...Some evidence also supports the notion that estrogens and progesterone might exert a protective effect on females, through direct antiviral activity or immune-mediated mechanisms, thus explaining the higher COVID-19 severity in post-menopausal women. In this perspective, we discuss the available evidence on sex hormones and hormone therapy in patients infected with SARS-CoV-2, and we highlight the possible implications for cancer patients, who can receive hormonal therapies during their treatment plans.
Clinical • Journal
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TMPRSS2 (Transmembrane serine protease 2)
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tamoxifen • Xtandi (enzalutamide) • bicalutamide • nafamostat