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Chemical Structure| 139110-80-8 Chemical Structure| 139110-80-8

Structure of Zanamivir
CAS No.: 139110-80-8

Chemical Structure| 139110-80-8

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Zanamivir is the first of two registered neuraminidase inhibitors for the treatment and prophylaxis of influenza. Zanamivir could inhibit SARS-CoV-2 3CLpro main protease.

Synonyms: GG 167; GR 121167X

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Product Details of Zanamivir

CAS No. :139110-80-8
Formula : C12H20N4O7
M.W : 332.31
SMILES Code : O=C(C1=C[C@H](NC(N)=N)[C@@H](NC(C)=O)[C@H]([C@H](O)[C@H](O)CO)O1)O
Synonyms :
GG 167; GR 121167X
InChI Key :ARAIBEBZBOPLMB-UFGQHTETSA-N
Pubchem ID :60855

Safety of Zanamivir

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Madin-Darby canine kidney cells 8.5 to 14.0 μM (EC50) 18 hours Zanamivir inhibited the replication of H6N1 and H9N2 influenza viruses in MDCK cells, with EC50 ranging from 8.5 to 14.0 μM. PMC90446
Madin-Darby canine kidney cells (MDCK) 0.418 ng/ml (1.254 nM) 24 hours Evaluate the inhibitory effect of Zanamivir on A/Hong Kong (H275Y) virus, results showed the virus was susceptible to Zanamivir PMC3067163
Calu-3 cells 35 μg/mL 48 hours Inhibition of H1N1 virus replication PMC9820929
A549 cells 35 μg/mL 48-72 hours Inhibition of H1N1 virus replication PMC9820929
MDCK cells 35 μg/mL 48-72 hours Inhibition of H1N1 virus replication PMC9820929

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice H1N1 infection model Intranasal administration 35 μg/mL Once daily for seven days Prevented weight loss, increased survival rate, and improved lung fibrosis PMC9820929
DBA/1J mice Collagen-induced arthritis (CIA) Intraperitoneal injection 50 mg/kg and 100 mg/kg Once daily, starting two days before immunization until the end of the experiment Zanamivir significantly ameliorated the clinical symptoms of CIA, delayed disease onset, and reduced the numbers of B-lineage cells, accompanied by inhibition of the humoral immune response. PMC7867009
BALB/c mice Avian influenza virus infection model Intranasal administration 10, 50, and 100 mg/kg Twice daily for 5 days Zanamivir significantly reduced virus titers in the lungs and completely blocked the spread of virus to the brain, increasing the mean survival day and the number of survivors infected with H6N1 and H5N1 viruses. PMC90446
Mice and ferrets Influenza virus infection model Intranasal administration 0.028 µmol/kg Dosing at 6, 24, and 48 hours post-infection, lasting for 72 hours To evaluate the inhibitory effect of polymer-attached Zanamivir (5a) on influenza virus infection in vivo. Results showed that 5a was more effective than small-molecule Zanamivir (1), reducing viral load by 190-fold in mice and 30-fold in ferrets. PMC3964776

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00705406 Acute, Uncomplicated Human Inf... More >>luenza Less << Phase 2 Completed - -
NCT00958776 Cough Sore Th... More >>roat Nasal Congestion Headache Fever Seasonal Influenza Less << Phase 3 Terminated(This study was term... More >>inated for futility) Less << - -
NCT00705406 - Completed - -
NCT01793883 Influenza Phase 2 Completed - -
NCT01052480 - Completed - -
NCT00958776 - Terminated(This study was term... More >>inated for futility) Less << - -
NCT01052480 Influenza A I... More >>nfluenza B Less << Phase 2 Completed - -
NCT02022761 Asthma Phase 1 Completed - United Kingdom ... More >> Respiratory Clinical Trials London, United Kingdom, W1G 8HU Less <<
NCT01793883 - Completed - -
NCT01506583 - Unknown July 2012 United States, Alabama ... More >> University of Alabama at Birmingham Recruiting Birmingham, Alabama, United States, 35294 Contact: David Kimberlin, M.D.    205-934-5316    dkimberlin@peds.uab.edu    Contact: Dusty Giles, R.N.    205-934-7807    dgiles@peds.uab.edu    Principal Investigator: David Kimberlin, M.D.          United States, Illinois Northwestern University Feinberg School of Medicine Recruiting Chicago, Illinois, United States, 61611 Contact: Mike Ison, M.S., M.D.    312-695-4186    mgison@northwestern.edu    Principal Investigator: Mike Ison, M.S., M.D.          United States, Maryland University of Maryland School of Medicine Completed Baltimore, Maryland, United States, 21201 Less <<
NCT01055990 Virus Diseases ... More >> Respiratory Tract Diseases Respiratory Tract Infections Influenza Orthomyxoviridae Infections Less << Phase 2 Unknown May 2010 China, Shanghai ... More >> Shanghai Public Health Clinical Center Shanghai, Shanghai, China, 201508 Less <<
NCT00867139 Influenza Phase 1 Phase 2 Completed - United States, Washington ... More >> Seattle Children's Seattle, Washington, United States, 98105 Fred Hutchinson Cancer Research Center Seattle, Washington, United States, 98109 Less <<
NCT02014649 Influenza Phase 1 Phase 2 Terminated(Study was terminate... More >>d as per BARDA decision to terminate contract.) Less << - -
NCT00640874 - Withdrawn - Australia, New South Wales ... More >> St Vincent's Hospital Sydney, New South Wales, Australia, 2010 Prince of Wales Hospital Sydney, New South Wales, Australia, 2031 Westmead Hospital Sydney, New South Wales, Australia, 2145 Australia, Queensland Royal Brisbane Hospital Brisbane, Queensland, Australia, 4000 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Flinders Medical Centre Adelaide, South Australia, Australia, 5042 Australia, Victoria The Alfred Hospital Melbourne, Victoria, Australia, 3004 Australia, Western Australia Royal Perth Hospital Perth, Western Australia, Australia, 6000 Less <<
NCT00867139 - Completed - -
NCT00640211 - Withdrawn - Australia, New South Wales ... More >> St Vincent's Hospital Sydney, New South Wales, Australia, 2010 Prince of Wales Hospital Sydney, New South Wales, Australia, 2031 Westmead Hospital Sydney, New South Wales, Australia, 2145 Australia, Queensland Royal Brisbane Hospital Brisbane, Queensland, Australia, 4000 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Flinders Medical Centre Adelaide, South Australia, Australia, 5042 Australia, Victoria The Alfred Hospital Melbourne, Victoria, Australia, 3004 Australia, Western Australia Royal Perth Hospital Perth, Western Australia, Australia, 6000 Less <<
NCT03684044 Influenza Phase 3 Recruiting July 10, 2021 -
NCT01353768 - Completed - -
NCT00979667 Upper Respiratory Tract Infect... More >>ion Influenza Less << Phase 3 Terminated(Decreased Influenza... More >> activity; thus decrease/no eligible patient to recruit) Less << - China, Hong Kong ... More >> Shau Kei Wan Jockey Club Clinic Hong Kong, Hong Kong, China, 852 Hong Kong Fanling Family Medicine Centre Hong Kong, Hong Kong Sai Ying Pun Jockey Club General Outpatient Clinic Hong Kong, Hong Kong Less <<
NCT01156701 - Completed - -
NCT01156701 - Completed - -
NCT00980109 Influenza Phase 4 Completed - Thailand ... More >> Faculty of Medicine Siriraj Hospital Bangkok, Bangkoknoi, Thailand, 10700 Hospital for Tropical Diseases Bangkok, Thailand, 10400 Less <<
NCT01353729 Influenza, Human Phase 1 Completed - United States, Texas ... More >> GSK Investigational Site Austin, Texas, United States, 78744 Less <<
NCT00989404 Influenza A Virus, H1N1 Subtyp... More >>e Less << Phase 1 Completed - United States, Minnesota ... More >> GSK Investigational Site Minneapolis, Minnesota, United States, 55404 Less <<
NCT00830323 Influenza A Infection Phase 2 Terminated August 2009 France ... More >> Hospices civils de Lyon Lyon, France Less <<
NCT00921726 Influenza Vir... More >>us Diseases Less << Phase 1 Completed - Thailand ... More >> Mathidol University Salaya, Thailand, 73170 Less <<
NCT01459081 Influenza A Virus Infection ... More >> Influenza B Virus Infection Less << Phase 3 Completed - China ... More >> The Third Xiangya Hospital Of Central South University Changsha, China West China Hospital, Sichuan University Chengdu, China The First People's Hospital of Hangzhou Hangzhou, China The Affiliated Hospital of Inner Mongolia Medical College Huhehaote, China The First Affiliated Hospital of Nanchang University Nanchang, China The First Affiliated Hospital of Nanjing Medical University Nanjing, China Qingdao Municipal Hospital Qingdao, China Shanghai 6th People's Hospital Shanghai, China Shanghai Changzheng Hospital Shanghai, China ShengJing Hospital of China Medical University Shenyang, China Tangdu Hospital Affiliated to the Fourth Military Medical University Xi'an, China Northern Jiangsu People's Hospital Yangzhou, China Less <<
NCT01199744 - Completed - -
NCT00540501 Healthy Subjects Phase 1 Withdrawn(Contract agreement n... More >>ot reached) Less << October 2007 -
NCT01199744 - Completed - -
NCT01014988 - Completed - -
NCT01014988 Influenza, Human Phase 2 Completed - -
NCT00799760 Gastric Influenza Phase 3 Terminated(Just Terminated for... More >> the end of the pandemia) Less << - France ... More >> Centre Investigateur 155 Deulemont, France, 59000 Less <<
NCT00784784 - Completed - -
NCT01462487 - Completed - -
NCT01231620 Influenza, Human Phase 3 Completed - -
NCT01231620 - Completed - -
NCT01390792 - Completed - -
NCT02377401 Influenza, Human PHASE1 COMPLETED 2015-06-19 GSK Investigational Site, Shan... More >>ghai, 200030, China Less <<
NCT01527110 Influenza, Human Phase 3 Completed - Japan ... More >> GSK Investigational Site Fukuoka, Japan, 816-0864 GSK Investigational Site Kanagawa, Japan, 247-8533 GSK Investigational Site Miyagi, Japan, 983-0824 GSK Investigational Site Miyagi, Japan, 985-8506 GSK Investigational Site Okayama, Japan, 700-8557 GSK Investigational Site Osaka, Japan, 581-0011 GSK Investigational Site Shizuoka, Japan, 432-8002 Less <<
NCT00784784 Influenza Phase 3 Completed - Canada, Ontario ... More >> Mount Sinai Hospital Toronto, Ontario, Canada, M5G 1X5 Less <<
NCT01527110 - Completed - -
NCT04494412 Influenza, Human|Arthralgia PHASE2 RECRUITING 2026-12-09 GSK Investigational Site, Nijm... More >>egen, 6525 GA, Netherlands|GSK Investigational Site, Bydgoszcz, 85-168, Poland|GSK Investigational Site, Esplugues De Llobregat. Barcelona, 08950, Spain|GSK Investigational Site, Madrid, 28046, Spain|GSK Investigational Site, Dundee, DD1 9SY, United Kingdom|GSK Investigational Site, London, SW17 0QT, United Kingdom|GSK Investigational Site, London, W2 1NY, United Kingdom Less <<
NCT04867707 Diabetes Mellitus, Type 2 PHASE2 COMPLETED 2024-10-18 University of Missouri, School... More >> of Medicine Clinical Research Center, Columbia, Missouri, 65212, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL

References

 

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