Drug name
Niclosamide
Developer(s)
Drug information
Not provided
Niclosamide
Niclocide
Small molecule
Niclosamide (NCL) is an anthelmintic medication used for the treatment of human tapeworm (Cestoda) infection. Recent drug repurposing studies have shown that NCL possesses high levels of in vitro activity against SARS-CoV-2 as it impedes viral entry through an endocytic pH augmentation mechanism. NCL is highly insoluble in water (0.23-1.6 μg/mL at room temperature) which contributes to its poor bioavailability. Pharmacokinetic modelling has also indicated that oral dosing would not generate sufficient concentrations of circulating NCL to induce anti-SARS-CoV-2 activity. Therefore, recent attempts have been made to formulate long-acting aqueous solutions of NCL capable of providing high levels of systemic exposure.
Unknown
Unknown
Therapeutic area(s)
- COVID 19
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
Aqueous drug particle suspension
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Comment & Information
Developer(s)
Bayer AG is a multinational pharmaceutical company that develops a wide range of chemical products and medicines for consumer healthcare, industrial biotechnology and agricultural purposes. Headquartered in Leverkusen, Bayer was originally founded in 1863 and is currently listed on the EURO STOXX 50 index.
Drug structure
Scale-up and manufacturing prospects
Formulations for long-acting NCL are currently in preclinical development. Researchers from the Centre of Excellence for Long-acting Therapeutics (CELT) at the University of Liverpool have recently developed a highly innovative redispersible solid drug nanoparticle (SDN) formulation that utilises nanoprecipitation methods similar to those already utilised in commercial-scale production of beta-carotene particles for foodstuffs and agriculture. Successful industrial scale-up of the spray-dried dispersion may require potential optimisation of the mixing process using high shear mixer geometries.
Detailed information regarding industrial manufacturing requirements and/or equipment lists is currently not available as long-acting niclosamide formulations have been only been produced at small-scale for research use.
The previously mentioned formulation developed by researchers from CELT at the University of Liverpool can be stored as a solid dry powder and reconstituted into an aqueous solution through the addition of water prior to administration.
Dynamic light scattering equipment (Malvern Panalytical ZetaSizer Ultra Photon Correlation Spectroscope) to characterise the dry powder formulation. 1H nuclear magnetic spectroscopy to determine drug loading at 60 wt% relative to excipients using BzMA internal standard.
Excipients
No proprietary excipient used
Not provided
No residual solvent used
Delivery device(s)
No delivery device
Gastropod combating compositions
Gastropod combating compositions
GB824345
compound
Bayer AG
Not provided
September 19, 1976
Expired
Publications
Hobson JJ , Savage AC , Dwyer AB , Unsworth C , Massam J , Arshad U , Pertinez H , Box H , Tatham L , Rajoli RKR , Neary M , Sharp J , Valentijn A , David C , Curley P , Liptrott NJ , McDonald TO , Owen A , Rannard SP . Scalable nanoprecipitation of niclosamide and in vivo demonstration of long-acting delivery after intramuscular injection. Nanoscale. 2021 Apr 7;13(13):6410-6416. DOI: https://doi.org/10.1039/d1nr00309g. Epub 2021 Mar 25. PMID: 33885522.
The control of COVID-19 across the world requires the formation of a range of interventions including vaccines to elicit an immune response and immunomodulatory or antiviral therapeutics. Here, we demonstrate the nanoparticle formulation of a highly insoluble drug compound, niclosamide, with known anti SARS-CoV-2 activity as a cheap and scalable long-acting injectable antiviral candidate.
Additional documents
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Useful links
There are no additional links
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Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology
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Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit
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In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing