access-principles-1access-principles-2access-principles-3backcarrierdevelopmentease_of_administrationexportimplantableinjectablenon-implantablenon_carriernon_injectableother_featuresprintroute_of_administrationtherapeutic_areatype_of_tech

Drug information

Drug's link(s)

Not provided

Generic name

Niclosamide

Brand names

Niclocide

Compound type

Small molecule

Drug class/category

Not provided

Summary

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.

Approval status

Unknown

Regulatory authorities

Unknown

Therapeutic area(s)

  • COVID 19
Use case(s)
  • Treatment

Administration route

Intramuscular

Associated long-acting platforms

Aqueous drug particle suspension

Use of drug

Ease of administration
  • Administered by a nurse
  • Administered by a specialty health worker
Frequency of administration

Not provided

User acceptance
Not provided

Dosage

Available dose and strength

Not provided

Maximum dose

Not provided

Recommended dosing regimen

Not provided

Additional comments

Not provided

Dosage link(s)

Not provided

Associated compounds, formulations and regimens

Not provided

Associated technologies

Compare
Scalable process to achieve LA injectable delivery of insoluble medicines

Additional information

Not provided

Developer(s)

Bayer
Germany

Bayer

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

Scale-up 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.

Tentative equipment list for manufacturing

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.

Manufacturing

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.

Specific analytical instrument required for characterization of formulation

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 & delivery device(s)

Proprietary excipients used

No proprietary excipient used

Novel excipients or existing excipients at a concentration above Inactive Ingredient Database (IID) for the specified route of administration

Not provided

Residual solvents used

No residual solvent used

Delivery device(s)

No delivery device

Safety, Efficacy and Evidence Summary

Safety

Not provided

Efficacy

Not provided

Evidence Summary

Not provided

References and relevant studies

Not provided

Description

Gastropod combating compositions

Brief description

Gastropod combating compositions

Representative patent

GB824345

Category

compound

Patent holder

Bayer AG

Exclusivity

Not provided

Expiration date

September 19, 1976

Status

Expired