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Publication Number
US-11744812-B2
Publication Date
2023-09-05
Expiration Date
Abstract
This disclosure features compounds and compositions that are useful in methods of treating coronavirus infections (e.g., useful in methods of treating COVID-19) in a subject in need thereof. The methods include administering to the subject niclosamide compounds (or pharmaceutically acceptable salts and/or co-crystals thereof, e.g., niclosamide). In some embodiments, the niclosamide compounds have one or more properties that include, but are not limited to: a particular purity (e.g., a chemical purity of greater than about 99.0%) or a particular particle size (e.g., a particular particle size distribution and/or a particular particle size range and/or a specific surface area range). In an aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for respiratory administration (e.g., via inhalation and/or intranasally). In another aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for administration to the GI tract (e.g., orally or rectally such as via enema)).
Core Innovation
The invention relates to treating a subject having a coronavirus infection by orally administering an effective amount of niclosamide or a pharmaceutically acceptable salt thereof. Niclosamide is defined by a particle size range of from about 0.1 μm to about 30 μm, and the disclosed approach is directed to treating the coronavirus infection using this oral niclosamide administration.
The disclosure emphasizes controlled solid-state properties of niclosamide to support targeted delivery. It includes particle size reduction and particle size distribution parameters such as D(0.1), D(0.5), and D(0.9), together with specific surface area, chemical purity, and purity analysis by UPLC, as well as control of water, hydrate, and crystalline form.
The document further extends the particle-size and quality-control concepts to niclosamide cocrystals, including co-crystals having hydrogen bonds, and discusses general pharmaceutical composition and local delivery concepts. It outlines respiratory administration and GI/colon targeting with local concentration ratios relative to plasma concentration, positioning the niclosamide material properties within broader therapeutic use in the gastrointestinal tract and other local delivery sites.
Claims Coverage
The independent claims cover oral treatment of a subject having a coronavirus infection by administering niclosamide or a pharmaceutically acceptable salt thereof, where niclosamide has a defined particle size range of about 0.1 μm to about 30 μm. The claim set further includes quantitative particle size distribution refinements, gastrointestinal location, viral load measurement by rRT-PCR, fecal/anal/rectal sampling, digestive symptom selection, and additional treatment response characterizations and subject/formulation constraints.
Oral niclosamide treatment for coronavirus infection
Treating a subject having a coronavirus infection in need of such treatment by orally administering an effective amount of niclosamide or a pharmaceutically acceptable salt thereof to treat the coronavirus infection.
Niclosamide particle size range for coronavirus treatment
Using niclosamide having a particle size range of from about 0.1 μm to about 30 μm in the oral treatment.
Particle size distribution D(0.9) refinement
The niclosamide has a particle size distribution D(0.9) between about 6.0 μm and about 8.0 μm.
GI/colon viral load monitoring with rRT-PCR
Measuring coronavirus viral load in the gastrointestinal tract using rRT-PCR.
Fecal/anal/rectal sampling for viral load measurement
Using a biological sample that is a fecal sample, an anal swab sample, or a rectal swab sample for the viral load measurement.
Digestive symptom selection
The digestive symptom is chosen from lack or loss of appetite, diarrhea, vomiting, abdominal pain, or combinations thereof.
Overall claim coverage centers on oral treatment of coronavirus infection using niclosamide defined by a specific particle size range, with further refinements to PSD parameters including D(0.9), and characterization of treatment effects via rRT-PCR viral load measurements in gastrointestinal tract samples obtained from fecal, anal, or rectal sources, optionally limited to subjects exhibiting selected digestive symptoms.
Stated Advantages
Treats the coronavirus infection by orally administering niclosamide or a pharmaceutically acceptable salt thereof.
Documented Applications
Treating a subject having a coronavirus infection, including COVID-19, by oral administration of niclosamide with the specified particle size range.
Monitoring SARS-CoV-2 RNA by PCR, including rRT-PCR, using respiratory or fecal/anal/rectal sample types.
Stratifying disease severity as mild versus severe using respiratory/oxygenation metrics and viral-load measures including ΔCt.
Combination therapy with other agents for coronavirus infection.
Clearing persistent infection in asymptomatic individuals.
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