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Publication Number
US-11564896-B2
Publication Date
2023-01-31
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 or a particular particle size. 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 a method of treating a symptom associated with a COVID-19 viral infection in a subject diagnosed as having the COVID-19 viral infection and exhibiting the symptom at the time of treatment. The method administers to the respiratory system an effective amount of a composition comprising niclosamide, or a pharmaceutically acceptable salt, hydrate, or co-crystal thereof, so as to treat the symptom.
The disclosed compositions are formulated and administered for delivery to the respiratory system, including delivery to the lungs and topical or local lung administration. The disclosure describes inhalation-device and spray or nebulizer type systems, including dry powder inhalers, metered dose and thermal aerosol inhalers, electrohydrodynamic-based solution misting inhaler configurations, and various nebulizers including unit-dose compatible designs.
The disclosure further characterizes niclosamide compositions with quality attributes including recrystallized niclosamide, crystalline niclosamide, an anhydrous form, and impurity and purity-related controls. Additional dependent refinements include particle size distribution metrics, inclusion of polyvinylpyrrolidone and beta cyclodextrin, and a symptom-onset timing window of 2 to 14 days after exposure to coronavirus.
Claims Coverage
The document provides an independent claim covering treatment of a COVID-19-associated symptom by respiratory administration of a niclosamide-containing composition, with multiple dependent refinements. Across the provided claims content, at least six inventive features further narrow the claim by administration modality, device selection, composition characteristics, and symptom-onset timing.
Respiratory-system administration of a niclosamide-containing composition
Administering to the respiratory system of the subject an effective amount of niclosamide, or a pharmaceutically acceptable salt, hydrate, or co-crystal thereof, to treat the symptom in the subject diagnosed as having the COVID-19 viral infection.
Topical or local lung administration
Administering the composition topically or locally to the subject’s lungs to treat the symptom.
Inhalation-device selection for administration
Using an inhalation device chosen from nebulizer and inhaler types, including dry powder inhaler, metered dose inhaler, jet nebulizer, ultrasonic wave nebulizer, heat vaporizer, soft mist inhaler, thermal aerosol inhaler, or electrohydrodynamic-based solution misting inhaler.
Composition particle size distribution constraint
Providing a composition in which the particle size distribution D(0.9) falls within about 1.0 μm to about 10.0 μm.
Inclusion of polyvinylpyrrolidone and beta cyclodextrin
The composition further includes polyvinylpyrrolidone and beta cyclodextrin.
Symptom onset timing window after coronavirus exposure
The symptom onset occurs 2 to 14 days after the subject’s exposure to coronavirus.
The claimed inventive concept centers on treating COVID-19-associated symptoms by administering a niclosamide-containing composition to the respiratory system, with dependent refinements directed to topical or local lung delivery, selected inhalation devices, particle size distribution, specific excipients, and a 2 to 14 day post-exposure symptom onset window.
Stated Advantages
Increase local bioavailability while reducing systemic toxicities.
Treat the symptom in a subject diagnosed as having the COVID-19 viral infection by administering an effective amount of a niclosamide-containing composition to the respiratory system.
Documented Applications
Treating and preventing coronavirus infections including COVID-19 by administering niclosamide-based compositions to a subject’s respiratory system to treat symptoms associated with COVID-19 viral infection.
Administering niclosamide-based compositions to the GI tract (oral/rectal) as an alternative route for treatment or prevention approaches.
Tailoring approaches for different disease severities using physiological criteria (respiratory rate, oxygen saturation at rest, PaO2/FiO2 ratio) and viral load assessed by ΔCt.
Clearing persistent infection in asymptomatic SARS-CoV-2 individuals.
Combination therapy approaches with other COVID-19 therapeutics including remdesivir, azithromycin, hydroxychloroquine, chloroquine, metformin, ACE inhibitors, and statins.
Treatment of a symptom associated with a COVID-19 viral infection in a subject diagnosed as having COVID-19 and exhibiting the symptom at the time of treatment, using respiratory administration of a niclosamide-containing composition.
Delivery to the lungs using inhalation devices, including nebulizers and inhalers, as part of administering the niclosamide-containing composition to treat the symptom.
Topical or local lung administration of the niclosamide-containing composition to treat the symptom.
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