Trends in the development of remdesivir based inventions against COVID-19 and other disorders: A patent review

The development of remdesivir has been a breakthrough for COVID-19 treatment. It has been approved in about 50 countries since 2020. The generic structure of remdesivir was first disclosed in 2009. This patent review summarizes the remdesivir based inventions to treat/prevent COVID-19 and other disorders from 2009 to May 16, 2021, emphasizing the patents related to medical and pharmaceutical sciences. The primary patents/patent applications of remdesivir are related to its compositions, new combinations with other therapeutic agents, delivery systems, and new indications. The inventive combinations have displayed synergistic effects against COVID-19, whereas the delivery systems/compositions have improved patient compliance. The inventions related to new indications of remdesivir to treat Ebola, hepatitis, idiopathic pulmonary fibrosis, diabetic nephropathy, and cardiovascular complications enhance its therapeutic area. Many new innovative combinations and delivery systems of remdesivir are anticipated to provide better treatment for COVID-19.

Some examples on innovative delivery systems:

CN111603408A claims a lipstick containing remdesivir. The development of such lipstick has positive significance in the ongoing pandemic. The claimed lipstick inhibits SARS-CoV-2 propagation on the exposed parts of the human body, shortens the virus’s survival time, and reduces the risk of infection. It has been demonstrated that the virus loses activity within 30 min after exposure to this lipstick. 

CN111956630A offers a liquid preparation (pH = 3.5–5.5) for nebulizers comprising 1−100 mg/ml of remdesivir and a solvent (e.g. sulfobutyl-β-cyclodextrin, ethanol, water, or their mixture). The atomized remdesivir released from the nebulizer acts on the primary site of infection (nasal cavity, oral cavity, and lungs), making the medication more effective. This also reduces the systemic exposure of the drug in the body and helps to minimize the side effects of remdesivir.

CN111956630A offers a liquid preparation (pH = 3.5–5.5) for nebulizers comprising 1−100 mg/ml of remdesivir and a solvent (e.g. sulfobutyl-β-cyclodextrin, ethanol, water, or their mixture). The atomized remdesivir released from the nebulizer acts on the primary site of infection (nasal cavity, oral cavity, and lungs), making the medication more effective. This also reduces the systemic exposure of the drug in the body and helps to minimize the side effects of remdesivir.

CN112891327A provides a liquid preparation for remdesivir atomized inhalation and its preparation. The content of remdesivir in the liquid preparation ranges from 0.1% to 0.5% (w/v), and the pH ranges from 5 to 7. This delivery system increases the exposure of remdesivir in the lungs much higher than that of intravenous injection

US11013688B1 claims a method for the treatment of a viral infection (COVID-19) by administering 1 μl–50 μl of a medically active liquid comprising remdesivir utilizing a soft-mist-inhaler. This patent exemplifies the preparation of remdesivir solutions employing water, ethanol, and ethylene glycol, which were dispensed utilizing a soft-mist-inhaler

Mohd. Imran, Ahmed Subeh Alshrari, Syed Mohammed Basheeruddin Asdaq, Abida (2021) Trends in the development of remdesivir based inventions against COVID-19 and other disorders: A patent review,
Journal of Infection and Public Health, 14, 1075-1086,
https://doi.org/10.1016/j.jiph.2021.06.013.