Coronavirus Mpro Inhibitor Exhibited Plasma and Lung Drug Concentration

Georgia-based Frontier Biotechnologies recently announced positive results from the Phase 1 clinical trial of its drug candidate, FB2001, in healthy adult volunteers.

FB2001 (Bofutrelvir) is a small molecule inhibitor of coronavirus main protease (Mpro).

A total of 120 participants received intravenous infusions of FB2001 at either single doses from 5 mg to 400 mg or multiple doses of 30 mg to 400 mg daily for five days.

The key findings from the study are as follows:

• FB2001 was safe and well tolerated up to 400 mg per day
• Without a pharmacokinetic enhancer, FB2001 exhibited plasma and lung drug concentrations above the in vitro antiviral EC50 value.
• No significant difference was observed between the Chinese and American populations.

The current intravenous formulation of FB2001 is ideal for hospitalized patients with its rapid onset of action and is suited for patients with dysphagia or other problems with swallowing, says the company.

Working with clinical research organizations, regional regulatory agencies, and local clinical centers, Frontier Biotechnologies has started a pivotal Phase 2/3 study (BRIGHT trial) to enroll about 1,200 hospitalized patients in hundreds of clinical centers worldwide.

"The phase 1 data were really promising", said Dr. Michael Hu, Chief Medical Officer of Frontier Biotechnologies, "and we are confident to carry out the pivotal trial to explore the utility of the drug in reducing the time to recovery in hospitalized patients due to COVID-19."

Frontier Biotechnologies is also developing a pulmonary formulation of FB2001 that could be used in out-patient settings for the treatment of mild Covid-19, as well as for post-exposure prophylaxis.

When inhaled directly into the respiratory tract and lungs, the tissue concentration of FB2001 is much higher than that in plasma; hence, the onset of action and viral clearance could potentially be faster than that of oral therapy.

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