Kintor Pharmaceutical Limited announced the top-line results of the Phase III MRCT of proxalutamide in outpatients with mild to moderate COVID-19 regardless of vaccination status and risk factors. Data from the study demonstrated that the protection rate of patients in the trial (regardless of age or risk factors) treated with proxalutamide for more than seven days reached 100% (p < 0.02). The treatment with proxalutamide significantly reduced hospitalization or death in COVID-19 patients, especially in the middle-aged and elderly with high-risk factors.

Proxalutamide effectively reduced the risk of hospitalization/death: Among all randomized patients with at least one day of treatment (N=730), 8 patients who received placebo were hospitalized (including one death) compared to 4 patients who received proxalutamide (zero death). All hospitalizations were COVID-19-related. Proxalutamide reduced the risk of hospitalization or death by 50% compared to the control group.

Among patients with more than 1 day of treatment (N=721), 7 patients in the control group were hospitalized (including one death) compared to 2 patients (zero deaths) in the proxalutamide group. Proxalutamide reduced the risk of hospitalization or death by 71% compared to the control group. Among patients with more than 7 days of treatment (N=693), 6 patients who received placebo were hospitalized (including one death) compared to no hospitalization/death in the proxalutamide group.

Proxalutamide reduced the risk of hospitalization or death by 100% compared to the control group (p?0.02). Proxalutamide significantly reduced the risk of hospitalization/death in patients with high-risk factors, especially in patients 50 years of age or older and with at least 1 day of treatment: In the patients aged 50 years or older and with obesity, proxalutamide significantly reduced the risk of hospitalization/death by100% (p?0.02), as there was no hospitalization or death in the proxalutamide group. In the patients aged 60 years or older with or without underlying medical conditions, proxalutamide significantly reduced the risk of hospitalization or death by 100% (p?0.02), as there was no hospitalization or deaths in the proxalutamide group.

In the patients with age 60 years or older and with at least one underlying medical condition (such as obesity, diabetes, hypertension, etc.), proxalutamide significantly reduced the risk of hospitalization or death by 100% (p?0.02), as there was no hospitalization or deaths in the proxalutamide group. Proxalutamide significantly and continuously reduced SARS-CoV-2 viral load from Day 3 to Day 28, compared to the control group (p?0.01 on Day 3 and Day 28, respectively). COVID-19 symptoms such as fever, shortness of breath, and cough were improved through Day 28 compared to patients in the control group.

The study demonstrated that proxalutamide was well tolerated and side effects were manageable in patients with mild to moderate COVID-19. The incidence of treatment-emergent adverse events (TEAEs) was comparable in the control and proxalutamide groups (7.9% and 9.6%, respectively). The majority of TEAEs were mild.

The most common adverse event was dizziness (1.1 % in both proxalutamide and control groups). The incidence of any other adverse events was less than 1%. There was no serious adverse event in the study.

The multi-center randomized, double-blind, placebo-controlled (1:1) registrational trial (NCT04870606), evaluated the efficacy and safety of proxalutamide in outpatients with mild to moderate COVID-19 illness. The study enrolled 733 male and female patients with a positive SARS-CoV-2 diagnostic test and symptoms onset whether vaccinated or not and regardless of risk factors. 99% of the patients were recruited in the United States.

The patients received either proxalutamide 200mg, once daily plus standard of care (SOC)("proxalutamide arm") or placebo plus SOC ("placebo arm") for 14 consecutive days. The study endpoints included the percentage of patients who did not experience all-cause hospitalization for at least 24 hours, or did not require supplemental oxygen for at least 24 hours in response to SpO2 =93% and were alive by Day 28; the proportion of patients with all-cause hospitalization (defined as =24 hours), requiring supplemental oxygen orall-cause death by Day 28, and changes of SARS-Cov-2 viral load frombaseline to Day 28 as well as safety assessments. Proxalutamide is an ACE2 (angiotensin-converting enzyme 2) and TMPRSS2 (transmembrane protease, serine 2) proteins inhibitor that inhibits the entry of the SARS-CoV-2 virus into host cells.

For COVID-19 patients with early symptoms, targeting the ACE2/TMPRSS2 signal axis by proxalutamide could significantly inhibit the entry of the virus into host cells. For severe patients, proxalutamide promotes the clearance of pathogens and decreases inflammation by activating the Nrf2 pathway, which inhibits the over-production of IL-6, proinflammatory cytokines, and chemokines, thus minimizing cytokine storms and tissues damage. In this way, proxalutamide might be well-positioned as an effective drug for COVID-19 patients from early symptoms to hospitalized/severe conditions.