One proposed mechanism of benefit of anti-androgens is the downregulation of TMPRSS2. Picture CC-BY Veronica Mollica, Rizzo, Massarii.

Anti-androgens are a proposed COVID-19 therapeutic. Anti-androgens are drugs that either block the binding of ligands at the androgen receptor (e.g. bicalutamide) or block the production of androgens in the body (e.g. dutasteride).

Possible mechanism of benefit in COVID-19

One proposed mechanism of benefit for anti-androgens in COVID-19 is by modulating the expression of serine protease TMPRSS2. In "SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor," it was shown that SARS-CoV-2 cell entry depends on TMPRSS2. TMPRSS2 may be regulated by androgens and estrogens.

Overview articles on potential mechanisms

Clinical trial results

N=588 double-blind, randomized controlled trial of proxalutamide in Brazil reported a > 90% reduction in mortality in hospitalized COVID-19 patients in an early press release:

The preliminary analysis conducted on March 9, 2021 was based on 294 patients (56.8% male) inthe Proxalutamide arm and 296 patients (57.8% male) in the control arm. According to the results on day 14, the mortality in Proxalutamide arm was 11(3.7%), compared to 141 (47.6%) in control arm, demonstrating a reduced mortality risk of 92%. The number of new mechanical ventilation (MV) and/ordeath in Proxalutamide arm was 13 (4.4%), compared to 156 (52.7%) in control arm, reducing mortality risk by 92%; and median hospital length stay (days) in Proxalutamide arm was 5, while it was 14 in control arm, which means Proxalutamide shortened hospital stay by 9 days.

Observational studies

Possibly contradictory to androgen-driven hypothesis:

In vitro & vivo animal studies

List of clinical trials

See also

COVID-19 therapeutics