| monoclonal antibodies |
| 1 |
Anakinra (Kineret) |
recombinant human interleukin-1 (IL-1) receptor antagonist |
competitive binding to the IL-1 receptor and subsequently reducing the inflammatory responses |
EUA in November 2022 |
Treatment of hospitalized
COVID-19 patients with pneumonia
requiring supplemental oxygen who are at risk of progression to severe
respiratory failure. |
| 2 |
Bamlanivimab |
neutralizing human IgG1κ monoclonal antibody |
disrupting the surface spike (S) protein of SARS-CoV-2 by binding
to the receptor binding domain (RBD) of the S protein at a position
that overlaps the ACE2 binding site |
EUA in November
2020. |
Bamlanivimab is used in combination
with etesevimab
to treat mild to moderate COVID-19 in
adults and pediatric patients and also in younger children (including
newborns), who are at high risk for progressing to severe COVID-19. |
| FDA revokes EUA
for Bamlanivimab when administered alone to
treat COVID-19 in April 2021. |
| EUA in February 2021 for the administration of bamlanivimab
in combination with etesevimab. |
| 3 |
Bebtelovimab |
human IgG1κ monoclonal antibody |
inhibition of spike (S) protein interaction with
ACE2 and disrupting the viral entry into human cells |
EUA in February 2022 |
mild-to-moderate COVID-19 patients |
| drug withdrawal: November 2022 |
The
EUA was officially withdrawn due to a lack of efficacy
against Omicron subvariants. |
| 5 |
Etesevimab |
human and recombinant monoclonal
antibody |
disrupting the surface spike (S) protein of SARS-CoV-2 and neutralizing the virus
by specifically
binding to the S protein receptor binding domain |
EUA
in February 2021, in combination with bamlanivimab |
Etesevimab
is used in combination with bamlanivimab for postexposure
prophylaxis of COVID-19 and to treat mild to moderate COVID-19 in
adults and pediatric patients and also in younger children (including newborns), who are at high risk for progressing
to severe COVID-19. |
| 6 |
Evusheld (Tixagevimab + Cilgavimab) |
co-packaged
the two human monoclonal antibodies
tixagevimab and cilgavimab |
targeted against
the surface SARS-CoV-2 spike (S) protein and disrupting
the viral entry into human cells |
EUA in December 2021 |
For the pre-exposure prophylaxis of COVID-19 in adult and pediatric
patients aged 12 years and older weighing at least 40 kg, and at increased risk for whom vaccination
is not recommended |
| drug withdrawal: January
2023 |
The FDA revised and withdrew the EUA for Evusheld
against SARS-CoV-2 in January 2023 |
| 9 |
REGN-COV2 |
a combination of the antibodies casirivimab and imdevimab |
REGN-COV2 was obtained from
some humanized mice as well as blood samples from recovered COVID-19
patients and was formulated to bind to different sites on the SARS-COV-2
spike protein. |
EUA in November 2020 |
Treatment
of patients with mild to moderate COVID-19 aged 12
years or older and weighing at least 40 kg, and who are at high risk
of progression to severe COVID-19. |
| 10 |
Sotrovimab |
recombinant human IgG1κ monoclonal antibody |
attaching to the SARS-CoV-2 spike (S) protein and disrupting the endocytosis process |
EUA in May 2021 |
For the treatment of mild-to-moderate
COVID-19 (especially
in patients at increased risk for death or hospitalization). |
| drug withdrawal: April 2022 |
The FDA withdrew the EUA of sotrovimab against SARS-CoV-2 due to lack of efficacy against the Omicron
variant. |
| 11 |
Tocilizumab (Actemra) |
recombinant humanized monoclonal
antibody |
binding to soluble and membrane-bound IL-6 receptors and then inhibiting IL-6-induced inflammation |
fully approved
in December 2022 |
Treatment of adults COVID-19 patients receiving systemic corticosteroids
and supplemental oxygen
or mechanical ventilation. |
| small molecules |
| 4 |
Baricitinib |
pyrrolopyrimidine-based small molecule |
suppressing the activity of Janus kinase (JAK) proteins (especially JAK1 and JAK2) and modulating
the signaling pathway of interleukins, interferons and various growth
factors |
EUA in combination with remdesivir in November
2020 |
Treatment of adults hospitalized COVID-19 patients requiring supplemental oxygen,
invasive/noninvasive mechanical ventilation, or extracorporeal membrane
oxygenation. |
| fully approved in May 2022 |
| 7 |
Paxlovid |
a copackaged medication containing two peptidomimetic molecules
nirmatrelvir and ritonavir |
Nirmatrelvir inhibits the SARS-CoV-2 3C-like protease (3CLpro), but ritonavir
acts as a pharmacokinetic enhancer and increases the
duration of Nirmatrelvir’s activity by inhibiting cytochrome
P450 3A4 |
EUA in December 2021 |
Treatment
of adults and pediatric patients (12 years of age
and older weighing at least 40 kg) COVID-19 patients with the mild-to-moderate condition,
and who are at high risk for progression to severe disease. |
| 8 |
Remdesivir |
nucleoside-based molecule |
impairing the function of viral RdRp enzyme |
EUA in May 2020 |
Treatment of adult
and pediatric (28 days of age
and older and weighing at least 3 kg) COVID-19 patients requiring hospitalization,
and also for nonhospitalized patients who are at high risk for progression
to severe COVID-19. |
| fully approved in October 2020 |
| 12 |
Molnupiravir |
isopropylester
cytidine analog (prodrug of N4-hydroxycytidine) |
in the physiological environment, this compound is
hydrolyzed
to N4-hydroxycytidine and then becomes the phosphorylated 5′-triphosphate
(active form), increasing the frequency of viral RNA mutations and
impairs SARS-CoV-2 replication by disrupting RdRp activity. |
EUA in December 2021 |
Reducing the risk of hospitalization
and death and treatment
of mild to moderate adult COVID-19 patients
with an increased risk of severe disease. |
