Skip to main content

Table 1 FDA approvals (small molecules) [20]

From: Beyond the vaccines: a glance at the small molecule and peptide-based anti-COVID19 arsenal

Drugs

FDA approval status

Mechanism

Indications

Remdesivir

2020/05/01 EUA

2020/10/22 (Formal medicine certificate)

– Developer—Gilead

– Brand Name—Veklury

– Type—nucleoside analogue prodrug (small molecule)

– Mechanism—Inhibits the replication of the virus (RNA polymerase inhibitor)

– Activity profile—Remdesivir (GS-5734) demonstrates inhibitory potential towards SARS-CoV-2 in vitro. The studies conducted in animal models revealed that the inhibitor is endowed with the ability to inhibit MERS-CoV, SARS-CoV-1, and SARS-CoV-2 replication in animal models [27]

Approved for hospitalized patients, Adults and children (> 12 yr)

(EUA) hospital, Children (3.5–40 kg or < 12 yr and > 3.5 kg) [20]

Baricitinib

2020/11/19 EUA

2021/07/28 EUA (can be used alone)

– Developer—Eli Lilly

– Brand Name—Olumiant

– Type—Small molecule

– Mechanism—oral selective Janus Kinase 1/2 inhibitor

– Activity profile—Baricitinib demonstrates antiviral and anti-inflammatory properties. Also, Barcitinib suppresses the overstimulation of the immune system [28]

– A study results revealed that baricitinib—remdesivir combination was more efficacious than remdesivir alone in terms of reduction in the recovery time. Also, the cocktail of drugs caused improvement in clinical status among COVID-19 patients receiving high-flow oxygen or noninvasive ventilation [29]

Hospitalized, severe cases, adult and child (> 2 yr) [20]

Nirmatrelvir and ritonavir

(Oral)

12/22/2021 EUA

– Developer—Pfizer

– Brand Name—Paxlovid (nirmatrelvir and ritonavir)

– Type—small molecule inhibitors

– Mechanism—Paxlovid is a SARS-CoV-2-3CL protease inhibitor composed of nirmatrelvir and ritonavir. It inhibits viral replication at a proteolysis stage occurring before viral RNA replication. Nirmatrelvir is packaged with a strong cytochrome P450 3A4 inhibitor (ritonavir) which is used to boost HIV protease inhibitors

– Activity profile—In comparison to the placebo, Paxlovid (PF-07321332; ritonavir) reduced the risk of hospitalization risk or death by 89% in high-risk adults with COVID-19 [30, 31]

Severe high risk and mild to medium, adult and child (> 12 yr or 40 kg) [20]

Molnupiravir

12/23/2021 EUA

– Developer—Merck

– Brand name—Lagevrio

– Type- Small-molecule nucleoside antiviral prodrug

– Mechanism—Molnupiravir acts by increasing the frequency of viral RNA mutations frequency and leads to impairment of the SARS-CoV-2 replication [32]

– Activity profile—effective reduction of viral load and complete prevention of virus transmission through direct contact with untreated animals was evidenced with Molnupiravir [33]

Severe high risk, mild and medium, adult [20]