TABLE 3.

Representative small molecule compounds for COVID-19 in human clinical trials with recruiting participants^a

Agents	Drug class and/or targets	Phase
Lopinavir/ritonavir	HIV protease inhibitor/CYP3A4 inhibitor	Phase 4
Darunavir/cobicistat	HIV protease inhibitor/CYP3A inhibitor	Phase 3
ASC09/ritonavir	HIV protease inhibitor/CYP3A4 inhibitor	Phase 3
Atazanavir	HIV protease inhibitor	Phase 2/3
Ribavirin	Broad antiviral agent/RdRp inhibitor	Phase 2 (completed)
Remdesivir	RdRp inhibitor	Approved
EIDD-2801	RdRp inhibitor	Phase 1/2
Favipiravir	RdRp inhibitor	Phase 2/3
Galidesivir	RdRp inhibitor	Phase 1
Oseltamivir	Influenza neuraminidase inhibitor	Phase 4
Arbidol	Broad antiviral agent/inhibit membrane fusion	N/A
Danoprevir	HCV NS3/4A protease inhibitor	Phase 4
Clevudine	Anti-HBV/nucleoside analog	Phase 2
Emtricitabine	HIV nucleoside reverse-transcriptase inhibitor	Phase 3
Tenofovir disoproxil	HIV nucleoside reverse-transcriptase inhibitor	Phase 3
Merimepodib	Noncompetitive IMPDH inhibitor	Phase 2
Cyclosporine	Immunosuppressive/cyclophilin inhibitors	Phase 4
Imatinib	Abl kinase inhibitor	Phase 2
Sirolimus	mTOR inhibitor	Phase 1/2
Acalabrutinib	Bruton′s tyrosine kinase inhibitor	Phase 2
Tacrolimus	Immunosuppressive	Phase 3
Baricitinib	JAK inhibitor	Phase 2/3
Ruxolitinib	JAK inhibitor	Phase 2/3
Tofacitinib	JAK inhibitor	Phase 2
TD-0903	JAK inhibitor	Phase 1/2
Camostat	Serine protease (TMPRSS2) inhibitor	Phase 2/3
Nafamostat	Serine protease (TMPRSS2) inhibitor	Phase 2/3
Chloroquine	Antimalarial/immunomodulatory	Phase 1–4
Hydroxychloroquine	Antimalarial/immunomodulatory	Phase 1–4
Amodiaquine	Antimalarial/immunomodulatory	Phase 2
GNS651	Chloroquine analog	Phase 2
Atovaquone	Antipneumocystis/antimalarial	Phase 2
Fingolimod	Immunomodulatory	Phase 2
Colchicine	Immunomodulatory	Phase 2
CM-4620	Inhibitor of CRAC channels/immunomodulatory	Phase 2
Azithromycin	Macrolide antibiotic/immunomodulatory	Phase 1–4
Methylprednisolone	Corticosteroid	Phase 3
Dexamethasone	Corticosteroid	Phase 3/4
Hydrocortisone	Corticosteroid	Phase 3/4
Budesonide	Corticosteroid	Phase 2–4
Prednisone	Corticosteroid	Phase 2
Ciclesonide	Corticosteroid	Phase 3
Aescin	Mixture of saponins/anti-inflammatory	Phase 2/3
N-Acetylcysteine	Replenish glutathione stores/anti-inflammatory	Phase 2
Aspirin	Inhibit cyclooxygenase (COX) enzyme	N/A
Ibuprofen	Nonsteroidal anti-inflammatory drug	Phase 4
Naproxen	Nonsteroidal anti-inflammatory drug	N/A
BLD-2260	Inhibitor of calpain 1, 2, and 9	Phase 2
Levamisole	Anthelmintic	Phase 2
Nitazoxanide	Antiprotozoal/broad antiviral agent	Phase 4
Niclosamide	Anthelmintic/broad antiviral agent	Phase 2/3
Ivermectin	Anthelmintic	Phase 2/3
Icosapent ethyl	Prodrug of eicosapentaenoic acid	Phase 2/4
Selinexor	Exportin 1 inhibitor	Phase 2
Spironolactone	Potassium-sparing diuretics	Phase 3
Triiodothyronine	A thyroid hormone	N/A
Tranexamic acid	Antifibrinolytic/lysine analog	Phase 2
Verapamil	Calcium channel blockers	Phase 2/3
Amiodarone	Class III antiarrhythmic agent	Phase 2/3
Valsartan	Angiotensin receptor blocker/antihypertensive	Phase 4
Losartan	Angiotensin receptor blocker/antihypertensive	Phase 2–4
Candesartan	Angiotensin receptor blocker/antihypertensive	Phase 2/3
Linagliptin	Inhibitor of dipeptidyl peptidase 4	Phase 3
Sildenafil	Inhibitor of PDE5	Phase 3
Simvastatin	HMG-CoA reductase inhibitor	Phase 2
Dapagliflozin	SGLT2 inhibitor/antidiabetic	Phase 3
Rivaroxaban	Factor Xa inhibitor	N/A
Clopidogrel	Antiplatelet/inhibit ADP P2Y12 receptor	N/A
Fluvoxamine	Serotonin reuptake inhibitor	Phase 2
Deferoxamine	Iron and aluminum chelator	Phase 1/2
Formoterol	β2 agonist/bronchodilator	Phase 2/3

Abbreviations: CRAC, Ca²⁺ release-activated Ca²⁺; HBV, hepatitis B virus; HCV, hepatitis C virus; HIV, human immunodeficiency virus; IMPDH, inosine-5′-monophosphate dehydrogenase; JAK, Janus kinase; mTOR, mammalian target of rapamycin; N/A, not applicable; PDE5, cGMP-specific phosphodiesterase type 5; RdRp, RNA-dependent RNA polymerase; SGLT2, sodium-glucose transport protein 2; TMPRSS2, transmembrane protease serine 2.

^aData were collected from https://clinicaltrials.gov/ when searching COVID-19 and SARS-CoV-2 for condition or disease. Access date: November 3, 2020. These compounds may be used as single treatment or combination use.