Table 2.
Summary of two potential antiviral drugs for monkeypox.
| Name | Tecovirimat | Brincidofovir, BCV |
|---|---|---|
| Synonym | Tpoxx®, ST-246 | Tembexa®; Hexadecyloxypropyl-cidofovir (HDP-CDV), CMX001 |
| US FDA approval | July 2018 for human smallpox | June 2021 for human smallpox |
| Pharmacological preparation | Capsule: 200 mg Injection: lyophilized powder for reconstitution, 200mg/20 mL |
Tablet: 100 mg Oral suspension: 10 mg/mL |
| Mechanism | Inhibit extracellular virus formation and prevent cell–cell and long-distance spread | A pro-drug of cidofovir conjugated with a lipid molecule; in infected cells, transformed into cidofovir diphosphate to inhibit DNA polymerase-mediated DNA synthesis and incorporate into the growing viral DNA chain, slow viral DNA synthesis rate |
| Treatment dose and duration | Oral - take within 30 min after eating full meal
|
|
| Renal or hepatic adjustment | Renal impairment
|
Renal or hepatic impairment: no dosage adjustment required with any degree of impairment |
| Pharmacokinetics |
|
Oral 100 mg tablet: Cmax, 251 ng/mL; area under curve, 1394 ng h/mL; oral bioavailability: 13.4% in tablet and 16.8% in suspension |
| Drug–drug interaction |
|
Concomitant use with OATP1B1 and 1B3 inhibitors increase BCV-associated adverse reactions |
| Efficacy in animal study | Survival rate of cynomolgus macaques with tecovirimat treatment at 5, 6, 7, or 8 days following monkeypox virus challenge: 100%, 67%, 100%, and 50% | Survival rate of prairie dogs intranasally challenged by monkeypox virus on the day of BCV therapy relative to inoculation day: 57% on ID-1, 43% on ID0, and 29% on ID1 |
| Adverse drug reactions |
|
Mild gastrointestinal events, such as diarrhea, nausea, vomiting, abdominal pain |
CrCl: creatinine clearance; CYP: cytochrome; ID-1: 1 day prior to viral challenge; ID0: the day of challenge; ID1: one day after viral challenge.
US FDA: Food and Drug Administration, United States.