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. 2022 Sep 6;55(5):795–802. doi: 10.1016/j.jmii.2022.08.016

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
  • 40 kg to <120 kg: 600 mg BID for 14 days

  • ≥120 kg: 600 mg TID for 14 days

  • Intravenous dosing -

  • 35 kg to <120 kg: 200 mg over 6 h q12 h for 14 days

  • ≥120 kg: 300 mg over 6 h q12 h for 14 days

  • ≥48 kg (tablet or oral suspension): 200 mg PO x 2 doses (on Day 1 and 8)

  • <48 kg (oral suspension): 4 mg/kg PO x 2 doses (on Day 1 and 8)

Renal or hepatic adjustment Renal impairment
  • Oral: mild, moderate, severe, or patients requiring hemodialysis: no dosage adjustment required

  • Intravenous: mild-to-moderate (CrCl 30–89 mL/min), no dosage adjustment necessary; severe (CrCl <30 mL/min), contraindicated

Hepatic impairment
  • Mild, moderate, or severe (Child-Pugh class A, B, or C): no dosage adjustment required

Renal or hepatic impairment: no dosage adjustment required with any degree of impairment
Pharmacokinetics
  • Plasma protein binding: 77.3%–96.3%

  • Route of elimination: feces (71–75%) and urine (18–24%) at 96 h post dose

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
  • May induce certain CYP enzymes, including CYP3A4, and its metabolites (M4 and M5) have the potential to produce drug–drug interactions by the induction of CYP2B6

  • Increased effect of repaglinide; decrease effectiveness of midazolam

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
  • Oral: headache, osteoarthritis, and hidradenitis

  • Intravenous: infusion site pain, swelling, erythema, extravasation; headache

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.