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Brincidofovir is an oral lipid prodrug of cidofovir used in the treatment of human smallpox disease. It is a lipid conjugate pro-drug of the acyclic nucleotide analogue cidofovir - this lipid conjugate improves drug delivery to the target cells and significantly reduces the nephrotoxicity typically associated with cidofovir therapy.
- Mechanism
- Curator reviewed · 5 references
Brincidofovir is a pro-drug comprising cidofovir conjugated to a lipid molecule - the lipid component mimics an endogenous lipid, lysophosphatidylcholine, which allows the molecule to hijack endogenous lipid uptake pathways to enter infected cells. Following uptake, the lipid molecule is cleaved to generate cidofovir, which is then phosphorylated to generate the active antiviral compound, cidofovir disphosphate.
The antiviral effects of cidofovir diphosphate appear to be the result of two distinct mechanisms. Mechanistic studies using recombinant vaccinia DNA polymerase suggest that it inhibits orthopoxvirus DNA polymerase-mediated DNA synthesis. In addition, cidofovir is an acyclic nucleotide analogue of deoxycytidine monophosphate - cidofovir diphosphate can therefore be incorporated into the growing viral DNA chain and consequently slow the rate of viral DNA synthesis.
- Primary indication
- Brincidofovir is indicated for the treatment of human smallpox disease in adult and pediatric patients.Curator reviewed · 1 structured indication
- Formula / weight
- C27H52N3O7P · 561.701 g/mol (avg)
- First approval
- Canada, 2023 · United States, 2022
- Also known as
- Cidofovir hexadecyloxypropyl ester · Hexadecyloxypropyl cidofovir
- Code names
- CMX-001 · SyB V-1901
- Brand names
- Tembexa
Resolves to
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Which drugs share a target with Brincidofovir, and which of those have an active Phase 3 trial?