- Molecular NameTrifluridine
- SynonymNA
- Weight296.201
- Drugbank_IDDB00432
- ACS_NO70-00-8
- Show 2D model
- LogP (experiment)-0.46
- LogP (predicted, AB/LogP v2.0)-0.5
- pkaN/A
- LogD (pH=7, predicted)-0.58
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.36
- LogSw (predicted, AB/LogsW2.0)2.92
- Sw (mg/ml) (predicted, ACD/Labs)1.09
- No.of HBond Donors3
- No.of HBond Acceptors7
- No.of Rotatable Bonds3
- TPSA99.1
- StatusFDA approved
- AdministrationEye drops
- PharmacologyAn anti-herpesvirus antiviral drug, used primarily on the eye.
- Absorption_valueN/A
- Absorption (description)Systemic absorption of trifluridine following therapeutic dosing with trifluridine ophthalmic appears to be negligible.
- Caco_2N/A
- BioavailabilityN/A
- Protein bindingN/A
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmOne major metabolite, 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea, indicating localized metabolism.
- Half life12 min
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityOverdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac. Acute overdosage by accidental oral ingestion has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of trifluridine is not likely to produce adverse effects. Single intravenous doses of 1.5 to 30 mg/kg/day in children and adults with neoplastic disease produce reversible bone marrow depression as the only potentially serious toxic effect and only after three to five courses of therapy. The acute oral LD50 in the mouse and rat was 4379 mg/kg or higher.
- LD50 (rat)N/A
- LD50 (mouse)N/A