- Molecular NameTadalafil
- SynonymCIA; ICOS 351; tadalafil; Tadanafil
- Weight389.411
- Drugbank_IDDB00820
- ACS_NO171596-29-5
- Show 3D model
- LogP (experiment)1.35
- LogP (predicted, AB/LogP v2.0)1.62
- pkaN/A
- LogD (pH=7, predicted)1.62
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-4.49
- LogSw (predicted, AB/LogsW2.0)0.1
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors1
- No.of HBond Acceptors7
- No.of Rotatable Bonds1
- TPSA74.87
- StatusFDA approved
- AdministrationN/A
- PharmacologyA PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; it has recently been approved for the treatment of pulmonary arterial hypertension, and has been used for other conditions.
- Absorption_valueN/A
- Absorption (description)After single oral-dose administration, the maximum observed plasma concentration (Cmax) of tadalafil is achieved between 30 minutes and 6 hours (median time of 2 hours). Absolute bioavailability of tadalafil following oral dosing has not been determined.
- Caco_2N/A
- Bioavailability16.0
- Protein binding94.0
- Volume of distribution (VD)0.89 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmTadalafil is predominantly metabolized by CYP3A4 to a catechol metabolite. The catechol metabolite undergoes extensive methylation and glucuronidation to form the methylcatechol and methylcatechol glucuronide conjugate, respectively. In vitro data suggests the metabolites are not expected to be pharmacologically active at observed metabolite concentrations.
- Half life17.5 h
- ExcretionFeces (> 60%), urine (> 30%)
- Urinary ExcretionN/A
- Clerance0.59 ml/min/kg
- ToxicityN/A
- LD50 (rat)LD50=2000 mg/kg
- LD50 (mouse)N/A