- Molecular NameTazarotene
- Synonymtazarotene
- Weight351.47
- Drugbank_IDDB00799
- ACS_NO118292-40-3
- Show 2D model
- LogP (experiment)5.96
- LogP (predicted, AB/LogP v2.0)5.34
- pkaN/A
- LogD (pH=7, predicted)5.33
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)-6.17
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors0
- No.of HBond Acceptors3
- No.of Rotatable Bonds5
- TPSA64.49
- StatusFDA approved
- AdministrationTopical
- PharmacologyA prescription topical retinoid sold as a cream or gel. This medication is approved for treatment of psoriasis, acne, and sun damaged skin (photodamage).
- Absorption_valueN/A
- Absorption (description)Minimal systemic absorption of tazarotene occurs due to its rapid metabolism in the skin to the active metabolite, tazarotenic acid, which can be systemically absorbed and further metabolized. Gender had no influence on the systemic bioavailability of tazarotenic acid.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding99.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmUndergoes esterase hydrolysis in skin to form its active metabolite, tazarotenic acid. Tazarotenic acid is further metabolized in skin and, after systemic absorption, hepatically metabolized to sulfoxides, sulfones, and other polar products for elimination.
- Half life19 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityExcessive topical use may lead to marked redness, peeling, or discomfort. Oral ingestion of the drug may affect liver function causing hypertriglyceridemia. Other symptoms may include conjunctival irritation, hair loss, headache, edema, fatigue, dermatitis, nausea, and visual disturbances. Oral administration of this material to rats and rabbits at doses of 0.20 mg/kg/day (rabbits) and 0.25 mg/kg/day (rats) resulted in developmental toxicity. A no effect level of 0.05 mg/kg/day was established. Similar teratogenic effects have been reported for other retinoid compounds.
- LD50 (rat)N/A
- LD50 (mouse)N/A