- Molecular NameExemestane
- Synonymexemestane; Exemestano [INN-Spanish]; Exemestanum [INN-Latin]
- Weight296.41
- Drugbank_IDDB00990
- ACS_NO107868-30-4
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)2.62
- pkaN/A
- LogD (pH=7, predicted)2.62
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-4.22
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors0
- No.of HBond Acceptors2
- No.of Rotatable Bonds0
- TPSA34.14
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. An aim in the treatment of hormone-receptor-positive patients in preventing recurrence is to lower estrogen levels that this breast cancer thrives on.
- Absorption_valueN/A
- Absorption (description)Exemestane is rapidly absorbed after oral administration; more rapidly in women with breast cancer compared with those without. The presence of food can enhance absorption.
- Caco_2N/A
- Bioavailability42.0
- Protein binding90.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)Distribution of the drug and its metabolites into blood cells is negligible.
- MetabollsmThe drug undergoes extensive metabolism, in the liver, by oxidation and reduction to inactive or active metabolites which are less active than the parent drug including the 17-dihydro metabolite. Plasma levels can increase, by up to 40%, when the drug is administered with a high-fat meal. Plasma levels of the metabolite, 17-hydroxyexemestane are less than one tenth of the corresponding unchanged drug level.
- Half life24~27 h
- ExcretionExemestane is excreted, equally, in both urine and faeces with less than 1% of the dose being detected unchanged in urine.
- Urinary ExcretionN/A
- Clerance517 L/h
- ToxicityConvulsions
- LD50 (rat)N/A
- LD50 (mouse)N/A