Abiraterone
DB05812
Approved Indication
Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.
1
Targets
0
Resistance Mutations
2
References
3RUK
Structure Loaded
Protein Targets
Mechanism of Action
Abiraterone is an orally active inhibitor of the steroidal enzyme CYP17A1 (17 alpha-hydroxylase/C17,20 lyase). It inhibits CYP17A1 in a selective and irreversible manner via covalent binding mechanism. CYP17A1 is an enzyme that catalyzes the biosynthesis of androgen and is highly expressed in testicular, adrenal, and prostatic tumor tissue. More specifically, abiraterone inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone (DHEA) by the enzyme CYP17A1 to decrease serum levels of testosterone and other androgens.
Details
DrugBank ID
DB05812 ↗
Approval Date
2011-04-28
Molecular Weight
349.509 g/mol
Drug Class
Other
ATC Codes
L02BX03
Synonyms
—
PubChem
CID: 132971 ↗
ChEMBL
CHEMBL254328 ↗
SMILES
[H][C@@]12CC=C(C3=CC=CN=C3)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC=C2C[C@@H](O)CC[C@]12C
ADMET Profile
Computing properties…
Drug References (DrugBank)