Drugs → Enzalutamide

Enzalutamide

Androgen Receptor Antagonist
DB08899
Approved Indication

Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.

1 Targets
8 Resistance Mutations
12 References
3D Structure No structure available
No co-crystal structure available
Protein Targets
AR P10275 ✓
Mechanism of Action

Enzalutamide is a competitive androgen receptor inhibitor that effects multiple stages of the signalling pathway. It is able to inhibit androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with DNA. As a result, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.

Resistance Mutations — 8 resistance samples observed in COSMIC
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AR
p.F345L p.F694L p.F877L 5 p.H733R p.T346A p.T695A 1 p.T878A 5 p.V732A

Resistance mutations sourced from COSMIC Drug Resistance database. Cyan = on-target · Amber = off-target · numbered badge = PubMed references for that mutation

Details
DrugBank ID DB08899 ↗
Approval Date 2012-08-31
Molecular Weight 464.436 g/mol
Drug Class Androgen Receptor Antagonist
ATC Codes L02BB04
Synonyms —
PubChem CID: 15951529 ↗
ChEMBL CHEMBL1082407 ↗
SMILES
CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F
ADMET Profile
Computing properties…
Drug References (DrugBank)
PMID:23699654