Drug intelligence / Profile preview

apalutamide

Development stage
Approved
Lead developer
Janssen Research & Development
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Apalutamide is a nonsteroidal antiandrogen (NSAA) and androgen receptor inhibitor used for the treatment of prostate cancer. It works by selectively binding to the ligand-binding domain of the androgen receptor, blocking its nuclear translocation, DNA binding, and transcriptional activity. This inhibits the effects of androgens like testosterone and dihydrotestosterone in prostate tissue, thereby slowing or stopping tumor growth. Apalutamide is indicated for metastatic castration-sensitive prostate cancer as well as non-metastatic castration-resistant prostate cancer. It was first described in 2007 and approved by regulatory agencies beginning in 2018[1][2][3][4][5][7].

Brand names
ErleadaErlyand
Other names
apalutamide
02

Targets

GABRR (GABA-A receptor subunit rho)AR (Adrenergic receptors)

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