Apalutamide (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- APALUTAMIDE
- ERLEADA
Indications and Usage
ERLEADA is indicated for the treatment of patients with Metastatic castration-sensitive prostate cancer (mCSPC) Non-metastatic castration-resistant prostate cancer (nmCRPC)
Adverse Reactions
The following are discussed in more detail in other sections of the labeling: Cerebrovascular and Ischemic Cardiovascular Events [see Warnings and Precautions (5.1)]. Fractures [see Warnings and Precautions (5.2)]. Falls [see Warnings and Precautions (5.3)]. Seizure [see Warnings and Precautions (5.4)]. Severe Cutaneous Adverse Reactions (SCARs) [see Warnings and Precautions (5.5)]. Interstitial Lung Disease (ILD) [see Warnings and Precautions (5.6)].
Mechanism of Action
Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide administration caused decreased tumor cell proliferation and increased apoptosis leading to decreased tumor volume in mouse xenograft models of prostate cancer.
Overdosage
There is no known specific antidote for apalutamide overdose. In the event of an overdose, stop ERLEADA, undertake general supportive measures until clinical toxicity has been diminished or resolved.