Drug reference

Apalutamide

Hormonal Anticancer Agent · Prostate cancer treatment

Also known as Erleada

Hormonal Anticancer AgentProstate cancer treatmentATC null

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AbemaciclibSevereDatabaseDDInter
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AlpelisibSevereDatabaseDDInter

Mechanism

Apalutamide is a nonsteroidal antiandrogen agent that binds to the androgen receptor (AR) and inhibits AR-mediated transcription. This action decreases tumour cell proliferation and increases apoptosis.

Indications

Prostate cancer (specialist use only)non-metastatic castration-resistant prostate cancerNonmetastatic castration-resistant prostate cancer (CRPC)Metastatic castration-sensitive prostate cancer

Dosing

Adult: 240 mg once daily

Pharmacokinetics

Onset

Median time to achieve peak plasma concentration (tmax) is 2 hours (may be increased with a high-fat meal). Steady state is achieved by approximately 4 weeks.

Half-life

Mean elimination half-life is 3 to 4 days.

Bioavailability

Mean absolute oral bioavailability is approximately 100%.

Metabolism

Strong inducer of CYP3A4 and CYP2C19, and a weak inducer of CYP2C9.

Side effects

Common

Arthralgiaautoimmune thyroiditisbone fracturesconjunctivitiscostal cartilage fracturedyslipidaemiafallfatiguegenital rashhypothyroidismoral disordersrash pustularsacrum fractureskin reactionsweight decreasedHypertensionRashNauseaHot flushWeight lossFallsDecreased appetiteDiarrheaFracturePeripheral edema

Serious

Seizure
QT interval prolongation
Hypothyroidism
Increase in QT interval
Seizures (0.2% of patients, possibly related to interaction with the GABAA receptor)