pharmacopeia
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/api/v1/drug/apalutamide

Mechanism of action

Sourced from openFDA

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.

Androgen ReceptorGABA A

Indications

Sourced from openFDA
  • ERLEADA is indicated for the treatment of patients with Metastatic castration-sensitive prostate cancer (mCSPC) Non-metastatic castration-resistant prostate cancer (nmCRPC) ERLEADA is an androgen receptor inhibitor indicated for the treatment of patients with metastatic castration-sensitive prostate cancer. ( 1 ) non-metastatic castration-resistant prostate cancer.ICD-10: C61

Contraindications

Sourced from openFDA
  • None. ( 4 ) None.contraindicated

Dosage & administration

Sourced from openFDA

ERLEADA 240 mg orally once daily. Swallow tablets whole. ERLEADA can be taken with or without food. ( 2.1 ) The recommended ERLEADA dosage in patients with severe hepatic impairment is 120 mg orally once daily. ( 2.3 ) Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. ( 2.1 ) 2.1 Recommended Dosage The recommended dosage of ERLEADA is 240 mg orally once daily. ERLEADA can be taken with or without food [see Clinical Pharmacology (12.3) ] . Swallow the tablet(s) whole. Do not crush or split tablet(s). Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy. 2.2 Dosage Modifications for Adverse Reactions If Grade 3 or 4 adverse reactions, or other intolerable adverse reactions occur, withhold ERLEADA. Consider permanent discontinuation of ERLEADA for Grade 3 or 4 cerebrovascular and ischemic cardiovascular events [see Warnings and Precautions (5.1) ] . Permanently discontinue ERLEADA for severe ILD/pneumonitis or if no other potential causes of ILD/pneumonitis are identified, or confirmed SCARs, or for other Grade 4 skin reactions [see Warnings and Precautions (5.5 , 5.6) and Adverse Reactions (6.1) ] . For other adverse reactions, including those that may be related to increased exposure to ERLEADA due to drug interactions [see Drug Interactions (7.1) ] , resume ERLEADA at the same dose or at a reduced dose (180 mg or 120 mg) when symptoms improve to less than or equal to Grade 1 or original grade, if warranted.

Warnings & precautions

Sourced from openFDA

Cerebrovascular and ischemic cardiovascular events occurred in patients receiving ERLEADA. Monitor for signs and symptoms of cerebrovascular disorders and ischemic heart disease. Optimize management of cardiovascular risk factors. ( 5.1 ). Fractures occurred in patients receiving ERLEADA. Evaluate patients for fracture risk and treat patients with bone-targeted agents according to established guidelines. ( 5.2 ) Falls occurred in patients receiving ERLEADA with increased incidence in the elderly. Evaluate patients for fall risk. ( 5.3 ) Seizure occurred in 0.4% of patients receiving ERLEADA. Permanently discontinue ERLEADA in patients who develop a seizure during treatment. ( 5.4 ) Severe Cutaneous Adverse Reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN) and drug reaction with eosinophilia and systemic symptoms (DRESS), occurred in patients treated with ERLEADA. Interrupt ERLEADA if signs or symptoms of SCARs develop. Permanently discontinue if SCARs are confirmed. ( 5.5 ) Interstitial Lung Disease (ILD)/pneumonitis occurred in patients treated with ERLEADA. Withhold ERLEADA for suspected ILD/pneumonitis. Permanently discontinue ERLEADA in patients with severe ILD/pneumonitis or if no other potential causes of ILD/pneumonitis are identified. ( 2.2 , 5.6 ) Embryo-Fetal Toxicity: ERLEADA can cause fetal harm. Advise males with female partners of reproductive potential to use effective contraception.

Adverse reactions

Sourced from openFDA

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) ] . The most common adverse reactions (≥10%) are fatigue, arthralgia, rash, decreased appetite, fall, weight decreased, hypertension, hot flush, diarrhea, and fracture. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Janssen Products, LP at 1-800-526-7736 (1-800-JANSSEN) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions (≥ 10%) that occurred more frequently in the ERLEADA-treated patients (≥ 2% over placebo) from the randomized placebo-controlled clinical trials (TITAN and SPARTAN) were fatigue, arthralgia, rash, decreased appetite, fall, weight decreased, hypertension, hot flush, diarrhea, and fracture. Metastatic Castration-sensitive Prostate Cancer (mCSPC) TITAN, a randomized (1:1), double-blind, placebo-controlled, multi-center clinical study, enrolled patients who had mCSPC.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary The safety and efficacy of ERLEADA have not been established in females. Based on findings from animals and its mechanism of action, ERLEADA can cause fetal harm and loss of pregnancy when administered to a pregnant female [see Clinical Pharmacology (12.1) ] . There are no available data on ERLEADA use in pregnant women to inform a drug-associated risk. In an animal reproduction study, oral administration of apalutamide to pregnant rats during and after organogenesis resulted in fetal abnormalities and embryo-fetal lethality at maternal exposures ≥ 2 times the human clinical exposure (AUC) at the recommended dose (see Data ) . Data Animal Data In a pilot embryo-fetal developmental toxicity study in rats, apalutamide caused developmental toxicity when administered at oral doses of 25, 50 or 100 mg/kg/day throughout and after the period of organogenesis (gestational days 6–20). Findings included embryo-fetal lethality (resorptions) at doses ≥50 mg/kg/day, decreased fetal anogenital distance, misshapen pituitary gland, and skeletal variations (unossified phalanges, supernumerary short thoracolumbar rib(s), and small, incomplete ossification, and/or misshapen hyoid bone) at ≥25 mg/kg/day. A dose of 100 mg/kg/day caused maternal toxicity.

Pharmacokinetics

Sourced from openFDA
Metabolism
Apalutamide and N-desmethyl apalutamide pharmacokinetic parameters were observed at steady state following the approved recommended dosage for ERLEADA and are presented as the mean [standard deviation (SD)] unless otherwise specified. Apalutamide maximum concentration (C max ) is 6 mcg/mL (1.7) and total systemic exposure (AUC) is 100 mcg∙h/mL (32).

Overdosage

Sourced from openFDA

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.

Approval history

Sourced from openFDA
  • Feb 14, 2018NDANDA210951Janssen Biotech

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
11,281 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Rash1,22911%
  2. 2Death1,16510%
  3. 3Fatigue1,13010%
  4. 4Hot Flush8467.5%
  5. 5Product Dose Omission Issue4363.9%
  6. 6Asthenia4203.7%
  7. 7Diarrhoea3913.5%
  8. 8Dizziness3593.2%
  9. 9Off Label Use3523.1%
  10. 10Arthralgia3383.0%
  11. 11Fall3232.9%
  12. 12Decreased Appetite3042.7%
  13. 13Prostatic Specific Antigen Increased3012.7%
  14. 14Incorrect Dose Administered2822.5%
  15. 15Pruritus2702.4%

Clinical trials

View JSON

The 10 most recently updated of 169 ClinicalTrials.gov registrations naming Apalutamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Apalutamide work?
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.
What is Apalutamide used for?
According to FDA labeling, Apalutamide carries indications including: ERLEADA is indicated for the treatment of patients with Metastatic castration-sensitive prostate cancer (mCSPC) Non-metastatic castration-resistant prostate cancer (nmCRPC) ERLEADA is an androgen receptor inhibitor indicated for the treatment of patients with metastatic castration-sensitive prostate cancer. ( 1 ) non-metastatic castration-resistant prostate cancer.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Apalutamide?
Apalutamide is classified as Anti-androgens, Androgen Receptor Antagonists, GABA A Antagonists, Cellular Proliferation Alteration, Cellular Transport Alteration.
What are the brand names for Apalutamide?
Apalutamide is marketed under brand names including Erleada.
What are the contraindications for Apalutamide?
Apalutamide labeling lists contraindications including: None. ( 4 ) None.. Always consult the full prescribing information and a clinician.
Note. Data for apalutamide is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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