Apalutamide
Generic Name: apalutamide
Brand Names:
Erleada
11 DESCRIPTION Apalutamide, the active ingredient of ERLEADA, is an androgen receptor inhibitor. Each ERLEADA tablet contains either 60 mg or 240 mg of apalutamide. The chemical name is (4-[7-(6-Cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide). Apalutamide is a white to slightly yellow powder. Apalutamide is practically insoluble in aqueous media over a wide range of pH values.
Overview
11 DESCRIPTION Apalutamide, the active ingredient of ERLEADA, is an androgen receptor inhibitor. Each ERLEADA tablet contains either 60 mg or 240 mg of apalutamide. The chemical name is (4-[7-(6-Cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide). Apalutamide is a white to slightly yellow powder. Apalutamide is practically insoluble in aqueous media over a wide range of pH values.
Uses
1 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) 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. ( 1 )
Dosage
2 DOSAGE AND ADMINISTRATION ERLEADA 240 mg administered orally once daily. Swallow tablets whole. ERLEADA can be taken with or without food. ( 2.1 , 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 dose of ERLEADA is 240 mg administered orally once daily. This could be administered as one 240 mg tablet or four 60 mg tablets. Swallow the tablet(s) whole. Do not crush or split tablet(s). ERLEADA can be taken with or without food. Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.
Side Effects
6 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) ] . The most common adverse reactions (≥10%) are fatigue, arthralgia, rash, decreased appetite, fall, weight decreased, hypertension, hot flush, diarrhea, and fracture.
Interactions
7 DRUG INTERACTIONS Concomitant use with medications that are sensitive substrates of CYP3A4, CYP2C19, CYP2C9, UGT, P-gp, BCRP, or OATP1B1 may result in loss of activity of these medications. ( 7.2 ) 7.1 Effect of Other Drugs on ERLEADA Strong CYP2C8 or CYP3A4 Inhibitors Co-administration of a strong CYP2C8 or CYP3A4 inhibitor is predicted to increase the steady-state exposure of the active moieties (sum of unbound apalutamide plus the potency-adjusted unbound N-desmethyl-apalutamide). No initial dose adjustment is necessary however, reduce the ERLEADA dose based on tolerability [see Dosage and Administration (2.2) ] . Mild or moderate inhibitors of CYP2C8 or CYP3A4 are not expected to affect the exposure of apalutamide.
Warnings
5 WARNINGS AND PRECAUTIONS 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. 4 CONTRAINDICATIONS None. ( 4 ) None.
Pregnancy
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.
Storage
Storage and Handling Store at 20 °C to 25 °C (68 °F to 77 °F); excursions permitted to 15 °C to 30 °C (59 °F to 86 °F) [see USP Controlled Room Temperature] . Store in original package to protect from light and moisture. Do not discard desiccant.
Frequently Asked Questions
What is Apalutamide used for?▼
1 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) 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. ( 1 )
What are the side effects of Apalutamide?▼
6 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) ] . The most common adverse reactions (≥10%) are fatigue, arthralgia, rash, decreased appetite, fall, weight decreased, hypertension, hot flush, diarrhea, and fracture.
Can I take Apalutamide during pregnancy?▼
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.
What are the important warnings for Apalutamide?▼
5 WARNINGS AND PRECAUTIONS 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. 4 CONTRAINDICATIONS None. ( 4 ) None.
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.