Apalutamide

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 )

• ERLEADA 240 mg orally once daily
• Swallow tablets whole
• ERLEADA can be taken with or without food
• The recommended ERLEADA dosage in patients with severe hepatic impairment is 120 mg orally once daily
• Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy
• Recommended Dosage The recommended dosage of ERLEADA is 240 mg orally once daily
• ERLEADA can be taken with or without food [see Clinical Pharmacology ]
• 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
• 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 ]
• 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 and Adverse Reactions ]
• For other adverse reactions, including those that may be related to increased exposure to ERLEADA due to drug interactions [see Drug Interactions ] , 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. …

Tablets: 240 mg: bluish grey to grey, oval, film-coated and debossed with "E240" on one side. 60 mg: slightly yellowish to greyish green, oblong, film-coated and debossed with "AR 60" on one side. Tablets: 240 mg ( 3 ) Tablets: 60 mg ( 3 )

• Safety and effectiveness of ERLEADA
• In pediatric patients have not been established

Of the 1327 patients who received ERLEADA in clinical studies, 19% of patients were less than 65 years, 41% of patients were 65 years to 74 years, and 40% were 75 years and over. No overall differences in effectiveness were observed between older and younger patients. …

• Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use)
• Cerebrovascular and Ischemic Cardiovascular Events Inform patients that ERLEADA has been associated with cerebrovascular and ischemic cardiovascular events
• Advise patients to seek immediate medical attention if any symptoms suggestive of a cardiovascular or a cerebrovascular event occur [see Warnings and Precautions ]
• Falls and Fractures Inform patients that ERLEADA is associated with an increased incidence of falls and fractures [see Warnings and Precautions ]
• Seizures Inform patients that ERLEADA has been associated with an increased risk of seizure. …

• None
• None

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 Reduce the ERLEADA dose as recommended for adverse reactions [see Dosage and Administration (2.2) ] . 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). …

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. …

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. …

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. …

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.

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.

تناولها عندما تتذكر، إلا إذا اقترب موعد الجرعة التالية. عندها تخطَّ الجرعة المنسية. لا تتناول جرعتين معًا أبدًا للتعويض. راجع النشرة، فبعض الأدوية مختلفة.