1. Indications and Usage
\nNon-Metastatic Castration-Resistant Prostate Cancer (nmCRPC):
\nIndicated for the treatment of adult patients with nmCRPC at high risk of metastasis.
\nMetastatic Hormone-Sensitive Prostate Cancer (mHSPC):
\nIndicated for the treatment of adult patients with mHSPC, in combination with androgen deprivation therapy (ADT).
\n2. Dosage and Administration
\nRoute of Administration:
\nFor Oral Use ONLY.
\nRecommended Dosage:
\nDose: 240 mg (four 60 mg tablets) once daily.
\nTreatment Duration: Continue until disease progression or unacceptable toxicity.
\nAdministration Instructions:
\nSwallow tablets whole with water; do not crush or split.
\nAdminister with or without food.
\nConcomitant Therapy: Must be used in combination with a GnRH analogue (continuous medical castration) or in patients who have undergone bilateral orchiectomy.
\nMissed Dose: If a dose is missed, take it as soon as possible on the same day. Resume the normal schedule the following day. Do not take a double dose.
\nDose Adjustments:
\nReduce dose (to 180 mg or 120 mg) for intolerable Grade \u22653 adverse reactions.
\nPermanently discontinue for seizures, severe cutaneous adverse reactions (SCARs), or interstitial lung disease (ILD).
\n3. Mechanism of Action
\nAndrogen Receptor (AR) Inhibition:
\nApalutamide is an androgen receptor inhibitor that binds directly to the ligand-binding domain of the AR.
\nBlocking Signaling Pathways:
\nIt inhibits multiple steps in the AR signaling pathway:
\n1. Inhibits the binding of testosterone and dihydrotestosterone (DHT) to the AR.
\n2. Inhibits the nuclear translocation of the activated AR.
\n3. Inhibits the binding of the AR to DNA, thereby blocking AR-mediated transcription and tumor cell growth.
\n4. Safety and Warnings
\nSeizures:
\nCan cause seizures. Monitor patients for signs of seizure activity. Permanently discontinue if a seizure occurs.
\nFalls and Fractures:
\nIncreased risk of falls and fractures due to fatigue and musculoskeletal effects. Assess fall risk and consider bone-modifying agents.
\nCardiovascular Events:
\nMay increase the risk of ischemic cardiovascular and cerebrovascular events. Monitor for symptoms and optimize risk factors.
\nSevere Cutaneous Adverse Reactions (SCARs):
\nCan cause serious rashes (e.g., Stevens-Johnson Syndrome). Monitor for rash symptoms.
\nEmbryo-Fetal Toxicity:
\nMales with female partners of reproductive potential must use effective contraception during treatment and for 3 months after the final dose.
\n5. Adverse Reactions
\nMost Common (Incidence \u226520%):
\nFatigue, arthralgia, rash, decreased appetite, fall, weight decrease, hypertension, and hot flashes.
\n6. Drug Interactions
\nCYP Enzyme Induction:
\nApalutamide is a strong inducer of CYP3A4 and CYP2C19, and a moderate inducer of CYP2C9.
\nImpact on Other Drugs:
\nConcomitant use may significantly decrease the exposure and efficacy of sensitive substrates (e.g., warfarin, certain statins, benzodiazepines). Dose adjustments or alternative therapies may be required.
\n7. Pharmaceutical Information
\nChemical Composition:
\nActive Ingredient: Apalutamide.
\nAvailable Strength: 60 mg tablets.
\nAppearance: Pale yellow to grayish-green, oval, film-coated tablets debossed with “AR 60”.
\nStorage: Store at room temperature (20\u00b0C\u201325\u00b0C \/ 68\u00b0F\u201377\u00b0F). Protect from moisture.<\/p>\n","protected":false},"excerpt":{"rendered":"
Brand Name:\u5b89\u68ee\u73c2 \u00ae(Erleada\u00ae)
\nGeneric Name: Apalutamide
\nStrength: 60 mg per tablet, 120 tablets per bottle\/box
\nManufacturer: Janssen Ortho, LLC
\nMarketing Authorization Holder: Janssen-Cilag International NV (Belgium); domestic filing entity: Xi’an Janssen Pharmaceutical Ltd.
\nApproval Date in China: September 5, 2019
\nRegistration Number: \u56fd\u836f\u51c6\u5b57H20190050
\nStorage: Store at 20\u00b0C\u201325\u00b0C (68\u00b0F\u201377\u00b0F) in the original package, protected from light and moisture. Brief exposure to 15\u00b0C\u201330\u00b0C (59\u00b0F\u201386\u00b0F) is permitted. Keep out of reach of children.<\/p>\n
Price&Cost:Contact Us now for the best price of Apalutamide\uff08Erleada\uff09<\/p>\n","protected":false},"featured_media":3933,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[],"product_cat":[27],"product_tag":[],"class_list":["post-3932","product","type-product","status-publish","has-post-thumbnail","product_cat-tablets","first","instock","shipping-taxable","product-type-simple"],"yoast_head":"\n