Ariane Rezvilutamide Tablets

1. Indications and Usage
Metastatic Hormone-Sensitive Prostate Cancer: Indicated for the treatment of adult patients with high-volume metastatic hormone-sensitive prostate cancer (mHSPC).
2. Dosage and Administration
Route of Administration: Oral administration.
Recommended Dosage: 240 mg once daily.
Administration Details: Swallow tablets whole without breaking, chewing, or crushing. May be taken with or without food.
Concomitant Therapy: Must be used in combination with androgen deprivation therapy (ADT), such as a GnRH agonist or bilateral orchiectomy.
Missed Dose: If a dose is missed, take it as soon as possible on the same day. If missed for a full day, skip the missed dose and resume the next day at the regular time. Do not take two doses at the same time.
Dose Adjustments: For Grade ≥3 toxicity or intolerable adverse reactions, suspend administration until symptoms improve to Grade ≤1 or baseline, then resume at the same dose or reduce to 160 mg or 80 mg as necessary.
3. Mechanism of Action
AR Inhibition: Rezvilutamide is a non-steroidal anti-androgen that competitively binds to the androgen receptor (AR).
Signal Blockade: It inhibits AR nuclear translocation and DNA binding, thereby blocking downstream signaling pathways that drive tumor cell proliferation and survival.
Blood-Brain Barrier: Optimized molecular structure results in low penetration of the blood-brain barrier, reducing the risk of central nervous system toxicity compared to first-generation agents.
4. Safety and Warnings
Hepatotoxicity: Elevations in liver enzymes (ALT/AST) are common. Liver function tests should be monitored regularly during treatment.
Embryo-Fetal Toxicity: Can cause fetal harm. Females of reproductive potential and males with female partners of reproductive potential must use effective contraception during and for at least 4 months after the last dose.
Renal and Hepatic Impairment: Not recommended for patients with moderate or severe hepatic or renal impairment due to lack of clinical data.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Weight gain, hypertension, hot flush, peripheral edema, fatigue, musculoskeletal pain, arthralgia, back pain, urinary retention, epistaxis, and constipation.
Clinical Research Highlights: The CHART study demonstrated significant improvements in radiographic progression-free survival and overall survival compared to first-generation anti-androgens when combined with ADT.
6. Drug Interactions
CYP450 Enzymes: Rezvilutamide is a strong inducer of CYP3A4, CYP2C8, CYP2C9, CYP2C19, and CYP2B6.
Substrate Drugs: May decrease exposure to concomitant medications metabolized by these enzymes. Concomitant use should be avoided or monitored closely.
7. Pharmaceutical Information
Chemical Composition: Active ingredient: Rezvilutamide.
Appearance: White to off-white film-coated tablets.
Packaging: Available in 40 mg or 80 mg tablets.
Storage: Store at controlled room temperature; protect from moisture.