Rezvilutamide Tablets belong to the second-generation androgen receptor (AR) inhibitors and represent China's first independently developed novel AR inhibitor.
1. Drug Overview
Its innovative molecular structure incorporates dihydroxyl groups to enhance hydrophilicity, resulting in higher plasma exposure and lower blood-brain barrier permeability. The mechanism of action involves blocking the binding pathway between androgens and their receptors, thereby reducing the activity of prostate cancer cells. It has received a Grade I recommendation (Category 1A evidence) in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Prostate Cancer (2022 Edition) and has been included in the National Reimbursement Drug List (Class B), with reimbursement restricted to patients with metastatic hormone-sensitive prostate cancer (mHSPC).
2. Indications
This product is indicated for the treatment of patients with metastatic hormone-sensitive prostate cancer (mHSPC) who have large tumor volumes (i.e., patients with high tumor burden mHSPC), aiming to alleviate symptoms associated with tumor enlargement or metastasis. Specific characteristics of the applicable population are as follows:
Presence of a large primary tumor or multiple metastatic lesions (high tumor burden state), with common metastatic sites including bones and lymph nodes;
Cancer cells have not developed resistance to hormonal therapy (hormone-sensitive stage);
Presence of tumor-related symptoms such as pelvic pain, dysuria, and bone pain, where conventional hormonal therapy may gradually lose efficacy.
It should be specifically noted that no clear survival-prolonging effect has been observed for this drug to date, and long-term efficacy requires continuous monitoring.
3. Dosage and Administration
3.1 Dosage Form and Strength
This product is available as tablets, each containing 80 mg of active ingredient rezvilutamide. Excipients include lactose, microcrystalline cellulose, croscarmellose sodium, hypromellose, magnesium stearate, polyethylene glycol 400, and gastric film coating premix. This product contains lactose; patients with rare lactose intolerance must not use this product.
3.2 Specific Administration
Route of Administration: Oral. The tablet must be swallowed whole and must not be broken, chewed, or crushed. It can be taken with or without food.
Standard Dose: 3 tablets (240 mg total) once daily.
Combination Therapy Requirements: During treatment, concomitant androgen deprivation therapy is required, specifically through simultaneous use of gonadotropin-releasing hormone analog (GnRHa) medications, or patients who have undergone bilateral orchiectomy may take this medication directly.
3.3 Management of Special Situations
Missed Dose: If a dose is forgotten on the same day, take it as soon as remembered. If an entire day's dose is missed, take the normal dose the next day; do not double the dose to make up for the missed one.
Dose Adjustment: In case of Grade 3 or higher severe adverse reactions or intolerable adverse reactions, treatment should be suspended. After symptoms have improved to Grade 1 or the original level, treatment may be resumed at the original dose or a reduced dose (160 mg/day or 80 mg/day).
Overdose Management: Currently, there is no specific antidote for rezvilutamide overdose. In case of overdose, discontinue medication immediately and implement routine monitoring measures until adverse reactions subside or disappear. During this period, closely monitor the patient's condition and seek medical attention promptly if discomfort occurs.
3.4 Dosage for Special Populations
Children and Adolescents (under 18 years): Safety and efficacy have not been confirmed; use is not recommended.
Elderly Patients (over 60 years): No dose adjustment is required; administer according to the standard dosage.
Patients with Hepatic or Renal Impairment: No dose adjustment is needed for mild hepatic or renal impairment; there is insufficient data on the use of this drug in patients with moderate or severe hepatic or renal impairment, and its use is not recommended.
All treatment regimens must strictly follow the doctor's instructions; do not adjust the administration method or dosage independently.
4. Contraindications
The following populations are strictly prohibited from using this product, as use may pose serious risks:
Patients with hypersensitivity to the main ingredient (rezvilutamide) or any excipients;
Women who are pregnant or planning to become pregnant;
Patients with rare lactose intolerance.
5. Precautions for Special Populations
The following populations may experience worsening of conditions or increased risks when using this product and require special caution. If the doctor assesses that medication is necessary, close monitoring is required:
Patients with Hepatic or Renal Impairment
No dose adjustment is needed for mild hepatic or renal impairment; use is not recommended for patients with moderate or severe hepatic or renal impairment;
Lactating Women
The drug may affect infants through breast milk; use with caution;
Drivers and Machine Operators
Although the drug itself has minimal impact on driving, convulsions have been reported with similar drugs. Relevant risks should be communicated in advance, and patients should avoid engaging in hazardous activities such as high-altitude work during treatment.
6. Use in Special Populations
Pregnant Women
Use is prohibited throughout pregnancy, as this product may impair fetal development;
Lactating Women
It is not yet clear whether the drug passes into breast milk, but potential risks exist; use is prohibited during lactation;
Children and Adolescents
Safety and efficacy have not been confirmed in individuals under 18 years of age; use is not recommended;
Elderly Patients
No dose adjustment is required. Do not combine with other medications independently. Doctors will develop individualized treatment plans based on tumor stage, degree of metastasis, and the patient's physical condition.
7. Adverse Reactions
Adverse reactions observed in clinical trials are categorized by body system below. Reactions may vary among patients depending on physical conditions and medication use. In case of the following reactions, contact a doctor immediately; monitoring of vital signs such as blood pressure and heart rate may be necessary if required:
Pain Reactions
May occur in teeth, gums, tongue, anus, face, armpits, injection sites, urethra, kidneys (possibly accompanied by colic), sciatic nerve, skin, oropharynx, larynx, incision sites, trauma sites, breasts, perineum, prostate, testicles, pelvis, scrotum, penis, gallbladder, eyes, ears, etc., and may also include cancer-related pain;
Swelling Reactions
May occur in the extremities, face, whole body, lips, or eyelids;
General Symptoms
Fatigue, general malaise, lassitude;
Abnormal Blood Pressure
Increased blood pressure, hypertension (some patients may experience Grade ≥3 hypertension; blood pressure monitoring is required);
Musculoskeletal Pain
May occur in limbs, bones, muscles, spine, pectoral muscles, groin, neck, or lumbocostal regions;
Urinary Abnormalities
Hematuria, positive occult blood test results, presence of red blood cells in urine;
Voiding Dysfunction
Difficulty urinating, urinary retention, weak and slow urinary stream, delayed urination, etc.;
Infections
Respiratory tract infections (upper respiratory tract infection, nasopharyngitis, sinusitis, influenza, pharyngitis, tonsillitis, etc.), urinary tract infections (urinary tract infection, cystitis, bacteriuria, kidney infection, etc.);
Gastrointestinal Issues
Constipation, difficulty defecating, abdominal discomfort (upper, lower, or generalized abdominal pain);
Skin Reactions
Rash, eczema, urticaria, acne, erythema, etc., some of which may occur in the genital area;
Cardiac Abnormalities
Arrhythmias, bradycardia or tachycardia, atrial fibrillation, and other cardiac rhythm problems; some patients may experience QT interval prolongation;
Sleep Disorders
Insomnia, poor sleep quality, sleep rhythm disturbances;
Others
Abnormal liver function (e.g., elevated alanine aminotransferase, elevated aspartate aminotransferase), anemia, hypertriglyceridemia, and other laboratory abnormalities.
8. Discontinuation Indications
Discontinue use of this product immediately and seek medical attention promptly if any of the following conditions occur:
Symptoms of Liver Injury
Nausea, vomiting, abdominal pain, fatigue, loss of appetite, flu-like symptoms, dark urine, yellowing of the skin or sclera, right upper quadrant pain, etc. Liver function tests should be performed immediately. If liver damage is confirmed, suspend medication and conduct regular rechecks. After liver function returns to Grade 1 or below, treatment may be resumed at the original dose or a reduced dose (160 mg/day or 80 mg/day). Continuous monitoring is required after resuming treatment. If Grade 3 or higher liver injury occurs again, permanent discontinuation is necessary;
Seizures During Treatment
This product carries a risk of inducing seizures. Once a seizure occurs, permanent discontinuation is required immediately. During treatment, patients should avoid engaging in activities that may pose risks due to sudden loss of consciousness, such as high-altitude work and driving;
Severe Intolerable Adverse Reactions (Grade 3 or higher)
If symptoms persist despite suspending medication.
9. Precautions
9.1 Pre-Administration Instructions
Before use, clarify whether there are contraindications or precautions for use. The drug is contraindicated in patients with hypersensitivity to the drug components and pregnant women. Caution is advised in patients with hepatic or renal impairment, lactating women, and drivers or machine operators;
If taking other medications, consult a doctor before using this product and inform them of your medical conditions and treatment history. Special notification is required if you are pregnant or breastfeeding;
It is recommended to monitor liver function regularly before starting treatment and within the first four months of medication. If symptoms related to liver dysfunction occur, liver function tests should be performed immediately;
For patients with a history of QT interval prolongation, risk factors for QT interval prolongation, or those taking medications that may prolong the QT interval, doctors should assess the benefit-risk ratio before administration.
9.2 Post-Administration Instructions
During treatment, use the medication rationally under the guidance of a doctor, pay close attention to changes in physical conditions, and seek medical attention promptly if adverse reactions occur;
Dietary Recommendations
Maintain a light diet and avoid spicy and irritating foods such as chili and Sichuan peppercorns, as these may affect drug efficacy or exacerbate adverse reactions;
Storage
Store in a sealed container below 30°C and keep out of the reach of children. If abnormal changes such as discoloration, deformation, or unusual odor are found in the appearance of the medication, discontinue use immediately;
Handling
This product should not be handled by anyone other than the patient and their caregivers, especially women who are or may become pregnant;
Efficacy Monitoring
The onset time of this drug varies among individuals. After a single dose of 240 mg, the average time to reach the maximum concentration in the body is approximately 7 hours. When taken at a fixed time every day, the drug concentration in the blood can reach a relatively stable state after 15 consecutive days of administration.
