The active ingredient of fluzoparib is fluzoparib, a PARP inhibitor targeted anticancer drug. It exerts its anticancer effect by inhibiting the DNA repair mechanism of cancer cells and suppressing tumor cell proliferation, and is primarily indicated for the treatment of cancers associated with BRCA gene mutations.
Indications
Fluzoparib is mainly indicated for the treatment of three types of gynecologic malignancies: platinum-sensitive recurrent ovarian cancer, fallopian tube cancer, and primary peritoneal cancer. The specific applicable populations are as follows:
Patients with platinum-sensitive recurrent ovarian, fallopian tube, or primary peritoneal cancer who have received two or more lines of chemotherapy and harbor germline BRCA gene mutations;
Adult patients with platinum-sensitive recurrent ovarian, fallopian tube, or primary peritoneal cancer, for maintenance therapy following tumor regression or disappearance achieved with platinum-containing chemotherapy;
Adult patients with advanced ovarian, fallopian tube, or primary peritoneal cancer, for subsequent maintenance therapy following tumor regression or disappearance achieved with first-line platinum-containing chemotherapy.
Relievable Symptoms
Fluzoparib administration is primarily targeted at the following symptoms caused by the aforementioned malignancies:
A feeling of pressure in the abdomen or pelvis (presenting as a persistent heavy sensation or pressure discomfort);
Recurrent or persistent pain in the pelvic region;
Abnormal vaginal bleeding occurring outside the menstrual period or in postmenopausal women.
Drug Combination Use
The combination of fluzoparib with apatinib mesylate (an anti-angiogenic agent) has demonstrated favorable efficacy in the treatment of advanced ovarian cancer, with the following key characteristics:
Clinical study data show that the combination therapy significantly prolongs the progression-free survival of patients;
The combination therapy yields therapeutic benefits regardless of whether patients harbor germline BRCA gene mutations;
This combination regimen is particularly suitable for patients whose disease is controlled after chemotherapy, helping to delay tumor recurrence.
Precautions Before Administration
Fluzoparib must be administered under the supervision of a physician experienced in anticancer therapy; self-administration is strictly prohibited.
Contraindicated populations
Patients with a known hypersensitivity to any component of fluzoparib; pregnant women and lactating women.
Populations requiring cautious use
Pediatric patients (under 18 years of age); individuals who regularly drive or operate precision equipment; patients with abnormal hepatic or renal function. If administration is deemed necessary for the above populations, the risks must be evaluated by a physician, and close monitoring of physical reactions is required during treatment.
Dosing Guidance for Special Populations
Dosing of fluzoparib in special populations requires individual adjustment based on clinical conditions, with specific guidance as follows:
Patients with hepatic impairment
No dose adjustment is required for mild hepatic impairment; administration is not recommended for patients with moderate to severe hepatic impairment, as the safety and efficacy of fluzoparib in this population have not been established.
Patients with renal impairment
No dose adjustment is required for mild renal impairment; administration is not recommended for patients with moderate to severe renal impairment due to the lack of supporting safety data.
Pediatric patients
The safety and efficacy of fluzoparib in patients under 18 years of age have not been determined, and its use is not recommended.
Geriatric patients
Limited dosing data are available for patients aged 65 years and above; administration must be under close physician supervision.
Pregnancy-related considerations
Strict contraception must be practiced during treatment, and continued for 6 months after the last dose of fluzoparib; treatment should be discontinued immediately if pregnancy occurs.
Lactation
Breastfeeding must be discontinued during treatment and for 1 month after the last dose, as it is not yet clear whether fluzoparib is excreted in human milk.
Individuals engaged in high-risk occupations
Dizziness, fatigue and other symptoms that may impair operational safety may occur after administration; driving or operating machinery should be avoided if such symptoms develop.
Drug Interactions
Fluzoparib is primarily metabolized by the hepatic CYP3A4 enzyme. Co-administration with other drugs that affect CYP3A4 activity may result in drug interactions, with specific precautions as follows:
Potent CYP3A4 inhibitors (e.g., itraconazole)
May significantly increase fluzoparib plasma concentrations; concomitant use should be avoided. If co-administration is unavoidable, fluzoparib must be suspended until the inhibitor is eliminated from the body.
Moderate CYP3A4 inhibitors (e.g., fluconazole)
May moderately increase fluzoparib plasma concentrations; a fluzoparib dose reduction is required when used concomitantly.
Potent CYP3A4 inducers (e.g., rifampicin)
May decrease fluzoparib plasma concentrations and compromise efficacy; concomitant use should be avoided.
Specific combination regimens must be adjusted by a physician based on the patient’s actual clinical condition; dose adjustment based solely on this package insert is strictly prohibited. All concomitant medications must be fully disclosed to the physician or pharmacist.
Dosage and Administration
Prerequisites for Administration
Fluzoparib must be prescribed and administered by a specialist physician experienced in antineoplastic therapy. Prior to the initiation of treatment, the presence of a pathogenic germline BRCA1 or BRCA2 mutation must be confirmed using a nationally certified professional detection method.
Dosage Form and Strength
Fluzoparib is available commercially as hard capsules, each containing 50 mg of fluzoparib. The capsules are white and opaque, with the drug identifier printed on the surface.
Specific Administration
Adult dosage: 150 mg (3 capsules) per dose, administered twice daily (morning and evening).
Administration method: Swallow the capsules whole; do not open or chew. Administration may be with or without food, and administration within 30 minutes after a meal is recommended to reduce gastrointestinal discomfort.
Treatment course: Once treatment is initiated, it should be continued until disease progression or unacceptable adverse reactions occur.
Special note: Package insert information (e.g., dosage and administration, precautions) for the same drug may vary among different manufacturers. If discrepancies exist between the package insert of the purchased drug and the physician’s instructions, contact the attending physician or a professional pharmacist immediately for confirmation.
Precautions After Administration
Routine Use Precautions
Administer the drug strictly in accordance with the physician’s instructions and undergo regular follow-up examinations to ensure treatment efficacy and medication safety.
Discontinue use immediately if the capsules show abnormal physical characteristics such as discoloration or deformation.
Store the drug in a place completely out of the reach of children.
Management of Missed Doses
Fluzoparib is administered twice daily. Missed doses should be managed according to the following principles: If a missed dose is discovered within 6 hours of the last administration, take the missed dose as soon as possible. If more than 6 hours have elapsed, skip the missed dose and resume the regular dosing schedule at the next scheduled time. Double dosing to make up for a missed dose is strictly prohibited to avoid the risk of toxicity. Consult the attending physician or a professional pharmacist if there are any questions about managing missed doses.
Management of Overdose
Limited research data are available on fluzoparib overdose, and specific toxic symptoms have not been established. Existing records indicate that no unexpected adverse reactions were observed in a small number of patients who received a daily dose of 450 mg. In case of suspected overdose, close monitoring of abnormal physical signs is required, and prompt symptomatic and supportive care should be initiated.
Adverse Reactions
The following common adverse reactions occur in more than 10% of patients: nausea and vomiting, dizziness, abdominal pain, anorexia, anemia, leukopenia, fatigue, thrombocytopenia, neutropenia, lymphopenia, increased serum creatinine, and hyperlipidemia.
The occurrence of adverse reactions is associated with individual differences in physical constitution and treatment regimens. Close monitoring of physical changes is required during treatment; contact a physician immediately if sudden severe discomfort develops or the above symptoms worsen. The physician may recommend monitoring vital signs such as blood pressure, heart rate, and respiratory rate, and adjust the treatment regimen in a timely manner.
Discontinuation Criteria
Seek immediate medical attention if physical discomfort occurs during treatment. The physician will comprehensively evaluate whether immediate treatment discontinuation is necessary or whether other medical interventions are required to ensure the patient’s health and safety, based on the severity of adverse reactions (e.g., whether they affect daily life or pose a life threat).
Medication Tips
Prior to fluzoparib administration, fully disclose all concurrent medications, ongoing treatments, and confirmed underlying diseases to the physician or pharmacist.
Prior to fluzoparib administration, immediately inform the physician of any pregnancy plans, confirmed pregnancy, or lactation status.
Avoid driving or operating precision instruments if dizziness, fatigue or other related symptoms occur during treatment.
All adjustments related to medication must be made after professional evaluation by a physician; independent decision-making is strictly prohibited.
