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Olaparib, as a PARP inhibitor, its main mechanism of action is to prevent the repair process of DNA damage by inhibiting the activity of PARP enzyme.
1. Generic name: Olaparib
2. Trade name: LYNPAR ZA®
1. For the maintenance treatment of recurrent epithelial ovarian cancer, fallopian tube cancer or primary peritoneal cancer in adults. Patients need to achieve complete or partial response to platinum-based chemotherapy.
2. For the treatment of adult patients with advanced ovarian cancer who carry harmful or suspected harmful germline BRCA mutations (gBRCAm) and who have received three or more chemotherapy regimens in the past. Mutation status needs to be confirmed by an FDA-approved companion diagnostic.
150 mg, tablets
1. Active ingredient:Olaparib (150 mg tablet contains 150 mg of olaparib, 100 mg tablet contains 100 mg of olaparib).
2. Excipients include: Copovidone, mannitol, colloidal silicon dioxide, sodium stearyl fumarate, etc.
1. Recommended dose: Take 300 mg orally twice a day (2 tablets of 150 mg), with food or on an empty stomach, until disease progression or intolerable toxicity.
2. Treatment of missed doses: If a dose is missed, skip the dose and take the next dose according to the originally planned time. It is prohibited to take a double dose.
3. Treatment of vomiting: If you vomit after taking the medicine, take the same dose as soon as possible and take the medicine normally the next day.
1. Adverse reaction adjustment:
(1) Anemia or bone marrow suppression: Suspend medication until recovery to level ≤ 1, reduce the dose to 250 mg (1 tablet of 150 mg + 1 tablet of 100 mg) twice a day for the first time, and reduce the dose to 200 mg (2 tablets of 100 mg) twice a day for the second time.
(2) Non-infectious pneumonia: permanently discontinue the drug after diagnosis.
(3) Adjustment for renal impairment: For moderate renal impairment (CLcr31-50mL/min), reduce the dose to 200 mg twice daily.
2. Adjustment of combined use of CYP3A inhibitors:
(1) Reduce the combined use of strong inhibitors (such as itraconazole) to 100 mg twice a day.
(2) The combined use of moderately effective inhibitors (such as fluconazole) is reduced to 150 mg twice daily.
1. Dietary taboos: Avoid grapefruit, grapefruit juice, Seville orange and fruit juice, which may increase blood drug concentration.
2. Differences in dosage forms: It is forbidden to substitute Lynparza capsules with olaparib capsules on a mg equivalent basis due to differences in bioavailability.
3. Monitoring requirements: Monitor blood routine before treatment and every month, and be alert to symptoms of myelodysplastic syndrome (MDS/AML) and pneumonia.
1. Pregnancy: Contraindicated as it may cause fetal malformations. Effective contraception is required during medication and for 6 months after stopping the medication.
2. Lactation period: Breastfeeding is prohibited during treatment and 1 month after the last dose.
3. Elderly people (≥65 years old): No dose adjustment is required, but close monitoring is required.
1. Common (≥20%): Anemia, nausea, fatigue, vomiting, upper respiratory tract infection, diarrhea, joint pain, dysgeusia, headache, and decreased appetite.
2. Laboratory abnormalities: Reduced hemoglobin (83%), decreased lymphocytes (67%), and increased serum creatinine (44%).
3. Severe reactions: MDS/AML (<1.5%), pneumonia (<1%).
There are no clear contraindications, but it is absolutely contraindicated during pregnancy.
1. CYP3A inhibitors: Strong inhibitors increase the AUC of olaparib by 170%, so combination use or dose adjustment must be avoided.
2. CYP3A inducers: Strong inducers (such as rifampicin) reduce AUC by 87%, which may weaken the efficacy.
1. Store in the original bottle to prevent moisture.
2. Store at room temperature (20°C-25°C). Short-term storage at 15°C-30°C is allowed.