As a PARP inhibitor, the main mechanism of action of Olaparib is to inhibit the activity of PARP enzyme and prevent the repair process of DNA damage.

1、 Drug name

1. Common name: Olaparib

2. Product Name: LYNPARZA ®

2、 Indications

1. For maintenance therapy of recurrent epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer in adults, patients need to achieve complete or partial remission with platinum based chemotherapy.

2. Used to treat adult patients with advanced ovarian cancer carrying harmful or suspected harmful germline BRCA mutations (gBRCAm), who have previously received three or more chemotherapy regimens. Confirmation of mutation status through FDA approved accompanying diagnosis is required.

3、 Specifications and characteristics

150mg, tablet

4、 Main components

1. Active ingredient: Olaparib (150mg tablet contains 150mg Olaparib, 100mg tablet contains 100mg Olaparib).

2. Auxiliary materials include: copolymer ketone, mannitol, colloidal silica, sodium stearate fumarate, etc.

5、 Usage and dosage

1. Recommended dosage: Take 300mg orally twice a day (2 tablets 150mg), with food or on an empty stomach, until disease progression or intolerable toxicity occurs.

2. Omission treatment: If missed, skip this dose and take the next dose according to the original plan. It is prohibited to take double the dose.

3. Vomiting treatment: If vomiting occurs after taking medication, take the same dose as soon as possible and take the medication normally the next day.

6、 Dose adjustment

1. Adverse reaction adjustment:

(1) Anemia or bone marrow suppression: Suspend medication until recovery to ≤ grade 1, first reduce to 250 milligrams (1 tablet 150 milligrams+1 tablet 100 milligrams) twice daily, and second reduce to 200 milligrams (2 tablets 100 milligrams) twice daily.

(2) Non infectious pneumonia: permanently discontinue medication after diagnosis.

(3) Renal injury adjustment: Reduce moderate renal injury (CLcr31-50mL/min) to 200mg twice daily.

2. CYP3A inhibitor combination adjustment:

(1) The combination of potent inhibitors (such as itraconazole) is reduced to 100 milligrams twice daily.

(2) Reduce the dosage of intermediate acting inhibitors (such as fluconazole) to 150 milligrams twice daily.

7、 Medication precautions

1. Dietary taboos: Avoid grapefruit, grapefruit juice, Seville orange, and fruit juice as they may increase blood drug concentration.

2. Formulation difference: It is prohibited to replace Olaparib capsules with equivalent milligrams due to differences in bioavailability.

3. Monitoring requirements: Monitor blood routine before treatment and monthly to be alert to symptoms of myelodysplastic syndrome (MDS/AML) and pneumonia.

8、 Medication for special populations

1. Pregnancy period: contraindicated, may cause fetal malformation, effective contraception is required during medication and 6 months after discontinuation.

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and one month after the last administration.

3. Elderly individuals (≥ 65 years old): No dose adjustment is required, but close monitoring is necessary.

9、 Adverse reactions

1. Common (≥ 20%): anemia, nausea, fatigue, vomiting, upper respiratory tract infection, diarrhea, joint pain, taste disorders, headache, decreased appetite.

2. Laboratory abnormalities: decreased hemoglobin (83%), decreased lymphocytes (67%), and increased serum creatinine (44%).

3. Serious reactions: MDS/AML (<1.5%), pneumonia (<1%).

10、 Contraindications

There are no clear contraindications, but it is absolutely prohibited during pregnancy.

11、 Drug interactions

1. CYP3A inhibitors: Strong inhibitors increase the AUC of olaparib by 170%, and should be avoided in combination or adjusted in dosage.

2. CYP3A inducer: Strong inducers (such as rifampicin) reduce AUC by 87%, which may weaken the therapeutic effect.

12、 Storage method

1. Store in original bottle, moisture-proof.

2. Store at room temperature (20 ° C-25 ° C) and allow short-term storage at 15 ° C-30 ° C.

Olaparibinformation