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Olaparib: Drug information

Olaparib: Drug information
2024© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Olaparib: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Lynparza
Brand Names: Canada
  • Lynparza
Pharmacologic Category
  • Antineoplastic Agent, PARP Inhibitor
Dosing: Adult

Dosage guidance:

Safety: Do not initiate treatment with olaparib until after hematologic toxicity due to prior chemotherapy has resolved to ≤ grade 1.

Dosage form information: Due to differences in dosing and bioavailability, in international markets where capsules may be available, do not substitute capsules for tablets (or vice versa).

Clinical considerations: Select patients for therapy based on an approved olaparib companion diagnostic test for detection of genetic mutations or biomarkers.

Breast cancer, early, high risk, HER2 negative, germline BRCA mutated, adjuvant therapy

Breast cancer, early, high risk, HER2 negative, germline BRCA mutated, adjuvant therapy: Oral: Tablets: 300 mg twice daily for 1 year or until disease progression or unacceptable toxicity, whichever occurs first (Ref).

Breast cancer, metastatic, HER2 negative, germline BRCA mutated

Breast cancer, metastatic, HER2 negative, germline BRCA mutated: Oral: Tablets: 300 mg twice daily until disease progression or unacceptable toxicity (Ref).

Ovarian cancer, advanced, BRCA mutated, first-line maintenance therapy

Ovarian cancer, advanced, BRCA mutated , first-line maintenance therapy (monotherapy): Oral: Tablets: 300 mg twice daily until disease progression or unacceptable toxicity or completion of 2 years of therapy. Patients with a complete response (no radiologic evidence of disease) at 2 years should discontinue olaparib; patients with evidence of disease at 2 years may continue treatment (beyond 2 years) if further olaparib treatment may provide benefit (Ref).

Ovarian cancer, advanced, homologous recombination deficient positive, first-line maintenance therapy

Ovarian cancer, advanced, homologous recombination deficient positive, first-line maintenance therapy (combination therapy): Oral: Tablets: 300 mg twice daily (in combination with bevacizumab) until disease progression or unacceptable toxicity or completion of 2 years of therapy (Ref). Patients with a complete response (no radiologic evidence of disease) at 2 years should discontinue olaparib; patients with evidence of disease at 2 years may continue treatment (beyond 2 years) if further olaparib treatment may provide benefit. Bevacizumab duration is for a total of 15 months (including when administered with chemotherapy as well as maintenance).

Ovarian cancer, recurrent, BRCA mutated, maintenance therapy

Ovarian cancer, recurrent, BRCA mutated, maintenance therapy: Oral: Tablets: 300 mg twice daily until disease progression or unacceptable toxicity (Ref).

Pancreatic cancer, metastatic, germline BRCA mutated, first-line maintenance therapy

Pancreatic cancer, metastatic, germline BRCA mutated , first-line maintenance therapy: Oral: Tablets: 300 mg twice daily until disease progression or unacceptable toxicity (Ref).

Prostate cancer, metastatic, castration resistant, BRCA mutated

Prostate cancer, metastatic, castration resistant, BRCA mutated: Oral: Tablets: 300 mg twice daily (in combination with abiraterone and prednisone or prednisolone) until disease progression or unacceptable toxicity (Ref). Patients should also receive a gonadotropin-releasing hormone analog or have had bilateral orchiectomy.

Prostate cancer, metastatic, castration resistant, homologous recombination repair gene mutated

Prostate cancer, metastatic, castration resistant, homologous recombination repair gene mutated: Oral: Tablets: 300 mg twice daily until disease progression or unacceptable toxicity (Ref). Patients should also receive a gonadotropin-releasing hormone analog or have had bilateral orchiectomy.

Missed doses: If a dose is missed, administer the next dose at its scheduled time.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Kidney function estimated by Cockcroft-Gault equation.

CrCl >50 mL/minute: No dosage adjustment necessary.

CrCl 31 to 50 mL/minute: Tablets: Reduce dose to 200 mg twice daily.

CrCl ≤30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

End-stage kidney disease: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Hepatic impairment prior to treatment initiation:

Mild to moderate impairment (Child-Turcotte-Pugh classes A, B): Tablets: No dosage adjustment necessary.

Severe impairment (Child-Turcotte-Pugh class C): Tablets: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Adjustment for Toxicity: Adult

Consider therapy interruption or dose reduction if adverse reactions occur.

Olaparib (Tablet) Dosage Reduction Levels

Dosage reduction levels

Recommended olaparib dosage and schedule

Initial (usual) dosage

300 mg twice daily

First dosage reduction

250 mg twice daily

Second dosage reduction

200 mg twice daily

Olaparib (Tablet) Recommended Dosage Modifications for Adverse Reactions

Adverse reaction

Severity

Olaparib dosage modification

a ASCO [Tew 2020]

Hematologic toxicity

Anemia (in the treatment ovarian cancer)

Hemoglobin <8 mg/dL and/or requiring a blood transfusion for symptom relief

Monitor patienta.

Repeated episodes of anemia

Reduce olaparib dose to avoid repeated transfusiona.

Neutropenia (in the treatment ovarian cancer)

Grade 4 (lasting ≥5 to 7 days or associated with fever)

Withhold olaparib until recovery of infection and granulocyte count; resume olaparib at a reduced dosea.

WBC growth factor support may be used while olaparib is withheld for neutropenia; however, growth factors are not indicated during daily olaparib dosinga.

Thrombocytopenia (in the treatment ovarian cancer)

Grade 3 to 4

Withhold olaparib until resolution; resume olaparib at a reduced dose.a

Persistent or significant bleeding despite dose reduction

Permanently discontinue olaparib.a

Hematologic toxicity

Prolonged

Withhold olaparib and monitor blood counts weekly.

If counts do not recover to ≤ grade 1 after 4 weeks, further evaluation (including bone marrow and cytogenetic analyses) is necessary.

Secondary acute myeloid leukemia/ myelodysplastic syndrome

Confirmed

Permanently discontinue olaparib.

Nonhematologic toxicity

GI toxicity (in the treatment of ovarian cancer)

Persistent nausea requiring daily antiemetics, resulting in performance status reduction and/or resulting in >5% weight loss

Consider olaparib dose reductiona.

Pulmonary toxicity

Pneumonitis (suspected)

Withhold olaparib and evaluate promptly for new or worsening respiratory symptoms (eg, cough, dyspnea, fever, wheezing) or for radiologic abnormalities

Pneumonitis (confirmed)

Discontinue olaparib and treat the patient appropriately.

Venous thromboembolism

Venous thrombosis and/or pulmonary embolism

Treat as medically appropriate; may include long-term anticoagulation as clinically indicated.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.

>10%:

Dermatologic: Skin rash (5% to 15%)

Endocrine & metabolic: Hypomagnesemia (14%)

Gastrointestinal: Abdominal pain (45%; upper abdominal pain: 5% to 7%), constipation (23% to 28%), decreased appetite (13% to 25%), diarrhea (18% to 37%; grades 3/4: ≤3%), dysgeusia (11% to 27%), dyspepsia (5% to 17%), nausea (45% to 77%; grades 3/4: ≤3%), stomatitis (10% to 20%; grades 3/4: ≤1%), vomiting (20% to 40%; grades 3/4: ≤3%)

Genitourinary: Urinary tract infection (13%)

Hematologic & oncologic: Anemia (24% to 44%; grades 3/4: 9% to 21%), increased MCV (≤89%), leukopenia (5% to 17%; grades 3/4: 3%), neutropenia (12% to 19%; grades 3/4: 4% to 6%), thrombocytopenia (4% to 14%; grades 3/4: 1% to 3%)

Infection: Influenza (≤36%)

Nervous system: Dizziness (7% to 20%), fatigue (67%; including asthenia), headache (7% to 26%)

Neuromuscular & skeletal: Arthralgia (≤30%), back pain (19%), myalgia (≤30%)

Renal: Increased serum creatinine (2% to 99%)

Respiratory: Bronchitis (≤28%), cough (9% to 18%), dyspnea (4% to 15%), nasopharyngitis (≤36%), rhinitis (≤36%), sinusitis (≤36%), upper respiratory tract infection (≤36%)

1% to 10%:

Cardiovascular: Edema (8%), venous thromboembolism (≤5%; including severe pulmonary embolism)

Dermatologic: Dermatitis (≤1%)

Hematologic & oncologic: Lymphocytopenia (1% to 7%), myelodysplastic syndrome (≤8%), myeloid leukemia (acute: ≤8%)

Hypersensitivity: Hypersensitivity reaction (≤2%)

Frequency not defined: Respiratory: Pneumonitis

Postmarketing:

Dermatologic: Erythema nodosum

Hypersensitivity: Angioedema

Contraindications

There are no contraindications listed in the manufacturer's US labeling.

Canadian labeling: Hypersensitivity to olaparib or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: Hypersensitivity reactions, including rash, dermatitis, and angioedema, have been reported.

• Pulmonary toxicity: Pneumonitis (including some fatalities) has occurred rarely in studies of single-agent olaparib in patients with various cancers. New or worsening respiratory symptoms include cough, dyspnea, fever, and/or wheezing.

• Secondary malignancy: Myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) have been reported (rarely) in clinical trials of patients with various cancers who received olaparib (as a single agent or as part of a combination regimen), including fatal cases. The median duration of olaparib therapy prior to development of the secondary cancers was ~2 years (range: <6 months to >4 years). All patients had received prior chemotherapy with platinum agents and/or other DNA-damaging agents, including radiation therapy. If prolonged hematologic toxicity occurs and blood counts do not recover to ≤ grade 1 after 4 weeks, further evaluation (including bone marrow and cytogenetic analyses) is necessary.

• Thromboembolic events: Venous thromboembolism, including severe or fatal pulmonary embolism, have been reported. In studies of patients with metastatic castration-resistant prostate cancer who received olaparib, venous thromboembolic events occurred at a higher rate compared to patients in the control arms.

Other warnings/precautions:

• Appropriate use: Select patients for olaparib therapy based on genetic mutations, biomarker status, and tumor sample type. Information on approved tests for the detection of genetic mutations may be found at http://www.fda.gov/companiondiagnostics. If testing fails or tissue sample is unavailable, or when germline testing is negative, consider using an alternative test (if available).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Lynparza: 100 mg, 150 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Lynparza Oral)

100 mg (per each): $163.64

150 mg (per each): $163.64

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral:

Lynparza: 50 mg [DSC]

Tablet, Oral:

Lynparza: 100 mg, 150 mg

Prescribing and Access Restrictions

Olaparib is available through the authorized specialty pharmacy providers. For further information on patient assistance, product availability, and prescribing instructions, please refer to the following website: https://providerportal.myaccess360.com or call 1-844-275-2360.

Administration: Adult

Oral: Administer approximately every 12 hours with or without food. Swallow tablets whole; do not chew, crush, dissolve, or divide tablet.

Based on a pharmacokinetic study (in tablets), the rate of absorption was slower and the peak exposure was decreased when administered with a high-fat meal; however, the extent of absorption was not affected (Ref).

Nausea and vomiting were reported more frequently when olaparib was administered in a fasted state (Ref). Administering olaparib after a small meal or snack may help alleviate potential nausea and vomiting (Ref). Consider providing patients with antiemetic therapy for at home use as needed on days of olaparib dosing (Ref).

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Olaparib may cause reproductive toxicity, teratogenicity, and genotoxicity.

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:

Lynparza tablets: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/208558s028lbl.pdf#page=58

Use: Labeled Indications

Breast cancer, early, high-risk, HER2-negative, germline BRCA-mutated, adjuvant therapy: Tablets: Adjuvant treatment of deleterious or suspected deleterious germline BRCA-mutated (gBRCAm), HER2-negative, high-risk, early breast cancer in adults who have been treated with neoadjuvant or adjuvant chemotherapy (select patients for therapy based on an approved olaparib companion diagnostic test for gBRCA1m or gBRCA2m in blood specimen).

Breast cancer, metastatic, HER2-negative, germline BRCA-mutated: Tablets: Treatment of deleterious or suspected deleterious gBRCAm, HER2-negative metastatic breast cancer in adults who have been treated with chemotherapy in the neoadjuvant, adjuvant, or metastatic setting; patients with hormone receptor-positive disease should have received a prior endocrine therapy or be considered inappropriate for endocrine therapy (select patients for therapy based on an approved olaparib companion diagnostic test for gBRCA1m or gBRCA2m in blood specimen).

Ovarian cancer, advanced, BRCA -mutated, first-line maintenance therapy: Tablets: First-line maintenance treatment (as monotherapy) of deleterious or suspected deleterious gBRCAm or somatic BRCA-mutated advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer in adults who are in complete or partial response to first-line, platinum-based chemotherapy (select patients for therapy based on an approved olaparib companion diagnostic test for BRCA1m or BRCA2m in tumor or blood specimen).

Ovarian cancer, advanced, homologous recombination deficient-positive, first-line maintenance therapy: Tablets: First-line maintenance treatment (in combination with bevacizumab) of advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer in adults who are in complete or partial response to first-line, platinum-based chemotherapy and whose cancer is associated with homologous recombination deficiency (HRD)–positive status, defined by either a deleterious or suspected deleterious BRCA mutation and/or genomic instability (select patients for therapy based on an approved olaparib companion diagnostic test for BRCA1m, BRCA2m, and/or genomic instability in tumor specimen).

Ovarian cancer, recurrent, BRCA-mutated, maintenance therapy: Tablets: Maintenance treatment (as monotherapy) of deleterious or suspected deleterious gBRCAm or somatic BRCA-mutated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer in adults who are in complete or partial response to platinum-based chemotherapy (select patients for therapy based on an approved olaparib companion diagnostic test for BRCA1m or BRCA2m in tumor or blood specimen).

Pancreatic cancer, metastatic, germline BRCA-mutated, first-line maintenance therapy: Tablets: First-line maintenance treatment of deleterious or suspected deleterious gBRCAm metastatic pancreatic adenocarcinoma in adults whose disease has not progressed on at least 16 weeks of a first-line, platinum-based chemotherapy regimen (select patients for therapy based on an approved olaparib companion diagnostic test for gBRCA1m or gBRCA2m in blood specimen).

Prostate cancer, metastatic, castration resistant, BRCA -mutated: Tablets: Treatment of deleterious or suspected deleterious BRCA-mutated metastatic castration-resistant prostate cancer (mCRPC) in adults (in combination with abiraterone and prednisone or prednisolone) (select patients for therapy based on an approved olaparib companion diagnostic test for BRCA1m or BRCA2m in tumor, blood, or plasma [ctDNA] specimen).

Prostate cancer, metastatic, castration-resistant, homologous recombination repair gene-mutated: Tablets: Treatment of deleterious or suspected deleterious germline or somatic homologous recombination repair (HRR) gene–mutated metastatic castration-resistant prostate cancer in adults who have progressed following prior enzalutamide or abiraterone treatment (select patients for therapy based on an approved olaparib companion diagnostic test for ATMm, BRCA1m, BRCA2m, BARD1m, BRIP1m, CDK12m, CHEK1m, CHEK2m, FANCLm, PALB2m, RAD51Bm, RAD51Cm, RAD51Dm, or RAD54Lm in tumor specimen, for gBRCA1m or gBRCA2m in blood specimen, or for ATMm, BRCA1m, or BRCA2m in plasma [ctDNA] specimen).

Medication Safety Issues
Sound-alike/look-alike issues

Olaparib may be confused with niraparib, osimertinib, rucaparib, talazoparib.

Lynparza may be confused with lenvatinib, Lenvima.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of CYP3A4 (major), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Bitter Orange: May increase the serum concentration of Olaparib. Risk X: Avoid combination

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Olaparib. Risk X: Avoid combination

CYP3A4 Inducers (Strong): May decrease the serum concentration of Olaparib. Risk X: Avoid combination

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Olaparib. Management: Avoid use of moderate CYP3A4 inhibitors with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib tablets should be reduced to 150 mg twice daily and the dose of olaparib capsules should be reduced to 200 mg twice daily. Risk D: Consider therapy modification

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Olaparib. Management: Avoid use of strong CYP3A4 inhibitors with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib tablets should be reduced to 100 mg twice daily and the dose of olaparib capsules should be reduced to 150 mg twice daily. Risk D: Consider therapy modification

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider therapy modification

Grapefruit Juice: May increase the serum concentration of Olaparib. Risk X: Avoid combination

Myelosuppressive Agents: May enhance the myelosuppressive effect of Olaparib. Risk C: Monitor therapy

Food Interactions

Coadministration with grapefruit, grapefruit juice, Seville oranges, or Seville orange juice may increase olaparib plasma concentrations. Management: Avoid concomitant administration with grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.

Reproductive Considerations

Verify pregnancy status prior to treatment initiation in patients who could become pregnant. Patients who could become pregnant should use highly effective contraception during therapy and for 6 months after the last olaparib dose. Patients with partners who could become or are pregnant should use effective contraception during treatment and for 3 months after the last olaparib dose; patients also should not donate sperm during therapy and for 3 months following the last olaparib dose.

Pregnancy Considerations

Based on the mechanism of action, and data from animal reproduction studies, in utero exposure to olaparib may cause fetal harm.

Breastfeeding Considerations

It is not known if olaparib is present in breast milk.

Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends that patients should not breastfeed during treatment and for 1 month after the last olaparib dose.

Dietary Considerations

Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.

Monitoring Parameters

Testing for genetic mutations or biomarker status (see table); CBC at baseline and monthly thereafter, or as clinically indicated (weekly until recovery for prolonged hematologic toxicity), renal function. Verify pregnancy status (prior to treatment initiation in patients who could become pregnant). Monitor for signs/symptoms of venous thrombosis, pulmonary embolism, and pneumonitis (evaluate promptly for new or worsening respiratory symptoms such as cough, dyspnea, fever, wheezing, or for radiologic abnormalities). Monitor for signs of acute myeloid leukemia/myelodysplastic syndrome (if prolonged hematologic toxicity occurs and blood counts do not recover to ≤ grade 1 after 4 weeks, further evaluation, including bone marrow and cytogenetic analyses is necessary). Monitor adherence.

Recommended Testing for Genetic Mutations or Biomarker Status in Patients Treated with Olaparib

Indication

Biomarker

Sample type

Tumor

Blood

Plasma (ctDNA)

a HRD = Homologous recombination deficiency; HRR = homologous recombination repair

Breast cancer, early, high-risk, HER2-negative, germline BRCA-mutated, adjuvant therapy

gBRCA1m, gBRCA2m

X

Breast cancer, metastatic, HER2-negative, germline BRCA-mutated

gBRCA1m, gBRCA2m

X

Ovarian cancer, advanced, BRCA-mutated, first-line maintenance therapy

BRCA1m, BRCA2m

X

X

Ovarian cancer, recurrent, BRCA-mutated, maintenance

BRCA1m, BRCA2m

X

X

Ovarian cancer, advanced, HRDa-positive, first-line maintenance therapy

BRCA1m, BRCA2m and/or genomic instability

X

Pancreatic cancer, metastatic, germline BRCA-mutated, first-line maintenance therapy

gBRCA1m, gBRCA2m

X

Prostate cancer, metastatic, castration resistant, BRCA-mutated (combination therapy)

BRCA1m, BRCA2m

X

X

X

Prostate cancer, metastatic, castration-resistant, HRRa gene-mutated

ATMm, BRCA1m, BRCA2m, BARD1m, BRIP1m, CDK12m, CHEK1m, CHEK2m, FANCLm, PALB2m, RAD51Bm, RAD51Cm, RAD51Dm, RAD54Lm

X

gBRCA1m, gBRCA2m

X

ATMm, BRCA1m, BRCA2m

X

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Olaparib is a poly (ADP-ribose) polymerase (PARP) enzyme inhibitor, including PARP1, PARP2, and PARP3. PARP enzymes are involved in DNA transcription, cell cycle regulation, and DNA repair. Olaparib is a potent oral PARP inhibitor which induces synthetic lethality in BRCA1/2 deficient tumor cells through the formation of double-stranded DNA breaks which cannot be accurately repaired, which leads to disruption of cellular homeostasis and cell death (Ledermann 2012). In prostate cancer models, PARP1 has demonstrated contribution to regulation of androgen receptor activity; combining olaparib with androgen receptor inhibition results in cytotoxicity (in vitro) and antitumor activity.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Rapid; delayed with a high-fat/high-calorie meal (extent of absorption not significantly altered).

Distribution: Tablet: 158 ± 136 L.

Protein binding: ~82%.

Metabolism: Primarily hepatic via CYP3A; the majority of metabolism is through oxidation with some metabolites undergoing subsequent glucuronide or sulfate conjugation.

Half-life elimination, terminal: Tablet: 14.9 ± 8.2 hours.

Time to peak: Tablet: 1.5 hours.

Excretion: Urine (44%, mostly as metabolites); feces (42%, mostly as metabolites).

Clearance: Tablet: 7.4 ± 3.9 hours.

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function:

Tablets: The mean AUC and Cmax increased by 24% and 15%, respectively, in patients with mild renal impairment (CrCl 51 to 80 mL/minute), and by 44% and 26%, respectively, in patients with moderate renal impairment (CrCl 31 to 50 mL/minute) compared with patients with normal renal function.

Hepatic function impairment: Tablets: The mean AUC and the mean Cmax increased by 15% and 13%, respectively, in patients with mild impairment (Child-Pugh class A), compared with patients with normal hepatic function. The mean AUC increased by 8% and the mean Cmax decreased by 13% in patients with moderate impairment (Child-Pugh class B), compared with patients with normal hepatic function.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Lynparza;
  • (AR) Argentina: Lynparza | Olapater;
  • (AT) Austria: Lynparza;
  • (AU) Australia: Lynparza;
  • (BD) Bangladesh: Inpoza | Olanib | Olaparix;
  • (BE) Belgium: Lynparza;
  • (BG) Bulgaria: Lynparza;
  • (BR) Brazil: Lynparza;
  • (CH) Switzerland: Lynparza;
  • (CL) Chile: Lynparza;
  • (CN) China: Lynparza;
  • (CO) Colombia: Lynparza;
  • (CZ) Czech Republic: Lynparza;
  • (DE) Germany: Lynparza;
  • (DO) Dominican Republic: Lynparza;
  • (EC) Ecuador: Lynparza;
  • (EE) Estonia: Lynparza;
  • (EG) Egypt: Lynparza;
  • (ES) Spain: Lynparza;
  • (FI) Finland: Lynparza;
  • (FR) France: Lynparza;
  • (GB) United Kingdom: Lynparza;
  • (GR) Greece: Lynparza;
  • (HK) Hong Kong: Lynparza;
  • (HR) Croatia: Lynparza;
  • (HU) Hungary: Lynparza;
  • (ID) Indonesia: Lynparza;
  • (IE) Ireland: Lynparza;
  • (IN) India: Bracanat | Lynparza;
  • (IT) Italy: Lynparza;
  • (JP) Japan: Lynparza;
  • (KR) Korea, Republic of: Lynparza;
  • (KW) Kuwait: Lynparza;
  • (LB) Lebanon: Lynparza;
  • (LT) Lithuania: Lynparza;
  • (LV) Latvia: Lynparza;
  • (MX) Mexico: Lynparza;
  • (MY) Malaysia: Lynparza;
  • (NL) Netherlands: Lynparza;
  • (NO) Norway: Lynparza;
  • (NZ) New Zealand: Lynparza;
  • (PE) Peru: Lynparza;
  • (PH) Philippines: Lynparza;
  • (PL) Poland: Lynparza;
  • (PR) Puerto Rico: Lynparza;
  • (PT) Portugal: Lynparza;
  • (QA) Qatar: Lynparza;
  • (RO) Romania: Lynparza;
  • (RU) Russian Federation: Lynparza;
  • (SA) Saudi Arabia: Lynparza;
  • (SE) Sweden: Lynparza;
  • (SG) Singapore: Lynparza;
  • (SI) Slovenia: Lynparza;
  • (SK) Slovakia: Lynparza;
  • (TH) Thailand: Lynparza;
  • (TN) Tunisia: Lynparza;
  • (TR) Turkey: Lynparza;
  • (TW) Taiwan: Lynparza;
  • (UA) Ukraine: Linparza;
  • (UY) Uruguay: Lynparza;
  • (ZA) South Africa: Lynparza
  1. <800> Hazardous Drugs—Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Clarke NW, Armstrong AJ, Thiery-Vuillemin A, et al. Abiraterone and olaparib for metastatic castration-resistant prostate cancer. NEJM Evidence. Published online June 3, 2022. doi:https://evidence.nejm.org/doi/10.1056/EVIDoa2200043
  3. de Bono J, Mateo J, Fizazi K, et al. Olaparib for metastatic castration-resistant prostate cancer. N Engl J Med. 2020;382(22):2091‐2102. doi:10.1056/NEJMoa1911440 [PubMed 32343890]
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