Olaparib

What is Olaparib?

• Olaparib (Lynparza) is a poly (ADP-ribose) polymerase (PARP) inhibitor used as an antineoplastic agent in the therapy of refractory and advanced ovarian carcinoma.

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What are the uses of this medicine?

This medicine is used to treat adults who have:

• advanced ovarian cancer, fallopian tube cancer, or primary peritoneal cancer with a certain type of inherited (germline) or acquired (somatic) abnormal BRCA gene. Lynparza is used alone as maintenance treatment after the cancer has responded to your first treatment with platinum-based chemotherapy. Your healthcare provider will perform a test to make sure that Lynparza is right for you.
• advanced ovarian cancer, fallopian tube cancer or primary peritoneal cancer with a certain type of abnormal BRCA gene or a positive laboratory tumor test for genomic instability called HRD. Lynparza is used in combination with another anti-cancer medicine, bevacizumab, as maintenance treatment after the cancer has responded to your first treatment with platinum-based chemotherapy. Your healthcare provider will perform a test to make sure that Lynparza is right for you.
• ovarian cancer, fallopian tube cancer, or primary peritoneal cancer, as maintenance treatment, when the cancer has come back. Lynparza is used after the cancer has responded to treatment with platinum-based chemotherapy.
• advanced ovarian cancer with a certain type of abnormal inherited BRCA gene, and have received treatment with 3 or more prior types of chemotherapy medicines. Your healthcare provider will perform a test to make sure that Lynparza is right for you.
• a certain type of abnormal inherited BRCA gene, human epidermal growth factor receptor 2 (HER2)-negative breast cancer that has spread to other parts of the body (metastatic). You should have received chemotherapy medicines, either before or after your cancer has spread. If you have hormone receptor (HR)-positive disease, you should have been treated with hormonal therapy. Your healthcare provider will perform a test to make sure that Lynparza is right for you.
• metastatic pancreatic cancer with a certain type of abnormal inherited BRCA gene. Lynparza is used as maintenance treatment after your cancer has not progressed on at least 16 weeks of treatment with platinum-based chemotherapy. Your healthcare provider will perform a test to make sure that Lynparza is right for you.
• prostate cancer with certain inherited or acquired abnormal genes called homologous recombination repair (HRR genes). Lynparza is used when the cancer has spread to other parts of the body (metastatic), and no longer responds to a medical or surgical treatment that lowers testosterone, and has progressed after treatment with enzalutamide or abiraterone. Your healthcare provider will perform a test to make sure Lynparza is right for you.

How does this medicine work?

• Olaparib (oh lap' a rib) is a small molecule inhibitor of poly adenine diphosphate (ADP)-ribose polymerase (PARP), an enzyme involved in DNA transcription and repair.
• Patients with mutations of the BRCA 1 and 2 genes are at increased risk for cancer, particularly ovarian and breast cancer in women.
• The BRCA gene encodes DNA repair enzymes, and tumor cells with BRCA mutations are dependent upon other DNA repair pathways and thus have an increased sensitivity to inhibition of PARP.
• Clinical trials of olaparib in women with BRCA 1 and 2 germline mutations and advanced, refractory ovarian carcinoma have shown response rates of 30% to 40% and prolongation of progression-free survival.
• Olaparib is also under evaluation as therapy for advanced breast cancer and other malignant diseases associated mutations in BRCA or other DNA repair enzymes.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid coadministration of strong or moderate CYP3A inhibitors. If the strong or moderate inhibitor must be coadministered, reduce the dose of Lynparza. strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, posaconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, boceprevir, telaprevir, telithromycin and conivaptan)
• moderate CYP3A inhibitors (e.g., amprenavir, aprepitant, atazanavir, ciprofloxacin, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, imatinib, verapamil).
• Avoid coadministration of strong or moderate CYP3A inducers. strong inducers of CYP3A (e.g., rifampin, carbamazepine, St. John's Wort and phenytoin).

Is this medicine FDA approved?

• This medicine is approved in the year 2014.

How should this medicine be used?

• Select patients for treatment with Lynparza based on the presence of deleterious or suspected deleterious HRR gene mutations, including BRCA mutations, or genomic instability based on the indication, biomarker, and sample type.

Recommended Dosage:

• Recommended dosage is 300 mg taken orally twice daily with or without food.

Dosage Modifications for Adverse Reactions

• To manage adverse reactions, consider interruption of treatment or dose reduction. The recommended dose reduction is 250 mg taken twice daily.

Dosage Modifications for Concomitant Use with Strong or Moderate CYP3A Inhibitors

• Avoid concomitant use of strong or moderate CYP3A inhibitors with Lynparza.

If concomitant use cannot be avoided, reduce Lynparza dosage to:

• 100 mg twice daily when used concomitantly with a strong CYP3A inhibitor.
• 150 mg twice daily when used concomitantly with a moderate CYP3A inhibitor.

Dosage Modifications for Renal Impairment Moderate Renal Impairment

• In patients with moderate renal impairment (CLcr 31-50 mL/min), reduce the Lynparza dosage to 200 mg orally twice daily

Administration

• Take Lynparza tablets exactly as your healthcare provider tells you.
• Do not change your dose or stop taking Lynparza unless your healthcare provider tells you to. Your healthcare provider may temporarily stop treatment with Lynparza or change your dose of Lynparza if you experience side effects.
• Your healthcare provider will decide how long you stay on treatment.
• Do not take more than 4 Lynparza tablets in 1 day. If you have any questions about Lynparza, please talk to your healthcare provider or pharmacist.
• Take Lynparza by mouth 2 times a day.
• Each dose should be taken about 12 hours apart.
• Swallow Lynparza tablets whole. Do not chew, crush, dissolve, or divide the tablets.
• Take Lynparza with or without food.
• If you are taking Lynparza for prostate cancer and you are receiving gonadotropin-releasing hormone (GnRH) analog therapy, you should continue with this treatment during your treatment with Lynparza unless you have had a surgery to lower the amount of testosterone in your body (surgical castration).
• If you miss a dose of Lynparza, take your next dose at your usual scheduled time. Do not take an extra dose to make up for a missed dose.
• If you take too much Lynparza, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 150 mg, 100 mg

This medicine is available in fallowing brand namesː

• Lynparza

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea or vomiting
• tiredness or weakness
• low red blood cell counts
• diarrhea
• loss of appetite
• headache
• changes in the way food tastes
• cough
• low white blood cell counts
• shortness of breath
• dizziness
• indigestion or heartburn
• low platelet counts

Lynparza may cause serious side effects Including:

• Bone marrow problems called Myelodysplastic Syndrome (MDS) or Acute Myeloid Leukemia (AML)
• Lung problems (pneumonitis)
• Blood clots (Venous Thromboembolic Events)

What special precautions should I follow?

• Myelodysplastic syndrome (MDS)/Acute Myeloid Leukemia (AML) has occurred in patients treated with Lynparza and some cases were fatal. Monitor patients for hematological toxicity at baseline and monthly thereafter. Discontinue if MDS/AML is confirmed.
• Pneumonitis have occurred in 0.8% of patients exposed to Lynparza, and some cases were fatal. Interrupt treatment if pneumonitis is suspected. Discontinue if pneumonitis is confirmed.
• Lynparza Can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception.
• Venous thromboembolic events including pulmonary embolism occurred in 7% of patients with mCRPC. Monitor patients for signs and symptoms of venous thrombosis and pulmonary embolism and treat as medically appropriate.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Lynparza can cause fetal harm when administered to a pregnant woman.
• There are no available data on Lynparza use in pregnant women to inform the drug-associated risk.

Can this medicine be used in children?

• Safety and effectiveness of Lynparza have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: olaparib
• Inactive ingredients:
• Tablet contains: copovidone, mannitol, colloidal silicon dioxide and sodium stearyl fumarate
• Tablet coating contains: hypromellose, polyethylene glycol 400, titanium dioxide, ferric oxide yellow and ferrosoferric oxide (150 mg tablet only)

Who manufactures and distributes this medicine?

Distributed by: AstraZeneca Pharmaceuticals LP Wilmington

What should I know about storage and disposal of this medication?

• Store Lynparza at room temperature, between 68°F to 77°F (20°C to 25°C).
• Store Lynparza in the original bottle to protect it from moisture.
• Keep Lynparza and all medicines out of reach of children.

• Dailymed label info on Olaparib
• FDA Olaparib

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