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OLAPARIB

OLAPARIB

Molecule Overview

Olaparib is an oral targeted medicine that blocks a DNA-repair enzyme, making it especially effective in cancers with certain faulty DNA-repair genes such as BRCA. It belongs to a class of medicines called PARP inhibitors, used across several cancer types including ovarian, breast, pancreatic, and prostate cancer. It is a prescription-only medicine.

Medical Classification

  • Therapeutic Class: Anti-cancer (oncology) targeted therapy.

  • Pharmacological Class: PARP (poly ADP-ribose polymerase) inhibitor.

  • Drug Family: Small-molecule DNA-damage-response inhibitors.

  • ATC Classification: L01XK01 (Olaparib).

Conditions Treated

Approved: Maintenance treatment of BRCA-mutated advanced ovarian cancer (first-line and recurrent settings); germline BRCA-mutated HER2-negative metastatic breast cancer; germline BRCA-mutated metastatic pancreatic adenocarcinoma (maintenance); and HRR gene-mutated or BRCA-mutated metastatic castration-resistant prostate cancer (alone or combined with abiraterone and prednisone).

Commonly used for: Patients with these cancer types who test positive for a BRCA mutation or other homologous recombination repair (HRR) gene mutations, identified through companion diagnostic testing.

Off-label use (only under medical guidance): Being studied in other HRR-deficient solid tumours in clinical trials; not routine outside its approved indications.

Available Strengths & Dosage Forms

● Oral tablets: 100 mg and 150 mg.

How the Molecule Works

Cells with a faulty BRCA gene rely more heavily on an enzyme called PARP to repair everyday DNA damage. Olaparib blocks PARP, so these already-vulnerable cancer cells accumulate DNA damage they can't fix and die, while normal cells (with working BRCA genes) are relatively less affected.

Dosage & Administration

  • Standard dose: 300 mg (two 150 mg tablets) taken orally twice daily, with or without food.

  • Condition-wise dose: For first-line maintenance treatment of BRCA-mutated advanced ovarian cancer, treatment generally continues until disease progression, unacceptable toxicity, or completion of 2 years.

  • Route: Oral; tablets should be swallowed whole and not chewed, crushed, dissolved, or divided.

  • Missed dose: Take the next dose at its scheduled time; don't double up.

  • Overdose: May worsen known side effects such as nausea or low blood counts; requires medical attention.

Side Effects

  • Common: Nausea, fatigue, vomiting, low blood counts (anaemia, low white cells, low platelets), and decreased appetite.

  • Serious: Myelodysplastic syndrome/acute myeloid leukaemia (rare but serious blood cancers reported with long-term use), pneumonitis, and severe anaemia sometimes requiring transfusion.

  • Emergency symptoms: New or worsening shortness of breath/cough, unusual bruising or bleeding, signs of infection with fever, or extreme fatigue that doesn't improve.

  • Recovery advice: Nausea is common, especially early in treatment, and is often manageable with anti-nausea medicines; blood counts are checked regularly so that dose adjustments can be made before symptoms become severe.

Warnings & Precautions

Pregnancy: Not recommended; can cause fetal harm.

Breastfeeding: Not recommended during treatment and for 1 month after the last dose.

Liver disease: Used with caution; specific dose adjustment guidance depends on severity.

Kidney disease: Dose adjustment needed in moderate impairment; used cautiously in severe impairment.

Elderly: Used with routine monitoring; no specific age-based dose adjustment defined beyond general precautions.

Children: Not approved for use in children.

Drug Interactions

● Strong or moderate CYP3A inhibitors (e.g., ketoconazole, clarithromycin): significantly increase olaparib levels; dose reduction is recommended, or the interacting drug avoided.

● Strong or moderate CYP3A inducers (e.g., rifampin, carbamazepine): can substantially reduce olaparib's effectiveness; co-administration is not recommended.

● Other myelosuppressive drugs or radiotherapy: may increase the risk of low blood counts when combined.

● Live vaccines and immunosuppressants: used with caution given effects on blood counts and general immune status.

Monitoring Requirements

● Complete blood counts monthly for the first year, then periodically thereafter.

● Monitoring for symptoms of pneumonitis (new cough, shortness of breath).

● Renal and hepatic function tests periodically.

● Regular clinical review for treatment response and tolerability

Alternative Molecules

Niraparib, Rucaparib, Talazoparib (other PARP inhibitors, indication and dosing specifics vary by cancer type).

Combination Therapies

Used as monotherapy maintenance in most approved indications; also approved in combination with abiraterone and prednisone/prednisolone for certain BRCA-mutated prostate cancers, and with bevacizumab in some ovarian cancer maintenance settings.

● Ovarian Cancer Medicines

● Breast Cancer Medicines

● Prostate Cancer Medicines

● PARP Inhibitors

FAQs

Q1.

What is olaparib used for?

It's used to treat several BRCA- or HRR-mutated cancers, including ovarian, breast, pancreatic, and prostate cancer, depending on genetic test results.

Q2.

Do I need a genetic test before starting olaparib?

Yes, treatment selection is based on an FDA-approved companion diagnostic test confirming a BRCA or relevant HRR gene mutation.

Q3.

Is olaparib a form of chemotherapy?

No, it's a targeted therapy (PARP inhibitor) that specifically exploits a DNA-repair weakness in cancer cells with certain gene mutations.

Q4.

What blood tests are needed during treatment?

Regular complete blood counts are needed, especially in the first year, to catch low blood cell counts early.

Q5.

How long is olaparib treatment continued?

It varies by indication — some maintenance uses have a defined 2-year endpoint, while others continue until disease progression or unacceptable side effects.

Disclaimer

The information on this page is for educational purposes only and is not a substitute for medical advice. Please consult your oncologist to know if this treatment is appropriate for your condition.

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