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Olaparib

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Information about Olaparib

Olaparib is a small molecule inhibitor of poly ADP-ribose polymerase and is used as an antineoplastic agent in the therapy of refractory and advanced ovarian carcinoma. 

Liver safety of Olaparib

Olaparib therapy is associated with a low rate of transient elevations in serum aminotransferase during therapy and has not been linked to instances of clinically apparent liver injury

Mechanism of action of Olaparib

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. 

FDA approval information for Olaparib

Olaparib received approval for use in the United States in 2014 for therapy of advanced and refractory ovarian carcinoma in women with BRAC 1 and 2 mutations. 

Dosage and administration for Olaparib

Olaparib is available in 50 mg capsules under the brand name Lynparza.  The recommended dose is 400 mg by mouth twice daily.  Lower doses are recommended for patients with renal impairment.

Side effects of Olaparib

Common side effects include anemia, fatigue, nausea, diarrhea, dyspepsia, abdominal pain, anorexia, cough, muscle and join pain, headache and rash.  Uncommon, but potentially severe side effects include pneumonitis, myelodysplastic syndrome and embryo-fetal toxicity.   

 

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