Description and Characteristics of Olaparib

Olaparib is an inhibitor of tumor cell replication that alters the DNA copying process in neoplastic cells. Scientific studies on this drug are promising.
Description and Characteristics of Olaparib

Last update: 29 March, 2021

Olaparib is a chemotherapy drug for the treatment of different cancers in advanced stages. Its brand name is Lynparza, originally developed by AstraZeneca, a pharmaceutical company.

There are different pharmaceutical formats of olaparib, and doctors prescribe one or the other depending on the disease and its stage. For example, the tablet format is a kind of monotherapy for the treatment of adult patients with high-grade epithelial ovarian and fallopian tube cancer. It also works in relapsed patients under platinum-based therapy.

Furthermore, olaparib capsules are for the treatment of cancers with a mutated gene: BRCA. This gene plays an important role in the development of cancer, especially breast and ovarian.

Note that olaparib capsules and tablets aren’t interchangeable, due to the differences in dosage and bioavailability of each formulation. In addition, the side effects these formulations may cause in patients who take them are:

  • Nausea
  • Diarrhea
  • Fatigue
  • Neutropenia
  • Thrombocytopenia
  • Dizziness

Olaparib and its mechanism of action

This drug inhibits the human enzymes responsible for proper DNA repair: PARP.

In-vitro samples demonstrated that it inhibits the growth of selected tumor cell lines and also tumor growth. One can use it both as monotherapy and in combination with previously established chemotherapies.

When olaparib binds to these DNA-associated enzymes, it prevents DNA repair through a series of reactions. In healthy cells, this repair requires those who have the BRCA-1 and BCRA-2 genes to function properly. Alternative error-prone repair pathways begin to be activated, leading to increased genomic instability in tumor cells that have malfunctioning in these proteins.

Genomic instability can reach intolerable levels after several rounds of replication of these tumor cells. The cancer cells die as a consequence. The reason for this is they show a high amount of DNA damage in comparison to normal cells.

Olaparib administration after platinum treatment proved beneficial in studies of patients who had a BRCA mutation and therefore didn’t have a functioning BRCA protein. The result was a delay in tumor progression and an increase in overall survival versus platinum treatment alone.

A DNA chain.
Olaparib interferes with DNA replication in tumor cells.

Olaparib and BRCA

As we mentioned above, olaparib is mainly used for the treatment of breast cancer although one can use it for the treatment of other cancers too. This is especially the case if there are advanced neoplasms or metastatic ovarian cancer.

As for breast cancer, one of the most frequent molecular events in triple-negative breast tumors is the alteration of the function of the BRCA protein. This oncologic variety is one of the most aggressive for women.

More than 80% of patients with a mutation in the BRCA1 gene have triple-negative breast cancer. Also, approximately 15% of patients with ovarian cancer and 5% of those who have breast, pancreatic, or prostate cancer have inherited BRCA1 or BRCA2 mutations.

A note about BRCA.
Olaparib has promising positive effects in patients with BRCA gene mutations.

Olaparib is a PARP inhibitor, which are proteins that help repair damaged DNA. Because BRCA mutations can also hinder DNA repair, a similar inhibition of this process with olaparib can lead to cancer cell death.

Researchers evaluated the efficacy of olaparib in monotherapy and in combination with other chemotherapy drugs in different phase II clinical trials. Also, its effectiveness in monotherapy in heavily pre-treated advanced breast cancer patients had a higher objective response rate.

Find out more about the drug Palbociclib to Treat Breast Cancer


Finally, olaparib represents a novel approach as an antineoplastic treatment through PARP inhibition. In fact, it can solve an unmet need in patients with BRCA-associated cancer.

Treatment isn’t easy because these neoplastic diseases are quite advanced. They require a combination of therapies and proper follow-up from the patient. Ideally, there must an advising oncology group that’s always attentive to the patient’s needs and considering all the factors.

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BRCA-1 and BRCA-2 Genes and Breast Cancer
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BRCA-1 and BRCA-2 Genes and Breast Cancer

The BRCA-1 and BRCA-2 gene are a pair of human genes that produce proteins and their function is to try to suppress tumor growth.

  • Robson, M., Im, S. A., Senkus, E., Xu, B., Domchek, S. M., Masuda, N., … Conte, P. (2017). Olaparib for metastatic breast cancer in patients with a germline BRCA mutation. New England Journal of Medicine.
  • Ledermann, J., Harter, P., Gourley, C., Friedlander, M., Vergote, I., Rustin, G., … Matulonis, U. (2012). Olaparib maintenance therapy in platinum-sensitive relapsed ovarian cancer. New England Journal of Medicine.
  • Oza, A. M., Cibula, D., Benzaquen, A. O., Poole, C., Mathijssen, R. H. J., Sonke, G. S., … Friedlander, M. (2015). Olaparib combined with chemotherapy for recurrent platinum-sensitive ovarian cancer: A randomised phase 2 trial. The Lancet Oncology.