PARP inhibitor

[2][3][4][5] PARP inhibitors appear to improve progression-free survival in women with recurrent platinum-sensitive ovarian cancer, as evidenced mainly by olaparib added to conventional treatment.

Radiotherapy has the potential to kill 100% of any targeted cells, but the dose required to do so would cause unacceptable side effects to healthy tissue.

[14] Chemotherapy and radiation therapy attempt to kill cancer cells by inducing high levels of DNA damage.

When the gene for one of these proteins is mutated, the change can lead to errors in DNA repair that can eventually cause breast cancer.

Cancer cells that are low in oxygen (e.g. in fast growing tumors) are sensitive to PARP inhibitors.

[23] PARP inhibitors such as olaparib, under experimental conditions, appear to be beneficial in limiting atrial fibrillation and other DNA damage associated cardiovascular diseases.

[24] Side effects of PARP inhibitor treatment for cancer may include neutropenia, and a risk of anaemia.

[25] The toxicity profile of PARP inhibitors when treating cancer has not been found to be more serious than chemotherapy agents, however, further research is needed to understand the effects of this medication on quality of life after treatment.

Other resistance mechanisms include enhanced drug efflux, restoration of DNA replication fork protection, mutations in PARP1, and PARG downregulation.

Model of the inhibitor olaparib (dark gray) occupying the NAD + -binding site of PARP1. From PDB : 5DS3 ​.