Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
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Poly(ADP-ribose) polymerases (PARP) are proteins responsible for DNA damage detection and signal transduction. PARP inhibitors (PARPi) are able to interact with the binding site for PARP cofactor (NAD+) and trapping PARP on the DNA. In this way, they inhibit single-strand DNA damage repair. These drugs have been approved in recent years for the treatment of ovarian cancer. Although they share some similarities, from the point of view of the chemical structure and pharmacodynamic, pharmacokinetic properties, these drugs also have some substantial differences. These differences may underlie the different safety profiles and activity of PARPi.
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Functional analyses, alongside molecular assays, are required to confirm the predicted response of women with ovarian cancer to PARP inhibitors such as olaparib, niraparib and rucaparib.
“Functional analyses, alongside molecular assays, are required to confirm the predicted response of women with ovarian cancer to PARPis such as the FDA-approved drugs olaparib, niraparib and rucaparib (Dickson et al., 2021; Lee et al., 2021; Valabrega et al., 2021).”
From Three-dimensional modelling of ovarian cancer: from cell lines to organoids for discovery and personalized medicine (2022) · cites this paper as Valabrega et al., 2021
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- Authors
- Valabrega, G., Scotto, G., Tuninetti, V., Pani, A., & Scaglione, F.
- Affiliations
- Candiolo Cancer Institute (IT)
- University of Milan (IT)
- Corresponding author
- Valabrega, Giorgio
- Venue
- International Journal of Molecular Sciences
- Publisher
- MDPI AG
- Published
- 2021-04-19
- Volume
- 22
- Issue
- 8
- Pages
- 4203
- ISSN
- 1422-0067 (ISSN-L)
- PMC
- PMC8073512
- OpenAlex
- W3156758253
- Cited by
- 93
- References
- 83
- Citations by year
- 2026: 9 · 2025: 14 · 2024: 19 · 2023: 21 · 2022: 24 · 2021: 6
- FWCI
- 2.12
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- International Journal of Molecular Sciences (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Institutional Research Information System University of Turin (University of Turin) (submittedVersion, other-oa)
- Archivio Istituzionale della Ricerca (Universita Degli Studi Di Milano) (submittedVersion, other-oa)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- GlaxoSmithKline
- Topics
- Health Sciences › Medicine › Oncology › PARP inhibition in cancer therapy
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › BRCA gene mutations in cancer
- Health Sciences › Medicine › Reproductive Medicine › Ovarian cancer diagnosis and treatment
- Keywords
- PARP inhibitors, ovarian cancer, poly(ADP-ribose) polymerase, NAD+ binding, pharmacokinetics, pharmacodynamics, drug safety, drug efficacy
- MeSH terms
- Poly(ADP-ribose) Polymerase Inhibitors, Female, Humans, Ovarian Neoplasms, Phthalazines, Piperazines
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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