rucaparib

Ligand id: 7736

Name: rucaparib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 3
Topological polar surface area 56.92
Molecular weight 323.14
XLogP 2.71
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
In December 2016, the US FDA granted accelerated approval to rucaparib for treatment of patients with deleterious germline and/or somatic BRCA mutation associated advanced ovarian cancer who have been treated with two or more chemotherapies. Link here to a list of clinical trials assessing rucaparib registered with ClinicalTrials.gov. Phase 2 trial results are published in [3].
Mechanism Of Action and Pharmacodynamic Effects
PARP-1 (poly(ADP-ribose) polymerase 1) inhibitors enhance the efficacy of drugs/therapies which cause DNA damage (eg alkylating agents such as temozolomide , topoisomerase poisons such as topotecan and irinotecan and ionizing radiation) [1-2]. This action helps to promote cancer cell death, by preventing the DNA repair which is required for cell survival. Cells with mutations in other DNA repair enzymes such as BRCA become more dependent on PARP for DNA repair. In such malignant cells, inhibition of PARP may therefore result in cell death due to accumulated therapy-induced DNA damage.