Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Rucaparib
Drug ID BADD_D02510
Description Rucaparib is a potent mammalian poly(ADP-ribose) polymerase (PARP) 1, 2 and 3 inhibitor with anticancer properties. PPAR is an enzyme that plays an essential role in DNA repair by activating response pathways and facilitating repair [A18745], and defects in these repair mechanisms have been demonstrated in various malignancies, including cancer. Regulation of repair pathways is critical in promoting necessary cell death. BRCA genes are tumor suppressor genes mediate several cellular process including DNA replication, transcription regulation, cell cycle checkpoints, apoptosis, chromatin structuring and homologous recombination (HR). Homologous recombination deficiency (HRD), along with PPAR inhibition, is a vulnerability that enhances the cell death pathway when the single mutations alone would permit viability. Ovarian cancer commonly possesses defects in DNA repair pathways such as HRD due to BRCA mutations or otherwise. There are three main types of ovarian cancer: epithelial (90%), germ cell (5%) and sex cord stromal cell (5%). Epithelial ovarian, being the most common, fifth leading cause of cancer-related deaths in women in the United States. Advanced ovarian cancer particularly poses challenges due to reduced therapeutic response rates from standard platinum-based chemotherapy and overall survival rates. Rucaparib has shown to induce cytotoxicity in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes [FDA Label]. Of all the BRCA1/2 mutations in ovarian cancer, most are due to germline mutations (18%), and approximately 7% represent somatic mutations acquired within the tumor [A31354]. The indication of rucaparib as an oral monotherapy in patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer was granted accelerated approval in 2016 for selected patients who have previously received greater than two lines of platinum-based therapy. It is currently marketed in the US under the brand name Rubraca that contains rucaparib camsylate as the active ingredient. The identification of patients who are eligible for rucaparib therapy is performed via *in vitro* diagnostic tests to detect the presence of a deleterious BRCA mutation (germline and/or somatic). The FDA-approved test qualitatively detects sequence alterations in BRCA1 and BRCA2 (BRCA1/2) genes. More information can be found on the FDA Website [L1047]. While rucaparib is indicated for deleterious BRCA mutation (germline and/or somatic)-associated advanced ovarian cancer, there is evidence that its antitumor activity is also clinically effective against ovarian tumors with high homologous recombination deficiency (HRD) loss of heterozygosity (LOH) [A31354].
Indications and Usage Indicated as monotherapy for the treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. Select patients for therapy based on an FDA-approved companion diagnostic for rucaparib.
Marketing Status approved; investigational
ATC Code L01XK03
DrugBank ID DB12332
KEGG ID D10079
MeSH ID C531549
PubChem ID 9931954
NDC Product Code 69660-202; 69660-203; 69660-201
Synonyms rucaparib | PF-01367338 | Rubraca | AG 014699 | AG014699 | AG-014699
Chemical Information
Molecular Formula C19H18FN3O
CAS Registry Number 283173-50-2
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.0010.015950%Not Available
Abdominal distension07.01.04.0010.009525%
Abdominal pain07.01.05.0020.021322%
Abdominal pain lower07.01.05.0100.001668%Not Available
Abdominal pain upper07.01.05.0030.017461%
Abdominal tenderness07.01.05.0040.001500%Not Available
Acne23.02.01.0010.001198%Not Available
Acute myeloid leukaemia16.01.05.001; Available
Ageusia17.02.07.001; Available
Asthenia08.01.01.0010.027725%Not Available
Back pain15.03.04.0050.007454%
Bladder discomfort20.02.02.0190.000246%Not Available
Blister23.03.01.001; Available
Bone disorder15.02.04.0040.000437%Not Available
Bone pain15.02.01.0010.002988%
Burning sensation17.02.06.001; Available
Cold sweat23.02.03.002; Available
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