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Rucaparib information


Rucaparib
Clinical data
Pronunciation/rˈkæpərɪb/ roo-KAP-ər-ib
Trade namesRubraca
Other namesCO-338, AG-014699, PF-0136738, PF-01367338
AHFS/Drugs.comMonograph
MedlinePlusa617002
License data
  • US DailyMed: Rucaparib
Pregnancy
category
  • Not recommended
Routes of
administration
By mouth
ATC code
  • L01XK03 (WHO)
Legal status
Legal status
  • UK: POM (Prescription only)[1]
  • US: ℞-only[2]
  • EU: Rx-only[3]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability30–45% (Tmax = 1.9 hours)
Protein binding70% (in vitro)
MetabolismLiver (primarily CYP2D6; 1A2 and 3A4 to a lesser extent)
Elimination half-life17–19 hours[2]
Identifiers
IUPAC name
  • 8-Fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
CAS Number
  • 283173-50-2
  • as salt: 1859053-21-6
PubChem CID
  • 9931954
  • as salt: 121490161
IUPHAR/BPS
  • 7736
DrugBank
  • DB12332
  • as salt: DBSALT001982
ChemSpider
  • 8107584
  • as salt: 57643660
UNII
  • 8237F3U7EH
  • as salt: 41AX9SJ8KO
KEGG
  • D10079
  • as salt: D10982
ChEBI
  • CHEBI:134689
  • as salt: CHEBI:134692
ChEMBL
  • ChEMBL1173055
  • as salt: ChEMBL3833368
PDB ligand
  • RPB (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID10182563 Edit this at Wikidata
ECHA InfoCard100.247.490 Edit this at Wikidata
Chemical and physical data
FormulaC19H18FN3O
Molar mass323.371 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CNCc1ccc(cc1)c2[nH]c3cc(F)cc4C(=O)NCCc2c34
InChI
  • InChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)
  • Key:HMABYWSNWIZPAG-UHFFFAOYSA-N

Rucaparib, sold under the brand name Rubraca, is a PARP inhibitor used as an anti-cancer agent.[2] Rucaparib is a first-in-class pharmaceutical drug targeting the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1). It is taken by mouth.[2][4]

The most common side effects include tiredness or weakness, nausea (feeling sick), increased levels of creatinine (which may indicate kidney problems) and liver enzymes in the blood (which may indicate liver damage), vomiting, anaemia (low red blood cell counts), decreased appetite, dysgeusia (taste disturbances), diarrhoea, thrombocytopenia (low levels of platelets) and abdominal pain (belly ache).[3][2]

  1. ^ "Rubraca 200mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 19 June 2019. Archived from the original on 29 August 2021. Retrieved 17 May 2020.
  2. ^ a b c d e "Rubraca- rucaparib tablet, film coated". DailyMed. 6 April 2018. Archived from the original on 9 May 2020. Retrieved 17 May 2020.
  3. ^ a b Cite error: The named reference Rubraca EPAR was invoked but never defined (see the help page).
  4. ^ "Cancer Research Launches New Drug Trial". netdoctor.co.uk. Hearst Magazines UK. 10 January 2012. Archived from the original on 26 December 2017. Retrieved 20 December 2016.

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