Rucaparib

Rucaparib, sold under the brand name Rubraca, is a PARP inhibitor used as an anti-cancer agent. 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.

Rucaparib
Clinical data
Pronunciation/ruːˈkæpərɪb/ roo-KAP-ər-ib
Trade namesRubraca
Other namesCO-338, AG-014699, PF-0136738, PF-01367338
AHFS/Drugs.comMonograph
MedlinePlusa617002
License data
Pregnancy
category
  • Not recommended
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • 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
Identifiers
  • 8-Fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.247.490
Chemical and physical data
FormulaC19H18FN3O
Molar mass323.371 g·mol−1
3D model (JSmol)
  • CNCc1ccc(cc1)c2[nH]c3cc(F)cc4C(=O)NCCc2c34
  • 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

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).

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.