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Tariquidar

Tariquidar
Clinical data
ATC code
  • none
Identifiers
  • N-[2-[[4-[2-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC38H38N4O6
Molar mass646.744 g·mol−1
3D model (JSmol)
  • COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC
  • InChI=1S/C38H38N4O6/c1-45-33-18-25-14-16-42(23-28(25)19-34(33)46-2)15-13-24-9-11-29(12-10-24)40-38(44)30-20-35(47-3)36(48-4)21-32(30)41-37(43)27-17-26-7-5-6-8-31(26)39-22-27/h5-12,17-22H,13-16,23H2,1-4H3,(H,40,44)(H,41,43) X markN
  • Key:LGGHDPFKSSRQNS-UHFFFAOYSA-N X markN
 X markNcheckY (what is this?)  (verify)

Tariquidar (INN/USAN) is a potent P-glycoprotein inhibitor and a substrate of breast cancer protein (BCRP/ABCG2)[1] undergoing research as an adjuvant against multi-drug resistance in cancer.[2]

Tariquidar progressed to phase III clinical trials in combination with vinorelbine in an effort to enhance the efficacy of this chemotherapeutic agent. However, several of these trials were terminated early due to adverse effects, and further development of Tariquidar was subsequently halted.[3]

References

  1. ^ Weidner LD, Fung KL, Kannan P, Moen JK, Kumar JS, Mulder J, et al. (February 2016). "Tariquidar Is an Inhibitor and Not a Substrate of Human and Mouse P-glycoprotein". Drug Metabolism and Disposition: The Biological Fate of Chemicals. 44 (2): 275–282. doi:10.1124/dmd.115.067785. PMC 4746486. PMID 26658428.
  2. ^ Fox E, Bates SE (April 2007). "Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor". Expert Review of Anticancer Therapy. 7 (4): 447–459. doi:10.1586/14737140.7.4.447. PMID 17428165.
  3. ^ Modok S, Mellor HR, Callaghan R (August 2006). "Modulation of multidrug resistance efflux pump activity to overcome chemoresistance in cancer". Current Opinion in Pharmacology. 6 (4): 350–354. doi:10.1016/j.coph.2006.01.009. PMID 16690355.
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