Title: Zosuquidar
CAS Registry Number: 167354-41-8
CAS Name: (aR)-4-[(1aa,6a,10ba)-1,1,-Difluoro-1,1a,6,10b-tetrahyrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-a-[(5-quinolinyloxy)methyl]-1-piperazineethanol
Additional Names: (2R)-anti-5-[3-[4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy]quinoline
Molecular Formula: C32H31F2N3O2
Molecular Weight: 527.60
Percent Composition: C 72.85%, H 5.92%, F 7.20%, N 7.96%, O 6.06%
Literature References: Multidrug resistance (MDR) modulator; selective inhibitor of P-glycoprotein (P-gp), q.v. Prepn: J. R. Pfister, D. L. Slate, WO 9424107; eidem, US 5654304 (1994, 1997 both to Syntex); J. R. Pfister et al., Bioorg. Med. Chem. Lett. 5, 2473 (1995). Improved synthesis: C. J. Barnett et al., J. Org. Chem. 69, 7653 (2004). Effect on multidrug resistant cell lines: L. J. Green et al., Biochem. Pharmacol. 61, 1393 (2001). Specificity for P-gp: R. L. Shepard et al., Int. J. Cancer 103, 121 (2003). Clinical pharmacology and pharmacokinetics in patients with advanced malignancies: E. H. Rubin et al., Clin. Cancer Res. 8, 3710 (2002). Effect on pharmacokinetics of doxorubicin: S. Callies et al., Cancer Chemother. Pharmacol. 51, 107 (2003).
Derivative Type: Trihydrochloride
CAS Registry Number: 167465-36-3
Manufacturers' Codes: LY-335979; RS-33295-198
Molecular Formula: C32H31F2N3O2.3HCl
Molecular Weight: 636.99
Percent Composition: C 60.34%, H 5.38%, F 5.97%, N 6.60%, O 5.02%, Cl 16.70%
Properties: mp 190°.
Melting point: mp 190°
Therap-Cat: Antineoplastic adjunct (chemosensitizer).
Keywords: Antineoplastic Adjunct; Chemosensitizer.
Zotepine Zoxamide Zoxazolamine Zygadenine

Systematic (IUPAC) name
Clinical data
Legal status  ?
CAS number 167354-41-8 N
ATC code None
PubChem CID 153997
ChemSpider 24599682 YesY
KEGG D06387 YesY
Chemical data
Formula C32H31F2N3O2 
Mol. mass 527.61 g/mol
 N (what is this?)  (verify)

Zosuquidar is a compound of antineoplastic drug candidates currently under development. It is now in "Phase 3" of clinical tests in the United States. Its action mechanism consists of the inhibition of P-glycoproteins; other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are proteins which convert the energy derived from the hydrolysis of ATP to structural changes in protein molecules, in order to perform coupling, thus discharging medicine from cells. If P-glycoprotein coded with the MDR1 gene manifests itself in cancer cells, it discharges much of the antineoplastic drugs from the cells, making cancer cells medicine tolerant, and rendering antineoplastic drugs ineffective. This protein also manifests itself in normal organs not affected by the cancer (such as the liver, small intestine, and skin cells in blood vessels of the brain), and participates in the transportation of medicine. The compound zosuquidar inhibits this P-glycoprotein, causing the cancer cells to lose their medicine tolerance, and making antineoplastic drugs effective.