Zosuquidar

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Zosuquidar
Clinical data
Other namesLY-335979
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
  • (2R)-1-{4-[(1aR,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c] [7]annulen-6-yl}-3-(quinolin-5-yloxy)propan-2-ol
JSmol)
  • Cl.Cl.Cl.FC4(F)[C@@H]3c1ccccc1C(c2c(cccc2)[C@@H]34)N5CCN(CC5)C[C@@H](O)COc7c6cccnc6ccc7
  • InChI=1S/C32H31F2N3O2/c33-32(34)29-22-7-1-3-9-24(22)31(25-10-4-2-8-23(25)30(29)32)37-17-15-36(16-18-37)19-21(38)20-39-28-13-5-12-27-26(28)11-6-14-35-27/h1-14,21,29-31,38H,15-20H2/t21-,29-,30+,31-/m1/s1 checkY
  • Key:IHOVFYSQUDPMCN-DBEBIPAYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Zosuquidar (development code LY-335979) is an experimental

inhibits P-glycoproteins.[2] Other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are trans-membrane proteins that pump foreign substances out of cells in an ATP dependent fashion. Cancers overexpressing P-glycoproteins are able to pump out therapeutic molecules before they are able to reach their target, effectively making the cancer multi-drug resistant. Zosuquidar inhibits P-glycoproteins, inhibiting the efflux pump and restoring sensitivity to chemotherapeutic agents.[2]

Zosuqidar was initially characterized by Syntex Corporation, which was acquired by

phase III clinical trial for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome did not meet its primary endpoint[3] and Eli Lilly discontinued its development.[4]

References

  1. ^ "Zosuquidar trihydrochloride". NCI Drug Dictionary. National Cancer Institute.
  2. ^
    PMID 20716770
    .
  3. ^ Clinical trial number NCT00046930 for "Daunorubicin & Cytarabine +/- Zosuquidar inTreating Older Patients With Newly Diagnosed Acute Myeloid Leukemia or Refractory Anemia" at ClinicalTrials.gov
  4. ^ "Zosuquidar - Kanisa Pharmaceuticals". Adis Insight. Springer Nature Switzerland AG.