Zosuquidar

Zosuquidar
Clinical data
ATC code	none;
Identifiers
	IUPAC name (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;
CAS Number	167354-41-8 ;
PubChem CID	153997;
ChemSpider	24599682 ;
UNII	AB5K82X98Y;
KEGG	D06387 ;
ChEMBL	ChEMBL444172 ;
CompTox Dashboard (EPA)	DTXSID9057894 ;
ECHA InfoCard	100.236.552
Chemical and physical data
Formula	C32H31F2N3O2
Molar mass	527.616 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cl.Cl.Cl.FC4(F)[C@@H]3c1ccccc1C(c2c(cccc2)[C@@H]34)N5CCN(CC5)C[C@@H](O)COc7c6cccnc6ccc7;
	InChI 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 ; Key:IHOVFYSQUDPMCN-DBEBIPAYSA-N ;
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Zosuquidar (also LY-335979) is an experimental antineoplastic drug. In 2010, it was announced that a phase III trial for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome did not meet its primary endpoint[1] and Eli Lilly discontinued its development.

Zosquidir inhibits P-glycoproteins. 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.

Zosuqidar was initially characterized by Syntex Corporation, which was acquired by Roche in 1990. Roche licensed the drug to Eli Lilly in 1997. It was granted orphan drug status by the FDA in 2006 for AML.

References

"Daunorubicin & Cytarabine +/- Zosuquidar inTreating Older Patients With Newly Diagnosed Acute Myeloid Leukemia or Refractory Anemia - Full Text View - ClinicalTrials.gov".

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[1] "Daunorubicin & Cytarabine +/- Zosuquidar inTreating Older Patients With Newly Diagnosed Acute Myeloid Leukemia or Refractory Anemia - Full Text View - ClinicalTrials.gov".