"目錄號: HY-15255

Membrane Transporter/Ion Channel-

Zosuquidar (LY335979)是P-糖蛋白（P-gp）介導的多藥抗性調節(jié)劑，Ki為60 nM。

P-glycoprotein

相關產(chǎn)品

Elacridar-Zosuquidar trihydrochloride-Tariquidar methanesulfonate, hydrate-Valspodar-(20S)-Protopanaxadiol-Dofequidar fumarate-Piperine-HM30181-Alisol F-Polyoxyethylene stearate-Biricodar-MCI826-

生物活性

Description

Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.IC50 value: 60 nM (Ki)Target:? P-glycoproteinZosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM. Zosuquidar binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents. Zosuquidar is a compound of antineoplastic drug candidates currently under development.

Clinical Trial

NCT00233909

Kanisa Pharmaceuticals

Leukemia, Myeloid

October 2005

Phase 1-Phase 2

NCT00046930

Eastern Cooperative Oncology Group-National Cancer Institute (NCI)-Eli Lilly and Company-Kanisa Pharmaceuticals

Leukemia-Myelodysplastic Syndromes

July 2002

Phase 3

NCT00129168

Kanisa Pharmaceuticals

Leukemia, Myeloid

August 2005

Phase 1-Phase 2

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References

[1].Dantzig AH, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.

[2].Marcelletti JF, Multani PS, Lancet JE et al. Leukemic blast and natural killer cell P-glycoprotein function and inhibition in a clinical trial of zosuquidar infusion in acute myeloid leukemia. Leuk Res. 2009 Jun;33(6):769-74.

[3].Ruff P, Vorobiof DA, Jordaan JP et al. A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen. Cancer Chemother Pharmacol. 2009 Sep;64(4):763-8.

[4].Cripe LD, Uno H, Paietta EM et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85.

[5].Abu Ajaj K, Graeser R, Kratz F. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin. Breast Cancer Res Treat. 2012 Jul;134(1):117-29.