"目录号: HY-13646
Membrane Transporter/Ion Channel-
HM30181是一种有效的选择性的P-glycoprotein抑制剂。
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生物活性
Description
HM30181 is a potent and selective inhibitor ofP-glycoprotein.
In Vitro
HM30181 is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, HM30181: 13.1±2.3 nM)[1]. HM30181 shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor[2].
In Vivo
PET scans with the Pgp substrate (R)-[11C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]verapamil brain uptake compared with vehicle treated animals[1]. HM30181 inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. HM30181 increases the oral bioavailability of co-administered paclitaxel by more than 12 times in rats[2].
Clinical Trial
Hanmi Pharmaceutical Company Limited
Healthy
June 2009
Phase 1
Hanmi Pharmaceutical Company Limited
Advanced Solid Malignancies
June 2008
Phase 1
Hanmi Pharmaceutical Company Limited
Advanced Solid Malignancies
July 2008
Phase 1
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Advanced Solid Tumors
August 2006
Phase 1
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References
