About: 2-Methoxyestradiol Nanocrystal Colloidal Dispersion     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • 2-Methoxyestradiol Nanocrystal Colloidal Dispersion
rdfs:subClassOf
Has_Target
Semantic_Type
  • Pharmacologic Substance
  • Steroid
Preferred_Name
  • 2-Methoxyestradiol Nanocrystal Colloidal Dispersion
UMLS_CUI
  • C1831865
PDQ_Open_Trial_Search_ID
  • 488412
PDQ_Closed_Trial_Search_ID
  • 488412
Legacy_Concept_Name
  • _2-Methoxyestradiol_Nanocrystal_Colloidal_Dispersion
FULL_SYN
  • Panzem NCDBRNCI
  • 2-Methoxyestradiol Nanocrystal Colloidal DispersionPTNCI
DEFINITION
  • An orally bioavailable liquid formulation containing the small molecule 2-methoxyestradiol with potential antineoplastic activity. 2-Methoxyestradiol, a naturally occurring estradiol metabolite, exerts its antitumor effect by inhibiting endothelial cells as well as tumor cells through multiple mechanisms. This agent binds to tubulin and disrupts microtubule formation, thereby preventing mitosis and subsequent cellular proliferation. In addition, 2-methoxyestradiol induces caspase activation, resulting in cell cycle arrest in G2 phase and apoptosis in due course. This agent also down-regulates hypoxia inducible factor-one alpha (HIF-1a). The nanocrystal colloidal dispersion increases the absorption of 2-methoxyestradiol, thereby improving its bioavailability, which results in enhanced drug plasma levels.NCI
code
  • C62603
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