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AttributesValues
rdf:type
rdfs:label
  • Poly-alendronate Dextran-Guanidine Conjugate
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
  • Organophosphorus Compound
Preferred_Name
  • Poly-alendronate Dextran-Guanidine Conjugate
NCI_META_CUI
  • CL436277
PDQ_Open_Trial_Search_ID
  • 733915
PDQ_Closed_Trial_Search_ID
  • 733915
FULL_SYN
  • Poly-alendronate Dextran-Guanidine ConjugatePTNCI
  • ODXABNCI
  • OsteodexFBNCI
  • Dextran/Alendronate/Guanidine-containing PolybisphosphonateSYNCI
DEFINITION
  • A polybisphosphonate dextran-guanidine conjugate with potential anti-resorptive and antineoplastic activities. Alendronic acid and aminoguanidine were conjugated sequentially to oxidized dextran resulting in an average of 8 alendronate and 50 guanidine groups coupled to the dextran backbone. Upon administration, the poly-alendronate dextran-guanidine conjugate inhibits the mevalonate pathway by inhibiting farnesyl diphosphate synthase (FDPS) which leads to a reduction in protein prenylation and to the loss of downstream metabolites essential for osteoclast function. This eventually leads to the induction of apoptosis in osteoclasts. Also, by preventing osteoclast-mediated bone resorption, this agent decreases bone turnover and stabilizes the bone matrix. The guanidine moiety increases the nitrogen content and possibly the activity of the bisphosphonate and its ability to inhibit FDPS. In addition, the guanidine moiety facilitates cell internalization and may contribute to this agent's cytotoxicity.NCI
code
  • C101894
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