NNC_45-0095

NNC 45-0095

NNC 45-0095

Chemical compound

NC 45-0095 is a synthetic nonsteroidal selective estrogen receptor modulator (SERM) which was under development by Novo Nordisk for the treatment of postmenopausal osteoporosis but was never marketed.[1][2][3][4][5] It is a partial agonist of the estrogen receptor (IC50Tooltip half-maximal inhibitory concentration (for binding inhibition) = 9.5 nM; EC50Tooltip half-maximal effective concentration = 13 nM) with mixed estrogenic and antiestrogenic activity, and shows full estrogenic activity in bone and uterus (EmaxTooltip maximal efficacy (relative to moxestrol, in Ishikawa endometrial cancer cell line) = 105%).[1][4] The compound is a pyrroloindolizine derivative.[1][2] Its development was discontinued by 2003.[5]

Quick Facts Clinical data, Other names ...

See also

References

  1. [1]
    Jørgensen AS, Jacobsen P, Christiansen LB, Bury PS, Kanstrup A, Thorpe SM, et al. (February 2000). "Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor". Bioorganic & Medicinal Chemistry Letters. 10 (4): 399–402. doi:10.1016/S0960-894X(00)00015-9. PMID 10714509.
  2. [2]
    Sharma V, Kumar V (2014). "Indolizine: a biologically active moiety". Medicinal Chemistry Research. 23 (8): 3593–3606. doi:10.1007/s00044-014-0940-1. ISSN 1054-2523. S2CID 2643469.
  3. [3]
    Wallace OB, Richardson TI, Dodge JA (2003). "Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity". Current Topics in Medicinal Chemistry. 3 (14): 1663–1682. doi:10.2174/1568026033451727. PMID 14683521.
  4. [4]
    Meegan MJ, Lloyd DG (January 2005). "Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators. Frontiers in Medicinal Chemistry-Online". In Atta-ur-Rahman, Reitz AB (eds.). Frontiers in Medicinal Chemistry. Vol. 2. Bentham Science Publishers. pp. 183–231 (206). ISBN 978-1-60805-205-9.
  5. [5]
    "NNC 450095". AdisInsight. Springer Nature Switzerland AG.


Stub icon

This drug article relating to the genito-urinary system is a stub. You can help Wikipedia by expanding it.
Share this article:

This article uses material from the Wikipedia article NNC_45-0095, and is written by contributors. Text is available under a CC BY-SA 4.0 International License; additional terms may apply. Images, videos and audio are available under their respective licenses.