Английская Википедия:Dinaciclib

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Шаблон:Short description Шаблон:Infobox drug

Dinaciclib (SCH-727965) is an experimental drug that inhibits cyclin-dependent kinases (CDKs).[1] It is being evaluated in clinical trials for various cancer indications.[2]

Dinaciclib is being developed by Merck & Co. It was granted orphan drug status by the FDA in 2011.[3]

Mechanisms of action

Anti-tumoral action

  • In melanoma
    • The anti-melanoma activity of dinaciclib is dependent on p53 signaling.[6]
  • In chronic lymphocytic leukemia (CLL)
    • Dinaciclib promotes apoptosis and abrogates microenvironmental cytokine protection in chronic lymphocytic leukemia cells.[7]
  • In pancreatic cancer
  • In osteosarcoma
    • Dinacliclib induces the apoptosis of osteosarcoma cells.[9]
    • Apoptosis of osteosarcoma cultures can be induced by the combination of the cyclin-dependent kinase inhibitor SCH727965 and a heat shock protein 90 inhibitor.[10]


Role in developing neurons

In primary cultured neurons, dinaciclib regulates neurogenesis, where it reduces expression of upper layer marker Satb2, and induces CTIP2, expressed in neurons of deeper layers.[11]

Clinical trials

  • Phase II
    • Advanced breast cancer[12]
    • Non-small cell lung cancer (NSCLC)[13]
    • Multiple myeloma[14]
    • Advanced melanoma[15]
  • Phase III
    • A comparison of dinaciclib and ofatumumab for treatment of CLL[16]

References

Шаблон:Reflist

External links