Clinical Development of Mammalian Target of Rapamycin Inhibitors

Hematol Oncol Clin North Am. 2002 Oct;16(5):1101-14. doi: 10.1016/s0889-8588(02)00051-5.

Abstract

Rapamycin and CCI-779 have significant in vitro and in vivo anti-proliferative activity against a broad range of human tumor cell lines, justifying the clinical evaluation of this class of agent in cancer patients. Preliminary results from phase I studies of CCI-779 suggest that the agent is well tolerated and has anti-tumor activity. The challenge to investigators is to efficiently determine what role this class of agent will play in the treatment of cancer patients.

Publication types

  • Review

MeSH terms

  • Adaptor Proteins, Signal Transducing
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Carrier Proteins / physiology
  • Cell Cycle Proteins
  • Cell Division / drug effects
  • Clinical Trials as Topic
  • Cyclic AMP-Dependent Protein Kinases / physiology
  • Drug Design
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Eukaryotic Initiation Factors
  • Everolimus
  • Humans
  • Immunosuppressive Agents / pharmacology*
  • Immunosuppressive Agents / therapeutic use
  • Mice
  • Neoplasm Proteins / antagonists & inhibitors
  • Neoplasm Proteins / physiology
  • Neoplasms / drug therapy
  • Phosphatidylinositol 3-Kinases / physiology
  • Phosphoproteins / physiology
  • Phosphorylation / drug effects
  • Protein Kinase Inhibitors*
  • Protein Kinases / physiology
  • Protein Processing, Post-Translational / drug effects
  • Ribosomal Protein S6 Kinases, 70-kDa / physiology
  • Signal Transduction / drug effects
  • Sirolimus / analogs & derivatives*
  • Sirolimus / pharmacology*
  • Sirolimus / therapeutic use
  • TOR Serine-Threonine Kinases
  • Xenograft Model Antitumor Assays

Substances

  • Adaptor Proteins, Signal Transducing
  • Antineoplastic Agents
  • Carrier Proteins
  • Cell Cycle Proteins
  • EIF4EBP1 protein, human
  • Eif4ebp1 protein, mouse
  • Enzyme Inhibitors
  • Eukaryotic Initiation Factors
  • Immunosuppressive Agents
  • Neoplasm Proteins
  • Phosphoproteins
  • Protein Kinase Inhibitors
  • temsirolimus
  • Everolimus
  • Protein Kinases
  • MTOR protein, human
  • TOR Serine-Threonine Kinases
  • mTOR protein, mouse
  • Ribosomal Protein S6 Kinases, 70-kDa
  • Cyclic AMP-Dependent Protein Kinases
  • Sirolimus