Mammalian Target of Rapamycin Inhibitor


Mammalian Target of Rapamycin Inhibitor, mTOR Inhibitor, Sirolimus, Rapamune, Rapamycin, Everolimus, Afinitor, Temsirolimus, Torisel

  • See Also
  • Mechanism
  1. Mammalian Target of Rapamycin Pathway (mTOR Pathway)
    1. Mammalian Target of Rapamycin Protein (mTOR Protein)
      1. Serine-Threonine Kinase composed of a Protein complex (5-6 components) with 2 types (mTOR1, mTOR2)
      2. Regulates Protein synthesis in response to cellular stress
      3. Part of the PI3K/AKT pathway
    2. mTOR has multiple associated triggers in pathophysiology
      1. Cancer formation and Angiogenesis
      2. Insulin Resistance and Diabetes Mellitus
      3. Adipogenesis
      4. T-Lymphocyte activation
  2. mTOR Inhibitors
    1. Rapamycin (a Macrolide), and its analogs bind and inhibit mTOR
    2. Block the Serine-Threonine kinase receptor signaling
    3. Inhibit mRNA expression related to cell cycle progression and arrest cell in G1 phase
  • Medications
  1. Sirolimus (Rapamune, Rapamycin)
  2. Everolimus (Afinitor)
  3. Temsirolimus (Torisel)
  • Adverse Effects
  1. Hyperlipidemia
  2. Hepatic artery thrombosis
  3. Myelosuppression
  4. Pulmonary fibrosis
  5. Rash
  6. Delayed Wound Healing
  • Drug Interactions
  1. See Cytochrome P-450 3A4
  2. Agents that increase Purine Synthesis Inhibitor concentrations
    1. Linezolid potentiates myelosuppression
    2. Erythromycin (and Clarithromycin to a lesser extent)
  3. Agents that decrease Purine Synthesis Inhibitor concentrations
    1. Rifampin