Pharm

Mammalian Target of Rapamycin Inhibitor

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

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
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

See Cytochrome P-450 3A4
Agents that increase Purine Synthesis Inhibitor concentrations
1. Linezolid potentiates myelosuppression
2. Erythromycin (and Clarithromycin to a lesser extent)
Agents that decrease Purine Synthesis Inhibitor concentrations
1. Rifampin