Mammalian Target of Rapamycin Inhibitor

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

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II. Indications

  1. Solid Organ Transplant Immunosuppression (maintenance prevention of rejection)
  2. Tuburous Sclerosis
  3. Cancer
    1. Renal Cell Carcinoma
  4. Ongoing research into mTOR Inhibitors as anti-aging drugs
    1. Resources
      1. Rapamycin (Peter Attia, Drive)
        1. https://peterattiamd.com/davidsabatini-mattkaeberlein/
    2. References
      1. Blagosklonny (2019) Aging 11(19):8048-67 +PMID: 31586989 [PubMed]
      2. Juricic (2022) Nat Aging 2(9):824-36 +PMID: 37118497 [PubMed]
      3. Lee (2024) Lancet Healthy Longev 5(2):e152-e162 +PMID: 38310895 [PubMed]

III. 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

IV. Medications

  1. Sirolimus (Rapamune, Rapamycin)
  2. Everolimus (Afinitor)
  3. Temsirolimus (Torisel)

V. Adverse Effects

  1. Hyperlipidemia
  2. Hepatic artery thrombosis
  3. Myelosuppression
  4. Pulmonary fibrosis
  5. Rash
  6. Delayed Wound Healing

VI. 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

VII. References

  1. Cimino (2016) Am Fam Physician 93(3): 203-10 [PubMed]
  2. Costanzo (2010) J Heart Lung Transplant 29(8): 914-56 [PubMed]

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Related Studies

Cost: Medications

sirolimus (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
SIROLIMUS 0.5 MG TABLET Generic $5.11 each
SIROLIMUS 1 MG TABLET Generic $4.36 each
SIROLIMUS 1 MG/ML SOLUTION Generic $8.60 per ml
SIROLIMUS 2 MG TABLET Generic $3.81 each
rapamune (on 1/1/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
RAPAMUNE 0.5 MG TABLET Generic $5.11 each
RAPAMUNE 1 MG TABLET Generic $4.36 each
RAPAMUNE 2 MG TABLET $66.73 each
everolimus (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
EVEROLIMUS 0.5 MG TABLET Generic $12.55 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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