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Everolimus

Afinitor

mTOR inhibitor (rapalog)

Evidence Score

55

preclinical
Mechanism of Action

Binds FKBP12 to form a complex that inhibits mTORC1, blocking downstream signaling including S6K1 and 4E-BP1. Reduces cell growth, proliferation, and angiogenesis. Rationale in SDH-deficient tumors comes from metabolic reprogramming-driven mTOR activation.

Pathway Connections
mTOR / PI3K / AKT

Metabolic reprogramming from SDH loss activates the PI3K/AKT/mTOR signaling axis, promoting cell growth, proliferation, and survival. Multiple upstream inputs converge on mTOR.

Upstream event:

HIF-mediated growth factor signaling + metabolic stress + AMPK dysregulation

Downstream effects:

Cell growth and proliferationProtein synthesisMetabolic reprogrammingSurvival signaling
Molecular Targets

MTOR

Mechanistic target of rapamycin

downstream

Central growth/metabolism regulator activated downstream of SDH loss. Target of everolimus and temsirolimus.

UniProt: P42345

Quick Facts
FDA Approved

Approved Indications

  • Advanced renal cell carcinoma
  • Pancreatic neuroendocrine tumors
  • Breast cancer (HR+/HER2-)
  • Tuberous sclerosis complex
ChEMBL IDCHEMBL1237021
PubChem CID6442177
Evidence

Evidence from PubMed, OpenTargets, and ChEMBL will appear here once external data integration is enabled.

Coming in Phase 3

AI Analysis

Have Claude analyze this drug's repurposing potential for SDH-deficient diseases.