iOnco
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This information is for educational purposes only. Off-label drug use carries risks. Always consult a qualified physician before using any drug outside its approved indication.

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Metformin

Metformin Hydrochloride

Brand names: Glucophage, Glumetza, Fortamet

BiguanideMetabolicstrong evidenceActive Clinical Trials

ORIGINALLY APPROVED FOR

Type 2 Diabetes

Metformin is the world's most prescribed diabetes drug and the most studied repurposed drug in oncology. It activates AMPK, which inhibits mTOR — the master regulator of cell growth and metabolism. Epidemiological studies consistently show diabetic patients on metformin have 20–40% lower cancer incidence and better survival outcomes. Over 100 clinical trials are currently investigating its role in cancer prevention and treatment.

Molecular Pathways Targeted

AMPKmTORHIF-1αNF-κBIGF-1

Mechanism of Action in Cancer

Inhibits mitochondrial complex I → reduces ATP → activates AMPK → suppresses mTOR signalling → slows cancer cell proliferation. Also reduces circulating insulin and IGF-1, which are tumour-promoting hormones. May selectively kill cancer stem cells.

Cancers Studied

BreastColorectalProstateLungOvarianPancreaticEndometrial

Typical Off-Label Dosing

500–2000 mg daily (standard diabetes dosing). Some protocols use 1000–1500 mg. Must be taken with food to reduce GI side effects. Not suitable for non-diabetics without physician supervision.

* Dosing information from research literature only. Not a prescription. Requires physician supervision.

Cautions & Drug Interactions

  • Not recommended in severe kidney impairment (eGFR < 30)
  • Risk of lactic acidosis — rare but serious
  • Avoid before contrast dye procedures — hold 48 hours
  • Can cause GI upset, nausea, diarrhoea — start low and titrate
  • Depletes B12 over time — monitor levels annually
  • Only use off-label under physician supervision
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