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.
LDN (Low Dose Naltrexone)
Naltrexone Hydrochloride (low dose)
Brand names: ReVia, Vivitrol (standard dose — must be compounded at low dose)
ORIGINALLY APPROVED FOR
Opioid/Alcohol Addiction (at standard 50 mg dose)
At doses of 1.5–4.5 mg (vs. the standard 50 mg), naltrexone transiently blocks opioid receptors for a few hours each night, causing a rebound overproduction of endogenous opioids (endorphins and met-enkephalin). This pulsed OGF (opioid growth factor) surge modulates the immune system profoundly — boosting NK cell activity, IL-12, and anti-tumour surveillance. Clinical evidence is growing for several cancers, with strongest data in pancreatic cancer and multiple myeloma.
Molecular Pathways Targeted
Mechanism of Action in Cancer
Transient nightly OGF receptor blockade → rebound upregulation of endogenous opioid growth factor → inhibits cell proliferation. Also reduces TLR4 microglial activation (anti-inflammatory) and boosts NK cell cytotoxicity against tumour cells.
Cancers Studied
Typical Off-Label Dosing
1.5–4.5 mg taken at bedtime (9–11 PM), typically as a compounded capsule or liquid. Must NOT be combined with opioid medications. Start at 1.5 mg and increase by 0.5 mg every 2 weeks.
* Dosing information from research literature only. Not a prescription. Requires physician supervision.
Cautions & Drug Interactions
- MUST NOT be used with opioid pain medications — will precipitate withdrawal
- Must be compounded — standard tablets are 50 mg and cannot be split accurately
- Vivid dreams or insomnia in first 2–4 weeks — often resolves
- May interfere with immunosuppressants
- Avoid in autoimmune conditions on biologic therapy without specialist review
- Not FDA-approved for cancer — off-label use only