Spotlight on Low Dose Naltrexone

Mechanisms of Action

• Opioid Growth Factor (OGF)-OGF Receptor Axis: Temporarily blocks opioid receptors, triggering compensatory upregulation in endorphin (OGF) and OGF receptor (OGFr) production.
• Cell Cycle Regulation: OGF-OGFr binding inhibits cancer cell cycle progression via increased p16 and p21 cyclin-dependent kinase inhibitory pathways, slowing DNA replication and tumor cell proliferation.
• Immunomodulation: Promotes maturation and activation of dendritic cells, increases NK and CD8+ cytotoxic T-cell activity, and shifts macrophages toward a pro-inflammatory M1 phenotype, all amplifying antitumor immune surveillance.
• Inflammation and Angiogenesis Modulation: Reduces pro-inflammatory cytokine release (e.g., IL-6, TNF-α), inhibits angiogenesis, and corrects immune dysfunction across chronic inflammatory and autoimmune conditions.

Clinical Evidence

• Cancer: Preclinical and select clinical studies show LDN inhibits cell proliferation, promotes apoptosis, and enhances immunity in:
• Ovarian, colon, liver, pancreas, stomach, leukemia, head/neck, and breast cancers.
• Shown to augment tumor response and mitigate toxicity in combination with cisplatin and immunotherapies.
• Notably, long-term stabilization and survival reported in case series for metastatic and chemo resistant cancers.
• Chronic Pain & Autoimmune States: Reduces pain, inflammation, and improves function in fibromyalgia, multiple sclerosis, Crohn’s, and other disorders.
• General Profile: LDN is non-addictive, with few side effects (occasional vivid dreams, minor GI upset); generally well-tolerated in compounded, low-dose form (1–4.5mg).
• Compounding Required: Due to low-dose requirement, pharmacy compounding is necessary. Clinical experience is vital for dosing and monitoring individualized protocols.

Integrative Medicine Applications

• Synergy & Personalization: Supports immune and metabolic health, fits well with anti-inflammatory, detoxification, and mitochondrial recovery plans post-treatment.
• Chronic Pain and Cancer Survivorship: Useful in supportive care, especially when opioid-sparing or immune-enhancing effects are desired.
• Safety & Accessibility: Non-toxic and affordable; requires avoidance of opioid drugs to prevent interference.

References & Published Protocols

• Cancers 2024 (OGF/OGFr mechanism)
• Integr Cancer Ther 2007 (case report)
• LDN Research Trust
• ALA/LDN Protocol in pancreatic cancer
• McLaughlin PJ et al. Exp Biol Med 2011 Jul;236(7):883-95 (OGF/OGFr, ovarian)
• Berkson BM et al., Integr Cancer Ther. 2006;5 (1):83‐89 (pancreatic/adjuvant)
• LDNScience.org (how LDN works)

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For Healthcare Professionals

These materials are for informational and educational use in professional settings. Prescribers are encouraged to review primary literature and consult experienced integrative/functional medicine colleagues prior to initiating therapy. All compounds described remain investigational or off-label for oncologic indications and should be prescribed with patient consent, appropriate monitoring, and as part of a holistic, patient-centered plan.

Brand, Availability & Personalized Compounding

Skip’s Pharmacy stands ready to support your clinic in the safe, evidence-based use of repurposed medications for cancer and chronic disease care.

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Contact Skip’s Pharmacy to learn more about optimized, protocol-backed access to these therapies for your patients today.

This is for professional informational purposes only. Not intended as patient medical advice. All therapies should be supervised by a qualified healthcare provider.