Itraconazole †Rx

Repurposed antifungal: Hedgehog inhibitor, anti-angiogenic, CYP3A4 modulator; active in prostate/NSCLC/BCC.

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👥⭐⭐⭐ Moderate — Supported by preclinical studies and phase I/II trials; larger RCTs needed.SporanoxITZOrungalTolsura

Forms: Oral capsules (100 mg) · Oral solution (10 mg/mL)

Educational only, not medical advice. OncoForge makes no claim that Itraconazole †Rx treats, prevents, or cures any condition, beyond what the linked studies show. Evidence levels vary; effects may not translate to people, and some compounds can cause harm. Always coordinate with your oncology team.

Key Takeaway

Antifungal with oncology repurposing signals: inhibits SMO→Gli (Hedgehog), exerts anti-angiogenic effects, and is a potent CYP3A4 inhibitor (PK booster). Phase I/II data show activity in select settings (e.g., prostate, NSCLC, BCC) though not yet standard of care.

Evidence at a glance

Tier 2 · animalProstateNSCLCBasal Cell CarcinomaPancreaticColorectalOvarian

Preclinical mechanistic support; phase I/II clinical signals in prostate, lung, skin cancers; synergies observed with chemo.

How it may work

Itraconazole (ITZ), an antifungal, inhibits the Hedgehog pathway by blocking Smoothened (SMO) activation, reducing Gli transcription factors and tumor proliferation. It exerts anti-angiogenic effects by suppressing VEGF and endothelial cell migration, and inhibits CYP3A4, potentially enhancing chemotherapy efficacy. ITZ also induces autophagy, cell cycle arrest, and apoptosis while reversing multidrug resistance. Clinical trials show benefits in prostate, lung, and basal cell carcinoma.

Targets & pathways

Curated mechanistic targets reported for this agent — how it may act on cells, not proof of a clinical effect.

Hedgehog↓SMO activation block → Gli ↓
Angiogenesis↓VEGF suppression and endothelial migration ↓
CYP3A4↓Inhibition enhances substrate drug levels
Autophagy↑Induces autophagic growth arrest
Apoptosis↑Cell death induction
Multidrug Resistance↓Reverses P-gp mediated resistance

HedgehogAngioCYP3A4

Often studied / combined with

Combinations reported in the literature, not a protocol or a recommendation.

Docetaxel: Enhanced PSA responses in metastatic prostate cancer.
Paclitaxel: Synergistic antitumor effects in colorectal/ovarian models.
Pemetrexed: Improved efficacy in NSCLC xenografts.
5-FU: Inhibits gastric cancer proliferation.
Hydroxychloroquine: Potent antitumor via lysosomal disruption.

Overlapping mechanisms

Hedgehog: Potential overlap with vismodegib/sonidegib; monitor for additive toxicity.
Angiogenesis: May amplify effects/toxicity with other anti-VEGF agents.

Safety & interactions

Severity and how well-established each signal is are shown separately. Verify everything with your oncologist or pharmacist — absence here does not mean safe.

Risk categories

HepatotoxicityQt ProlongationHeart FailureEdema

Potential interactions

CYP3A4 substratesContraindicate Or AdjustHighTheoreticalPotent inhibitor; increases levels of e.g., simvastatin, lovastatin, ergotamines, midazolam.
P-gp substratesMonitorModerateTheoreticalInhibits P-gp; may increase digoxin, etc.
RituximabCautionModerateTheoreticalMay impair anti-lymphoma efficacy.
HMG-CoA reductase inhibitors (statins)ContraindicateHighTheoreticalRhabdomyolysis risk.

Timing

With-meal: Enhances bioavailability.
BID: Divided doses for steady levels.

References

Research

No published studies for Itraconazole yet

New studies appear here once they’ve been reviewed. Browse all studies.

Dose: as studied, not a recommendation

These are doses as studied or reported, never a recommendation. The right amount of Itraconazole †Rx depends on you, your other medicines, and your situation; decide it with your oncology team and pharmacist, not from a web page.

Ranges seen in adjunct / practice use: 200–600 mg/day (po) divided BID; with food for better absorption, Cancer trials use 300-600 mg/day (e.g., 300 mg BID); adjust for interactions; monitor ECG/LFTs..

Trials studying Itraconazole †Rx

No actively-recruiting trials matched right now. Recruiting is not the same as proven. Search ClinicalTrials.gov →

Inclusion here is not an endorsement. OncoForge makes no claim beyond what the linked studies show. Discuss anything on this page with your oncology team before acting on it.

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