Itraconazole

Inhibits fungal CYP51 (lanosterol 14α-demethylase), blocking ergosterol synthesis and destabilizing the fungal membrane.

AntimicrobialAntimicrobial actionEnzyme inhibition

Primary Mechanism of Action

Clinical / Scientific

Itraconazole binds fungal lanosterol 14α-demethylase (CYP51), preventing conversion of lanosterol to ergosterol. Membrane sterol depletion and accumulation of methylated sterols impair membrane function in susceptible fungi. It is also a potent human .

Pathway Targets

CYP51 (lanosterol 14α-demethylase)

Scientific explanation

Blockade of ergosterol biosynthesis.

CYP3A4

Scientific explanation

Host inhibition relevant to drug–drug interactions, not antifungal efficacy.

Pathway Convergence

Clinical / Scientific

Target → pathway → downstream effect → biological consequence. This is a mechanistic map, not a treatment claim.

Membrane sterol failure

Target to downstream effect: CYP51 inhibition → Ergosterol depletion → Fungal membrane dysfunction

CYP51 inhibition
↓
Ergosterol depletion
↓
Fungal membrane dysfunction

Mechanistically Relevant Repurposed & Adjunctive Applications

Susceptible fungal infections

Established

Mechanistic rationale

Established systemic azole for labelled susceptible mycoses.

Mechanistic Application Matrix

Biological TargetMechanismPotential RelevanceEvidence Level
Fungal CYP51InhibitionErgosterol synthesisEstablished mechanism
Human CYP3A4InhibitionPharmacokinetic interactionsEstablished mechanism

Mechanistic Interaction Considerations

Strong inhibition creates many serious interaction risks (including some QT-prolonging and immunosuppressant drugs). Use labelled interaction tables; this page does not list a complete contraindication set.

In Plain Language

Itraconazole stops fungi from making ergosterol, the sterol they need in their membranes — similar to how humans need cholesterol in cell membranes.

Compounds Sharing Pathways

Other library compounds whose structured pathway data overlap this ingredient. Shared pathways are not combination recommendations.

CYP51 (lanosterol 14α-demethylase)

Oncology Mechanistic Relevance

Cancers in the atlas where this compound has a mapped mechanistic rationale. Evidence tiers are not equivalent and do not imply treatment.

Lung cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Non-small-cell lung cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

MesotheliomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Gastric cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Hepatocellular carcinomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

CholangiocarcinomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Ovarian cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Prostate cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Castration-resistant prostate cancerEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Kidney / renal cell carcinomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

GlioblastomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

KIT-associated melanomaEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Skin cancersEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Head and neck cancersEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Neuroendocrine tumorsEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

SarcomasEarly Clinical · In Vivo · In Vitro

Hedgehog antagonism and anti-angiogenic endothelial reports exist, including early clinical probes. Not a licensed antineoplastic.

Mechanistic information is provided for scientific and educational purposes. Discussion of biological pathways or investigational applications does not establish clinical efficacy or constitute individualized medical advice.