Betulinic Acid

Triterpenoid inducing mitochondrial ROS-mediated apoptosis, angiogenesis inhibition, and immune modulation; strong preclinical anticancer signals with low toxicity.

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🔬⭐⭐ Low to Moderate — Strong preclinical data in ovarian and other cancers; nano-formulations in early trials, but limited human studies.MairinBetulic acidLupatic acid

Forms: Betulinic acid capsules or powder (10–100 mg)

Educational only, not medical advice. OncoForge makes no claim that Betulinic Acid 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.

Simple Summary

A triterpenoid from birch bark, betulinic acid collapses tumor mitochondria, spikes ROS, and reduces new blood-vessel growth. Preclinical work—especially in ovarian cancer—shows apoptosis and G2/M arrest, with hints of immune reprogramming (M2→M1). Delivery tech (nanoformulations) is being explored to improve exposure.

Evidence at a glance

Tier 2 · animalOvarianProstateMelanomaBreastLungLiverNSCLCPancreatic

Low to Moderate — Robust in vitro/in vivo data; early nano-trials, but few human studies.

How it may work

Betulinic acid induces mitochondrial apoptosis through a ROS burst, cytochrome c release, and caspase activation. It inhibits angiogenesis by downregulating VEGF and suppresses topoisomerase I/II, leading to DNA damage. In ovarian cancer models, it promotes apoptosis and cell cycle arrest at G2/M phase by upregulating metallothionein 1G. It also reprograms tumor-associated macrophages from M2 (pro-tumor) to M1 (anti-tumor) phenotype, reducing immunosuppression in the tumor microenvironment.

Targets & pathways

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

Mitochondrial Apoptosis↑Via ROS burst, cytochrome c release, caspase activation
ROS Production↑
Angiogenesis↓Downregulation of VEGF
DNA Damage↑Via topoisomerase I/II inhibition
Cell Cycle Arrest↑At G2/M phase
Macrophage ReprogrammingModulationM2 to M1 phenotype

MitoROSAngiogenesis

Often studied / combined with

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

Sorafenib: Enhanced inhibition in NSCLC.
EGFR-TKIs (e.g., Gefitinib): Synergistic anti-tumor in lung cancer.
Irradiation: Potentiates effects in melanoma.
Mithramycin A: Suppresses pancreatic cancer growth.

Overlapping mechanisms

ROS ↑: Caution with other ROS inducers to avoid excessive oxidative stress.

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

Gi Upset MildAllergic ReactionsHepatotoxicity RiskLow Bioavailability

Potential interactions

NSAIDs or anticoagulantsMonitorModerateTheoreticalMay increase risk of gastrointestinal bleeding.
CYP3A4 substratesMonitorMinorTheoreticalPotential for drug interactions due to metabolic pathways.
Chemotherapy (e.g., Cisplatin, Sorafenib)ConsiderBeneficialTheoreticalSynergistic anticancer effects in preclinical models.

Timing

Anytime: Daily dosing; timing flexible due to long half-life.
With food: To improve absorption and reduce GI upset.

References

Research

No published studies for Betulinic Acid 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 Betulinic Acid 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: 50–500 mg (po) Once daily. No established human anticancer dose; range based on HED from preclinical mouse studies (10–100 mg/kg → HED 0.8–8 mg/kg, ~50–480 mg for 60 kg adult) and dog studies (5 mg/kg → HED ~2.7 mg/kg, ~160 mg)., No Rx required, but oncology use experimental—consult clinician. Low bioavailability; nanoformulations may improve. Start low; monitor for GI effects..

Trials studying Betulinic Acid

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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