betulinic acid

Action and Spectrum

Actions and Spectrum: 

Anticancer Properties: 

• Apoptosis Induction: betulinic acid has been found to induce apoptosis (programmed cell death) in cancer cells. It can trigger multiple pathways leading to apoptosis, making it a potential candidate for cancer therapy. 
• Mitochondrial disruption: betulinic acid can disrupt mitochondrial function in cancer cells, leading to the release of cytochrome c and activation of caspases, key components of the apoptotic pathway. 
• NF-κB Pathway Inhibition: betulinic acid may inhibit the nuclear factor-kappa B (NF-κB) pathway, which is involved in the regulation of inflammation and cell survival. Inhibition of NF-κB can contribute to the suppression of cancer cell growth. 

Anti-inflammatory Effects: 

• betulinic acid has shown anti-inflammatory properties by inhibiting inflammatory mediators, such as prostaglandins and cytokines. This may contribute to its potential in managing inflammatory conditions. 

Antiviral Activity: 

• betulinic acid has demonstrated antiviral activity against various viruses, including HIV. It interferes with viral entry into host cells and inhibits the replication of the virus. 

Antioxidant Activity: 

• betulinic acid exhibits antioxidant properties, helping to neutralize reactive oxygen species (ROS) and protect cells from oxidative stress. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Headache 

Vomiting 

Diarrhea 

Black Box Warning

None 

Contraindication / Caution

betulinic acid is primarily studied in preclinical models, and while it shows promise in various areas, including anticancer and antiviral activities, comprehensive clinical data on its safety profile, contraindications, and potential interactions in humans are limited. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

betulinic acid exhibits diverse pharmacological activities with potential therapeutic implications. It induces programmed cell death (apoptosis) in cancer cells through caspase activation and mitochondrial disruption. It also hinders cell survival and inflammation by inhibiting the NF-κB signaling pathway, contributing to the suppression of cancer cell growth. Additionally, betulinic acid displays antiangiogenic effects, limiting the formation of new blood vessels in tumors. Its antiviral activity, particularly against HIV, involves interference with the viral life cycle, making it a candidate for antiretroviral therapy. 

Pharmacokinetics: 

N/A

Adminstartion

Administration: 

Topical administration 

It is topically administered. betulinic acid was primarily studied in preclinical research, and its clinical use was still in the early stages of development.

Patient Information Leaflet

Patient information leaflet 

Generic Name: betulinic acid 

Why do we use betulinic acid? 

betulinic acid, a naturally occurring triterpenoid, has been studied for various potential therapeutic applications due to its diverse pharmacological properties. 

• Anticancer Activity: It acts through multiple pathways, including mitochondrial disruption and caspase activation. Studies have explored its potential in different types of cancer, such as  breast cancer, lung cancer, and more. 
• Anti-inflammatory Effects: It exhibits the anti-inflammatory properties by inhibiting the production of the inflammatory mediators, including prostaglandins and cytokines. This suggests its potential in managing inflammatory conditions. 
• Antiviral Activity: It has demonstrated antiviral activity against HIV by interfering with the maturation of the virus. It has been explored as a potential candidate for antiretroviral therapy.