bardoxolone

Action and Spectrum

Actions and Spectrum: 

bardoxolone activates a transcription factor called Nrf2, which is involved in regulating the expression of genes that protect cells from oxidative stress and inflammation. By activating Nrf2, bardoxolone helps to reduce inflammation and improve cellular function in the kidneys and other organs. 

The spectrum of bardoxolone’s actions is primarily focused on the kidneys and other organs affected by chronic kidney disease. Bardoxolone has been shown to improve kidney function and decrease proteinuria (excess protein in the urine) in patients with type 2 diabetes and chronic kidney disease. 

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

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 available 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:  

bardoxolone has been studied for its potential therapeutic effects in various medical conditions, including chronic kidney disease, pulmonary arterial hypertension, and diabetic nephropathy. It is believed to work by reducing inflammation, improving mitochondrial function, and promoting cell survival. 

Pharmacodynamics: 

In particular, bardoxolone has shown promising results in improving kidney function in patients with chronic kidney disease, including those with type 2 diabetes. It has been studied in clinical trials as a potential treatment for various stages of chronic kidney disease, with some studies showing significant improvement in kidney function and a reduction in the need for dialysis or kidney transplantation. 

Pharmacokinetics: 

Absorption  

bardoxolone is administered orally, and its absorption occurs in the gastrointestinal tract. After oral administration, the medication is absorbed quickly and reaches its peak concentration in the blood within 1-2 hours.  

Distribution  

bardoxolone is distributed throughout the body and has a large volume of distribution. It binds to plasma proteins such as albumin and is distributed into tissues, including the liver, kidney, and lungs.  

Metabolism  

bardoxolone is metabolized in the liver by the cytochrome P450 enzyme system, primarily by the CYP1A1 and CYP1B1 enzymes. The primary metabolites of bardoxolone are less active than the parent compound.  

Elimination and Excretion  

bardoxolone and its metabolites are excreted primarily in the feces and to a lesser extent in the urine. The elimination half-life of bardoxolone is approximately 4-6 hours.

Adminstartion

Administration:  

bardoxolone is a medication used to treat chronic kidney disease in patients with type 2 diabetes. The administration of bardoxolone should always be under the guidance of a healthcare professional, as they will determine the appropriate dosage and frequency of administration based on your individual medical condition and other factors. 

bardoxolone is taken orally, usually with food, and should be swallowed whole. The dosage and frequency of administration will vary depending on the medical condition being treated, the patient’s age, weight, and overall health, and other factors. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: bardoxolone (Pending FDA Approval) 

Why do we use bardoxolone? 

bardoxolone (Pending FDA Approval) is used to treat chronic kidney disease in patients with type 2 diabetes. Chronic kidney disease is a long-term condition that can cause damage to the kidneys and eventually lead to kidney failure. Type 2 diabetes is a common cause of chronic kidney disease.