roxadustat

Action and Spectrum

Actions and spectrum: 

Actions: 

It functions by lessening the breakdown of a transcription factor called hypoxia-inducible factor (HIF), which increases the synthesis of red blood cells in response to low oxygen levels. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Vascular access thrombosis 

Peripheral edema 

Hypertension 

Hyperkalemia 

Diarrhea 

Nausea 

Black Box Warning

Black Box Warning  

No specific black box warnings are available 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hypersensitivity 

Caution: 

It is known to activate a signaling protein called VEGF that promotes the growth of tumors. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not safe to use this drug in pregnancy 

Lactation:  

Data about the excretion of roxadustat into human milk has yet to be studied. 

Pregnancy category:  

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 was a lack of studies on pregnant women and no evidence of risk to the fetus 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 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: 

Roxadustat is a highly effective and reversible inhibitor of HIF-PHD enzymes. By inhibiting HIF-PHD, functional HIF accumulates, plasma endogenous EPO production rises, erythropoiesis is enhanced, and hepcidin—an iron regulator protein that is elevated during inflammation in chronic kidney disease—is indirectly suppressed. 

Pharmacodynamics: 

In patients with anemia, roxadustat dose-dependently enhances hemoglobin synthesis, red blood cell mass, and iron bioavailability. Roxadustat preserved Hb in anemia-stricken CKD patients not on dialysis for up to two years. In eliciting a Hb response, it is as effective as erythropoietin-stimulating drugs. Moreover, roxadustat lowers baseline cholesterol levels independent of the usage of statins or other lipid-lowering medications. 

Pharmacokinetics:  

Absorption 

AUC and Cmax for roxadustat plasma exposure raise dosage proportionately within the advised therapeutic dose range. When using roxadustat three times a week, steady-state plasma concentrations are reached after just one week (three doses) with little accumulation. In the fasting state, maximum plasma concentrations (Cmax) are typically reached two hours after dosage. When roxadustat was administered with meals, the Cmax was reduced by 25%, but the AUC remained unchanged when compared to the fasted condition. 

Distribution 

The steady-state volume of distribution apparently found is 24litres with a blood-to-plasma ratio of 0.6 

Metabolism 

Roxadustat is mainly metabolized to Roxadustat O-glucuronide and hydroxy-roxadustat, and the unchanged form circulates in the bloodstream. 

Elimination and excretion 

After oral administration, 50% of the drug is eliminated through feces and 46% through urine. About 28% of unchanged drugs are known to be eliminated through feces. 

Half-life: 

About 15 hours 

Adminstartion

Administration: 

To be administered as advised by the doctor 

Patient Information Leaflet

Patient information leaflet 

Generic Name: roxadustat  

Why do we use roxadustat? 

Roxadustat is a first-in-class HIF-PH inhibitory drug. It is indicated in the treatment of adult patients with symptomatic anemia related to chronic kidney disease (CKD), roxadustat is recommended.