恩瑞格作用功效

(deferasirox) is the only oral iron ion chelator developed by Novartis. So, how effective is Enrig?

Deferasirox is the first oral iron-removing agent approved by the U.S. FDA for routine use. It is approved for use in patients ≥2 years old with chronic iron overload caused by blood transfusion. In Europe, it is recommended as a first-line drug for patients with thalassemia iron overload over 6 years old.

Phase II and III clinical trials and pharmacokinetic studies have shown that it has good safety and tolerability, can significantly reduce iron load on the heart and liver, and is easily accepted by patients.

At the same time, deferasirox also has pharmaceutical properties such as antifungal (such as Mucor growing in an iron-rich environment), anti-cell proliferation, anti-malarial, anti-oxidative stress damage, anti-cytotoxic-induced apoptosis, etc.; it can be used for the treatment of secondary hemochromatosis, porphyria cutanea tarda and other diseases.

Pharmacology and toxicology of deferasirox:

1. Enrig is an oral active chelating agent that is highly selective with iron (Fe3+). It is a ligand with 3 protrusions that binds iron with high affinity in a 2:1 ratio.

2. Although the affinity of Enrige to zinc and copper is very low, the concentrations of these trace metals in the serum still decreased to varying degrees after administration. The clinical significance of these reductions in metal concentrations is unclear.

3. Repeated dose toxicity: The main findings in long-term toxicity studies are nephrotoxicity, bile duct changes and lens opacity (cataract). 

4. Reproductive toxicity, genotoxicity, and carcinogenicity: There is no evidence that daily oral doses up to 75 mg/kg (equivalent to 0.6 times the MRHD calculated in mg/m2) have adverse effects on the fertility and reproduction of male and female rats.