Ilaprazole: A New Height in Acid Suppression, A New Hope for Gastric Diseases

Peptic ulcer disease is a common chronic condition of the digestive system, characterized by ease of diagnosis and treatment, but also a tendency for recurrence. There are various treatment options available, including antacids, gastric mucosal protectants, H2 receptor antagonists, proton pump inhibitors (PPIs), and traditional Chinese medicine. Among these, PPIs are currently the most potent acid suppressants, with the best clinical efficacy and the widest application, holding over 90% of the market share.

Ilaprazole is a PPI that belongs to the class of irreversible proton pump inhibitors and is structurally classified as a benzimidazole.

After oral administration, Ilaprazole selectively enters the gastric parietal cells and is converted into a sulfenamide active metabolite. This active metabolite covalently binds to the thiol group on the H+/K+-ATPase, forming a disulfide bond, thereby irreversibly inhibiting the H+/K+-ATPase and suppressing gastric acid secretion.

Drug Functionality

1. As a new type of PPI, Ilaprazolehas distinct pharmacological and pharmacokinetic properties compared to other PPIs due to the different substituents on its pyrazole and benzimidazole rings. Its longer half-life allows for prolonged efficacy, making it effective in preventing nighttime acid breakthrough. Its metabolism in the human body is not affected by the polymorphism of the CYP2C19 gene. Compared to other PPIs, Ilaprazolehas the advantage of a different metabolic pathway. It does not metabolize through the CYP2C19 pathway, generally avoiding competition for receptors with many cardiovascular drugs, thus maintaining its efficacy, which is particularly advantageous in treating patients with cardiovascular diseases.

2. In clinical applications, whether used alone or in combination with antibiotics for the treatment of peptic ulcers, Ilaprazoleconsistently outperforms control drugs. Its clinical advantages include minimal dosage, a significantly prolonged half-life compared to other PPIs, strong acid suppression activity, minimal individual variability, and fewer drug interactions.

Drug Advantages

1.Prolonged Efficacy: Ilaprazole has a half-life of 3-4 hours, with gastric acid suppression lasting 17-23 hours, requiring only once-daily dosing.

2.Minimal Dosage: The standard dosage of Ilaprazole is 10 mg once daily, lower than the recommended 20 mg for omeprazole.

3.Minimal Individual Variability: Ilaprazole is metabolized through non-hepatic pathways, reducing dependence on liver CYP450 enzymes and effectively minimizing individual variability.

4.Fewer Drug Interactions: Ilaprazole's metabolism does not rely on hepatic enzymes, having no impact on their activity, and significantly reducing the incidence of interactions with other drugs or food compared to omeprazole.

5.Different Metabolic Pathway: Ilaprazole does not metabolize through the CYP2C19 pathway, avoiding receptor competition with cardiovascular drugs and maintaining efficacy, making it more advantageous in treating patients with cardiovascular diseases.

Applicable Populations

1. Patients with gastroesophageal reflux disease or duodenal ulcers: Ilaprazoleenteric-coated tablets can be used for the treatment of these conditions.
2. Patients with bleeding peptic ulcers: Injectable Ilaprazolesodium is suitable for treating bleeding peptic ulcers.
3. Patients with Helicobacter pylori infection: Ilaprazolecan be used in combination with antibiotics to enhance antibacterial effects and improve the eradication rate of Helicobacter pylori (Hp).
4. Patients with stress ulcers: Ilaprazolecan be used to prevent and treat stress ulcers, as well as peptic ulcers or bleeding caused by non-steroidal anti-inflammatory drugs and antiplatelet medications.