Ilaprazole:Korea Original Drug’s Rapid Growth in China by Livzon

Ilaprazole, a proton pump inhibitor drug, has rapid growth in China in 2020. Ilaprazole was first developed by developed by Il-Yang Pharmaceutical (Korea) in 2001. By cooperating with the originator, Livezon, one of the leading pharmaceutical company in China, successfully get marketing approval for iprazole API and iprazole enteric-coated tablets in 2007. Iprazole sodium for injection has approval in 2017 also, and is listed in the catalog of medicines covered by national medical insurance system in 2019 (with 40% price decrease).

Proton pump inhibitors are the main drugs for gastric acid-related diseases. The market size of anti-acid and anti-ulcer drugs is huge, of which gastric proton pump inhibitors account for around 40% of the share. The main marketed proton pump inhibitors in China include omeprazole, lansoprazole, esomeprazole, rabeprazole, pantoprazole and ilaprazole, among which omeprazole occupies over 5o% market share. Ilaprazole is small in scale now, but growing rapidly. Above studies have shown that the therapeutic effect of ilaprazole on peptic ulcers is not inferior or even better than the current proton pump inhibitors.

Livzon’s overall performance exceeded expectations due to the increased volume of ilaprazole in 2020. Sales volume of ilaprazole sodium for injection increased more than 400% and reaches 255 million Yuan ; the sales revenue of ilaprazole enteric-coated tablets was 408 million Yuan.

Introduction of ilaprazole products

API name:Ilaprazole

Finished Dosage Formulation name: Ilaprazole Enteric-Coated Tablets 5mg ; Ilaprazole Powder for Injection 10mg

Brands(s): Noltec, 壹丽安

Indication: Ilaprazole are use for stomach problems.  It is indicated for treatment of duodenal ulcer, reflux esophagitis(tablets) and peptic ulcer hemorrhage(powder for injection).

Dosage:

• For duodenal ulcer treatment (Ilaprazole Enteric-Coated Tablets): 5-10mg once daily for 4 weeks, or use it as directed by your doctor.
• For reflux esophagitis treatment(Ilaprazole Enteric-Coated Tablets): 10mg once daily for consecutive 4 weeks. It is recommended that an additional 4-week treatment is given to the patients who have not healed from the treatment; and dosage adjustment by using 5 mg of Ilaprazole daily for additional 4 weeks is recommended for the patients who have not healed but have persistent symptoms or use Ilaprazole as directed by the doctor.
• Intravenous drip(Ilaprazole Powder for Injection): the initial dose is 20mg, followed by 10mg of injection each time for three consecutive days. After the treatment course, oral medication may be given as appropriate.

Ilaprazole side effects

• Common: Diarrhea , headache and dizziness , abnormal liver function (increased ALT and AST) ,
• Rare: Skin rash, urticaria, low back pain, abdominal distension, dry mouth, bitter mouth, palpitations, chest tightness, prolonged menstrual time, abnormal urine routine (proteinuria), elevated urea nitrogen, abnormal electrocardiogram (ventricular premature contraction, first-degree atrioventricular block) Stagnation), abnormal blood routine (leukopenia)

Contraindications:

• People who are allergic to any ingredients in this medicine should not use it.
• People who are allergic to ilaprazole and other benzimidazole compounds should not use it.

Precautions:

• Ilaprazole Enteric-Coated Tablets should be swallowed, but cannot be chewed or crushed.
• This product has a strong inhibitory effect on gastric acid secretion. For general peptic ulcer and other diseases, it is not suitable to take long-term high-dose.
• Malignant lesions of the stomach and esophagus should be excluded before use to avoid delay in diagnosis due to relief of symptoms.
• Due to insufficient clinical research data for patients with liver and kidney dysfunction, use with caution in patients with liver and kidney dysfunction.
• Pay attention to the possible fracture risk for patients who take proton pump inhibitors for a long time.
• Patients who are using clopidogrel drugs should pay attention to the interaction with proton pump inhibitor drugs.

Ilaprazole mechanism of action

Ilaprazole is a proton pump inhibitor suppress gastric acid secretion is similar as omeprazole. It inhibits the parietal cell H+ / K+ ATP pump the secretory surfaces of gastric parietal cells by protonated substituted benzimidazoles, and suppress gastric acid secretion. ^[1] Kwon D, Chae JB, Park CW, Kim YS, Lee SM, Kim EJ, Huh IH, Kim DY, Cho KD. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo. … Continue reading

Preclinical studies shows that ilaprazole works well in preventing the development of reflux oesophagitis and gastric secretion in a dose-dependent manner with broad dose range and less side effects.

It is reported that the efficacy of ilaprazole to be similar to that of omeprazole by some clinical research. However, the report also mentions that the trials conducted were limited in numbers, so more trials need to be done in order to approve superiority of ilaprazole over the existing PPIs. ^[2]N P Bohidar, K Krishna, B K Panda, C Patel, Ilaprazole: Is this a superior proton pump inhibitor for duodenal ulcer? . Apr-Jun 2013;34(2):95-8. doi: 10.7869/tg.2012.105.