ILAPRAZOLE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C19H18N4O2S
Molecular Weight	366.437
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC=NC(C[S+]([O-])C2=NC3=C(N2)C=CC(=C3)N4C=CC=C4)=C1C

InChI

InChIKey=HRRXCXABAPSOCP-UHFFFAOYSA-N

InChI=1S/C19H18N4O2S/c1-13-17(20-8-7-18(13)25-2)12-26(24)19-21-15-6-5-14(11-16(15)22-19)23-9-3-4-10-23/h3-11H,12H2,1-2H3,(H,21,22)

HIDE SMILES / InChI

Molecular Formula	C19H18N4O2S
Molecular Weight	366.437
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11304936 | https://www.ncbi.nlm.nih.gov/pubmed/11215326 | http://www.drugsupdate.com/generic/view/1243 | http://eng.dailypharm.com/News/news_view.html?ID=362 | https://www.ncbi.nlm.nih.gov/pubmed/28388576 | http://www.pharmalink.kr/detailinfo.php?code=20081068801

Ilaprazole or IY-81149 (2-[(4-methoxy-3-methyl)-2-pyridinyl]methylsulfinyl -5-(1H-pyrrol-1-yl)-1H-benzimidazole, CAS 172152-36-2) is a proton pump inhibitor. Ilaprazole revealed the characteristics as a strong proton pump inhibitor, and its potency against gastric acid secretion was superior to that of the reference drug, omeprazole. Ilaprazole is approved in China and South Korea for the treatment of gastroesophageal reflux disorders (GERD), dyspepsia and peptic ulcers. Recently it was discovered that ilaprazole inhibited the cancer growth by targeting T-cell-originated protein kinase (TOPK) both in vitro and in vivo.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sodium/potassium-transporting ATPase 34 Target ID: CHEMBL2095186 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11304936	Inhibitor 8504		6.0 µM [IC50]
PDZ-binding kinase 2 Target ID: CHEMBL4896 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28388576	Inhibitor 8504		111.0 µM [Kd]

Conditions

Condition	Modality	Highest Phase	Product
Colon cancer 66 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28388576	Primary	Preclinical	Unknown Approved Use Unknown
Gastroesophageal reflux disease 68 Sources: http://adisinsight.springer.com/drugs/800010706	Primary	Approved 8583	Noltec Approved Use Ilaprazole is used for the treatment of gastroesophageal reflux disorders (GERD), dyspepsia and peptic ulcers. Launch Date 2007
Peptic ulcer 72 Sources: http://adisinsight.springer.com/drugs/800010706	Primary	Approved 8583	Noltec Approved Use Ilaprazole is used for the treatment of gastroesophageal reflux disorders (GERD), dyspepsia and peptic ulcers. Launch Date 2007

C_max

Value	Dose	Analyte	Population
305 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
293 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
565 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
638 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1103 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1114 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
834.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
836.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
482.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
834.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1718.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
347.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
497.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
464.25 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
844.01 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
824.62 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1848.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1570.48 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
2051 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2092 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3948 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4463 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7630 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7918 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2774.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2654.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1754.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3562.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7056.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1984.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2010.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1462.49 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3940.26 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
3184.85 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8042.04 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
5930.34 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
4.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25041486/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27067231/	10 mg 1 times / day steady-state, intravenous dose: 10 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.56 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
2.93 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
3.22 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.36 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
2.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26998954/	20 mg single, intravenous dose: 20 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ILAPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
20 mg single, intravenous Highest studied dose Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/	Other AEs: Activated partial thromboplastin time increased, Prothrombin time increased... Other AEs: Activated partial thromboplastin time increased (grade 1) Prothrombin time increased (grade 1) Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/
40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	Disc. AE: Rash... Other AEs: Erythema, Headache... AEs leading to discontinuation/dose reduction: Rash (3%) Other AEs: Erythema (9%) Headache (3%) Pruritus (6%) Abdominal distension (3%) Epistaxis (6%) Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/

AEs

AE	Significance	Dose	Population
Activated partial thromboplastin time increased	grade 1	20 mg single, intravenous Highest studied dose Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/
Prothrombin time increased	grade 1	20 mg single, intravenous Highest studied dose Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/26998954/
Abdominal distension	3%	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/
Headache	3%	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/
Rash	3% Disc. AE	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/
Epistaxis	6%	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/
Pruritus	6%	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/
Erythema	9%	40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25041486/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193	substrate 1388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	CYP2E1 729 CYP2B6 776 CYP2C19 1119 CYP2A6 626 CYP3A5 446 CYP1A2 1197 CYP2C8 810

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	likely
CYP2B6 776	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	likely
CYP2E1 729	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	likely
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/19701234/ \| https://pubmed.ncbi.nlm.nih.gov/22022918/	major
CYP2C19 1119	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/19701234/ \| https://pubmed.ncbi.nlm.nih.gov/22022918/	minor
CYP2A6 626	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	no
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	no
CYP2C9 1193	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	no
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/22022918/	no
CYP3A5 446	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/19701234/ \| https://pubmed.ncbi.nlm.nih.gov/22022918/	yes

PubMed

Title	Date	PubMed
Comparison of IY81149 with omeprazole in rat reflux oesophagitis.	2000 Oct-Dec	11350494
The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study.	2014 Sep	25041486
Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase.	2017 Jun 13	28388576

Patents

Sample Use Guides

In Vivo Use Guide

Short-term treatment of duodenal ulcer: Normally, 10 mg of adult is administered orally once a day. It is usually administered for up to 4 weeks. Short-term treatment of gastric ulcer: Normally, an adult dose of 10 mg is orally administered once a day. It is usually administered for 4 to 6 weeks. This medicine should be swallowed with water 1 hour before meals and should not be chewed or crushed. The recommended adult dosage of Ilaprazole is 5-20 mg/day.

Route of Administration: Oral

In Vitro Use Guide

Ilaprazole exhibited potent inhibitory activities against the growth of HCT116 cells (IC50 = 40 uM) and ES-2 cells (IC50 = 33.2 uM). Ilaprazole (100 and 50 uM) induces apoptosis in ES-2 and HCT116 cells.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:16:53 GMT 2025` Edited by `admin` on `Mon Mar 31 18:16:53 GMT 2025`
Record UNII	776Q6XX45J
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NOLTEC

Preferred Name

English

ILAPRAZOLE

Official Name

English

Ilaprazole [WHO-DD]

Common Name

English

IY-81149

Systematic Name

English

ilaprazole [INN]

Common Name

English

2-((RS)-((4-METHOXY-3-METHYLPYRIDIN-2-YL)METHYL)SULFINYL)-5-(1H-PYRROL-1-YL)-1H-BENZIMIDAZOLE

Systematic Name

English

ILAPRAZOLE [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29723