Details of the Drug

General Information of Drug (ID: DM1DBV5)

• Drug Name: Dexlansoprazole
• Synonyms: dexlansoprazole; (R)-Lansoprazole; 138530-94-6; Kapidex; dexilant; R-(+)-LANSOPRAZOLE; Dexilant Solutab; TAK 390; UNII-UYE4T5I70X; TAK-390; (r)-(+)-lansoprazole; T 168390; UYE4T5I70X; AK170558; TAK-390MR; T-168390; 2-((R)-((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1H-benzimidazole; 2-[(R)-[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methylsulfinyl]-1H-benzimidazole; (R)-2-(((3-Methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methyl)sulfinyl)-1H-benzo[d]imidazole; Dexlansoprazole (INN/USAN); Kapidex; KS-1075; Lansoprazole

Indication

Disease Entry	ICD 11	Status	REF
Erosive esophagitis	DA25.0	Approved	[1]
Non-erosive gastro-esophageal reflux disease	DA22.0	Approved	[1]
Peptic ulcer	DA61	Approved	[2]
NSAID-associated gastric ulcer	DA60	Phase 3	[2]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 369.4
  Logarithm of the Partition Coefficient (xlogp); 2.8
  Rotatable Bond Count (rotbonds); 5
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 8
• ADMET Property:
  Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 3275 mcgh/L. []
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 688 mcg/L []
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 4 h []
  Half-life: The concentration or amount of drug in body reduced by one-half in 1 - 2 hours [3]
  Metabolism: The drug is metabolized via the liver []
  Vd: The volume of distribution (Vd) of drug is 40.3 L []
• Chemical Identifiers:
  Formula: C16H14F3N3O2S
  IUPAC Name: 2-[(R)-[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole
  Canonical SMILES: CC1=C(C=CN=C1C[S@@](=O)C2=NC3=CC=CC=C3N2)OCC(F)(F)F
  InChI: InChI=1S/C16H14F3N3O2S/c1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22)/t25-/m1/s1
  InChIKey: MJIHNNLFOKEZEW-RUZDIDTESA-N
• Cross-matching ID:
  PubChem CID: 9578005
  ChEBI ID: CHEBI:135931
  CAS Number: 138530-94-6
  DrugBank ID: DB05351
  TTD ID: D06YYD
  VARIDT ID: DR00643
  INTEDE ID: DR0469
  ACDINA ID: D00187
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gastric H(+)/K(+) ATPase (Proton pump)	TTLOKXP	ATP4A_HUMAN ; ATP4B_HUMAN	Modulator	[4]
Gastric H(+)/K(+) ATPase alpha (ATP4A)	TTF1QVM	ATP4A_HUMAN	Inhibitor	[5]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[6]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[7]
Mephenytoin 4-hydroxylase (CYP2C19) Main DME	DEGTFWK	CP2CJ_HUMAN	Substrate	[8]

Molecular Expression Atlas of This Drug

• The Studied Disease: Erosive esophagitis
• ICD Disease Classification: DA25.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Gastric H(+)/K(+) ATPase alpha (ATP4A)	DTT	ATP4A	1.42E-02	-0.15	-1.5
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.16E-04	-1.07E+00	-2.77E+00
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	5.51E-02	1.95E-01	1.20E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	3.90E-02	-3.45E-01	-1.49E+00

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Dexlansoprazole (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Vismodegib	DM5IXKQ	Minor	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Vismodegib.	Basal cell carcinoma [2C32]	[9]
Pexidartinib	DMS2J0Z	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[10]
HKI-272	DM6QOVN	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by HKI-272.	Breast cancer [2C60-2C6Y]	[9]
Bosutinib	DMTI8YE	Moderate	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Bosutinib.	Breast cancer [2C60-2C6Y]	[11]
Lumacaftor	DMCLWDJ	Moderate	Increased metabolism of Dexlansoprazole caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[12]
Brivaracetam	DMSEPK8	Minor	Decreased metabolism of Dexlansoprazole caused by Brivaracetam mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[13]
GS-5885	DMSL3DX	Moderate	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by GS-5885.	Hepatitis virus infection [1E50-1E51]	[9]
Rilpivirine	DMJ0QOW	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[14]
Raltegravir	DMYURI6	Minor	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Raltegravir.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Dacomitinib	DMOH8VY	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Dacomitinib.	Lung cancer [2C25]	[13]
Selpercatinib	DMZR15V	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Selpercatinib.	Lung cancer [2C25]	[13]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Dexlansoprazole caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[16]
Acalabrutinib	DM7GCVW	Major	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Acalabrutinib.	Mature B-cell lymphoma [2A85]	[17]
Prasugrel	DM7MT6E	Minor	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Prasugrel.	Myocardial infarction [BA41-BA43]	[18]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Dexlansoprazole caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[19]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Dexlansoprazole caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[20]
Choline salicylate	DM8P137	Minor	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Choline salicylate.	Postoperative inflammation [1A00-CA43]	[21]
Riociguat	DMXBLMP	Moderate	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Riociguat.	Pulmonary hypertension [BB01]	[22]
Axitinib	DMGVH6N	Minor	Decreased absorption of Dexlansoprazole due to altered gastric pH caused by Axitinib.	Renal cell carcinoma [2C90]	[23]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Dexlansoprazole caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[24]
Plazomicin	DMKMBES	Moderate	Increased risk of hypomagnesemia by the combination of Dexlansoprazole and Plazomicin.	Urinary tract infection [GC08]	[25]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Glyceryl monostearate	E00310	24699	Emollient; Emulsifying agent; Emulsion stabilizing agent; Solubilizing agent; Surfactant; Viscosity-controlling agent
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Potassium chloride	E00074	4873	Tonicity agent
Sucralose	E00370	71485	Flavoring agent
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium carbonate	E00205	11029	Adsorbent; Diluent
Magnesium stearate	E00208	11177	lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Saccharose	E00091	5988	Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triethyl citrate	E00128	6506	Plasticizing agent; Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Dexlansoprazole 30 mg tablet	30 mg	Disintegrating Oral Tablet	Oral
Dexlansoprazole 30 mg capsule	30 mg	Delayed Release Oral Capsule	Oral
Dexlansoprazole 60 mg capsule	60 mg	Delayed Release Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022287.
• [2] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7208).
• [3] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] Clinical pipeline report, company report or official report of Takeda (2009).
• [6] A novel screening strategy to identify ABCB1 substrates and inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):11-26.
• [7] Absorption, distribution, metabolism and excretion of [14C]dexlansoprazole in healthy male subjects. Clin Drug Investig. 2012 May 1;32(5):319-32.
• [8] Pharmacological and safety profile of dexlansoprazole: a new proton pump inhibitor - implications for treatment of gastroesophageal reflux disease in the Asia Pacific region. J Neurogastroenterol Motil. 2016 Jul 30;22(3):355-66.
• [9] Cerner Multum, Inc. "Australian Product Information.".
• [10] Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
• [11] Product Information. Bosulif (bosutinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [12] Cerner Multum, Inc. "Canadian Product Information.".
• [13] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [14] Product Information. Edurant (rilpivirine). Tibotec Pharmaceuticals, Titusville, NJ.
• [15] Product Information. Isentress (raltegravir). Merck & Company Inc, West Point, PA.
• [16] Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
• [17] Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
• [18] Product Information. Effient (prasugrel). Lilly, Eli and Company, Indianapolis, IN.
• [19] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [20] Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
• [21] Miner PB Jr, Fort JG, Zhang Y. Intragastric acidity and omeprazole exposure during dosing with either PA32540 (enteric-coated aspirin 325?mg + immediate-release omeprazole 40?mg) or enteric-coated aspirin 325?mg + enteric-coated omeprazole 40?mg - a randomised, phase 1, crossover study.?Aliment Pharmacol Ther. 2013;38(1):62-71. [PMID: 23692061]
• [22] Product Information. Adempas (riociguat). Bayer Pharmaceutical Inc, West Haven, CT.
• [23] Product Information. Inlyta (axitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [24] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
• [25] FDA. U.S. Food and Drug Administration "FDA Drug Safety Communication: Low magnesium levels can be associated with long-term use of proton pump inhibitor drugs (PPIs).".