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lansoprazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antiulcer, benzimidazole derivatives	1547	103577-45-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: prevacid lansoprazole A-65006 AG 1749 AG-1749	A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. Molecular weight: 369.36 Formula: C16H14F3N3O2S CLOGP: 2.79 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 67.87 ALOGS: -3.17 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

prevacid
lansoprazole
A-65006
AG 1749
AG-1749

A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.

Molecular weight: 369.36
Formula: C16H14F3N3O2S
CLOGP: 2.79
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 67.87
ALOGS: -3.17
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
30	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	81 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	4.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.35 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	1 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.28 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
May 10, 1995	FDA	TAKEDA PHARMS USA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Chronic kidney disease	911.70	9.14	921	206207	44477	63237417
Drug ineffective	725.08	9.14	1454	205674	1043311	62238583
Colitis microscopic	425.96	9.14	304	206824	9035	63272859
Hyponatraemia	400.34	9.14	1026	206102	110874	63171020
Renal injury	398.05	9.14	293	206835	9146	63272748
Acute kidney injury	318.06	9.14	1696	205432	261719	63020175
Completed suicide	304.23	9.14	54	207074	145619	63136275
End stage renal disease	298.65	9.14	215	206913	6478	63275416
Product dose omission issue	211.95	9.14	272	206856	234041	63047853
Therapeutic product effect incomplete	207.93	9.14	74	207054	124982	63156912

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Chronic kidney disease	560.35	10.11	748	136483	40462	34779238
Drug ineffective	415.78	10.11	725	136506	456026	34363674
Death	296.80	10.11	708	136523	397341	34422359
Completed suicide	264.48	10.11	36	137195	98132	34721568
End stage renal disease	254.63	10.11	238	136993	8623	34811077
Hyponatraemia	198.32	10.11	744	136487	81947	34737753
Colitis microscopic	184.99	10.11	115	137116	2222	34817478
Interstitial lung disease	182.74	10.11	618	136613	64664	34755036
Renal injury	175.18	10.11	218	137013	10977	34808723
Toxicity to various agents	172.45	10.11	328	136903	200034	34619666

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	885.58	9.32	1677	294821	1079236	78368654
Completed suicide	647.49	9.32	77	296421	245690	79202200
Chronic kidney disease	564.34	9.32	938	295560	65216	79382674
Colitis microscopic	558.62	9.32	399	296099	10369	79437521
Hyponatraemia	534.56	9.32	1664	294834	176184	79271706
Death	364.22	9.32	999	295499	565515	78882375
Toxicity to various agents	314.18	9.32	688	295810	420852	79027038
Product dose omission issue	256.62	9.32	326	296172	247211	79200679
Interstitial lung disease	248.39	9.32	951	295547	111649	79336241
Acute kidney injury	245.30	9.32	2979	293519	516425	78931465

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A02BC03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Proton pump inhibitors
ATC	A02BC53	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Proton pump inhibitors
ATC	A02BD02	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Combinations for eradication of Helicobacter pylori
ATC	A02BD03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Combinations for eradication of Helicobacter pylori
ATC	A02BD07	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Combinations for eradication of Helicobacter pylori
ATC	A02BD09	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Combinations for eradication of Helicobacter pylori
ATC	A02BD10	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Combinations for eradication of Helicobacter pylori
CHEBI has role	CHEBI:49200	proton pump inhibitors
CHEBI has role	CHEBI:49201	anti-ulcer drugs
FDA EPC	N0000175525	Proton Pump Inhibitor

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Peptic ulcer	indication	13200003	DOID:750
Erosive esophagitis	indication	40719004
Duodenal ulcer disease	indication	51868009	DOID:1724
Zollinger-Ellison syndrome	indication	53132006	DOID:0050782
Gastroesophageal reflux disease	indication	235595009	DOID:8534
Gastric ulcer	indication	397825006	DOID:10808
NSAID-Induced Gastric Ulcer	indication
Gastric Hypersecretory Conditions	indication
Duodenal Ulcer due to H. Pylori	indication
Maintenance of Healing Duodenal Ulcer	indication

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.23	acidic
pKa2	3.35	Basic
pKa3	2.72	Basic

Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Potassium-transporting ATPase	Transporter	P20648 P51164	ATP4A_HUMAN ATP4B_HUMAN	INHIBITOR			CHEMBL	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.84	CHEMBL
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	6.47	DRUG MATRIX
Fatty acid synthase	Enzyme	P49327	FAS_HUMAN		Ki	5.28	CHEMBL
Phosphoethanolamine/phosphocholine phosphatase	Enzyme	Q8TCT1	PHOP1_HUMAN		IC50	6.36	CHEMBL
Microtubule-associated protein tau	Structural	P10636	TAU_HUMAN		Ki	8.60	CHEMBL
N(G),N(G)-dimethylarginine dimethylaminohydrolase 1	Enzyme	O94760	DDAH1_HUMAN		IC50	4.29	CHEMBL
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5.28	DRUG MATRIX
Cytosolic endo-beta-N-acetylglucosaminidase	Enzyme	Q8NFI3	ENASE_HUMAN		IC50	4.61	CHEMBL
Indoleamine 2,3-dioxygenase 2	Enzyme		I23O2_MOUSE		IC50	5.09	CHEMBL

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External reference:

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ID	Source
004456	NDDF
0K5C5T2QPG	UNII
108666007	SNOMEDCT_US
169151	MMSL
17128	RXNORM
330	MMSL
386888004	SNOMEDCT_US
3883	PUBCHEM_CID
4020922	VANDF
4958	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Basic Care Lansoprazole	HUMAN OTC DRUG LABEL	1	0113-7003	CAPSULE, DELAYED RELEASE	15 mg	ORAL	ANDA	16 sections
basic care lansoprazole	HUMAN OTC DRUG LABEL	1	0113-7116	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	15 mg	ORAL	NDA	16 sections
Good Sense Lansoprazole	HUMAN OTC DRUG LABEL	1	0113-0116	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	15 mg	ORAL	NDA	16 sections
Good Sense lansoprazole	HUMAN OTC DRUG LABEL	1	0113-0117	CAPSULE, DELAYED RELEASE	15 mg	ORAL	ANDA	16 sections
Good Sense Lansoprazole	HUMAN OTC DRUG LABEL	1	0113-1114	CAPSULE, DELAYED RELEASE	15 mg	ORAL	ANDA	16 sections
Good Sense Lansoprazole	HUMAN OTC DRUG LABEL	1	0113-1114	CAPSULE, DELAYED RELEASE	15 mg	ORAL	ANDA	16 sections
Lansoprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3008	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	15 mg	ORAL	ANDA	29 sections
Lansoprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3008	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	15 mg	ORAL	ANDA	29 sections
Lansoprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3008	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	15 mg	ORAL	ANDA	29 sections
Lansoprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3009	TABLET, ORALLY DISINTEGRATING, DELAYED RELEASE	30 mg	ORAL	ANDA	29 sections

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