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

Stem definition	Drug id	CAS RN
proton pump inhibitors, not dependent on acid activation	4993	881681-00-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: vonoprazan vonoprazan fumarate takecab TAK-438	Vonoprazan is a potassium-competitive proton pump blocker which was approved in Japan for the treatment of gastroduodenal ulcer. FDA approved a co-packaged combination of vonoprazan and antibiotics (amoxicillin and clarithromycin) to eradicate Helicobacter pyroli. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19. Molecular weight: 345.39 Formula: C17H16FN3O2S CLOGP: 2.54 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 63.99 ALOGS: -3.85 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

vonoprazan
vonoprazan fumarate
takecab
TAK-438

Vonoprazan is a potassium-competitive proton pump blocker which was approved in Japan for the treatment of gastroduodenal ulcer. FDA approved a co-packaged combination of vonoprazan and antibiotics (amoxicillin and clarithromycin) to eradicate Helicobacter pyroli. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19.

Molecular weight: 345.39
Formula: C17H16FN3O2S
CLOGP: 2.54
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 63.99
ALOGS: -3.85
ROTB: 4

Status: OFM

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

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 26, 2014	PMDA

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
Hepatic function abnormal	87.21	26.00	40	2948	37102	63448932
Interstitial lung disease	70.57	26.00	41	2947	61867	63424167
Platelet count decreased	68.72	26.00	51	2937	116071	63369963
Decreased appetite	56.40	26.00	64	2924	250988	63235046
Anaemia	51.51	26.00	66	2922	293364	63192670
Cardiac failure	45.75	26.00	36	2952	89106	63396928
White blood cell count decreased	33.79	26.00	37	2951	139067	63346967
Renal impairment	33.55	26.00	30	2958	88325	63397709
Cerebral infarction	33.09	26.00	18	2970	23875	63462159
Marasmus	32.56	26.00	7	2981	518	63485516

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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
Interstitial lung disease	155.26	23.06	93	3668	65189	34887981
Hepatic function abnormal	94.53	23.06	59	3702	44304	34908866
Cardiac failure	49.87	23.06	55	3706	91193	34861977
Cerebral infarction	49.72	23.06	33	3728	27422	34925748
Renal impairment	44.92	23.06	53	3708	94460	34858710
Pneumonia aspiration	41.36	23.06	35	3726	41868	34911302
Radiation pneumonitis	40.88	23.06	14	3747	2626	34950544
Immune-mediated enterocolitis	40.08	23.06	14	3747	2785	34950385
Adrenal insufficiency	35.82	23.06	21	3740	14026	34939144
Decreased appetite	35.72	23.06	64	3697	166328	34786842

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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
Interstitial lung disease	220.07	21.56	132	6926	112468	79624862
Hepatic function abnormal	169.96	21.56	96	6962	73011	79664319
Cardiac failure	89.74	21.56	88	6970	154754	79582576
Platelet count decreased	83.14	21.56	94	6964	194570	79542760
Decreased appetite	78.81	21.56	122	6936	342296	79395034
Renal impairment	70.43	21.56	78	6980	157705	79579625
Cerebral infarction	70.03	21.56	46	7012	45630	79691700
Pneumonia aspiration	58.45	21.56	48	7010	66919	79670411
Neutrophil count decreased	53.62	21.56	53	7005	93906	79643424
Liver disorder	49.22	21.56	45	7013	72372	79664958

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A02BC08	ALIMENTARY TRACT AND METABOLISM DRUGS FOR ACID RELATED DISORDERS DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) Proton pump inhibitors
ATC	A02BD14	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	A02BD15	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

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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
Duodenal ulcer disease	indication	51868009	DOID:1724
Gastro-esophageal reflux disease with esophagitis	indication	266433003
Gastric ulcer	indication	397825006	DOID:10808
Infection caused by Helicobacter pylori	indication	721730009

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🐶 Veterinary Drug Use

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🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.09	Basic
pKa2	2.72	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
500MG;500MG;EQ 20MG BASE	VOQUEZNA TRIPLE PAK	PHATHOM	N215152	May 3, 2022	DISCN	CAPSULE, TABLET, TABLET	ORAL	May 3, 2027	NEW CHEMICAL ENTITY
500MG;500MG;EQ 20MG BASE	VOQUEZNA TRIPLE PAK	PHATHOM	N215152	May 3, 2022	DISCN	CAPSULE, TABLET, TABLET	ORAL	May 3, 2032	GENERATING ANTIBIOTIC INCENTIVES NOW
500MG;EQ 20MG BASE	VOQUEZNA DUAL PAK	PHATHOM	N215153	May 3, 2022	DISCN	CAPSULE, TABLET	ORAL	May 3, 2027	NEW CHEMICAL ENTITY
500MG;EQ 20MG BASE	VOQUEZNA DUAL PAK	PHATHOM	N215153	May 3, 2022	DISCN	CAPSULE, TABLET	ORAL	May 3, 2032	GENERATING ANTIBIOTIC INCENTIVES NOW

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Potassium-transporting ATPase	Transporter	P20648 P51164	ATP4A_HUMAN ATP4B_HUMAN	INHIBITOR	Ki	8		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
HKT	PDB_CHEM_ID
019050	NDDF
019051	NDDF
11549	IUPHAR_LIGAND_ID
15981397	PUBCHEM_CID
1R5L3J156G	UNII
2604576	RXNORM
4041456	VANDF
40790	MMSL
881681-01-2	SECONDARY_CAS_RN

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Pharmaceutical products:

None