Identification
- Summary
Vonoprazan is a potassium-competitive acid blocker used in the treatment of acid-related disorders and as an adjunct to Helicobacter pylori eradication.
- Brand Names
- Voquezna 14 Day Dualpak 20;500, Voquezna 14 Day Triplepak 20;500;500
- Generic Name
- Vonoprazan
- DrugBank Accession Number
- DB11739
- Background
Vonoprazan is a potassium-competitive acid blocker (PCAB) that inhibits H+, K+-ATPase-mediated gastric acid secretion. PCABs represent an alternative to proton-pump inhibitors for the treatment of acid-related disorders. Unlike proton-pump inhibitors, PCABs are not affected by CYP2C19 genetic polymorphisms and do not require acid-resistant formulations.1 Furthermore, vonoprazan is 350-times more potent than the proton-pump inhibitor lansoprazole, thanks to its ability to accumulate in the gastric corpus mucosa, specifically in the parietal cells.2
In February 2015, vonoprazan was first marketed in Japan for the treatment of acid-related disorders and as an adjunct to Helicobacter pylori (H. pylori) eradication.1 In May 2022, the FDA approved the use of vonoprazan in a co-packaged product containing amoxicillin and clarithromycin for the treatment of H. pylori infection.5 Studies have shown that the concomitant use of vonoprazan, amoxicillin, and clarithromycin leads to an H. pylori eradication rate of approximately 90%.3
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Vonoprazan (DB11739)
- Weight
- Average: 345.39
Monoisotopic: 345.094726104 - Chemical Formula
- C17H16FN3O2S
- Synonyms
- 1-[5-(2-fluorophenyl)-1-pyridin-3-ylsulfonylpyrrol-3-yl]-N-methylmethanamine
- Vonoprazan
- External IDs
- TAK-438
Pharmacology
- Indication
Vonoprazan, in combination with amoxicillin and clarithromycin in a co-packaged product, is indicated for the treatment of Helicobacter pylori (H. pylori) infection in adults. Another co-packaged product with only vonoprazan and amoxicillin is also indicated for the treatment of H. pylori infection in adults.5
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
The use of vonoprazan leads to an increase in intragastric pH. The inhibitory effect of vonoprazan on acid secretion increases with repeated daily dosing. Although the antisecretory effect of vonoprazan decreases after drug discontinuation, intragastric pH remains elevated for 24 to 48 hours. Vonoprazan does not have a clinically significant effect on QT prolongation.5
Compared to other potassium-competitive acid blockers (PCABs), vonoprazan has a higher point-positive charge (pKa of 9.06). This allows vonoprazan to accumulate at higher concentrations in the canalicular space of the gastric parietal cells, where it binds H+, K+-ATPase in a K+-competitive and reversible manner. Compared to other PCABs, such as SCH28080, or proton-pump inhibitors, such as lansoprazole, vonoprazan has a more potent H+, K+-ATPase inhibitory activity.1
- Mechanism of action
Vonoprazan is a potassium-competitive acid blocker (PCAB) that inhibits the H+, K+-ATPase enzyme system in a potassium-competitive manner. Through this mechanism, vonoprazan suppresses basal and stimulated gastric acid secretion at the secretory surface of gastric parietal cells.5
Although both classes of drugs inhibit the H+, K+-ATPase, the mechanism of action of PCABs differs from that of proton-pump inhibitors (PPIs). PPIs form a covalent disulphide bond with a cysteine residue on the H+, K+-ATPase, which leads to the inactivation of the enzyme, while PCABs interfere with the binding of K+ to the H+, K+-ATPase.1
Target Actions Organism AHydrogen potassium ATPase inhibitorHumans - Absorption
Vonoprazan has time-independent pharmacokinetics, and steady-state concentrations are reached after 3 to 4 days. In patients given a single dose of vonoprazan, the AUC0-12h, Cmax and Tmax were 154.8 nghr/mL, 25.2 ng/mL, and 2.5 h. In patients given vonoprazan twice daily, the AUC0-12h, Cmax and Tmax were 272.5 nghr/mL, 37.8 ng/mL, and 3.0 h.5 In patients given 10 mg to 40 mg of vonoprazan daily for 7 days, the AUC and Cmax increased in a dose-proportional manner. In healthy subjects given 20 mg of vonoprazan, a high-fat meal led to a 5% and 15% increase in Cmax and AUC; however, these changes were not considered clinically significant.5
- Volume of distribution
Vonoprazan has an apparent oral volume of distribution of 1001 L following a single dose (20 mg). At steady state, the apparent oral volume of distribution of vonoprazan is 782.7 L.5
- Protein binding
In healthy subjects, the plasma protein binding of vonoprazan ranges from 85% to 88%. At plasma concentrations between 0.1 and 10 mcg/mL, the plasma protein binding of vonoprazan is independent of concentration.5
- Metabolism
Vonoprazan is metabolized by several cytochrome P450 (CYP) isoforms, mainly CYP3A4, and to a lesser extent CYP3A5, CYP2B6, CYP2C19, CYP2C9 and CYP2D6. Sulfo- and glucuronosyl-transferases also participate in the metabolism of vonoprazan, and all metabolites are pharmacologically inactive.5,1 CYP3A4 converts vonoprazan into metabolites M-I and M-II, which are then converted to glucuronic-acid-conjugated products M-I-G and M-II-G, respectively.2 Unlike proton pump inhibitors, the presence of CYP2C19 polymorphisms does not have a significant effect on the pharmacokinetics of vonoprazan.5
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- Route of elimination
Vonoprazan is excreted in urine (67%) and feces (31%). Approximately 8% and 1.4% of the dose administered are recovered unchanged in urine and feces, respectively.5
- Half-life
Vonoprazan has an elimination half-life of 7.1 h following a single dose (20 mg). At steady state, the elimination half-life of vonoprazan is 6.8 h.5
- Clearance
Vonoprazan has an apparent oral clearance of 97.3 L/h following a single dose (20 mg). At steady state, the apparent oral clearance of vonoprazan is 81.3 L/h.5
- Adverse Effects
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Overdose with vonoprazan has not been reported. No serious adverse reactions were observed during clinical studies in subjects given a single dose of 120 mg of vonoprazan. Vonoprazan is not removed from the circulation by hemodialysis. In case of overdose, the FDA label for Voquezna Triple Pak and Voquezna Dual Pak recommends symptomatic and supportive treatment.5
Animal studies evaluating vonoprazan mutagenicity (Ames test) have reported negative results. No effects on fertility and reproductive performance were observed in rats given 300 mg/kg/day of vonoprazan orally (133, the maximum recommended human dose). Mice given 6, 20, 60 and 200 mg/kg/day of vonoprazan orally (0.4, 4, 19, and 93 times the maximum recommended human dose) developed hyperplasia of neuroendocrine cells, gastropathy and benign and/or malignant neuroendocrine cell tumors (carcinoids) in the stomach.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Vonoprazan can be increased when it is combined with Abametapir. Abatacept The metabolism of Vonoprazan can be increased when combined with Abatacept. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Vonoprazan. Acalabrutinib The metabolism of Vonoprazan can be decreased when combined with Acalabrutinib. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Vonoprazan. Adalimumab The metabolism of Vonoprazan can be increased when combined with Adalimumab. Albendazole The metabolism of Albendazole can be decreased when combined with Vonoprazan. Alfentanil The metabolism of Vonoprazan can be decreased when combined with Alfentanil. Alprazolam The metabolism of Vonoprazan can be decreased when combined with Alprazolam. Ambrisentan The metabolism of Vonoprazan can be decreased when combined with Ambrisentan. 
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- Take with or without food. High-fat meals may decrease the absorption of vonoprazan; however, these changes are not considered clinically significant.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Voquezna Dual Pak Vonoprazan (26.72 mg/1) + Amoxicillin Trihydrate (500 mg/1) Capsule; Kit; Tablet Oral Phathom Pharmaceuticals Inc. 2022-05-04 Not applicable US 
Voquezna Triple Pak Vonoprazan (26.72 mg/1) + Amoxicillin Trihydrate (500 mg/1) + Clarithromycin (500 mg/1) Capsule; Kit; Tablet Oral Phathom Pharmaceuticals Inc. 2022-05-04 Not applicable US
Categories
- ATC Codes
- A02BD14 — Vonoprazan, amoxicillin and clarithromycin
- A02BD — Combinations for eradication of Helicobacter pylori
- A02B — DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
- A02 — DRUGS FOR ACID RELATED DISORDERS
- A — ALIMENTARY TRACT AND METABOLISM
- A02BD — Combinations for eradication of Helicobacter pylori
- A02B — DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
- A02 — DRUGS FOR ACID RELATED DISORDERS
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- Amides
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs for Acid Related Disorders
- Drugs for Peptic Ulcer and Gastro-Oesophageal Reflux Disease (Gord)
- Gastric Acid Lowering Agents
- P-glycoprotein inhibitors
- Potassium-competitive Acid Blockers
- Sulfones
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpyrroles. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrrole ring through a CC or CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyrroles
- Sub Class
- Substituted pyrroles
- Direct Parent
- Phenylpyrroles
- Alternative Parents
- Pyridinesulfonamides / Fluorobenzenes / Aralkylamines / Aryl fluorides / Sulfonyls / Organosulfonic acids and derivatives / Heteroaromatic compounds / Dialkylamines / Azacyclic compounds / Organofluorides show 2 more
- Substituents
- 2-phenylpyrrole / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle / Benzenoid / Fluorobenzene / Halobenzene show 17 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1R5L3J156G
- CAS number
- 881681-00-1
- InChI Key
- BFDBKMOZYNOTPK-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H16FN3O2S/c1-19-10-13-9-17(15-6-2-3-7-16(15)18)21(12-13)24(22,23)14-5-4-8-20-11-14/h2-9,11-12,19H,10H2,1H3
- IUPAC Name
- {[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrol-3-yl]methyl}(methyl)amine
- SMILES
- CNCC1=CN(C(=C1)C1=CC=CC=C1F)S(=O)(=O)C1=CC=CN=C1
References
- Synthesis Reference
Ikemoto, T., et al. (2016). Process for producing pyrrole compound (U.S. Patent No. US 9,266,831 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/62/60/80/823d4e469ef018/US9266831.pdf
- General References
- Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7. [Article]
- Sugano K: Vonoprazan fumarate, a novel potassium-competitive acid blocker, in the management of gastroesophageal reflux disease: safety and clinical evidence to date. Therap Adv Gastroenterol. 2018 Jan 9;11:1756283X17745776. doi: 10.1177/1756283X17745776. eCollection 2018. [Article]
- Kiyotoki S, Nishikawa J, Sakaida I: Efficacy of Vonoprazan for Helicobacter pylori Eradication. Intern Med. 2020 Jan 15;59(2):153-161. doi: 10.2169/internalmedicine.2521-18. Epub 2019 Jun 27. [Article]
- FDA Thailand Product Information: Vocinti (vonoprazan fumarate) oral tablets [Link]
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- External Links
- Human Metabolome Database
- HMDB0259872
- PubChem Compound
- 15981397
- PubChem Substance
- 347828097
- ChemSpider
- 13112797
- BindingDB
- 394392
- 2604577
- ChEBI
- 136048
- ChEMBL
- CHEMBL2079130
- ZINC
- ZINC000034842823
- PDBe Ligand
- HKT
- Wikipedia
- Vonoprazan
- PDB Entries
- 5ylu
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Erosive Esophagitis 1 4 Completed Treatment Helicobacter Pylori Infection 1 4 Completed Treatment Reflux Esophagitis (RE) 1 4 Not Yet Recruiting Prevention Acute Coronary Syndrome (ACS) / Helicobacter Pylori Infection 1 4 Not Yet Recruiting Treatment Helicobacter Pylori Eradication Rate 1 4 Not Yet Recruiting Treatment Helicobacter Pylori Infection 2 4 Not Yet Recruiting Treatment Proton Pump Inhibitors / Upper GI Bleeding 1 4 Recruiting Treatment Eradication Therapy of Helicobacter Pylori 1 4 Recruiting Treatment Gastritis Chronic / Helicobacter Pylori Infection 1 4 Recruiting Treatment Gastro-esophageal Reflux Disease (GERD) / Gastroesophageal Reflux 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral Capsule; kit; tablet Oral Tablet, film coated Oral 10 mg Tablet, film coated Oral 20 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9186411 No 2015-11-17 2030-08-11 US US7977488 No 2011-07-12 2028-08-11 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 194.8°C FDA label water solubility Slightly soluble FDA label - Predicted Properties
Property Value Source Water Solubility 0.049 mg/mL ALOGPS logP 1.78 ALOGPS logP 2.03 Chemaxon logS -3.8 ALOGPS pKa (Strongest Basic) 9.01 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 63.99 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 90.16 m3·mol-1 Chemaxon Polarizability 34.23 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Sodium:potassium-exchanging atpase activity
- Specific Function
- Catalyzes the hydrolysis of ATP coupled with the exchange of H(+) and K(+) ions across the plasma membrane. Responsible for acid production in the stomach.
Components:
| Name | UniProt ID |
|---|---|
| Potassium-transporting ATPase alpha chain 1 | P20648 |
| Potassium-transporting ATPase subunit beta | P51164 |
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7. [Article]
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- FDA Approved Drug Products: VOQUEZNA TRIPLE PAK (vonoprazan tablets; amoxicillin capsules; clarithromycin tablets), co-packaged for oral use and VOQUEZNA DUAL PAK (vonoprazan tablets; amoxicillin capsules) co-packaged for oral use [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7. [Article]
Drug created at October 20, 2016 20:43 / Updated at December 01, 2022 11:26