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Identification
- Summary
Vericiguat is a soluble guanylate cyclase stimulator used to reduce heart failure-related hospitalization and cardiovascular death in patients with chronic systolic heart failure.
- Brand Names
- Verquvo
- Generic Name
- Vericiguat
- DrugBank Accession Number
- DB15456
- Background
Vericiguat is a direct stimulator of soluble guanylate cyclase (sGC) used in the management of systolic heart failure to reduce mortality and hospitalizations.5 A key component of the NO-sGC-cGMP signaling pathway that helps to regulate the cardiovascular system, sGC enzymes are intracellular enzymes found in vascular smooth muscle cells (amongst other cell types) that catalyze the synthesis of cyclic guanosine monophosphate (cGMP) in response to activation by nitric oxide (NO).1,4 Cyclic GMP acts as a second messenger, activating a number of downstream signaling cascades that elicit a broad variety of effects, and these diverse cellular effects have implicated deficiencies in its production (primarily due to insufficient NO bioavailability) in the pathogenesis of various cardiovascular diseases.1 As a direct stimulator of sGC, vericiguat mitigates the need for a functional NO-sGC-cGMP axis and thereby helps to prevent the myocardial and vascular dysfunction associated with decreased sGC activity in heart failure.6
Vericiguat was approved by the FDA in January 2021 - developed by Merck under the brand name Verquvo - for use in certain patients with systolic heart failure.6 Although not the first sGC stimulator to be granted FDA approval (riociguat was approved in 2013 for use in pulmonary hypertension),7 vericiguat is unique amongst its peers in that modifications to its structure have dramatically decreased its susceptibility to oxidative metabolism,1 resulting in a relatively long half-life and allowing for once-daily dosing.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Vericiguat (DB15456)
- Weight
- Average: 426.388
Monoisotopic: 426.136428113 - Chemical Formula
- C19H16F2N8O2
- Synonyms
- Vericiguat
- Vériciguat
- Vericiguatum
- External IDs
- BAY 1021189
- BAY-1021189
- BAY1021189
- MK-1242
- WHO 9805
Pharmacology
- Indication
Vericiguat is indicated in adults with symptomatic, chronic heart failure and an ejection fraction of <45% to reduce the risk of cardiovascular death and heart failure-related hospitalization following a hospitalization for heart failure or need for outpatient intravenous diuretics.5
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Cardiovascular mortality •••••••••••• •••••••• •••••••• ••••• ••••••• •••••••• ••••• ••••••• •••••• Prevention of Heart failure hospitalization •••••••••••• ••••••• •••••••• ••••• •••••••• •••••••• •••••••• •••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
By directly stimulating the increased production of intracellular cyclic guanosine monophosphate (cGMP), vericiguat causes the relaxation of vascular smooth muscle and vasodilation.5 Vericiguat has a relatively long half-life (~30h) that allows for once-daily dosing.5
Animal reproduction studies have demonstrated the potential for embryo-fetal toxicity when vericiguat is administered to pregnant females - defects in major vessel and heart formation, as well as spontaneous abortions/resorptions, were observed when vericiguat was administered to pregnant rabbits during organogenesis.5 The possibility of pregnancy should be excluded prior to beginning therapy with vericiguat, and adequate contraception should be used throughout therapy and for one month following cessation of treatment.5
- Mechanism of action
Heart failure (HF) involves, amongst other morphologic and physiologic changes, the impaired synthesis of nitric oxide (NO) and decreased activity of soluble guanylate cyclase (sGC). Functioning normally, NO binds to sGC and stimulates the synthesis of intracellular cyclic guanosine monophosphate (cGMP),4 a second messenger involved in the maintenance of vascular tone, as well as cardiac contractility and remodeling. Defects in this pathway are thought to contribute to the myocardial and vascular dysfunction associated with heart failure and are therefore a desirable target in its treatment.5,1
Vericiguat directly stimulates sGC by binding to a target site on its beta-subunit,4 bypassing the need for NO-mediated activation, and in doing so causes an increase in the production of intracellular cGMP that results in vascular smooth muscle relaxation and vasodilation.5
Target Actions Organism ARetinal guanylyl cyclase 1 modulatorHumans AGuanylate cyclase soluble subunit beta-1 stimulatorHumans - Absorption
Following the administration of 10mg of vericiguat by mouth once daily, the average steady-state Cmax and AUC in patients with heart failure is 350 mcg/L and 6,680 mcg•h/L, respectively, with a Tmax of 1 hour.5 The absolute bioavailability of orally-administered vericiguat is approximately 93% when taken with food - co-administration with meals has been shown to reduce pharmacokinetic variability, increase Tmax to roughly 4 hours, and increase Cmax and AUC by 41% and 44%, respectively.5
- Volume of distribution
In healthy subjects the steady-state volume of distribution of vericiguat is approximately 44 liters.5
- Protein binding
Vericiguat is extensively (~98%) protein-bound in plasma, primarily to serum albumin.5
- Metabolism
Vericiguat is primarily metabolized via phase II conjugation reactions, with CYP-mediated oxidative metabolism comprising a small (<5%) portion of its overall biotransformation. The major inactive metabolite, vericiguat N-glucuronide (M1), is formed by UGT1A9 and, to a lesser extent, UGT1A1.5 Other identified metabolites include a denbenzylated compound1 and an M15 metabolite thought to be the result of oxidative metabolism,3 although these metabolites are poorly characterized.
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- Route of elimination
Following the oral administration of radiolabeled vericiguat, approximately 53% of the administered radioactivity was recovered in the urine and 45% in the feces.5 A human mass balance study found that the portion recovered in the urine comprised approximately 40.8% N-glucuronide metabolite, 7.7% other metabolites, and 9% unchanged parent drug, while virtually the entire portion recovered in the feces comprised unchanged vericiguat.3
- Half-life
In patients with heart failure, the half-life of vericiguat is 30 hours.5
- Clearance
Vericiguat is a low-clearance drug, with an observed plasma clearance of 1.6 L/h in healthy volunteers and 1.3 L/h in patients with systolic heart failure.5,3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Data regarding overdosage with vericiguat are unavailable. Doses of up to 15mg once daily (50% greater than the recommended maintenance dose) have been studied and found to be well-tolerated. Symptoms of overdose are likely to be consistent with the adverse effect profile of vericiguat and may therefore involve significant hypotension for which symptomatic and supportive measures should be provided. Dialysis is unlikely to be of benefit in vericiguat overdose given its high degree of protein binding.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 softwareAbaloparatide The risk or severity of adverse effects can be increased when Abaloparatide is combined with Vericiguat. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Vericiguat. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Vericiguat. Aliskiren The risk or severity of adverse effects can be increased when Aliskiren is combined with Vericiguat. Ambrisentan Vericiguat may increase the hypotensive activities of Ambrisentan. - Food Interactions
- Take with food. Administration with food has been shown to reduce pharmacokinetic variability and significantly improve absorption.
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.- International/Other Brands
- Verquvo (Merck)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Verquvo Tablet, film coated 5 mg/1 Oral Merck Sharp & Dohme Llc 2021-02-01 Not applicable US 
Verquvo Tablet, film coated 2.5 mg Oral Bayer Ag 2021-10-29 Not applicable EU 
Verquvo Tablet, film coated 10 mg Oral Bayer Ag 2021-10-29 Not applicable EU Verquvo Tablet, film coated 2.5 mg Oral Bayer Ag 2021-10-29 Not applicable EU Verquvo Tablet, film coated 10 mg Oral Bayer Ag 2021-10-29 Not applicable EU
Categories
- ATC Codes
- C01DX22 — Vericiguat
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- LV66ADM269
- CAS number
- 1350653-20-1
- InChI Key
- QZFHIXARHDBPBY-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H16F2N8O2/c1-31-19(30)25-14-15(22)26-17(27-16(14)23)13-11-6-10(20)7-24-18(11)29(28-13)8-9-4-2-3-5-12(9)21/h2-7H,8H2,1H3,(H,25,30)(H4,22,23,26,27)
- IUPAC Name
- methyl N-(4,6-diamino-2-{5-fluoro-1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}pyrimidin-5-yl)carbamate
- SMILES
- COC(=O)NC1=C(N)N=C(N=C1N)C1=NN(CC2=CC=CC=C2F)C2=C1C=C(F)C=N2
References
- Synthesis Reference
Follmann M, Ackerstaff J, Redlich G, Wunder F, Lang D, Kern A, Fey P, Griebenow N, Kroh W, Becker-Pelster EM, Kretschmer A, Geiss V, Li V, Straub A, Mittendorf J, Jautelat R, Schirok H, Schlemmer KH, Lustig K, Gerisch M, Knorr A, Tinel H, Mondritzki T, Trubel H, Sandner P, Stasch JP: Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. J Med Chem. 2017 Jun 22;60(12):5146-5161. doi: 10.1021/acs.jmedchem.7b00449. Epub 2017 Jun 12.
- General References
- Follmann M, Ackerstaff J, Redlich G, Wunder F, Lang D, Kern A, Fey P, Griebenow N, Kroh W, Becker-Pelster EM, Kretschmer A, Geiss V, Li V, Straub A, Mittendorf J, Jautelat R, Schirok H, Schlemmer KH, Lustig K, Gerisch M, Knorr A, Tinel H, Mondritzki T, Trubel H, Sandner P, Stasch JP: Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. J Med Chem. 2017 Jun 22;60(12):5146-5161. doi: 10.1021/acs.jmedchem.7b00449. Epub 2017 Jun 12. [Article]
- Tomasoni D, Adamo M, Anker MS, von Haehling S, Coats AJS, Metra M: Heart failure in the last year: progress and perspective. ESC Heart Fail. 2020 Dec 5. doi: 10.1002/ehf2.13124. [Article]
- Boettcher M, Gerisch M, Lobmeyer M, Besche N, Thomas D, Gerrits M, Lemmen J, Mueck W, Radtke M, Becker C: Metabolism and Pharmacokinetic Drug-Drug Interaction Profile of Vericiguat, A Soluble Guanylate Cyclase Stimulator: Results From Preclinical and Phase I Healthy Volunteer Studies. Clin Pharmacokinet. 2020 Nov;59(11):1407-1418. doi: 10.1007/s40262-020-00895-x. [Article]
- Friebe A, Sandner P, Schmidtko A: cGMP: a unique 2nd messenger molecule - recent developments in cGMP research and development. Naunyn Schmiedebergs Arch Pharmacol. 2020 Feb;393(2):287-302. doi: 10.1007/s00210-019-01779-z. Epub 2019 Dec 18. [Article]
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
- BusinessWire: Merck Announces U.S. FDA Approval of VERQUVO® (vericiguat) [Link]
- Adempas (Riociguat) FDA Label [Link]
- External Links
- KEGG Drug
- D11051
- ChemSpider
- 32700337
- BindingDB
- 50239781
- 2475830
- ChEBI
- 142432
- ChEMBL
- CHEMBL4066936
- ZINC
- ZINC000072318626
- Wikipedia
- Vericiguat
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Chronic Heart Failure With Reduced Ejection Fraction (HFrEF) 1 somestatus stop reason just information to hide Not Available Not Yet Recruiting Diagnostic Chest Pain 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Chronic Heart Failure (CHF) 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Chronic Heart Failure With Reduced Ejection Fraction (HFrEF) 3 somestatus stop reason just information to hide 4 Active Not Recruiting Treatment Chronic Heart Failure With Reduced Ejection Fraction (HFrEF) / Worsening of heart failure 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 10 mg Tablet Oral 2.5 mg Tablet Oral 5 mg Tablet Oral 5.000 mg Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 2.5 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral 10 mg Tablet, film coated Oral 2.5 mg Tablet, film coated Oral 5 mg Tablet, coated Oral 10 mg Tablet, coated Oral 2.5 mg Tablet, coated Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9993476 No 2018-06-12 2031-05-19 US US8921377 No 2014-12-30 2031-05-19 US US9604948 No 2017-03-28 2032-11-26 US US10736896 No 2020-08-11 2031-05-19 US US8420656 No 2013-04-16 2031-05-19 US US11439642 No 2011-05-19 2031-05-19 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP 2.99 Chemaxon pKa (Strongest Acidic) 11.84 Chemaxon pKa (Strongest Basic) 3.53 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 146.86 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 132.35 m3·mol-1 Chemaxon Polarizability 40.69 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M-H]- 193.505 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+H]+ 195.863 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.3329 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Catalyzes the synthesis of cyclic GMP (cGMP) in rods and cones of photoreceptors. Plays an essential role in phototransduction, by mediating cGMP replenishment (PubMed:15123990, PubMed:21928830, PubMed:26100624, PubMed:30319355, PubMed:9600905). May also participate in the trafficking of membrane-asociated proteins to the photoreceptor outer segment membrane (By similarity)
- Specific Function
- adenylate cyclase activity
- Gene Name
- GUCY2D
- Uniprot ID
- Q02846
- Uniprot Name
- Retinal guanylyl cyclase 1
- Molecular Weight
- 120057.18 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Stimulator
- Curator comments
- Soluble guanylate cyclase (sGC) is composed of two subunits, alpha (1 or 2) and beta - the binding site of vericiguat is believed to be found on the beta subunit.
- General Function
- Mediates responses to nitric oxide (NO) by catalyzing the biosynthesis of the signaling molecule cGMP
- Specific Function
- adenylate cyclase activity
- Gene Name
- GUCY1B1
- Uniprot ID
- Q02153
- Uniprot Name
- Guanylate cyclase soluble subunit beta-1
- Molecular Weight
- 70513.89 Da
References
- Friebe A, Sandner P, Schmidtko A: cGMP: a unique 2nd messenger molecule - recent developments in cGMP research and development. Naunyn Schmiedebergs Arch Pharmacol. 2020 Feb;393(2):287-302. doi: 10.1007/s00210-019-01779-z. Epub 2019 Dec 18. [Article]
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:12181437, PubMed:15470161, PubMed:15472229, PubMed:18004212, PubMed:18052087, PubMed:18674515, PubMed:19545173). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:12181437, PubMed:18004212). Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol and estrone (PubMed:15472229). Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties (PubMed:18052087, PubMed:19545173). Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II (PubMed:18674515). Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan (PubMed:12181437, PubMed:20610558). Also metabolizes mycophenolate, an immunosuppressive agent (PubMed:15470161, PubMed:18004212)
- Specific Function
- enzyme binding
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1A9
- Molecular Weight
- 59940.495 Da
References
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:12181437, PubMed:15472229, PubMed:18004206, PubMed:18004212, PubMed:18719240, PubMed:19830808, PubMed:23288867). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:12181437, PubMed:18004206, PubMed:18004212). Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol, estrone and estriol (PubMed:15472229, PubMed:18719240, PubMed:23288867). Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates (PubMed:17187418, PubMed:18004206, PubMed:19830808, PubMed:24525562). Also catalyzes the glucuronidation the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties (PubMed:18052087, PubMed:19545173). Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist losartan, a drug which can inhibit the effect of angiotensin II (PubMed:18674515). Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan (PubMed:12181437, PubMed:18004212, PubMed:20610558)
- Specific Function
- enzyme binding
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1A1
- Molecular Weight
- 59590.91 Da
References
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells (PubMed:11306452, PubMed:12958161, PubMed:19506252, PubMed:20705604, PubMed:28554189, PubMed:30405239, PubMed:31003562). Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme (PubMed:20705604, PubMed:23189181). Also mediates the efflux of sphingosine-1-P from cells (PubMed:20110355). Acts as a urate exporter functioning in both renal and extrarenal urate excretion (PubMed:19506252, PubMed:20368174, PubMed:22132962, PubMed:31003562, PubMed:36749388). In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates (PubMed:12682043, PubMed:28554189, PubMed:30405239). Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux (PubMed:11306452, PubMed:12477054, PubMed:15670731, PubMed:18056989, PubMed:31254042). In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- Broad substrate specificity ATP-binding cassette transporter ABCG2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: Verquvo (vericiguat) oral tablets [Link]
Drug created at May 20, 2019 15:34 / Updated at October 03, 2024 04:25