Maribavir
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Identification
- Summary
Maribavir is a cytomegalovirus (CMV) pUL97 kinase inhibitor used for the treatment of refractory post-transplant CMV infection.
- Brand Names
- Livtencity
- Generic Name
- Maribavir
- DrugBank Accession Number
- DB06234
- Background
Maribavir is an inhibitor of the cytomegalovirus (CMV; HHV5) pUL97 kinase which is used to treat CMV infections in patients post-transplantation.5 Most standard CMV therapies, such as ganciclovir or foscarnet, target CMV DNA polymerase - while generally effective, these medications tend to promote the development of CMV resistance to DNA polymerase-based therapies, and their use is often limited by toxicities like myelosuppression and renal injury.4 Maribavir is novel in that it instead targets the CMV pUL97 kinase, thereby providing an effective alternative treatment option in cases of resistant infections.
Maribavir was approved by the FDA in November 2021, under the name Livtencity (Takeda), for the treatment of resistant CMV infections in post-transplant patients.6 The drug was also approved by Health Canada in September 2022 7 and by European Commission in November 2022.9
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 376.23
Monoisotopic: 375.0752615 - Chemical Formula
- C15H19Cl2N3O4
- Synonyms
- Maribavir
- External IDs
- 1263-W-94
- 1263W94
Pharmacology
- Indication
Maribavir is indicated for the treatment of post-transplant cytomegalovirus (CMV) infection (following hematopoietic stem cell transplant or solid organ transplant) which is refractory to standard treatment with ganciclovir, valganciclovir, cidofovir, or foscarnet.5,7,8
In the US, patients receiving the treatment should weigh more than 35 kg and be at least 12 years old.5 In Canada and Europe, maribavir is only approved in adults.7,8
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 Treatment of Post-transplant cytomegalovirus (cmv) infection •••••••••••• ••••• •••••••••• •• •••••••• ••••••••• •••••• Treatment of Post-transplant cytomegalovirus (cmv) infection •••••••••••• •••••••••• •• •••••••• •••••••••• •••••• •• ••••• •• •• •••••• - 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
Maribavir exerts its antiviral efficacy via an alternative target as compared to traditional CMV antivirals and is thus useful in the treatment of CMV infections that have proven resistant to standard therapy.6
Maribavir should not be used concomitantly with ganciclovir or valganciclovir, as these molecules both require activation via CMV pUL97 in order to exert their antiviral effect. Taking them alongside maribavir - an inhibitor of this same kinase - will therefore significantly reduce their antiviral activity.5
- Mechanism of action
Human cytomegalovirus (CMV) is a herpesvirus commonly causing infection in patients following stem cell or organ transplants.6 As with other herpesviruses, CMV tends to persist in the host and become reactivated under immunosuppressive conditions3 - patients requiring multiple immunosuppressive medications to combat transplant rejection are thus at a much higher risk of developing serious CMV infections.3,6
Maribavir belongs to a class of anti-cytomegalovirus antivirals called benzimidazole ribosides.3 It competitively inhibits the human CMV pUL97 viral protein kinase, which results in viable but severely defective viruses upon replication,4 although the reasons for this remain poorly defined. In addition, maribavir also inhibits viral release from the nucleus to the cytoplasm by inhibiting pUL97-dependent phosphorylation of the nuclear lamina component lamin A/C, although the extent to which this activity contributes to its antiviral efficacy is unclear.4
Target Actions Organism ASerine/threonine protein kinase UL97 inhibitorHHV-5 - Absorption
Population pharmacokinetic modeling in patients receiving maribavir 400mg twice daily showed an AUC0-tau and Cmax of 128 µg.h/mL and 17.2 µg/mL, respectively.5 It has a median Tmax of one to three hours.5
- Volume of distribution
The mean apparent steady-state volume of distribution for maribavir was 27.3 L.5
- Protein binding
Across all concentration ranges tested, maribavir was extensively (~98%) protein-bound in plasma,5 likely primarily to serum albumin and alpha-1-acid glycoprotein.3
- Metabolism
Maribavir is extensively metabolized following oral administration, primarily by CYP3A4 and, to a lesser extent, by CYP1A2.5 Its major circulating metabolite is VP 44469, an inactive N-dealkylated metabolite.5
Hover over products below to view reaction partners
- Route of elimination
Maribavir is eliminated primarily via hepatic metabolism.5 Following the oral administration of radiolabeled maribavir, 61% of the dose was excreted in the urine (<2% as unchanged drug) and 14% was excreted in the feces (5.7% as unchanged drug).5
- Half-life
In post-transplant patients, the mean half-life of elimination was 4.32 hours.5
- Clearance
In post-transplant patients, the mean oral clearance of maribavir was 2.85 L/h.5
- 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 are limited regarding overdosage with maribavir. As there is no specific antidote for maribavir overdose, patients suspected of overdosage should be monitored closely for adverse reactions and treated symptomatically as clinically indicated.5 As maribavir is extensively protein-bound in plasma, dialysis is unlikely to be of benefit.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 Maribavir can be increased when it is combined with Abametapir. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Maribavir. Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Maribavir. Afatinib The serum concentration of Afatinib can be increased when it is combined with Maribavir. Allopurinol Maribavir may decrease the excretion rate of Allopurinol which could result in a higher serum level. - Food Interactions
- Avoid St. John's Wort. Co-administration with St. John's wort decreases serum levels of maribavir and may decrease its therapeutic efficacy.
- Take with or without food. The co-administration of food with maribavir does not significantly affect its disposition.
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
- Camvia (ViroPharma Inc.) / Livtencity (Takeda Pharmaceuticals America, Inc.)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Livtencity Tablet, film coated 200 mg Oral Takeda Pharmaceuticals International Ag Ireland Branch 2023-02-08 Not applicable EU Livtencity Tablet, film coated 200 mg Oral Takeda Pharmaceuticals International Ag Ireland Branch 2023-02-08 Not applicable EU Livtencity Tablet 200 mg Oral Takeda 2022-10-25 Not applicable Canada Livtencity Tablet, film coated 200 mg Oral Takeda Pharmaceuticals International Ag Ireland Branch 2023-02-08 Not applicable EU Livtencity Tablet, coated 200 mg/1 Oral Takeda Pharmaceuticals America, Inc. 2021-11-23 Not applicable US
Categories
- ATC Codes
- J05AX10 — Maribavir
- Drug Categories
- Anti-Infective Agents
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- BCRP/ABCG2 Inhibitors
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Cytomegalovirus pUL97 Kinase Inhibitor
- Direct Acting Antivirals
- Glycosides
- Heterocyclic Compounds, Fused-Ring
- Nucleic Acids, Nucleotides, and Nucleosides
- Nucleosides
- P-glycoprotein inhibitors
- Ribonucleosides
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzimidazole ribonucleosides and ribonucleotides. These are nucleosides with a structure that consists of an imidazole moiety of benzimidazole is N-linked to a ribose (or deoxyribose). Nucleotides have a phosphate group linked to the C5 carbon of the ribose (or deoxyribose) moiety.
- Kingdom
- Organic compounds
- Super Class
- Nucleosides, nucleotides, and analogues
- Class
- Benzimidazole ribonucleosides and ribonucleotides
- Sub Class
- Not Available
- Direct Parent
- Benzimidazole ribonucleosides and ribonucleotides
- Alternative Parents
- Glycosylamines / Pentoses / Benzimidazoles / Secondary alkylarylamines / N-substituted imidazoles / Aminoimidazoles / Benzenoids / Aryl chlorides / Heteroaromatic compounds / Tetrahydrofurans show 7 more
- Substituents
- 1-ribofuranosylbenzimidazole / Alcohol / Amine / Aminoimidazole / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Azole / Benzenoid show 23 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- HHV-5
Chemical Identifiers
- UNII
- PTB4X93HE1
- CAS number
- 176161-24-3
- InChI Key
- KJFBVJALEQWJBS-XUXIUFHCSA-N
- InChI
- InChI=1S/C15H19Cl2N3O4/c1-6(2)18-15-19-9-3-7(16)8(17)4-10(9)20(15)14-13(23)12(22)11(5-21)24-14/h3-4,6,11-14,21-23H,5H2,1-2H3,(H,18,19)/t11-,12-,13-,14-/m0/s1
- IUPAC Name
- (2S,3S,4R,5S)-2-{5,6-dichloro-2-[(propan-2-yl)amino]-1H-1,3-benzodiazol-1-yl}-5-(hydroxymethyl)oxolane-3,4-diol
- SMILES
- CC(C)NC1=NC2=CC(Cl)=C(Cl)C=C2N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O
References
- Synthesis Reference
Glover BN, Huang LF, Lancaster RW, Long ST, Rizzolio MC, Schmitt EA, Sickles BR. (2010). Crystalline forms of an antiviral benzimidazole compound (US Patent No. US7714123B2).
- General References
- Sun K, Welty D: Elucidation of Metabolic and Disposition Pathways for Maribavir in Nonhuman Primates through Mass Balance and Semi-Physiologically Based Modeling Approaches. Drug Metab Dispos. 2021 Nov;49(11):1025-1037. doi: 10.1124/dmd.121.000493. Epub 2021 Aug 30. [Article]
- Goldwater DR, Dougherty C, Schumacher M, Villano SA: Effect of ketoconazole on the pharmacokinetics of maribavir in healthy adults. Antimicrob Agents Chemother. 2008 May;52(5):1794-8. doi: 10.1128/AAC.00951-07. Epub 2008 Mar 3. [Article]
- Koszalka GW, Johnson NW, Good SS, Boyd L, Chamberlain SC, Townsend LB, Drach JC, Biron KK: Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 2002 Aug;46(8):2373-80. doi: 10.1128/AAC.46.8.2373-2380.2002. [Article]
- Hakki M: Moving Past Ganciclovir and Foscarnet: Advances in CMV Therapy. Curr Hematol Malig Rep. 2020 Apr;15(2):90-102. doi: 10.1007/s11899-020-00557-6. [Article]
- FDA Approved Drug Products: Livtencity (maribavir) tablets for oral use [Link]
- FDA News Release: FDA Approves First Treatment for Common Type of Post-Transplant Infection that is Resistant to Other Drugs [Link]
- Health Canada Approved Drug Products: LIVTENCITY (maribavir) Oral Tablets [Link]
- EMA Approved Drug Products: LIVTENCITY (maribavir) Oral Tablets [Link]
- Takeda: European Commission (EC) Approves LIVTENCITYTM▼ (maribavir) for the Treatment of Adults With Post-transplant Cytomegalovirus (CMV) Infection And/or Disease That Are Refractory (With or Without Resistance) to One or More Prior Therapies [Link]
- External Links
- ChemSpider
- 413807
- 2586068
- ChEMBL
- CHEMBL515408
- ZINC
- ZINC000003824412
- Wikipedia
- Maribavir
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 Not Yet Recruiting Not Available Cytomegalovirus (CMV) 2 somestatus stop reason just information to hide 4 Recruiting Prevention CMV / Transplantation complications 1 somestatus stop reason just information to hide 3 Completed Prevention Cytomegalovirus (CMV) Infections 2 somestatus stop reason just information to hide 3 Completed Treatment Cytomegalovirus (CMV) 3 somestatus stop reason just information to hide 3 Not Yet Recruiting Treatment Cytomegalovirus (CMV) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 200 mg Tablet, coated Oral 200 mg/1 Tablet, film coated Oral 200 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US11684632 No 2012-01-04 2032-01-04 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.72 mg/mL ALOGPS logP 2.15 ALOGPS logP 1.84 Chemaxon logS -2.7 ALOGPS pKa (Strongest Acidic) 12.45 Chemaxon pKa (Strongest Basic) 6.38 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 99.77 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 90.01 m3·mol-1 Chemaxon Polarizability 37.49 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 splash10-002f-0095000000-6ef44332dfa1629cdc72 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-00e9-0079000000-ff97fec70a7880b739f7 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-052f-0092000000-274a477099d51a662b4e Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0gx3-0293000000-7f44a4abd9c0a2e9adbb Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0zmi-1196000000-2ed5cf55d4a0a300485c Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0059-3792000000-1db97438d94e9bb7faa0 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 177.5251 predictedDeepCCS 1.0 (2019) [M+H]+ 179.92067 predictedDeepCCS 1.0 (2019) [M+Na]+ 187.14189 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- HHV-5
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine/threonine protein kinase that plays important roles in several processes including nuclear viral egress, viral replication or regulation of host cell cycle progression (PubMed:25339763, PubMed:31291580, PubMed:31548682). Participates in the acquisition of tegument during virion morphogenesis in the nucleus. Phosphorylates the viral nuclear egress complex (NEC) subunits UL50 and UL53 (PubMed:25339763). Redistributes the host nuclear lamina by phosphorylating cellular Lamins-A/C. Plays a role in viral DNA synthesis by phosphorylating the DNA polymerase processivity factor UL44. Stimulates host cell cycle to support viral DNA synthesis by phosphorylating host retinoblastoma/RB1 protein. Additional substrates have been identified including host EF1D or H2B. Phosphorylates also host SAMHD1 and thereby counteracts its antiviral effect by reducing its dNTP hydrolase activity (PubMed:31291580, PubMed:31548682).
- Specific Function
- ATP binding
- Gene Name
- UL97
- Uniprot ID
- P16788
- Uniprot Name
- Serine/threonine protein kinase UL97
- Molecular Weight
- 78231.9 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]
- FDA Approved Drug Products: Livtencity (maribavir) tablets for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981).
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- FDA Approved Drug Products: Livtencity (maribavir) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable).
- Specific Function
- aromatase activity
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58406.915 Da
References
- FDA Approved Drug Products: Livtencity (maribavir) tablets for oral use [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- Koszalka GW, Johnson NW, Good SS, Boyd L, Chamberlain SC, Townsend LB, Drach JC, Biron KK: Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 2002 Aug;46(8):2373-80. doi: 10.1128/AAC.46.8.2373-2380.2002. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Functions as a 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 the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
- Specific Function
- Not Available
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23539.43 Da
References
- Koszalka GW, Johnson NW, Good SS, Boyd L, Chamberlain SC, Townsend LB, Drach JC, Biron KK: Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 2002 Aug;46(8):2373-80. doi: 10.1128/AAC.46.8.2373-2380.2002. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Livtencity (maribavir) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Livtencity (maribavir) tablets for oral use [Link]
Drug created at March 19, 2008 16:18 / Updated at December 23, 2022 00:49