Identification
- Summary
Brincidofovir is an oral lipid prodrug of cidofovir used in the treatment of human smallpox disease.
- Brand Names
- Tembexa
- Generic Name
- Brincidofovir
- DrugBank Accession Number
- DB12151
- Background
Brincidofovir is an oral antiviral drug used in the treatment of human smallpox infections. It is a lipid conjugate pro-drug of the acyclic nucleotide analogue cidofovir7,3 - this lipid conjugate improves drug delivery to the target cells and significantly reduces the nephrotoxicity typically associated with cidofovir therapy.3,4 Due to its formulation as a pro-drug brincidofovir also carries a greater bioavailability than cidofovir,5,3 allowing for oral administration rather than intravenous. Cidofovir itself has broad antiviral activity against several DNA viruses,3 resulting in brincidofovir being investigated for the prevention and treatment of cytomegalovirus (CMV), BK Virus (BKV), adenoviruses (AdV), and Epstein-Barr virus (EBV), amongst others.
Brincidofovir, developed by Chimerix under the brand name Tembexa, was approved by the FDA for the treatment of smallpox infection in June 2021.8 As smallpox has been eradicated, the efficacy of Tembexa was assessed in animals infected with viruses closely related to variola. The approval was granted under the agency’s Animal Rule,9 which allows for a drug to be approved based on the results of well-controlled animal studies when human trials would be unethical or infeasible.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Brincidofovir (DB12151)
- Weight
- Average: 561.701
Monoisotopic: 561.354288024 - Chemical Formula
- C27H52N3O7P
- Synonyms
- Brincidofovir
- Cidofovir hexadecyloxypropyl ester
- External IDs
- CMX 001
- CMX-001
- CMX001
Pharmacology
- Indication
Brincidofovir is indicated for the treatment of human smallpox disease in adult and pediatric patients.7
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
- 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 pharmacologically active agent resulting from brincidofovir metabolism, cidofovir diphosphate, has an exceedingly long duration of action that allows for it to be dosed once weekly. The entirety of a brincidofovir smallpox treatment consists of only two doses, on days 1 and 8, which seemingly reduces the risk of adverse reactions. Regimens involving a longer duration of administration (i.e. more than a single dose on days 1 and 8) have been shown to increase mortality compared to placebo and should therefore be avoided.7 Brincidofovir is considered a potential human carcinogen and has demonstrated the potential to cause infertility7 - as such, its use should be restricted to situations in which it is absolutely necessary.
- Mechanism of action
Brincidofovir is a pro-drug comprising cidofovir conjugated to a lipid molecule - the lipid component mimics an endogenous lipid, lysophosphatidylcholine, which allows the molecule to hijack endogenous lipid uptake pathways to enter infected cells.7,4 Following uptake, the lipid molecule is cleaved to generate cidofovir, which is then phosphorylated to generate the active antiviral compound, cidofovir disphosphate.7
The antiviral effects of cidofovir diphosphate appear to be the result of two distinct mechanisms. Mechanistic studies using recombinant vaccinia DNA polymerase suggest that it inhibits orthopoxvirus DNA polymerase-mediated DNA synthesis. In addition, cidofovir is an acyclic nucleotide analogue of deoxycytidine monophosphate - cidofovir diphosphate can therefore be incorporated into the growing viral DNA chain and consequently slow the rate of viral DNA synthesis.7,3
Target Actions Organism ADNA polymerase inhibitorVariola virus AVariola virus DNA incorporation into and destabilizationVariola virus - Absorption
The oral bioavailability of brincidofovir is 13.4% in its tablet formulation and 16.8% in its suspension formulation.7 Following oral administration, the Cmax and AUCtau of brincidofovir were 480 ng/mL and 3400 ng·hr/mL, respectively. The Cmax and AUCtau of the active metabolite, cidofovir diphosphate, were 9.7 pg/106 cells and 1200 pg·hr/106 cells, respectively.7
Maximum plasma concentrations (Tmax) of brincidofovir are reached at approximately 3 hours post-administration, while maximal plasma concentrations for cidofovir diphosphate are reached at approximately 47 hours post-administration.7
- Volume of distribution
The apparent volume of distribution of brincidofovir is 1230 L.7
- Protein binding
Brincidofovir is >99% protein-bound in plasma,7,4 although the specific protein(s) to which it binds have not been elucidated.
- Metabolism
Brincidofovir is a pro-drug of cidofovir and as such must undergo some basic metabolic reactions to become pharmacologically active. Upon entering the target cell, the phosphodiester bond of brincidofovir is hydrolyzed to generate cidofovir, which is then phosphorylated to generate the active agent: cidofovir diphosphate.7 The specific enzyme(s) responsible for this reaction have not been elucidated, but in vitro findings suggest sphingomyelin phosphodiesterase plays a major role in the initial hydrolysis of brincidofovir.7
There are two major inactive metabolites of brincidofovir, CMX103 and CMX064, which are generated via carboxylation of the terminal carbon followed by several cycles of CYP-mediated oxidative reactions and fatty acid oxidation.7,4 These reactions are mediated, at least in part, by CYP4F2.7
Hover over products below to view reaction partners
- Route of elimination
Brincidofovir is eliminated as metabolites in both the urine (~51%) and feces (~40%).7
- Half-life
The mean terminal half-lives of brincidofovir and its pharmacologically active metabolite, cidofovir diphosphate, are 19.3 hours and 113 hours, respectively.7
- Clearance
The apparent clearance of brincidofovir in healthy adult patients is 44.1 L/h.7
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is no clinical experience with brincidofovir overdose. Patients experiencing overdosage should be monitored closely and provided supportive therapy as clinically indicated.7
- 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 softwareAcetylcysteine The serum concentration of Brincidofovir can be increased when it is combined with Acetylcysteine. Aminohippuric acid The serum concentration of Brincidofovir can be increased when it is combined with Aminohippuric acid. Amprenavir The serum concentration of Brincidofovir can be increased when it is combined with Amprenavir. Apalutamide The excretion of Brincidofovir can be increased when combined with Apalutamide. Asunaprevir The serum concentration of Brincidofovir can be increased when it is combined with Asunaprevir. Ataluren The serum concentration of Brincidofovir can be increased when it is combined with Ataluren. Atazanavir The serum concentration of Brincidofovir can be increased when it is combined with Atazanavir. Atorvastatin The serum concentration of Brincidofovir can be increased when it is combined with Atorvastatin. Axitinib The serum concentration of Brincidofovir can be increased when it is combined with Axitinib. Beclomethasone dipropionate The serum concentration of Brincidofovir can be increased when it is combined with Beclomethasone dipropionate. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take on an empty stomach. Brincidofovir is best absorbed on an empty stomach or alongside a low-fat meal.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Brincidofovir sodium 8UN8SA9Z5C 496765-79-8 CRDDLOITBKEPRN-UQIIZPHYSA-M - Active Moieties
Name Kind UNII CAS InChI Key Cidofovir prodrug 768M1V522C 113852-37-2 VWFCHDSQECPREK-LURJTMIESA-N - International/Other Brands
- Tembexa (Chimerix)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Tembexa Suspension 10 mg/1mL Oral Chimerix, Inc. 2022-04-20 Not applicable US 
Tembexa Tablet, film coated 100 mg/1 Oral Chimerix, Inc. 2022-04-20 Not applicable US
Categories
- Drug Categories
- Anti-Infective Agents
- Antiviral Agents
- BCRP/ABCG2 Inhibitors
- BSEP/ABCB11 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytomegalovirus Nucleoside Analog DNA Polymerase Inhibitor
- OAT1/SLC22A6 inhibitors
- OAT3/SLC22A8 Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 substrates
- Organophosphorus Compounds
- Pyrimidines
- Pyrimidinones
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as pyrimidones. These are compounds that contain a pyrimidine ring, which bears a ketone. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazines
- Sub Class
- Pyrimidines and pyrimidine derivatives
- Direct Parent
- Pyrimidones
- Alternative Parents
- Aminopyrimidines and derivatives / Phosphonic acid esters / Imidolactams / Hydropyrimidines / Organic phosphonic acids / Heteroaromatic compounds / Dialkyl ethers / Azacyclic compounds / Primary amines / Primary alcohols show 4 more
- Substituents
- Alcohol / Amine / Aminopyrimidine / Aromatic heteromonocyclic compound / Azacycle / Dialkyl ether / Ether / Heteroaromatic compound / Hydrocarbon derivative / Hydropyrimidine show 14 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Human Cytomegalovirus
- Variola virus
Chemical Identifiers
- UNII
- 6794O900AX
- CAS number
- 444805-28-1
- InChI Key
- WXJFKKQWPMNTIM-VWLOTQADSA-N
- InChI
- InChI=1S/C27H52N3O7P/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-19-35-20-16-21-37-38(33,34)24-36-25(23-31)22-30-18-17-26(28)29-27(30)32/h17-18,25,31H,2-16,19-24H2,1H3,(H,33,34)(H2,28,29,32)/t25-/m0/s1
- IUPAC Name
- ({[(2S)-1-(4-amino-2-oxo-1,2-dihydropyrimidin-1-yl)-3-hydroxypropan-2-yl]oxy}methyl)[3-(hexadecyloxy)propoxy]phosphinic acid
- SMILES
- CCCCCCCCCCCCCCCCOCCCOP(O)(=O)CO[C@H](CO)CN1C=CC(N)=NC1=O
References
- Synthesis Reference
Hostetler KY: Synthesis and early development of hexadecyloxypropylcidofovir: an oral antipoxvirus nucleoside phosphonate. Viruses. 2010 Oct;2(10):2213-25. doi: 10.3390/v2102213. Epub 2010 Sep 30.
- General References
- Quenelle DC, Prichard MN, Keith KA, Hruby DE, Jordan R, Painter GR, Robertson A, Kern ER: Synergistic efficacy of the combination of ST-246 with CMX001 against orthopoxviruses. Antimicrob Agents Chemother. 2007 Nov;51(11):4118-24. Epub 2007 Aug 27. [Article]
- Parker S, Touchette E, Oberle C, Almond M, Robertson A, Trost LC, Lampert B, Painter G, Buller RM: Efficacy of therapeutic intervention with an oral ether-lipid analogue of cidofovir (CMX001) in a lethal mousepox model. Antiviral Res. 2008 Jan;77(1):39-49. Epub 2007 Sep 4. [Article]
- Delaune D, Iseni F: Drug Development against Smallpox: Present and Future. Antimicrob Agents Chemother. 2020 Mar 24;64(4). pii: AAC.01683-19. doi: 10.1128/AAC.01683-19. Print 2020 Mar 24. [Article]
- Tippin TK, Morrison ME, Brundage TM, Mommeja-Marin H: Brincidofovir Is Not a Substrate for the Human Organic Anion Transporter 1: A Mechanistic Explanation for the Lack of Nephrotoxicity Observed in Clinical Studies. Ther Drug Monit. 2016 Dec;38(6):777-786. doi: 10.1097/FTD.0000000000000353. [Article]
- Painter W, Robertson A, Trost LC, Godkin S, Lampert B, Painter G: First pharmacokinetic and safety study in humans of the novel lipid antiviral conjugate CMX001, a broad-spectrum oral drug active against double-stranded DNA viruses. Antimicrob Agents Chemother. 2012 May;56(5):2726-34. doi: 10.1128/AAC.05983-11. Epub 2012 Mar 5. [Article]
- Hostetler KY: Synthesis and early development of hexadecyloxypropylcidofovir: an oral antipoxvirus nucleoside phosphonate. Viruses. 2010 Oct;2(10):2213-25. doi: 10.3390/v2102213. Epub 2010 Sep 30. [Article]
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- FDA News Release: FDA approves drug to treat smallpox [Link]
- FDA MCM Regulatory Science: Animal Rule Information [Link]
- External Links
- PubChem Compound
- 483477
- PubChem Substance
- 347828447
- ChemSpider
- 424003
- ChEMBL
- CHEMBL203321
- ZINC
- ZINC000014141521
- Wikipedia
- Brincidofovir
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Adenovirus Infections 1 3 Completed Treatment CMV 1 3 Completed Treatment Double-stranded DNA Virus 1 3 Terminated Prevention Cytomegalovirus Disease 1 3 Terminated Prevention Cytomegalovirus Disease / Kidney Transplant Infection 1 2 Completed Prevention Cytomegalovirus (CMV) Infection 1 2 Completed Treatment Adenovirus Disease 1 2 Terminated Treatment Adenovirus 1 2 Withdrawn Treatment Adenovirus 1 2 Withdrawn Treatment Ebola Viruses 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Suspension Oral 10 mg/1mL Tablet, film coated Oral 100 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9303051 No 2016-04-05 2031-08-31 US US10112909 No 2018-10-30 2034-10-10 US US10487061 No 2019-11-26 2034-10-10 US US9371344 No 2016-06-21 2034-10-10 US US8962829 No 2015-02-24 2034-10-10 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Practically insoluble https://www.chimerix.com/wp-content/uploads/2021/06/TEMBEXA-USPI-and-PPI-04June2021.pdf - Predicted Properties
Property Value Source Water Solubility 0.00124 mg/mL ALOGPS logP 4.4 ALOGPS logP 4.42 ChemAxon logS -5.6 ALOGPS pKa (Strongest Acidic) 1.32 ChemAxon pKa (Strongest Basic) 4.66 ChemAxon Physiological Charge -1 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 143.91 Å2 ChemAxon Rotatable Bond Count 26 ChemAxon Refractivity 149.9 m3·mol-1 ChemAxon Polarizability 65.31 Å3 ChemAxon Number of Rings 1 ChemAxon Bioavailability 0 ChemAxon Rule of Five No 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
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
- Organism
- Variola virus
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Catalyzes DNA synthesis. Acquires processivity by associating with a heterodimeric processivity factor comprised of the viral A20 and D4 proteins, thereby forming the DNA polymerase holoenzyme. Displays 3'- to 5' exonuclease activity. Might participate in viral DNA recombination. Does not perform translesion synthesis across an abasic site (By similarity).
- Specific Function
- Dna binding
- Gene Name
- POL
- Uniprot ID
- P0DOO6
- Uniprot Name
- DNA polymerase
- Molecular Weight
- 116714.76 Da
References
- Griffiths P, Lumley S: Cytomegalovirus. Curr Opin Infect Dis. 2014 Dec;27(6):554-9. doi: 10.1097/QCO.0000000000000107. [Article]
- Tippin TK, Morrison ME, Brundage TM, Mommeja-Marin H: Brincidofovir Is Not a Substrate for the Human Organic Anion Transporter 1: A Mechanistic Explanation for the Lack of Nephrotoxicity Observed in Clinical Studies. Ther Drug Monit. 2016 Dec;38(6):777-786. doi: 10.1097/FTD.0000000000000353. [Article]
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Not Available
- Specific Function
- Not Available
- Gene Name
- CYP4F2
- Uniprot ID
- P78329
- Uniprot Name
- Phylloquinone omega-hydroxylase CYP4F2
- Molecular Weight
- 59852.825 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sphingomyelin phosphodiesterase activity
- Specific Function
- Converts sphingomyelin to ceramide. Also has phospholipase C activities toward 1,2-diacylglycerolphosphocholine and 1,2-diacylglycerolphosphoglycerol. Isoform 2 and isoform 3 have lost catalytic ac...
- Gene Name
- SMPD1
- Uniprot ID
- P17405
- Uniprot Name
- Sphingomyelin phosphodiesterase
- Molecular Weight
- 69751.3 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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: Tembexa (brincidofovir) for oral administration [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Drug created at October 20, 2016 21:29 / Updated at June 16, 2021 12:31