NAV

Brincidofovir

Identification

Summary

Brincidofovir is an oral lipid prodrug of cidofovir used in the treatment of human smallpox disease.

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
Thumb
Similar Structures
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

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

TargetActionsOrganism
ADNA polymerase
inhibitor
Variola virus
AVariola virus DNA
incorporation into and destabilization
Variola 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
Adverseeffects
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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.
DrugInteraction
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interactions in your software
AcetylcysteineThe serum concentration of Brincidofovir can be increased when it is combined with Acetylcysteine.
Aminohippuric acidThe serum concentration of Brincidofovir can be increased when it is combined with Aminohippuric acid.
AmprenavirThe serum concentration of Brincidofovir can be increased when it is combined with Amprenavir.
ApalutamideThe excretion of Brincidofovir can be increased when combined with Apalutamide.
AsunaprevirThe serum concentration of Brincidofovir can be increased when it is combined with Asunaprevir.
AtalurenThe serum concentration of Brincidofovir can be increased when it is combined with Ataluren.
AtazanavirThe serum concentration of Brincidofovir can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Brincidofovir can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Brincidofovir can be increased when it is combined with Axitinib.
BaricitinibThe serum concentration of Brincidofovir can be increased when it is combined with Baricitinib.
Interactions
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Food Interactions
  • Take on an empty stomach. Brincidofovir is best absorbed on an empty stomach or alongside a low-fat meal.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Brincidofovir sodium8UN8SA9Z5C496765-79-8CRDDLOITBKEPRN-UQIIZPHYSA-M
Active Moieties
NameKindUNIICASInChI Key
Cidofovirprodrug768M1V522C113852-37-2VWFCHDSQECPREK-LURJTMIESA-N
International/Other Brands
Tembexa (Chimerix)

Categories

Drug Categories
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
  8. FDA News Release: FDA approves drug to treat smallpox [Link]
  9. FDA MCM Regulatory Science: Animal Rule Information [Link]
PubChem Compound
483477
PubChem Substance
347828447
ChemSpider
424003
ChEMBL
CHEMBL203321
ZINC
ZINC000014141521
Wikipedia
Brincidofovir

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentAdenovirus Infections1
3CompletedTreatmentCMV1
3CompletedTreatmentDouble-stranded DNA Virus1
3TerminatedPreventionCytomegalovirus Disease1
3TerminatedPreventionCytomegalovirus Disease / Kidney Transplant Infection1
2CompletedPreventionCytomegalovirus (CMV) Infection1
2CompletedTreatmentAdenovirus Disease1
2TerminatedTreatmentAdenovirus1
2WithdrawnTreatmentAdenovirus1
2WithdrawnTreatmentEbola Viruses1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9303051No2011-08-312031-08-31US flag
US10112909No2014-10-102034-10-10US flag
US10487061No2014-10-102034-10-10US flag
US9371344No2014-10-102034-10-10US flag
US8962829No2014-10-102034-10-10US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityPractically insolublehttps://www.chimerix.com/wp-content/uploads/2021/06/TEMBEXA-USPI-and-PPI-04June2021.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00124 mg/mLALOGPS
logP4.4ALOGPS
logP4.42ChemAxon
logS-5.6ALOGPS
pKa (Strongest Acidic)1.32ChemAxon
pKa (Strongest Basic)4.66ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area143.91 Å2ChemAxon
Rotatable Bond Count26ChemAxon
Refractivity149.9 m3·mol-1ChemAxon
Polarizability65.31 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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Details1. DNA polymerase
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
  1. Griffiths P, Lumley S: Cytomegalovirus. Curr Opin Infect Dis. 2014 Dec;27(6):554-9. doi: 10.1097/QCO.0000000000000107. [Article]
  2. 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]
  3. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details2. Variola virus DNA
Kind
Nucleotide
Organism
Variola virus
Pharmacological action
Yes
Actions
Incorporation into and destabilization
A portion of the Variola virus genome meant to represent Variola viral DNA as a drug target.
References
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]

Enzymes

Details1. Leukotriene-B(4) omega-hydroxylase 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details2. Sphingomyelin phosphodiesterase
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details3. Cytochrome P450 1A2
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details4. Cytochrome P450 2B6
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details5. Cytochrome P450 2C8
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details6. Cytochrome P450 2C9
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details7. Cytochrome P450 2C19
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details8. Cytochrome P450 2D6
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]

Transporters

Details1. Solute carrier organic anion transporter family member 1B1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details2. Solute carrier organic anion transporter family member 1B3
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details3. ATP-binding cassette sub-family G member 2
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details4. Canalicular multispecific organic anion transporter 1
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details5. Solute carrier family 22 member 6
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details6. Solute carrier family 22 member 8
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]
Details7. Bile salt export pump
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
  1. FDA Approved Drug Products: Tembexa (brincidofovir) for oral administration [Link]

Drug created on October 20, 2016 21:29 / Updated on June 16, 2021 12:31