NAV

Tenofovir

Identification

Summary

Tenofovir is a nucleotide analog indicated in the treatment of HIV infections.

Generic Name
Tenofovir
DrugBank Accession Number
DB14126
Background

Tenofovir is an acyclic nucleotide diester analog of adenosine monophosphate.4 In the most strict sense and due to the fact that it presents a phosphate group bound to the nitrogenous base, it is determined as an actual nucleotide analog.4 The antiviral activities of tenofovir were first reported in 1993 and this agent was commercially available since 2008 in the form of tenofovir disoproxil and tenofovir alafenamide in order to obtain oral bioavailability.3,6

Type
Small Molecule
Groups
Experimental, Investigational
Structure
3D
Similar Structures
Weight
Average: 287.2123
Monoisotopic: 287.078340473
Chemical Formula
C9H14N5O4P
Synonyms
  • (R)-PMPA
  • Anhydrous tenofovir
  • Tenofovir
  • Tenofovir (anh.)
  • Tenofovir (anhydrous)
  • Tenofovir anhydrous
External IDs
  • GS 1275
  • GS-1275
Poor quality drug data slowing you down?
Unlock 38% more drug discovery time and eliminate decision-making doubts with this one-stop guide to quality drug data.
Download eBook
Poor quality drug data slowing you down?
Download eBook

Pharmacology

Indication

Tenofovir has been shown to be effective against HIV, herpes simplex virus-2, and hepatitis B virus.5

To know more about the specific product indications, please visit the information in the orally available forms of tenofovir, tenofovir alafenamide and tenofovir disoproxil.

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
Pharmacodynamics

Tenofovir has been shown to be highly effective in patients that have never had an antiretroviral therapy and it seemed to have lower toxicity than other antivirals such as stavudine. In phase 3 clinical trials, tenofovir presented a similar efficacy than efavirenz in treatment-naive HIV patients.5 In hepatitis B infected patients, after one year of tenofovir treatment, the viral DNA levels were undetectable.6

Mechanism of action

Once tenofovir is activated by a bi-phosphorylation it acts as an antiviral acyclic nucleoside phosphonate. It is a potent inhibitor of the viral reverse transcriptase with an inhibitory constant of approximately 0.022 micromolar.3

Once activated, tenofovir acts with different mechanisms including the inhibition of viral polymerase causing chain termination and the inhibition of viral synthesis.12 All these activities are attained by its competition with deoxyadenosine 5'-triphosphate in the generation of new viral DNA. Once tenofovir is incorporated in the chain, it induces a chain termination which in order inhibits viral replication.5 The safety of tenofovir relies on its low affinity towards the cellular DNA polymerase including the mitochondrial DNA polymerase gamma.11

TargetActionsOrganism
AReverse transcriptase/RNaseH
inhibitor
Human immunodeficiency virus 1
AReverse transcriptase
inhibitor
HBV
ADNA polymerase
inhibitor
Human herpesvirus 2 (strain 186)
Absorption

Tenofovir as the active moiety presents a very low bioavailability when orally administered. Hence, the administration of this active agent is required to be under its two prodrug forms, tenofovir disoproxil and tenofovir alafenamide. This reduced absorption is suggested to be related to the presence of two negative charges among its structure. This negative charge limits its cellular penetration, and its passive diffusion across cellular membranes and intestinal mucosa hindering its availability for oral administration.1

Intravenous tenofovir has been shown to produce a maximum plasma concentration of 2500 ng/ml with an AUC of 4800 ng.h/ml.3

Volume of distribution

Accumulation of tenofovir in plasma is related to the presence of nephrotoxic effects.1 It is reported that tenofovir presents a volume of distribution of 0.813 L/kg.7

Protein binding

Tenofovir is minimally bound to plasma proteins and only about 7.2% of the administered dose is found in the bound state.7

Metabolism

Tenofovir activation is performed by a bi-phosphorylation which in order forms the biologically active compound, tenofovir biphosphate.1 This metabolic activation has been shown to be performed in hepG2 cells and human hepatocytes.8

Hover over products below to view reaction partners

Route of elimination

Tenofovir is eliminated in the urine by tubular secretion and glomerular filtration. The elimination of this compound is driven by the activity of the human organic anion transporters 1 and 3 and its secretion is mainly ruled by the activity of the multidrug resistance-associated protein 4.1

Half-life

The reported half-life of tenofovir is of 32 hours.2

Clearance

The clearance of tenofovir is highly dependent on the patient renal stage and hence the clearance rate in patients with renal impairment is reported to be of 134 ml/min while in patients with normal function the clearance rate can be of 210 ml/min.9

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
Toxicity

There haven't been reports regarding the LD50 of the parent compound nor the effects of an overdose. However, based on the reports with the derivative that most rapidly transforms into tenofovir, tenofovir disoproxil, it is recommended to monitor overdose patients. As well, it is widely known that tenofovir is efficiently removed by hemodialysis.10

Administration of high doses of tenofovir has been reported to produce bone toxicity reported as osteomalacia and reduced bone mineral density and to produce some degree of renal toxicity.14

To know more about the carcinogenicity and mutagenic potential of tenofovir, as well as the effect on fertility, please visit the drug entries for the derivatives tenofovir disoproxil and tenofovir alafenamide.

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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
Integrate drug-drug
interactions in your software
AbacavirTenofovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Tenofovir.
AbrocitinibThe serum concentration of Tenofovir can be increased when it is combined with Abrocitinib.
AceclofenacAceclofenac may increase the nephrotoxic activities of Tenofovir.
AcemetacinAcemetacin may increase the nephrotoxic activities of Tenofovir.
Food Interactions
  • Take with food.

Products

Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Product Ingredients
IngredientUNIICASInChI Key
Tenofovir hydrate99YXE507IL206184-49-8PINIEAOMWQJGBW-FYZOBXCZSA-N

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 6-aminopurines. These are purines that carry an amino group at position 6. Purine is a bicyclic aromatic compound made up of a pyrimidine ring fused to an imidazole ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Imidazopyrimidines
Sub Class
Purines and purine derivatives
Direct Parent
6-aminopurines
Alternative Parents
Aminopyrimidines and derivatives / N-substituted imidazoles / Imidolactams / Organic phosphonic acids / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds
show 2 more
Substituents
6-aminopurine / Amine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Azole / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Imidolactam
show 12 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
phosphonic acids (CHEBI:63625)
Affected organisms
  • Herpes simplex virus
  • Hepatitis B virus
  • HIV-1

Chemical Identifiers

UNII
W4HFE001U5
CAS number
147127-20-6
InChI Key
SGOIRFVFHAKUTI-ZCFIWIBFSA-N
InChI
InChI=1S/C9H14N5O4P/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17)/t6-/m1/s1
IUPAC Name
({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonic acid
SMILES
C[C@H](CN1C=NC2=C1N=CN=C2N)OCP(O)(O)=O

References

General References
  1. Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192. [Article]
  2. Deeks ED: Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7. [Article]
  3. Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27. [Article]
  4. Margolis AM, Heverling H, Pham PA, Stolbach A: A review of the toxicity of HIV medications. J Med Toxicol. 2014 Mar;10(1):26-39. doi: 10.1007/s13181-013-0325-8. [Article]
  5. McConville C, Boyd P, Major I: Efficacy of Tenofovir 1% Vaginal Gel in Reducing the Risk of HIV-1 and HSV-2 Infection. Clin Med Insights Womens Health. 2014 Feb 13;7:1-8. doi: 10.4137/CMWH.S10353. eCollection 2014. [Article]
  6. Ridruejo E: Treatment of chronic hepatitis B in clinical practice with entecavir or tenofovir. World J Gastroenterol. 2014 Jun 21;20(23):7169-80. doi: 10.3748/wjg.v20.i23.7169. [Article]
  7. Fung HB, Stone EA, Piacenti FJ: Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48. [Article]
  8. Delaney WE 4th, Ray AS, Yang H, Qi X, Xiong S, Zhu Y, Miller MD: Intracellular metabolism and in vitro activity of tenofovir against hepatitis B virus. Antimicrob Agents Chemother. 2006 Jul;50(7):2471-7. doi: 10.1128/AAC.00138-06. [Article]
  9. Kearney BP, Yale K, Shah J, Zhong L, Flaherty JF: Pharmacokinetics and dosing recommendations of tenofovir disoproxil fumarate in hepatic or renal impairment. Clin Pharmacokinet. 2006;45(11):1115-24. doi: 10.2165/00003088-200645110-00005. [Article]
  10. Izzedine H, Launay-Vacher V, Jullien V, Aymard G, Duvivier C, Deray G: Pharmacokinetics of tenofovir in haemodialysis. Nephrol Dial Transplant. 2003 Sep;18(9):1931-3. doi: 10.1093/ndt/gfg327. [Article]
  11. Sivapalasingam S., Steigbigel N. (2015). Mandell, Douglas and Bennett's Principles and practice of infectious diseases (8th ed.). Elsevier.
  12. Pubmed books [Link]
  13. FDA Approved Drug Products: Bictegravir, Emtricitabine, and Tenofovir Alafenamide Oral Tablets [Link]
  14. FDA Approved Drug Products: VIREAD (tenofovir disoproxil fumarate), for oral use [Link]
  15. INVIMA: Emtricitabine and Tenofovir Oral Tablet [Link]
Human Metabolome Database
HMDB0014445
ChemSpider
408154
BindingDB
50450813
RxNav
117466
ChEBI
63625
ChEMBL
CHEMBL483
ZINC
ZINC000001543475
PharmGKB
PA10204
PDBe Ligand
TFO
Wikipedia
Tenofovir_disoproxil
PDB Entries
1t03 / 8bvs
MSDS
Download (79.7 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAcute HIV Infection1
4Active Not RecruitingTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection2
4Active Not RecruitingTreatmentViral Hepatitis B1
4CompletedNot AvailableHealthy Subjects (HS)1
4CompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)279 ºC'ChemicalBook'
boiling point (°C)616 ºC at 760 mmHg'MSDS'
water solubility13.4 mg/ml'ChemicalBook'
logP-1.6Lastours V. et al. 2011. Antimicrob Agents Chemother.
pKa3.8 and 6.7Zhang T. et al. 2012. Eur J Pharm Biopharm.
Predicted Properties
PropertyValueSource
Water Solubility1.87 mg/mLALOGPS
logP-1.5ALOGPS
logP-3.4Chemaxon
logS-2.2ALOGPS
pKa (Strongest Acidic)1.35Chemaxon
pKa (Strongest Basic)3.74Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count8Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area136.38 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity67.54 m3·mol-1Chemaxon
Polarizability25.54 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0002-2920000000-93fa3e16e2deed5b1e92
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-000i-0290000000-3e1938b3d02b375e35df
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001r-1930000000-d365f36771addeb5b51c
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-2900000000-c8f91e6bb9d4588f055d
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-2900000000-099f967e8f8229f1fb82
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-3900000000-521761795a56429a8f51
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-06si-5900000000-b88fc7e5619f18889624
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-0090000000-e85e6b9ea88e6c214687
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-0190000000-405fbe60309faffed10c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004r-0950000000-d7cec4ba580879c76061
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0910000000-f2abf612e945d8c69371
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-056r-1900000000-c48435c099065334ef3e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0570-1900000000-7b90db7cba32420df6d1
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0190000000-98bc38f0c3a428241c75
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-6f9751e1d101c43ba894
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0920000000-8478d55592f6b67418b2
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03gi-9360000000-1a03b9d8134cad207667
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-1900000000-d375901232a9891e38f7
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-01si-9600000000-52c5a51d7959e22f3d6c
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0190000000-98bc38f0c3a428241c75
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-6f9751e1d101c43ba894
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0920000000-8478d55592f6b67418b2
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03gi-9360000000-1a03b9d8134cad207667
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-1900000000-d375901232a9891e38f7
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-01si-9600000000-52c5a51d7959e22f3d6c
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-166.1954645
predicted
DarkChem Lite v0.1.0
[M-H]-165.3513645
predicted
DarkChem Lite v0.1.0
[M-H]-149.29541
predicted
DeepCCS 1.0 (2019)
[M-H]-166.1954645
predicted
DarkChem Lite v0.1.0
[M-H]-165.3513645
predicted
DarkChem Lite v0.1.0
[M-H]-149.29541
predicted
DeepCCS 1.0 (2019)
[M+H]+166.0326645
predicted
DarkChem Lite v0.1.0
[M+H]+164.1548645
predicted
DarkChem Lite v0.1.0
[M+H]+151.69096
predicted
DeepCCS 1.0 (2019)
[M+H]+166.0326645
predicted
DarkChem Lite v0.1.0
[M+H]+164.1548645
predicted
DarkChem Lite v0.1.0
[M+H]+151.69096
predicted
DeepCCS 1.0 (2019)
[M+Na]+165.9300645
predicted
DarkChem Lite v0.1.0
[M+Na]+157.69391
predicted
DeepCCS 1.0 (2019)
[M+Na]+165.9300645
predicted
DarkChem Lite v0.1.0
[M+Na]+157.69391
predicted
DeepCCS 1.0 (2019)

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Details1. Reverse transcriptase/RNaseH
Kind
Protein
Organism
Human immunodeficiency virus 1
Pharmacological action
Yes
Actions
Inhibitor
General Function
Rna-dna hybrid ribonuclease activity
Specific Function
Not Available
Gene Name
pol
Uniprot ID
Q72547
Uniprot Name
Reverse transcriptase/RNaseH
Molecular Weight
65223.615 Da
References
  1. McConville C, Boyd P, Major I: Efficacy of Tenofovir 1% Vaginal Gel in Reducing the Risk of HIV-1 and HSV-2 Infection. Clin Med Insights Womens Health. 2014 Feb 13;7:1-8. doi: 10.4137/CMWH.S10353. eCollection 2014. [Article]
  2. Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27. [Article]
  3. Cost M, Dezzutti CS, Clark MR, Friend DR, Akil A, Rohan LC: Characterization of UC781-tenofovir combination gel products for HIV-1 infection prevention in an ex vivo ectocervical model. Antimicrob Agents Chemother. 2012 Jun;56(6):3058-66. doi: 10.1128/AAC.06284-11. Epub 2012 Mar 19. [Article]
Details2. Reverse transcriptase
Kind
Protein
Organism
HBV
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Rna-directed dna polymerase activity
Gene Name
rt
Uniprot ID
Q3MS49
Uniprot Name
Reverse transcriptase
Molecular Weight
4735.565 Da
References
  1. Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27. [Article]
  2. McConville C, Boyd P, Major I: Efficacy of Tenofovir 1% Vaginal Gel in Reducing the Risk of HIV-1 and HSV-2 Infection. Clin Med Insights Womens Health. 2014 Feb 13;7:1-8. doi: 10.4137/CMWH.S10353. eCollection 2014. [Article]
  3. Friend DR: Pharmaceutical development of microbicide drug products. Pharm Dev Technol. 2010 Dec;15(6):562-81. doi: 10.3109/10837450903369879. Epub 2009 Dec 17. [Article]
Details3. DNA polymerase
Kind
Protein
Organism
Human herpesvirus 2 (strain 186)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Dna binding
Gene Name
Not Available
Uniprot ID
I6TLU5
Uniprot Name
DNA polymerase
Molecular Weight
137296.405 Da
References
  1. McConville C, Boyd P, Major I: Efficacy of Tenofovir 1% Vaginal Gel in Reducing the Risk of HIV-1 and HSV-2 Infection. Clin Med Insights Womens Health. 2014 Feb 13;7:1-8. doi: 10.4137/CMWH.S10353. eCollection 2014. [Article]
  2. Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27. [Article]

Enzymes

Details1. Nucleoside diphosphate kinase A
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Ribosomal small subunit binding
Specific Function
Major role in the synthesis of nucleoside triphosphates other than ATP. The ATP gamma phosphate is transferred to the NDP beta phosphate via a ping-pong mechanism, using a phosphorylated active-sit...
Gene Name
NME1
Uniprot ID
P15531
Uniprot Name
Nucleoside diphosphate kinase A
Molecular Weight
17148.635 Da
Details2. Nucleoside diphosphate kinase B
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transcription factor activity, sequence-specific dna binding
Specific Function
Major role in the synthesis of nucleoside triphosphates other than ATP. Negatively regulates Rho activity by interacting with AKAP13/LBC. Acts as a transcriptional activator of the MYC gene; binds ...
Gene Name
NME2
Uniprot ID
P22392
Uniprot Name
Nucleoside diphosphate kinase B
Molecular Weight
17297.935 Da
Details3. Adenylate kinase isoenzyme 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Nucleoside diphosphate kinase activity
Specific Function
Catalyzes the reversible transfer of the terminal phosphate group between ATP and AMP. Also displays broad nucleoside diphosphate kinase activity. Plays an important role in cellular energy homeost...
Gene Name
AK1
Uniprot ID
P00568
Uniprot Name
Adenylate kinase isoenzyme 1
Molecular Weight
21634.725 Da
Details4. Adenylate kinase 2, mitochondrial
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Atp binding
Specific Function
Catalyzes the reversible transfer of the terminal phosphate group between ATP and AMP. Plays an important role in cellular energy homeostasis and in adenine nucleotide metabolism. Adenylate kinase ...
Gene Name
AK2
Uniprot ID
P54819
Uniprot Name
Adenylate kinase 2, mitochondrial
Molecular Weight
26477.44 Da

Carriers

Details1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Deeks ED: Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7. [Article]

Transporters

Details1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Murakami E, Wang T, Park Y, Hao J, Lepist EI, Babusis D, Ray AS: Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy. Antimicrob Agents Chemother. 2015;59(6):3563-9. doi: 10.1128/AAC.00128-15. Epub 2015 Apr 13. [Article]
  2. Droste JA, Verweij-van Wissen CP, Kearney BP, Buffels R, Vanhorssen PJ, Hekster YA, Burger DM: Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers. Antimicrob Agents Chemother. 2005 Feb;49(2):680-4. doi: 10.1128/AAC.49.2.680-684.2005. [Article]
  3. Begley R, Das M, Zhong L, Ling J, Kearney BP, Custodio JM: Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals. J Acquir Immune Defic Syndr. 2018 Aug 1;78(4):465-472. doi: 10.1097/QAI.0000000000001699. [Article]
  4. Custodio JM, Fordyce M, Garner W, Vimal M, Ling KH, Kearney BP, Ramanathan S: Pharmacokinetics and Safety of Tenofovir Alafenamide in HIV-Uninfected Subjects with Severe Renal Impairment. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5135-40. doi: 10.1128/AAC.00005-16. Print 2016 Sep. [Article]
  5. Moss DM, Domanico P, Watkins M, Park S, Randolph R, Wring S, Rajoli RKR, Hobson J, Rannard S, Siccardi M, Owen A: Simulating Intestinal Transporter and Enzyme Activity in a Physiologically Based Pharmacokinetic Model for Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: AAC.00105-17. doi: 10.1128/AAC.00105-17. Print 2017 Jul. [Article]
  6. Soriano V, Labarga P, Fernandez-Montero JV, Mendoza C, Benitez-Gutierrez L, Pena JM, Barreiro P: Drug interactions in HIV-infected patients treated for hepatitis C. Expert Opin Drug Metab Toxicol. 2017 Aug;13(8):807-816. doi: 10.1080/17425255.2017.1351942. Epub 2017 Jul 13. [Article]
Details2. Solute carrier family 22 member 6
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192. [Article]
Details3. Solute carrier family 22 member 8
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192. [Article]
Details4. Multidrug resistance-associated protein 4
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192. [Article]

Drug created at June 24, 2018 16:23 / Updated at July 03, 2021 01:49