Identification
- Summary
Ganciclovir is a DNA polymerase inhibitor used to treat cytomegalovirus and herpetic keratitis of the eye.
- Brand Names
- Cytovene, Zirgan
- Generic Name
- Ganciclovir
- DrugBank Accession Number
- DB01004
- Background
An acyclovir analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ganciclovir (DB01004)
- Weight
- Average: 255.2306
Monoisotopic: 255.096753929 - Chemical Formula
- C9H13N5O4
- Synonyms
- 2-(6-Amino-purin-9-ylmethoxy)-propane-1,3-diol
- 2-amino-9-((1,3-dihydroxypropan-2-yloxy)methyl)-1H-purin-6(9H)-one
- 2-amino-9-((1,3-dihydroxypropan-2-yloxy)methyl)-3H-purin-6(9H)-one
- 2-amino-9-((1,3-dihydroxypropan-2-yloxy)methyl)-9H-purin-6-ol
- 2-Amino-9-(2-hydroxy-1-hydroxymethyl-ethoxymethyl)-1,9-dihydro-purin-6-one
- 2-amino-9-(2-hydroxy-1-hydroxymethylethoxymethyl)-6,9-dihydro-1H-6-purinone
- 9-((2-Hydroxy-1-(hydroxymethyl)ethoxy)methyl)guanine
- 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine
- GA2
- Ganciclovir
- Ganciclovirum
- Gancyclovir
- External IDs
- BW 759U
- BW-759U
- RS-21592
Pharmacology
- Indication
For induction and maintenance in the treatment of cytomegalovirus (CMV) retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS). Also used in the treatment of severe cytomegalovirus (CMV) disease, including CMV pneumonia, CMV gastrointestinal disease, and disseminated CMV infections, in immunocompromised patients.
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 Prophylaxis of Cmv infection •••••••••••• Prophylaxis of Cmv infection ••• ••••• Treatment of Cmv colitis ••• ••••• Treatment of Cmv esophagitis ••• ••••• Treatment of Cmv neurological disease ••• ••••• - 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
Ganciclovir is a synthetic nucleoside analogue of 2'-deoxyguanosine that inhibits replication of herpes viruses both in vitro and in vivo. Sensitive human viruses include cytomegalovirus (CMV), herpes simplex virus -1 and -2 (HSV-1, HSV-2), Epstein-Barr virus (EBV) and varicella zoster virus (VZV), however clinical studies have been limited to assessment of efficacy in patients with CMV infection. Ganciclovir is a prodrug that is structurally similar to acyclovir. It inhibits virus replication by its encorporation into viral DNA. This encorporation inhibits dATP and leads to defective DNA, ceasing or retarding the viral machinery required to spread the virus to other cells.
- Mechanism of action
Ganciclovir's antiviral activity inhibits virus replication. This inhibitory action is highly selective as the drug must be converted to the active form by a virus-encoded cellular enzyme, thymidine kinase (TK). TK catalyzes phosphorylation of ganciclovir to the monophosphate, which is then subsequently converted into the diphosphate by cellular guanylate kinase and into the triphosphate by a number of cellular enzymes. In vitro, ganciclovir triphosphate stops replication of herpes viral DNA. When used as a substrate for viral DNA polymerase, ganciclovir triphosphate competitively inhibits dATP leading to the formation of 'faulty' DNA. This is where ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed.
Target Actions Organism ADNA polymerase catalytic subunit inhibitorHHV-1 ADNA incorporation into and destabilizationHumans AThymidine kinase substrateHHV-1 - Absorption
Poorly absorbed systemically following oral administration. Bioavailability under fasting conditions is approximately 5%, and when administered with food, 6 to 9% (about 30% with a fatty meal).
- Volume of distribution
- 0.74 ± 0.15 L/kg
- Protein binding
1 to 2%
- Metabolism
Little to no metabolism, about 90% of plasma ganciclovir is eliminated unchanged in the urine.
- Route of elimination
Renal excretion of unchanged drug by glomerular filtration and active tubular secretion is the major route of elimination of ganciclovir.
- Half-life
2.5 to 3.6 hours (mean 2.9 hours) when administered intravenously in adults. 3.1 to 5.5 hours when administered orally in adults. Renal function impairment causes a marked increase in half life (9 to 30 hours intravenously, 15.7 to 18.2 hours orally).
- Clearance
- 128 +/- 63 mL/min [Patients with Renal Impairment (Clcr=50-79 mL/min)]
- 57+/- 8 mL/min [Patients with Renal Impairment (Clcr=25-49 mL/min)]
- 30 +/- 13 mL/min [Patients with Renal Impairment (Clcr<25 mL/min)]
- 4.7+/- 2.2 mL/min/kg [pediatric patients, aged 9 months to 12 years]
- 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
Oral, mouse LD50: > 2g/kg. Intravenous, dog LD50: > 150mg/kg. Symptoms of overdose include irreversible pancytopenia, worsening GI symptoms, and acute renal failure. Suspected cancer agent.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir The risk or severity of cytopenia can be increased when Ganciclovir is combined with Abacavir. Abemaciclib The excretion of Abemaciclib can be decreased when combined with Ganciclovir. Acamprosate The excretion of Acamprosate can be decreased when combined with Ganciclovir. Aceclofenac Aceclofenac may decrease the excretion rate of Ganciclovir which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Ganciclovir which could result in a higher serum level. - Food Interactions
- Take with food. Food increases bioavailability.
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 Ganciclovir sodium 02L083W284 107910-75-8 JJICLMJFIKGAAU-UHFFFAOYSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cytovene Powder, for solution 500 mg / vial Intravenous Cheplapharm Arzneimittel Gmbh Germany 1995-12-31 Not applicable Canada 
Cytovene - Cap 250mg Capsule 250 mg / cap Oral Hoffmann La Roche 1995-12-31 2007-08-02 Canada Cytovene Inj 500mg/vial Powder, for solution 500 mg / vial Intravenous Syntex Inc. 1990-12-31 1996-09-30 Canada Cytovene IV Injection, powder, lyophilized, for solution 500 mg/10mL Intravenous H2-Pharma, LLC 1989-06-23 Not applicable US 
Cytovene IV Injection, powder, lyophilized, for solution 500 mg/10mL Intravenous Genentech, Inc. 1989-06-23 2020-01-31 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ganciclovir Injection, solution 50 mg/1mL Intravenous Sagent Pharmaceuticals 2018-02-15 Not applicable US Ganciclovir Injection, powder, lyophilized, for solution 50 mg/1mL Intraventricular Hainan Poly Pharm. Co., Ltd. 2019-02-11 Not applicable US Ganciclovir Injection, powder, lyophilized, for solution 50 mg/1mL Intravenous Bedford Pharmaceuticals 2010-12-30 2010-12-31 US Ganciclovir Injection, powder, lyophilized, for solution 50 mg/1mL Intravenous Hikma Pharmaceuticals USA Inc. 2021-06-17 Not applicable US Ganciclovir Injection, powder, lyophilized, for solution 500 mg/10mL Intravenous Fresenius Kabi USA, LLC 2010-06-28 Not applicable US
Categories
- ATC Codes
- J05AB06 — Ganciclovir
- J05AB — Nucleosides and nucleotides excl. reverse transcriptase inhibitors
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Agents Causing Muscle Toxicity
- Agents that reduce seizure threshold
- Anti-Infective Agents
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- Cytomegalovirus Nucleoside Analog DNA Polymerase Inhibitor
- Direct Acting Antivirals
- Drugs that are Mainly Renally Excreted
- Ganciclovir and prodrug
- Heterocyclic Compounds, Fused-Ring
- MATE 1 Substrates
- MATE 2 Substrates
- MATE substrates
- Nucleic Acid Synthesis Inhibitors
- Nucleoside Analog Antiviral
- Nucleosides and Nucleotides
- Nucleosides and Nucleotides Excl. Reverse Transcriptase Inhibitors
- OAT1/SLC22A6 inhibitors
- OAT3/SLC22A8 Inhibitors
- OCT1 inhibitors
- OCT1 substrates
- Ophthalmologicals
- Purines
- Purinones
- Sensory Organs
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as hypoxanthines. These are compounds containing the purine derivative 1H-purin-6(9H)-one. 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
- Hypoxanthines
- Alternative Parents
- 6-oxopurines / Pyrimidones / Glycerolipids / Aminopyrimidines and derivatives / N-substituted imidazoles / Vinylogous amides / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Primary alcohols show 3 more
- Substituents
- 6-oxopurine / Alcohol / Amine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Azole / Glycerolipid / Heteroaromatic compound / Hydrocarbon derivative show 14 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- oxopurine, 2-aminopurines (CHEBI:465284)
- Affected organisms
- Human Herpes Virus
Chemical Identifiers
- UNII
- P9G3CKZ4P5
- CAS number
- 82410-32-0
- InChI Key
- IRSCQMHQWWYFCW-UHFFFAOYSA-N
- InChI
- InChI=1S/C9H13N5O4/c10-9-12-7-6(8(17)13-9)11-3-14(7)4-18-5(1-15)2-16/h3,5,15-16H,1-2,4H2,(H3,10,12,13,17)
- IUPAC Name
- 2-amino-9-{[(1,3-dihydroxypropan-2-yl)oxy]methyl}-6,9-dihydro-1H-purin-6-one
- SMILES
- NC1=NC2=C(N=CN2COC(CO)CO)C(=O)N1
References
- Synthesis Reference
- US4355032
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015139
- KEGG Drug
- D00333
- PubChem Compound
- 3454
- PubChem Substance
- 46507294
- ChemSpider
- 3336
- BindingDB
- 50237614
- 4678
- ChEBI
- 465284
- ChEMBL
- CHEMBL182
- ZINC
- ZINC000000001505
- Therapeutic Targets Database
- DAP000645
- PharmGKB
- PA449733
- PDBe Ligand
- GA2
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ganciclovir
- PDB Entries
- 1ki2 / 4da6
- FDA label
- Download (489 KB)
- MSDS
- Download (119 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Cytomegalovirus (CMV) Infections 1 4 Completed Prevention Cytomegalovirus (CMV) Infections / DNA Virus Infections / Herpes virus infection 1 4 Completed Treatment Cytomegalovirus (CMV) Infections 2 4 Completed Treatment Cytomegalovirus (CMV) Infections / Hematologic Disease and Disorders 1 4 Completed Treatment Cytomegalovirus Retinitis / Human Immunodeficiency Virus (HIV) Infections 1
Pharmacoeconomics
- Manufacturers
- Roche palo alto llc
- Ranbaxy laboratories ltd
- Bausch and lomb inc
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Packagers
- Alliance Medical Products
- APP Pharmaceuticals
- Bausch & Lomb Inc.
- Bedford Labs
- F Hoffmann La Roche Ltd.
- F Hoffmann-La Roche Ltd.
- JHP Pharmaceuticals LLC
- Physicians Total Care Inc.
- Ranbaxy Laboratories
- Sirion Therapeutics
- Dosage Forms
Form Route Strength Solution Intravenous 543.08 mg Solution Intravenous 500.000 mg Capsule Oral 250 MG Injection, powder, for solution Parenteral 500 MG Capsule Oral Injection, powder, for solution Injection, powder, for solution Intravenous Powder Injection, powder, for solution Intravenous 500 MG Capsule, liquid filled Oral 250 mg Injection, powder, lyophilized, for solution Intravenous 500 mg Capsule Oral 250 mg / cap Powder, for solution Intravenous 500 mg / vial Capsule Oral 500 mg / cap Gel Ophthalmic 0.15 % w/w Capsule Oral 250 mg/1 Capsule Oral 500 mg/1 Injection, powder, lyophilized, for solution Intravenous 50 mg/1mL Injection, powder, lyophilized, for solution Intravenous 500 mg/10mL Injection, powder, lyophilized, for solution Intraventricular 50 mg/1mL Injection, solution Intravenous 2 mg/1mL Injection, solution Intravenous 50 mg/1mL Injection, solution Intravenous 500 mg/10mL Injection, powder, for solution 500 MG Powder, for solution Intravenous Injection, solution, concentrate Intravenous 500 mg/1vial Solution, gel forming / drops Conjunctival 150 mg Injection, solution, concentrate Intravenous 500 mg Injection, solution, concentrate Intravenous 50 mg Solution Intravenous 543.10 mg Injection, solution Intravenous 500 mg Injection Intravenous 500 mg Solution Intravenous 543.000 mg Solution Parenteral 500.000 mg Gel Ophthalmic Gel Ophthalmic 1.5 MG/G Ointment Ophthalmic 0.15 g/100g Solution, gel forming / drops Ophthalmic 0.15 g Gel Ophthalmic 1.500 mg Implant Intravitreal 4.5 mg/1 Implant Intravitreal 4.5 mg / imp Gel Ophthalmic 1.5 mg/1g Injection, powder, lyophilized, for solution 500 mg/1vial Injection, powder, lyophilized, for solution Intravenous 500 mg/1vial - Prices
Unit description Cost Unit Vitrasert 4.5 mg implant 19200.0USD implant Cytovene 500 mg vial 81.06USD vial Cytovene 500 mg/vial 46.41USD vial Zirgan 0.15% ophthalmic gel 33.6USD g Ganciclovir 500 mg capsule 19.66USD capsule Cytovene 500 mg capsule 10.99USD capsule Cytovene 250 mg capsule 5.61USD capsule Ganciclovir 250 mg capsule 4.72USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5378475 No 1995-01-03 2012-01-03 US US9486530 No 2016-11-08 2034-09-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 250 dec °C PhysProp water solubility 4300 mg/L (at 25 °C) MERCK INDEX (1996); pH 7 logP -1.66 SANGSTER (1993) Caco2 permeability -6.27 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 11.5 mg/mL ALOGPS logP -1.8 ALOGPS logP -2.2 Chemaxon logS -1.4 ALOGPS pKa (Strongest Acidic) 10.16 Chemaxon pKa (Strongest Basic) 0.58 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 134.99 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 61.03 m3·mol-1 Chemaxon Polarizability 24.15 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9443 Blood Brain Barrier + 0.9866 Caco-2 permeable - 0.8957 P-glycoprotein substrate Substrate 0.5767 P-glycoprotein inhibitor I Non-inhibitor 0.932 P-glycoprotein inhibitor II Non-inhibitor 0.8381 Renal organic cation transporter Non-inhibitor 0.8459 CYP450 2C9 substrate Non-substrate 0.8907 CYP450 2D6 substrate Non-substrate 0.8225 CYP450 3A4 substrate Non-substrate 0.5919 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.96 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.935 Ames test Non AMES toxic 0.6094 Carcinogenicity Non-carcinogens 0.8875 Biodegradation Not ready biodegradable 0.9368 Rat acute toxicity 2.0348 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9611 hERG inhibition (predictor II) Non-inhibitor 0.8943
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 160.101906 predictedDarkChem Lite v0.1.0 [M-H]- 157.643106 predictedDarkChem Lite v0.1.0 [M-H]- 155.05626 predictedDeepCCS 1.0 (2019) [M+H]+ 159.431206 predictedDarkChem Lite v0.1.0 [M+H]+ 157.667306 predictedDarkChem Lite v0.1.0 [M+H]+ 157.41426 predictedDeepCCS 1.0 (2019) [M+Na]+ 160.061206 predictedDarkChem Lite v0.1.0 [M+Na]+ 164.71614 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- HHV-1
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Rna-dna hybrid ribonuclease activity
- Specific Function
- Replicates viral genomic DNA. The replication complex is composed of six viral proteins: the DNA polymerase, processivity factor, primase, primase-associated factor, helicase, and ssDNA-binding pro...
- Gene Name
- Not Available
- Uniprot ID
- P04293
- Uniprot Name
- DNA polymerase catalytic subunit
- Molecular Weight
- 136419.66 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Boivin G, Goyette N, Gilbert C, Covington E: Analysis of cytomegalovirus DNA polymerase (UL54) mutations in solid organ transplant patients receiving valganciclovir or ganciclovir prophylaxis. J Med Virol. 2005 Nov;77(3):425-9. [Article]
- Wang JT, Yang PW, Lee CP, Han CH, Tsai CH, Chen MR: Detection of Epstein-Barr virus BGLF4 protein kinase in virus replication compartments and virus particles. J Gen Virol. 2005 Dec;86(Pt 12):3215-25. [Article]
- Shi R, Azzi A, Gilbert C, Boivin G, Lin SX: Three-dimensional modeling of cytomegalovirus DNA polymerase and preliminary analysis of drug resistance. Proteins. 2006 Aug 1;64(2):301-7. [Article]
Yes
Incorporation into and destabilization
References
- Martin M, Azzi A, Lin SX, Boivin G: Opposite effect of two cytomegalovirus DNA polymerase mutations on replicative capacity and polymerase activity. Antivir Ther. 2010;15(4):579-86. doi: 10.3851/IMP1565. [Article]
- Boivin G, Goyette N, Gilbert C, Covington E: Analysis of cytomegalovirus DNA polymerase (UL54) mutations in solid organ transplant patients receiving valganciclovir or ganciclovir prophylaxis. J Med Virol. 2005 Nov;77(3):425-9. [Article]
- Marfori JE, Exner MM, Marousek GI, Chou S, Drew WL: Development of new cytomegalovirus UL97 and DNA polymerase mutations conferring drug resistance after valganciclovir therapy in allogeneic stem cell recipients. J Clin Virol. 2007 Feb;38(2):120-5. Epub 2006 Dec 8. [Article]
- Potena L, Holweg CT, Chin C, Luikart H, Weisshaar D, Narasimhan B, Fearon WF, Lewis DB, Cooke JP, Mocarski ES, Valantine HA: Acute rejection and cardiac allograft vascular disease is reduced by suppression of subclinical cytomegalovirus infection. Transplantation. 2006 Aug 15;82(3):398-405. [Article]
- Kind
- Protein
- Organism
- HHV-1
- Pharmacological action
- Yes
- Actions
- Substrate
- General Function
- Thymidine kinase activity
- Specific Function
- In latent infection, may allow the virus to be reactivated and to grow in cells lacking a high concentration of phosphorylated nucleic acid precursors, such as nerve cells that do not replicate the...
- Gene Name
- TK
- Uniprot ID
- Q9QNF7
- Uniprot Name
- Thymidine kinase
- Molecular Weight
- 40896.475 Da
References
- Champness JN, Bennett MS, Wien F, Visse R, Summers WC, Herdewijn P, de Clerq E, Ostrowski T, Jarvest RL, Sanderson MR: Exploring the active site of herpes simplex virus type-1 thymidine kinase by X-ray crystallography of complexes with aciclovir and other ligands. Proteins. 1998 Aug 15;32(3):350-61. [Article]
- Beck C, Cayeux S, Lupton SD, Dorken B, Blankenstein T: The thymidine kinase/ganciclovir-mediated "suicide" effect is variable in different tumor cells. Hum Gene Ther. 1995 Dec;6(12):1525-30. doi: 10.1089/hum.1995.6.12-1525. [Article]
- Garin MI, Garrett E, Tiberghien P, Apperley JF, Chalmers D, Melo JV, Ferrand C: Molecular mechanism for ganciclovir resistance in human T lymphocytes transduced with retroviral vectors carrying the herpes simplex virus thymidine kinase gene. Blood. 2001 Jan 1;97(1):122-9. doi: 10.1182/blood.v97.1.122. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. [Article]
- Wagner DJ, Hu T, Wang J: Polyspecific organic cation transporters and their impact on drug intracellular levels and pharmacodynamics. Pharmacol Res. 2016 Sep;111:237-246. doi: 10.1016/j.phrs.2016.06.002. Epub 2016 Jun 16. [Article]
- Shugarts S, Benet LZ: The role of transporters in the pharmacokinetics of orally administered drugs. Pharm Res. 2009 Sep;26(9):2039-54. doi: 10.1007/s11095-009-9924-0. Epub 2009 Jun 30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
- Gene Name
- SLC22A7
- Uniprot ID
- Q9Y694
- Uniprot Name
- Solute carrier family 22 member 7
- Molecular Weight
- 60025.025 Da
References
- Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Monovalent cation:proton antiporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
- Gene Name
- SLC47A1
- Uniprot ID
- Q96FL8
- Uniprot Name
- Multidrug and toxin extrusion protein 1
- Molecular Weight
- 61921.585 Da
References
- Tanihara Y, Masuda S, Sato T, Katsura T, Ogawa O, Inui K: Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71. doi: 10.1016/j.bcp.2007.04.010. Epub 2007 Apr 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Drug transmembrane transporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
- Gene Name
- SLC47A2
- Uniprot ID
- Q86VL8
- Uniprot Name
- Multidrug and toxin extrusion protein 2
- Molecular Weight
- 65083.915 Da
References
- Tanihara Y, Masuda S, Sato T, Katsura T, Ogawa O, Inui K: Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71. doi: 10.1016/j.bcp.2007.04.010. Epub 2007 Apr 13. [Article]
- Nies AT, Damme K, Schaeffeler E, Schwab M: Multidrug and toxin extrusion proteins as transporters of antimicrobial drugs. Expert Opin Drug Metab Toxicol. 2012 Dec;8(12):1565-77. doi: 10.1517/17425255.2012.722996. Epub 2012 Sep 13. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54