NAV

Acyclovir

Identification

Summary

Acycloviris a guanosine analog used to treat herpes simplex, varicella zoster, herpes zoster.

Brand Names
Sitavig, Xerese, Zovirax
Generic Name
Acyclovir
DrugBank Accession Number
DB00787
Background

Acyclovir is a nucleotide analog antiviral used to treat herpes simplex,Varicella zoster, herpes zoster, herpes labialis, and acute herpetic keratitis10,11,12,13,14,15. Acyclovir is generally used first line in the treatment of these viruses and some products are indicated for patients as young as 6 years old.13

Acyclovir was granted FDA approval on 29 March 1982.12

Type
Small Molecule
Groups
Approved
Structure
 3D
Similar Structures
Weight
Average: 225.2046
Monoisotopic: 225.086189243
Chemical Formula
C8H11N5O3
Synonyms
  • Aciclovir
  • Aciclovirum
  • Acycloguanosine
  • Acyclovir
External IDs
  • NSC-645011

Pharmacology

Indication

An acyclovir topical cream is indicated to treat recurrent herpes labialis in immunocompetent patients 12 years and older.10阿昔洛韦口服片剂、胶囊和悬浮液are indicated to treat herpes zoster, genital herpes, and chickenpox.11An acyclovir topical ointment is indicated to treat initial genital herpes and limited non-life-threatening mucocutaneous herpes simplex in immunocompromised patients.12An acyclovir cream with hydrocortisone is indicated to treat recurrent herpes labialis, and shortening lesion healing time in patients 6 years and older.13An acyclovir buccal tablet is indicated for the treatment of recurrent herpes labialis.14An acyclovir ophthalmic ointment is indicated to treat acute herpetic keratitis.15

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Acyclovir is a nucleoside analog that inhibits the action of viral DNA polymerase and DNA replication of different herpesvirus.10,11,12,13,14,15Acyclovir has a wide therapeutic window as overdose is rare in otherwise healthy patients.11

Mechanism of action

Acyclovir is becomes acyclovir monophosphate due to the action of viral thymidine kinase.5Acyclovir monophosphate is converted to the diphosphate form by guanylate kinase.1无环鸟苷二磷酸转化为无环鸟苷triphosphate by nucleoside diphosphate kinase, pyruvate kinase, creatine kinase, phosphoglycerate kinase, succinyl-CoA synthetase, phosphoenolpyruvate carboxykinase and adenylosuccinate synthetase.1,7Acyclovir triphosphate has higher affinity for viral DNA polymerase than cellular DNA polymerase and incorporates into the DNA where the missing 2' and 3' carbons causes DNA chain termination.5In other cases acyclovir triphosphate competes so strongly for viral DNA polymerase that other bases cannot associate with the enzyme, inactivating it.5

Target Actions Organism
ADNA polymerase catalytic subunit
inhibitor
 HHV-1
ADNA polymerase catalytic subunit
inhibitor
 HHV-3
AThymidine kinase
potentiator
Absorption

The oral bioavailability of acyclovir is 10-20% but decreases with increasing doses.11Acyclovir ointment is <0.02-9.4% absorbed.12Acyclovir buccal tablets and ophthalmic ointment are minimally absorbed.14,15The bioavailability of acyclovir is not affected by food.11

Acyclovir has a mean Tmaxof 1.1±0.4 hours, mean Cmaxof 593.7-656.5ng/mL, and mean AUC of 2956.6-3102.5h/*ng/mL.9

Volume of distribution

The volume of distribution of acyclovir is 0.6L/kg.6

Protein binding

Acyclovir is 9-33% protein bound in plasma.6,11

Metabolism

Acyclovir is <15% oxidized to 9-carboxymethoxymethylguanine by alcohol dehydrogenase and aldehyde dehydrogenase and 1% 8-hydroxylated to 8-hydroxy-acyclovir by aldehyde oxidase.4

Acyclovir is becomes acyclovir monophosphate due to the action of viral thymidine kinase.5Acyclovir monophosphate is converted to the diphosphate form by guanylate kinase.1无环鸟苷二磷酸转化为无环鸟苷triphosphate by nucleoside diphosphate kinase, pyruvate kinase, creatine kinase, phosphoglycerate kinase, succinyl-CoA synthetase, phosphoenolpyruvate carboxykinase and adenylosuccinate synthetase.1,7

Hover over products below to view reaction partners

Route of elimination

The majority of acyclovir is excreted in the urine as unchanged drug.4,1490-92% of the drug can be excreted unchanged through glomerular filtration and tubular secretion.5<2% of the drug is recovered in feces and <0.1% is expired as CO2.8

Half-life

The clearance of acyclovir varies from 2.5-3 hours depending on the creatinine clearance of the patient.5The plasma half life of acyclovir during hemodialysis is approximately 5 hours.11The mean half life in patients from 7 months to 7 years old is 2.6 hours.11

Clearance

The renal clearance of acyclovir is 248mL/min/1.73m2.8The total clearance in neonates if 105-122mL/min/1.73m2.8

Adverse Effects
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Toxicity

Symptoms of overdose include agitation, coma, seizures, lethargy, and precipitation in renal tubules.11These symptoms are more common in patients given high doses without monitoring of fluid and electrolyte balance or reduced kidney function.11,4,6In the case of an overdose, treat with symptomatic and supportive care.13

Pathways
Not Available
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Interactions

Drug InteractionsLearn More" title="" 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
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Abacavir Acyclovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abametapir The serum concentration of Acyclovir can be increased when it is combined with Abametapir.
Abatacept The metabolism of Acyclovir can be increased when combined with Abatacept.
Abemaciclib The excretion of Abemaciclib can be decreased when combined with Acyclovir.
Abiraterone The serum concentration of Acyclovir can be increased when it is combined with Abiraterone.
Acamprosate The excretion of Acamprosate can be decreased when combined with Acyclovir.
Aceclofenac The risk or severity of nephrotoxicity can be increased when Acyclovir is combined with Aceclofenac.
Acemetacin The risk or severity of nephrotoxicity can be increased when Acyclovir is combined with Acemetacin.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Acyclovir.
Acetaminophen The metabolism of Acyclovir can be decreased when combined with Acetaminophen.
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Food Interactions
  • Drink plenty of fluids. Dehydration with acyclovir predisposes patients to nephrotoxicity.
  • Take with or without food. The absorption is unaffected by food.

Products

Drug product information from 10+ global regions
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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
Ingredient UNII CAS InChI Key
Acyclovir sodium 927L42J563 69657-51-8 RMLUKZWYIKEASN-UHFFFAOYSA-M
Product Images
International/Other Brands
Zovir
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Acyclovir Tablet 200 mg Oral Apotex Corporation 1996-12-31 Not applicable Canada flag
Acyclovir Tablet 800 mg Oral Apotex Corporation 1996-12-31 Not applicable Canada flag
Acyclovir Capsule 200 mg/1 Oral Boscogen, Inc. 2004-08-01 Not applicable US flag
Acyclovir Tablet 800 mg Oral Sanis Health Inc 2010-04-05 2014-08-01 Canada flag
Acyclovir Tablet 400 mg Oral Apotex Corporation 1996-12-31 Not applicable Canada flag
Acyclovir Tablet 400 mg Oral Sanis Health Inc 2010-04-05 2017-07-31 Canada flag
Acyclovir Tablet 200 mg Oral Sanis Health Inc 2010-04-05 2014-08-01 Canada flag
Acyclovir Sodium for Injection Powder, for solution 1 g / vial Intravenous Novopharm Limited 1998-02-04 2005-08-10 Canada flag
Acyclovir Sodium for Injection Powder, for solution 500 mg / vial Intravenous Novopharm Limited 1998-02-04 2018-05-08 Canada flag
Acyclovir Sodium for Injection Powder, for solution 1 g / vial Intravenous Abbott 1998-02-11 2007-07-31 Canada flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Acyclovir Tablet 400 mg/1 Oral Remedy Repack 2011-07-13 2012-07-14 US flag
Acyclovir Tablet 800 mg/1 Oral AvPAK 2014-07-18 Not applicable US flag
Acyclovir Capsule 200 mg/1 Oral Mylan Pharmaceuticals Inc. 2010-03-23 2010-02-11 US flag
Acyclovir Ointment 50 mg/1g Topical NorthStar Rx LLC 2017-07-31 Not applicable US flag
Acyclovir Tablet 800 mg/1 Oral Nucare Pharmaceuticals,inc. 2018-05-04 Not applicable US flag
Acyclovir Ointment 50 mg/1g Topical Amneal Pharmaceuticals LLC 2014-01-03 Not applicable US flag
Acyclovir Tablet 800 mg/1 Oral Clinical Solutions Wholesale 1997-04-30 2017-06-15 US flag
Acyclovir Tablet 400 mg/1 Oral REMEDYREPACK INC. 2018-08-09 Not applicable US flag
Acyclovir Tablet 400 mg/1 Oral Camber Pharmaceuticals, Inc. 2013-11-29 Not applicable US flag
Acyclovir Injection, solution 50 mg/1mL Intravenous Zydus Pharmaceuticals (USA) Inc. 2018-11-27 Not applicable US flag
Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Acyclovir Ointment 50 mg/1g Topical OASIS TRADING 2018-11-15 Not applicable US flag
มาร์เวียร์ Cream 5 %w/w Topical บริษัท โรงงานเภสัชกรรมแหลมทองการแพทย์ จำกัด จำกัด 1998-03-18 Not applicable Thailand flag
ไวราซิน 200 Tablet 200 mg บริษัท ซีฟาม จำกัด จำกัด 1998-12-18 Not applicable Thailand flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Activir Duo 50 mg/g + 10 mg/g Creme Acyclovir(50 mg/g)+Hydrocortisone(10 mg/g) Cream Topical Gsk Gebro Consumer Healthcare Gmb H 2010-02-09 Not applicable Austria flag
Acyclovix Acyclovir(200 mg/1)+Benzyl alcohol(0.1 g/1g) Kit Oral; Topical Primary Pharmaceuticals, Inc. 2020-09-20 Not applicable US flag
HERPAZON % 5 + % 1 KREM, 5 GRAM Acyclovir(5 %)+Hydrocortisone(1 %) Cream Topical İLKO İLAÇ SAN.VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
Xerese Acyclovir(5 % w/w)+Hydrocortisone(1 % w/w) Cream Topical Bausch Health, Canada Inc. 2013-07-26 Not applicable Canada flag
Xerese Acyclovir(50 mg/1g)+Hydrocortisone(10 mg/1g) Cream Topical Bausch Health US LLC 2009-07-31 Not applicable US flag
Xerese Acyclovir(50 mg/1g)+Hydrocortisone(10 mg/1g) Cream Topical Meda Pharmaceuticals Ltd 2010-07-15 2013-02-28 US flag
Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Acyclovir Acyclovir(50 mg/1g) Ointment Topical OASIS TRADING 2018-11-15 Not applicable US flag

Categories

ATC Codes
J05AB01 — Aciclovir D06BB03 — Aciclovir S01AD03 — Aciclovir D06BB53 — Aciclovir, combinations
Drug Categories
Chemical TaxonomyProvided byClassyfire
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/Aminopyrimidines and derivatives/N-substituted imidazoles/Vinylogous amides/Heteroaromatic compounds/Azacyclic compounds/Primary amines/Primary alcohols/Organopnictogen compounds
show 2 more
Substituents
6-oxopurine/Alcohol/Amine/Aminopyrimidine/Aromatic heteropolycyclic compound/Azacycle/Azole/Heteroaromatic compound/Hydrocarbon derivative/Hypoxanthine
show 13 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
oxopurine, 2-aminopurines (CHEBI:2453)
Affected organisms
  • Human Herpes Virus

Chemical Identifiers

UNII
X4HES1O11F
CAS number
59277-89-3
InChI Key
MKUXAQIIEYXACX-UHFFFAOYSA-N
InChI
InChI=1S/C8H11N5O3/c9-8-11-6-5(7(15)12-8)10-3-13(6)4-16-2-1-14/h3,14H,1-2,4H2,(H3,9,11,12,15)
IUPAC Name
2-amino-9-[(2-hydroxyethoxy)methyl]-6,9-dihydro-3H-purin-6-one
SMILES
NC1=NC(=O)C2=C(N1)N(COCCO)C=N2

References

Synthesis Reference
US4294831
General References
  1. O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309. [Article]
  2. Gunness P, Aleksa K, Bend J, Koren G: Acyclovir-induced nephrotoxicity: the role of the acyclovir aldehyde metabolite. Transl Res. 2011 Nov;158(5):290-301. doi: 10.1016/j.trsl.2011.07.002. Epub 2011 Aug 3. [Article]
  3. Morrel EM, Spruance SL, Goldberg DI: Topical iontophoretic administration of acyclovir for the episodic treatment of herpes labialis: a randomized, double-blind, placebo-controlled, clinic-initiated trial. Clin Infect Dis. 2006 Aug 15;43(4):460-7. Epub 2006 Jul 3. [Article]
  4. Smith JP, Weller S, Johnson B, Nicotera J, Luther JM, Haas DW: Pharmacokinetics of acyclovir and its metabolites in cerebrospinal fluid and systemic circulation after administration of high-dose valacyclovir in subjects with normal and impaired renal function. Antimicrob Agents Chemother. 2010 Mar;54(3):1146-51. doi: 10.1128/AAC.00729-09. Epub 2009 Dec 28. [Article]
  5. King DH: History, pharmacokinetics, and pharmacology of acyclovir. J Am Acad Dermatol. 1988 Jan;18(1 Pt 2):176-9. doi: 10.1016/s0190-9622(88)70022-5. [Article]
  6. Sadjadi SA, Regmi S, Chau T: Acyclovir Neurotoxicity in a Peritoneal Dialysis Patient: Report of a Case and Review of the Pharmacokinetics of Acyclovir. Am J Case Rep. 2018 Dec 9;19:1459-1462. doi: 10.12659/AJCR.911520. [Article]
  7. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
  8. Laskin OL: Clinical pharmacokinetics of acyclovir. Clin Pharmacokinet. 1983 May-Jun;8(3):187-201. doi: 10.2165/00003088-198308030-00001. [Article]
  9. Yuen KH, Peh KK, Billa N, Chan KL, Toh WT: Bioavailability and pharmacokinetics of acyclovir tablet preparation. Drug Dev Ind Pharm. 1998 Feb;24(2):193-6. doi: 10.3109/03639049809085607. [Article]
  10. FDA Approved Drug Products: Zovirax Topical Cream [Link]
  11. FDA Drug Approval Package: Zovirax Oral Capsules, Oral Tablets, Oral Suspension [Link]
  12. FDA Approved Drug Products: Zovirax Topical Ointment [Link]
  13. FDA Approved Drug Products: Xerese (Acyclovir and Hydrocortisone) Topical Cream [Link]
  14. FDA Approved Drug Products: Sitavig Buccal Tablets [Link]
  15. FDA Approved Drug Products: Avaclyr Ophthalmic Ointment (Discontinued) [Link]
  16. FDA Approved Drug Products: Zovirax Acyclovir Intravenous Infusion (Discontinued) [Link]
Human Metabolome Database
HMDB0014925
KEGG Drug
D00222
KEGG Compound
C06810
PubChem Compound
2022
PubChem Substance
46506002
ChemSpider
1945
BindingDB
50021776
RxNav
281
ChEBI
2453
ChEMBL
CHEMBL184
ZINC
ZINC000001530555
Therapeutic Targets Database
DNC000157
PharmGKB
PA448045
PDBe Ligand
AC2
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aciclovir
PDB Entries
1pwy/2ki5/3ix2/3mjr/4da7/5i3c
MSDS
Download (37 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Active Not Recruiting Treatment Viral Pneumonia 1
4 Completed Prevention Herpes/Human Immunodeficiency Virus (HIV) Infections 1
4 Completed Treatment Genital Herpes 3
4 Completed Treatment Genital Herpes/Human Immunodeficiency Virus (HIV) Infections 1
4 Completed Treatment Healthy Subjects (HS) 1
4 Completed Treatment Herpes Simplex Infections/Human Immunodeficiency Virus (HIV) Infections 1
4 Completed Treatment Herpes Zoster 1
4 Completed Treatment Relapsing Remitting Multiple Sclerosis (RRMS) 1
4 Not Yet Recruiting Treatment Herpes Simplex 2/Viral Meningitis 1
4 Recruiting Treatment Acyclovir and Candida Antigen in Treatment of Plantar Wart 1

Pharmacoeconomics

Manufacturers
  • Actavis elizabeth llc
  • Apotex inc etobicoke site
  • Belcher pharmaceuticals inc
  • Dava pharmaceuticals inc
  • Genpharm inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lek pharmaceutical and chemical co dd
  • Mylan pharmaceuticals inc
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
  • Stason industrial corp
  • Teva pharmaceuticals usa inc
  • Teva pharmaceuticals usa
  • Watson laboratories inc
  • Glaxosmithkline
  • Actavis mid atlantic llc
  • Hi tech pharmacal co inc
  • Carlsbad technology inc
  • Mylan laboratories inc
  • Abbott laboratories
  • Baxter healthcare corp anesthesia and critical care
  • Apothecon inc div bristol myers squibb
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Teva parenteral medicines inc
Packagers
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Amneal Pharmaceuticals
  • Apotex Inc.
  • Apotheca Inc.
  • Apothecary Shop Wholesale
  • APP Pharmaceuticals
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Bryant Ranch Prepack
  • BTA Pharmaceuticals
  • Cardinal Health
  • Carlsbad Technology Inc.
  • Comprehensive Consultant Services Inc.
  • Corepharma LLC
  • DAVA Pharmaceuticals
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • DSM Corp.
  • East Coast Medical Network Inc.
  • Eczacibasi Health Products Co.
  • GlaxoSmithKline Inc.
  • Goldline Laboratories Inc.
  • H.J. Harkins Co. Inc.
  • Heritage Pharmaceuticals
  • Hi Tech Pharmacal Co. Inc.
  • Hospira Inc.
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medvantx Inc.
  • Meridian Medical Technologies Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Neuman Distributors Inc.
  • Novopharm Ltd.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • Patheon Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Pharmpak Inc.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stason Pharmaceuticals Inc.
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • Watson Pharmaceuticals
  • Xactdose Inc.
  • Yung Shin Pharmaceutical Industry Ltd.
Dosage Forms
Form Route Strength
Cream Topical 3 G
Granule, for suspension Oral 800 MG
Powder, for solution 250 MG
Cream Topical
Injection, powder, for solution Parenteral
Injection, solution Intravenous
Powder, for solution Topical
Tablet Oral
Tablet, for suspension
Tablet, soluble
Tablet Oral 204 mg
Tablet, coated Oral 800 mg
Injection, solution, concentrate Intravenous
Cream Cutaneous
Cream Topical 5 g
Ointment Topical 5 %
Syrup Oral 8 g/100ml
Powder, for solution Parenteral 500 MG
Powder Parenteral 250 MG
Powder Parenteral 500 MG
Solution Parenteral 25 MG/ML
Cream Cutaneous 5 %
Powder, for suspension Oral 2 g
Powder, for suspension Oral 4 g
Suspension Oral 2 g
Powder, for solution Parenteral 250 MG
Suspension Oral 8 G/100ML
Powder Intravenous 250 mg/1vial
Powder Intravenous 250 MG
Tablet Oral 800 mg
Ointment Topical 5 g
Solution Topical 5 g
Ointment Ophthalmic 30 MG/G
Cream Topical 50 mg
Cream 50 mg/g
Capsule Oral 200 mg/1
Capsule Oral 400 mg/1
Cream
Injection, powder, lyophilized, for solution Intravenous 1 g/1
Injection, powder, lyophilized, for solution Intravenous 1000 mg/20mL
Injection, powder, lyophilized, for solution Intravenous 1000 mg/1
Injection, powder, lyophilized, for solution Intravenous 500 mg/1
Injection, powder, lyophilized, for solution Intravenous 500 mg/10mL
Injection, solution Intravenous 25 mg/1mL
Injection, solution Intravenous 50 mg/1mL
Ointment Cutaneous 50 mg/1g
Suspension Oral 200 mg/5mL
Tablet Oral 200 mg/1
Tablet Oral 400 mg/1
Tablet Oral 400 MG
Tablet Oral 400.00 mg/1
Tablet Oral 800 mg/1
Tablet Oral 800.00 mg/1
Injection, solution Intravenous 1000 mg/20mL
Injection, solution Intravenous 500 mg/10mL
Powder, for solution Intravenous 500 mg / vial
Solution Intravenous 25 mg / mL
Solution Intravenous 50 mg / mL
Tablet, coated Oral 200 mg
Tablet Oral 400 mg / tab
Tablet Oral 800 mg / tab
Kit Oral; Topical
Tablet 200 mg
Suspension Oral
Stick Topical
Tablet Oral 200 mg / tab
Capsule Oral
Tablet Oral 1 g
Cream 5 %
Suspension Oral 8 G/ML
Tablet
Injection, powder, for solution Intravenous 500 MG
Injection Intravenous 250 mg
Ointment Topical 5000 mg
Suspension Oral 400 MG/5ML
Ointment Ophthalmic 3 %
Suspension Oral 8 %
Tablet 400 mg
Tablet 800 mg
Ointment Topical 5 % w/w
Injection Parenteral
Tablet 50 MG
Ointment Ophthalmic
Kit Not applicable
Injection, powder, for suspension Parenteral 250 mg
Tablet, film coated Oral 200 mg
Injection Intravenous
Tablet, film coated Oral 400 mg
Tablet, film coated Oral 800 mg
Cream Extracorporeal; Topical
Ointment
Cream Topical 5 %
Ointment Topical
Powder, for solution
Tablet Buccal 50 mg
Tablet, delayed release Buccal 50 mg/1
Cream Topical 5 % w/w
Tablet Topical
Injection, powder, for solution Intravenous 250 mg
Injection Parenteral 250 mg
Ointment Conjunctival; Ophthalmic 3 g
Ointment Ophthalmic 3 g
Tablet Oral 200.00 MG
Cream 阴道 5 g
Injection, powder, lyophilized, for solution Intravenous 250 mg
Ointment Ophthalmic; Topical 3 g
Powder, for suspension Oral 8 g
Cream Topical 50 mg/g
Ointment Topical
Tablet Oral 200 mg
Ointment Ophthalmic 30 mg
Cream Topical
Cream Topical 50 mg/1g
Injection, powder, lyophilized, for solution Intravenous 50 mg/1mL
Ointment Topical 50 mg/1g
Powder, for solution Intravenous 1 g / vial
Suspension Oral 200 mg / 5 mL
Tablet, film coated Oral
Solution Oral
Injection, powder, lyophilized, for solution Parenteral 250 mg
Injection, powder, for solution Intravenous
Injection, powder, lyophilized, for solution Intravenous
Ointment Ophthalmic 3 % w/w
Injection, powder, for solution Intravenous 250 mg/1vial
Injection, powder, for solution Intravenous 500 mg/1vial
Cream Topical 5 %w/w
Capsule Oral 200 mg
Powder 250 mg/1vial
Prices
Unit description Cost Unit
Zovirax 200 mg/5ml Suspension 473ml Bottle 264.95USD bottle
Zovirax 5% Ointment 15 gm Tube 191.56USD tube
Zovirax 5% Cream 5 gm Tube 165.07USD tube
Zovirax 5% Cream 2 gm Tube 69.44USD tube
Zovirax 5% cream 30.22USD g
Zovirax 800 mg tablet 11.83USD tablet
Zovirax 400 mg tablet 6.09USD tablet
Zovirax 800 mg Tablet 5.71USD tablet
Acyclovir 800 mg tablet 3.81USD tablet
Zovirax 200 mg capsule 3.08USD capsule
Acyclovir 800 mg Tablet 2.99USD tablet
Apo-Acyclovir 800 mg Tablet 2.99USD tablet
Mylan-Acyclovir 800 mg Tablet 2.99USD tablet
Novo-Acyclovir 800 mg Tablet 2.99USD tablet
Nu-Acyclovir 800 mg Tablet 2.99USD tablet
Ratio-Acyclovir 800 mg Tablet 2.99USD tablet
Zovirax 400 mg Tablet 2.9USD tablet
Acyclovir 400 mg tablet 2.26美元 tablet
Acyclovir 400 mg Tablet 1.63USD tablet
Apo-Acyclovir 400 mg Tablet 1.63USD tablet
Mylan-Acyclovir 400 mg Tablet 1.63USD tablet
Novo-Acyclovir 400 mg Tablet 1.63USD tablet
Nu-Acyclovir 400 mg Tablet 1.63USD tablet
Ratio-Acyclovir 400 mg Tablet 1.63USD tablet
Zovirax 200 mg Tablet 1.44USD tablet
Acyclovir 200 mg capsule 1.01USD capsule
Acyclovir 200 mg Tablet 0.81USD tablet
Apo-Acyclovir 200 mg Tablet 0.81USD tablet
Mylan-Acyclovir 200 mg Tablet 0.81USD tablet
Novo-Acyclovir 200 mg Tablet 0.81USD tablet
Ratio-Acyclovir 200 mg Tablet 0.81USD tablet
Acyclovir 200 mg/5ml Suspension 0.3USD ml
Zovirax 40 mg/ml Suspension 0.28USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region
CA2098108 No 2001-07-03 2012-01-29 Canada flag
USRE39264 No 2006-09-05 2016-08-02 US flag
US6514980 No 2003-02-04 2019-01-24 US flag
US7223387 No 2007-05-29 2021-07-24 US flag
US8747896 No 2014-06-10 2027-06-03 US flag
US8791127 No 2014-07-29 2027-03-23 US flag
US8592434 No 2013-11-26 2030-06-16 US flag

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 255 °C http://www.chemspider.com/Chemical-Structure.1945.html
boiling point (°C) 595 http://www.chemspider.com/Chemical-Structure.1945.html
water solubility 1.41mg/mL at 25°C Avaclyr Ophthalmic Ointment FDA label
logP -1.76 http://www.chemspider.com/Chemical-Structure.1945.html
Caco2 permeability -6.15 ADME Research, USCD
pKa 2.52 and 9.35 Avaclyr Ophthalmic Ointment FDA label
Predicted Properties
Property Value Source
Water Solubility 9.08 mg/mL ALOGPS
logP -0.95 ALOGPS
logP -1 ChemAxon
logS -1.4 ALOGPS
pKa (Strongest Acidic) 11.98 ChemAxon
pKa (Strongest Basic) 3.02 ChemAxon
Physiological Charge 0 ChemAxon
Hydrogen Acceptor Count 7 ChemAxon
Hydrogen Donor Count 3 ChemAxon
Polar Surface Area 114.76 Å2 ChemAxon
Rotatable Bond Count 4 ChemAxon
Refractivity 54.63 m3·mol-1 ChemAxon
Polarizability 21.51 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
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available
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
预测MS / MS谱- 40 v -(注释d) Predicted LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-QQ , negative LC-MS/MS splash10 - 00 - di - 0090000000 - 59599385810 - ae2952ce5
LC-MS/MS Spectrum - LC-ESI-QQ , negative LC-MS/MS splash10-00di-0290000000-9410504409e66bcd08f9
LC-MS/MS Spectrum - LC-ESI-QQ , negative LC-MS/MS splash10-0uyi-1900000000-0930eb38cecf2a197001
LC-MS/MS Spectrum - LC-ESI-QQ , negative LC-MS/MS splash10-05nf-4900000000-10d8c1e33c5d46d6ff80
LC-MS/MS Spectrum - LC-ESI-QQ , negative LC-MS/MS splash10-05mo-9600000000-e25ed55283d7d66d80c5
LC-MS/MS Spectrum - LC-ESI-QQ , positive LC-MS/MS splash10-004i-0390000000-079dc309c9ffbbde3375
LC-MS/MS Spectrum - LC-ESI-QQ , positive LC-MS/MS splash10-0udi-0900000000-201a17a51960fdc3bcef
LC-MS/MS Spectrum - LC-ESI-QQ , positive LC-MS/MS splash10-0udi-0900000000-6c63ec4268a52381191c
LC-MS/MS Spectrum - LC-ESI-QQ , positive LC-MS/MS splash10-0f79-1900000000-20fdfa17569c6b2f479f
LC-MS/MS Spectrum - LC-ESI-QQ , positive LC-MS/MS splash10-000i-2900000000-4f7a822e6652ec471aee
LC-MS/MS Spectrum - LC-ESI-IT , positive LC-MS/MS splash10-0udi-0900000000-69b23ed6f334f4571ecc
MS/MS Spectrum - , positive LC-MS/MS splash10-0udr-2910100000-2b1624536b0084ca299c

Targets

构建、预测和验证机器学习模型
Use our structured and evidence-based datasets tounlock new
insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Details 1.DNA polymerase catalytic subunit
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
分子量
136419.66 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. 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]
  3. Sergerie Y, Boivin G: Hydroxyurea enhances the activity of acyclovir and cidofovir against herpes simplex virus type 1 resistant strains harboring mutations in the thymidine kinase and/or the DNA polymerase genes. Antiviral Res. 2008 Jan;77(1):77-80. Epub 2007 Sep 17. [Article]
  4. 铃木M,奥田硕T, Shiraki K:自那时起rgistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61. Epub 2006 May 30. [Article]
  5. Liu S, Knafels JD, Chang JS, Waszak GA, Baldwin ET, Deibel MR Jr, Thomsen DR, Homa FL, Wells PA, Tory MC, Poorman RA, Gao H, Qiu X, Seddon AP: Crystal structure of the herpes simplex virus 1 DNA polymerase. J Biol Chem. 2006 Jun 30;281(26):18193-200. Epub 2006 Apr 24. [Article]
Details 2.DNA polymerase catalytic subunit
Kind
Protein
Organism
HHV-3
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
P09252
Uniprot Name
DNA polymerase catalytic subunit
分子量
134046.615 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. 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]
  3. Sergerie Y, Boivin G: Hydroxyurea enhances the activity of acyclovir and cidofovir against herpes simplex virus type 1 resistant strains harboring mutations in the thymidine kinase and/or the DNA polymerase genes. Antiviral Res. 2008 Jan;77(1):77-80. Epub 2007 Sep 17. [Article]
  4. 铃木M,奥田硕T, Shiraki K:自那时起rgistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61. Epub 2006 May 30. [Article]
  5. Liu S, Knafels JD, Chang JS, Waszak GA, Baldwin ET, Deibel MR Jr, Thomsen DR, Homa FL, Wells PA, Tory MC, Poorman RA, Gao H, Qiu X, Seddon AP: Crystal structure of the herpes simplex virus 1 DNA polymerase. J Biol Chem. 2006 Jun 30;281(26):18193-200. Epub 2006 Apr 24. [Article]
Details 3.Thymidine kinase
Kind
Protein
Organism
Not Available
Pharmacological action
Yes
Actions
Potentiator
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
P03176
Uniprot Name
Thymidine kinase
分子量
40971.555 Da
References
  1. 班纳特小姐,维恩F,钱伯尼斯约,Batuwangala T, Rutherford T, Summers WC, Sun H, Wright G, Sanderson MR: Structure to 1.9 A resolution of a complex with herpes simplex virus type-1 thymidine kinase of a novel, non-substrate inhibitor: X-ray crystallographic comparison with binding of aciclovir. FEBS Lett. 1999 Jan 25;443(2):121-5. [Article]

Enzymes

Details 1.Thymidine kinase
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
分子量
40896.475 Da
References
  1. King DH: History, pharmacokinetics, and pharmacology of acyclovir. J Am Acad Dermatol. 1988 Jan;18(1 Pt 2):176-9. doi: 10.1016/s0190-9622(88)70022-5. [Article]
Details 2.Guanylate kinase
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Guanylate kinase activity
Specific Function
Essential for recycling GMP and indirectly, cGMP.
Gene Name
GUK1
Uniprot ID
Q16774
Uniprot Name
Guanylate kinase
分子量
21725.41 Da
References
  1. O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309. [Article]
Details 3.Nucleoside diphosphokinase (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The paper referencing these enzymes does not specify which nucleoside diphosphate kinase is responsible for this action.
General Function
Ribosomal small subunit binding
Specific Function
ν的合成的主要角色cleoside 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...
Components:
Name UniProt ID
Nucleoside diphosphate kinase A P15531
Nucleoside diphosphate kinase B P22392
References
  1. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 4.Pyruvate Kinases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The papers referencing these enzymes do not specify which pyruvate kinase is responsible for this action.
General Function
Pyruvate kinase activity
Specific Function
Plays a key role in glycolysis.
Components:
Name UniProt ID
Pyruvate kinase PKLR P30613
Pyruvate kinase PKM P14618
References
  1. O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309. [Article]
  2. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 5.Creatine Kinases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The papers referencing these enzymes do not specify which creatine kinase is responsible for this action.
General Function
Ubiquitin protein ligase binding
Specific Function
Reversibly catalyzes the transfer of phosphate between ATP and various phosphogens (e.g. creatine phosphate). Creatine kinase isoenzymes play a central role in energy transduction in tissues with l...
Components:
Name UniProt ID
Creatine kinase B-type P12277
Creatine kinase M-type P06732
Creatine kinase S-type, mitochondrial P17540
Creatine kinase U-type, mitochondrial P12532
References
  1. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 6.Phosphoglycerate Kinases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The papers referencing these enzymes do not specify which phosphoglycerate kinase is responsible for this action.
General Function
Phosphoglycerate kinase activity
Specific Function
In addition to its role as a glycolytic enzyme, it seems that PGK-1 acts as a polymerase alpha cofactor protein (primer recognition protein).
Components:
Name UniProt ID
Phosphoglycerate kinase 1 P00558
Phosphoglycerate kinase 2 P07205
References
  1. O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309. [Article]
  2. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 7.Succinyl-CoA Synthetases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The paper referencing these enzymes does not specify which Succinyl-CoA synthetase is responsible for this action.
General Function
Succinate-coa ligase (adp-forming) activity
Specific Function
Catalyzes the ATP-dependent ligation of succinate and CoA to form succinyl-CoA.
Components:
Name UniProt ID
Succinyl-CoA ligase [ADP-forming] subunit beta, mitochondrial Q9P2R7
Succinyl-CoA ligase [ADP/GDP-forming] subunit alpha, mitochondrial P53597
Succinyl-CoA ligase [GDP-forming] subunit beta, mitochondrial Q96I99
References
  1. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 8.Phosphoenolpyruvate Carboxykinases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The paper referencing these enzymes does not specify which Phosphoenolpyruvate Carboxykinase is responsible for this action.
General Function
Catalyzes the conversion of oxaloacetate (OAA) to phosphoenolpyruvate (PEP), the rate-limiting step in the metabolic pathway that produces glucose from lactate and other precursors derived from the citric acid cycle.
Specific Function
Gtp binding
Components:
Name UniProt ID
Phosphoenolpyruvate carboxykinase [GTP], mitochondrial Q16822
Phosphoenolpyruvate carboxykinase, cytosolic [GTP] P35558
References
  1. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]
Details 9.Adenylosuccinate Synthetases (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The paper referencing these enzymes does not specify which Adenylosuccinate Synthetase is responsible for this action.
General Function
Phosphate ion binding
Specific Function
Component of the purine nucleotide cycle (PNC), which interconverts IMP and AMP to regulate the nucleotide levels in various tissues, and which contributes to glycolysis and ammoniagenesis. Catalyz...
Components:
Name UniProt ID
Adenylosuccinate synthetase isozyme 1 Q8N142
Adenylosuccinate synthetase isozyme 2 P30520
References
  1. Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7. [Article]

Carriers

Details 1.Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
分子量
69365.94 Da
References
  1. Abdelhameed AS, Bakheit AH, Almutairi FM, AlRabiah H, Kadi AA: Biophysical and In Silico Studies of the Interaction between the Anti-Viral Agents Acyclovir and Penciclovir, and Human Serum Albumin. Molecules. 2017 Nov 5;22(11). pii: molecules22111906. doi: 10.3390/molecules22111906. [Article]

Transporters

Details 1.Solute carrier family 22 member 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
分子量
61153.345 Da
References
  1. 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]
  2. 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]
  3. Boxberger KH, Hagenbuch B, Lampe JN: Common drugs inhibit human organic cation transporter 1 (OCT1)-mediated neurotransmitter uptake. Drug Metab Dispos. 2014 Jun;42(6):990-5. doi: 10.1124/dmd.113.055095. Epub 2014 Mar 31. [Article]
  4. 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]
Details 2.Solute carrier family 22 member 6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
分子量
61815.78 Da
References
  1. 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]
  2. Wada S, Tsuda M, Sekine T, Cha SH, Kimura M, Kanai Y, Endou H: Rat multispecific organic anion transporter 1 (rOAT1) transports zidovudine, acyclovir, and other antiviral nucleoside analogs. J Pharmacol Exp Ther. 2000 Sep;294(3):844-9. [Article]
Details 3.Solute carrier family 22 member 8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
分子量
59855.585 Da
References
  1. 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]
  2. Ohtsuki S, Asaba H, Takanaga H, Deguchi T, Hosoya K, Otagiri M, Terasaki T: Role of blood-brain barrier organic anion transporter 3 (OAT3) in the efflux of indoxyl sulfate, a uremic toxin: its involvement in neurotransmitter metabolite clearance from the brain. J Neurochem. 2002 Oct;83(1):57-66. [Article]
  3. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [Article]
Details 4.Ileal sodium/bile acid cotransporter
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Bile acid:sodium symporter activity
Specific Function
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
Gene Name
SLC10A2
Uniprot ID
Q12908
Uniprot Name
Ileal sodium/bile acid cotransporter
分子量
37713.405 Da
References
  1. Tolle-Sander S, Lentz KA, Maeda DY, Coop A, Polli JE: Increased acyclovir oral bioavailability via a bile acid conjugate. Mol Pharm. 2004 Jan 12;1(1):40-8. [Article]
Details 5.Multidrug and toxin extrusion protein 1
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
分子量
61921.585 Da
References
  1. 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]
  2. Xu Y, Liu X, Wang Y, Zhou N, Peng J, Gong L, Ren J, Luo C, Luo X, Jiang H, Chen K, Zheng M: Combinatorial Pharmacophore Modeling of Multidrug and Toxin Extrusion Transporter 1 Inhibitors: a Theoretical Perspective for Understanding Multiple Inhibitory Mechanisms. Sci Rep. 2015 Sep 2;5:13684. doi: 10.1038/srep13684. [Article]
Details 6.Multidrug and toxin extrusion protein 2
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
分子量
65083.915 Da
References
  1. 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]
  2. Yonezawa A, Inui K: Importance of the multidrug and toxin extrusion MATE/SLC47A family to pharmacokinetics, pharmacodynamics/toxicodynamics and pharmacogenomics. Br J Pharmacol. 2011 Dec;164(7):1817-25. doi: 10.1111/j.1476-5381.2011.01394.x. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 16, 2022 02:33