Cortisone acetate

Identification

Summary

Cortisone acetate is a steroid hormone used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses and endocrine disorders associated with inadequate production of steroid hormones.

Generic Name
Cortisone acetate
DrugBank Accession Number
DB01380
Background

Cortisone acetate was first isolate in 1935 and became more widely researched in 1949.1 Since then, glucocorticoids such as cortisone acetate have been used to treat a number of inflammatory conditions such as endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, and gastrointestinal diseases and disorders.2,8

Cortisone acetate was granted FDA approval on 13 June 1950.7

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 402.4807
Monoisotopic: 402.204238692
Chemical Formula
C23H30O6
Synonyms
  • Cortisone 21-acetate
  • Cortisone acetate
  • Cortone acetate

Pharmacology

Indication

Cortisone acetate is indicated to treat a wide variety of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, and gastrointestinal diseases and disorders.2,8

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.3 The duration of action is moderate as it is generally given once daily.8 Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces.3 Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.3

Mechanism of action

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.3 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.3 Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.3 Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.3 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.3

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
UAnnexin A1
inducer
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin5 and serum albumin4 in plasma.

Metabolism
Not Available
Route of elimination

Corticosteroids are eliminated predominantly in the urine.4

Half-life

Not Available

Clearance

Data regarding the clearance of cortisone acetate is not readily available.8

Adverse Effects
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Toxicity

Data regarding acute overdoses of glucocorticoids are rare.8 Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.6 Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.6

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Cortisone acetate can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Cortisone acetate.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Cortisone acetate.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Cortisone acetate.
AcarboseThe risk or severity of hyperglycemia can be increased when Cortisone acetate is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Cortisone acetate is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Cortisone acetate is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Cortisone acetate.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Cortisone acetate is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Acetyldigitoxin.
Interactions
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Food Interactions
  • Take with food. Taking cortisone acetate with food may reduce gastrointestinal upset.

Products

Products
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Active Moieties
NameKindUNIICASInChI Key
CortisoneprodrugV27W9254FZ53-06-5MFYSYFVPBJMHGN-ZPOLXVRWSA-N
Product Images
International/Other Brands
Cortisyl
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Cortisone AcetateTablet5 mg/1OralUNSPECIFIED2006-01-04Not applicableUS flag
Cortisone AcetateTablet25 mgOralBausch Health, Canada Inc.1973-12-31Not applicableCanada flag
Cortisone AcetateTablet10 mg/1OralUNSPECIFIED2006-01-04Not applicableUS flag
Cortone Sus 50mg/mlSuspensionIntramuscularMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1951-12-311999-08-06Canada flag
Cortone Tab 25mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1954-12-312002-07-29Canada flag
Cortone Tab 5mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1951-12-312002-07-29Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Cortisone AcetateTablet25 mg/1OralHikma Pharmaceuticals USA Inc.1972-06-13Not applicableUS flag00143 1202 01 nlmimage10 7a053d59
Cortisone AcetateTablet25 mg/1OralHikma Pharmaceutical2013-08-26Not applicableUS flag
Cortisone AcetateTablet25 mg/1OralHikma Pharmaceuticals USA Inc.2013-08-22Not applicableUS flag
Cortisone AcetateTablet25 mg/1OralGolden State Medical Supply1972-06-132017-01-02US flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Pregnane steroids
Direct Parent
Gluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
20-oxosteroids / 3-oxo delta-4-steroids / 17-hydroxysteroids / 11-oxosteroids / Delta-4-steroids / Cyclohexenones / Alpha-acyloxy ketones / Tertiary alcohols / Alpha-hydroxy ketones / Cyclic alcohols and derivatives
show 4 more
Substituents
11-oxosteroid / 17-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-acyloxy ketone / Alpha-hydroxy ketone / Carbonyl group
show 16 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
corticosteroid hormone (CHEBI:3897) / C21 steroids (gluco/mineralocorticoids, progestogens) and derivatives (C08173) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030120)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
883WKN7W8X
CAS number
50-04-4
InChI Key
ITRJWOMZKQRYTA-RFZYENFJSA-N
InChI
InChI=1S/C23H30O6/c1-13(24)29-12-19(27)23(28)9-7-17-16-5-4-14-10-15(25)6-8-21(14,2)20(16)18(26)11-22(17,23)3/h10,16-17,20,28H,4-9,11-12H2,1-3H3/t16-,17-,20+,21-,22-,23-/m0/s1
IUPAC Name
2-[(1R,3aS,3bS,9aR,9bS,11aS)-1-hydroxy-9a,11a-dimethyl-7,10-dioxo-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl]-2-oxoethyl acetate
SMILES
[H][C@@]12CC[C@](O)(C(=O)COC(C)=O)[C@@]1(C)CC(=O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

References

Synthesis Reference

Reichstein,T.; US. Patent 2,403,683; July 9, 1946. Gallagher,T.F.; US. Patent 2,447,325; August 17,1948; assigned to Research Corporation. Sarett, L.H.; U.S. Patent 2,541,104; February 13, 1951; assigned to Merck & Co., Inc.

General References
  1. BOLAND EW, HEADLEY NE: Effects of cortisone acetate on rheumatoid arthritis. J Am Med Assoc. 1949 Oct 1;141(5):301-8. doi: 10.1001/jama.1949.02910050001001. [Article]
  2. Hardy RS, Raza K, Cooper MS: Therapeutic glucocorticoids: mechanisms of actions in rheumatic diseases. Nat Rev Rheumatol. 2020 Mar;16(3):133-144. doi: 10.1038/s41584-020-0371-y. Epub 2020 Feb 7. [Article]
  3. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
  4. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
  5. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
  6. Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [Article]
  7. FDA Approved Drug Products: Cortone Cortisone Acetate Injection (Discontinued) [Link]
  8. DailyMed Label: Cortisone acetate tablet [Link]
Human Metabolome Database
HMDB0015459
KEGG Drug
D00973
KEGG Compound
C08173
PubChem Compound
5745
PubChem Substance
46508852
ChemSpider
5543
BindingDB
50455157
RxNav
21655
ChEBI
3897
ChEMBL
CHEMBL1650
ZINC
ZINC000003875334
PharmGKB
PA449130
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cortisone_acetate
AHFS Codes
  • 68:04.00 — Adrenals
MSDS
Download (74.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentPrimary adrenocoritical insufficiency / Secondary Adrenal Insufficiency1
4RecruitingTreatmentCongenital Adrenal Hyperplasia (CAH)1
3CompletedTreatmentAcute ACE-induced Angioedema1
2Unknown StatusTreatmentAdrenal Hyperplasia, Congenital1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bergen Brunswig
  • Consolidated Midland Corp.
  • CVS Pharmacy
  • Major Pharmaceuticals
  • Medicine Shop
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Pharmacia Inc.
  • Qualitest
  • West-Ward Pharmaceuticals
Dosage Forms
FormRouteStrength
Injection
TabletOral10 mg/1
TabletOral25 mg
TabletOral25 mg/1
TabletOral5 mg/1
SuspensionIntramuscular
TabletOral
Prices
Unit descriptionCostUnit
Cortisone acetate powder24.18USD g
Cortisone Acetate 25 mg Tablet0.47USD tablet
Cortisone 25 mg tablet0.46USD tablet
Cortaid 1% cream0.21USD g
CVS Pharmacy cortisone 1% cream0.18USD g
CVS Pharmacy anti-itch 1% cream0.13USD g
Hydrocortisone 0.5% cream0.11USD g
Medi-cortisone 1% cream0.1USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)227-229Reichstein,T.; US. Patent 2,403,683; July 9, 1946. Gallagher,T.F.; US. Patent 2,447,325; August 17,1948; assigned to Research Corporation. Sarett, L.H.; U.S. Patent 2,541,104; February 13, 1951; assigned to Merck & Co., Inc.
water solubility20 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.10HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0278 mg/mLALOGPS
logP2.35ALOGPS
logP2.1ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)12.6ChemAxon
pKa (Strongest Basic)-3.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area97.74 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity105.63 m3·mol-1ChemAxon
Polarizability43.06 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.983
Blood Brain Barrier+0.9851
Caco-2 permeable-0.6606
P-glycoprotein substrateSubstrate0.7382
P-glycoprotein inhibitor IInhibitor0.7341
P-glycoprotein inhibitor IIInhibitor0.5925
Renal organic cation transporterNon-inhibitor0.7452
CYP450 2C9 substrateNon-substrate0.8551
CYP450 2D6 substrateNon-substrate0.9294
CYP450 3A4 substrateSubstrate0.7841
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9556
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8588
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9246
Ames testNon AMES toxic0.9409
CarcinogenicityNon-carcinogens0.9551
BiodegradationNot ready biodegradable0.9354
Rat acute toxicity2.1280 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9599
hERG inhibition (predictor II)Non-inhibitor0.6638
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0643900000-f8c82718aaac7d5f1097
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-2941000000-b0ec70aa310131ced784

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. [Article]
  2. Rautanen A, Eriksson JG, Kere J, Andersson S, Osmond C, Tienari P, Sairanen H, Barker DJ, Phillips DI, Forsen T, Kajantie E: Associations of body size at birth with late-life cortisol concentrations and glucose tolerance are modified by haplotypes of the glucocorticoid receptor gene. J Clin Endocrinol Metab. 2006 Nov;91(11):4544-51. Epub 2006 Aug 8. [Article]
  3. Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. [Article]
  4. Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. [Article]
  5. Sher L: Combined dexamethasone suppression-corticotropin-releasing hormone stimulation test in studies of depression, alcoholism, and suicidal behavior. ScientificWorldJournal. 2006 Oct 31;6:1398-404. [Article]
  6. Schlechte JA, Ginsberg BH, Sherman BM: Regulation of the glucocorticoid receptor in human lymphocytes. J Steroid Biochem. 1982 Jan;16(1):69-74. [Article]
  7. Schlechte JA, Sherman BM: Decreased glucocorticoid receptor binding in adrenal insufficiency. J Clin Endocrinol Metab. 1982 Jan;54(1):145-9. [Article]
  8. DailyMed Label: Cortisone acetate tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Structural molecule activity
Specific Function
Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
Gene Name
ANXA1
Uniprot ID
P04083
Uniprot Name
Annexin A1
Molecular Weight
38713.855 Da
References
  1. Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [Article]
  2. Luo X, Zhu LJ, Cai NF, Zheng LY, Cheng ZN: Prediction of tacrolimus metabolism and dosage requirements based on CYP3A4 phenotype and CYP3A5(*)3 genotype in Chinese renal transplant recipients. Acta Pharmacol Sin. 2016 Apr;37(4):555-60. doi: 10.1038/aps.2015.163. Epub 2016 Feb 29. [Article]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Steroid binding
Specific Function
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name
SERPINA6
Uniprot ID
P08185
Uniprot Name
Corticosteroid-binding globulin
Molecular Weight
45140.49 Da
References
  1. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
  2. SLAUNWHITE WR Jr, SANDBERG AA: Transcortin: a corticosteroid-binding protein of plasma. J Clin Invest. 1959 Feb;38(2):384-91. doi: 10.1172/JCI103812. [Article]
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
Molecular Weight
69365.94 Da
References
  1. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
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. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [Article]
  2. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]

Drug created on July 06, 2007 20:32 / Updated on May 11, 2021 01:04