Apremilast

Identification

Summary

Apremilast is a non-steroidal medication used for the treatment of inflammatory conditions such as psoriasis and psoriatic arthritis.

Brand Names
Otezla
Generic Name
Apremilast
DrugBank Accession Number
DB05676
Background

Apremilast, also known as Otezla, is a phosphodiesterase 4 (PDE4) inhibitor used to treat various types of symptoms resulting from certain inflammatory autoimmune diseases. It belongs to the same drug class as Roflumilast and Crisaborole.11,12 Initially approved in 2014, it is marketed by Celgene.14 In July 2019, apremilast was granted a new FDA approval for the treatment of oral ulcers associated with Behcet's disease, an autoimmune condition that causes recurrent skin, blood vessel, and central nervous system inflammation.4

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 460.5
Monoisotopic: 460.130422295
Chemical Formula
C22H24N2O7S
Synonyms
  • Aprémilast
  • Apremilast
  • Apremilastum
  • N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
External IDs
  • CC 10004
  • CC-10004
  • CC10004

Pharmacology

Indication

Apremilast is indicated for the treatment of adults with active psoriatic arthritis and adults with oral ulcers associated with Behcet's Disease. In addition, apremilast is indicated for the treatment of plaque psoriasis, of any severity, in adult patients who are candidates for phototherapy or systemic therapy.14

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofPsoriasis vulgaris (plaque psoriasis)•••••••••••••••••••••••••• ••• •••••••• •••••••
Management ofPsoriasis vulgaris (plaque psoriasis)••••••••••••••••••••••••••• ••• ••••••••••••
Treatment ofPsoriasis vulgaris (plaque psoriasis)••••••••••••••••••••••••••• ••• ••••••••••••••••••
Treatment ofPsoriasis vulgaris (plaque psoriasis)••••••••••••••••••••••••••• ••• •••••••• ••••••• ••• •••••••••••••••
Management ofActive psoriatic arthritis•••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Apremilast reduces but does not completely inhibit various inflammatory cytokines such as IL-1α, IL-6, IL-8, IL-10 MCP-1, MIP-1β, MMP-3, and TNF-α, relieving the symptoms of psoriasis and Behcet's disease, which are caused by an increase in these inflammatory mediators.6,13 This drug has also been proven to be effective in relieving the pain associated with oral ulcers in Behcet's disease.11

Apremilast may cause unwanted weight loss and worsen depression, leading to suicidal thoughts or actions. It is advisable to monitor for symptoms of depression and seek medical attention if they occur, especially in patients with pre-existing depression. The need for apremilast should be carefully assessed along with the risk of worsening depression and suicide. If weight loss occurs, the degree of weight loss should be evaluated, and consideration should be made for the possible discontinuation of apremilast.14

Mechanism of action

The full mechanism of action of this drug is not fully established, however, it is known that apremilast is an inhibitor of phosphodiesterase 4 (PDE4), which mediates the activity of cyclic adenosine monophosphate (cAMP), a second messenger.5 The inhibition of PDE4 by apremilast leads to increased intracellular cAMP levels.14 An increase in cAMP results in the suppression of inflammation by decreasing the expression of TNF-α, IL-17, IL-23, and other inflammatory mediators. The above inflammatory mediators have been implicated in various psoriatic conditions as well as Behcet's disease, leading to their undesirable inflammatory symptoms such as mouth ulcers, skin lesions, and arthritis.6,13,14 Apremilast administration leads to a cascade which eventually decreases the levels of the above mediators, relieving inflammatory symptoms.

TargetActionsOrganism
APhosphodiesterase isozyme 4
antagonist
Humans
Absorption

An oral dose of apremilast is well-absorbed and the absolute bioavailability is approximately 73%. Tmax is approximately 2.5 hours14 and Cmax has been reported to be approximately 584 ng/mL in one pharmacokinetic study.8 Food intake does not appear to affect apremilast absorption.14

Volume of distribution

The average apparent volume of distribution (Vd) is about 87 L, suggesting that apremilast is distributed in the extravascular compartment.13

Protein binding

The plasma protein binding of apremilast is about 68%.13

Metabolism

Apremilast is heavily metabolized by various pathways, which include oxidation, hydrolysis, in addition to conjugation. About 23 metabolites are produced from its metabolism.3 The CYP3A4 primarily mediates the oxidative metabolism of this drug, with smaller contributions from CYP1A2 and CYP2A6 enzymes.13 The main metabolite of apremilast, M12, is an inactive glucuronide conjugate form of the O-demethylated drug.13 Some other major metabolites, M14 and M16, are significantly less active in the inhibition of PDE4 and inflammatory mediators than their parent drug, apremilast. After an oral dose, unchanged apremilast (45%) and the inactive metabolite, O-desmethyl apremilast glucuronide (39%) are found in the plasma. 10 Minor metabolites M7 and M17 are active, but are only present in about 2% or less of apremilast concentrations, and likely not significant contributors to the actions of apremilast.10

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Route of elimination

Only 3% and 7% of an apremilast dose are detected in the urine and feces as unchanged drug, respectively, indicating extensive metabolism and high absorption.13

Half-life

The average elimination half-life of this drug ranges from 6-9 hours.7,14

Clearance

In healthy patients, the plasma clearance of apremilast is about 10 L/hour.13

Adverse Effects
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Toxicity

The oral LD50 in mice was greater than 2000 mg/kg in mice. In rats, oral LD50 was 2000 mg/kg males and 300 mg/kg in females.16

Overdose information

In healthy subjects receiving a maximum dose of 100 mg (given as 50 mg twice daily) for about 5 days, no significant toxicity was observed. In cases of an overdose, supportive and symptomatic treatment should be administered. Contact the local poison control center for the most recent overdose management for apremilast.15

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

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Apremilast which could result in a higher serum level.
AbametapirThe serum concentration of Apremilast can be increased when it is combined with Abametapir.
AbataceptThe therapeutic efficacy of Apremilast can be decreased when used in combination with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Apremilast.
AbirateroneThe serum concentration of Apremilast can be increased when it is combined with Abiraterone.
Food Interactions
  • Avoid St. John's Wort. Apremilast is a CYP3A substrate; therefore, co-administration with St. John's wort, a CYP3A inducer, may reduce the serum level of apremilast.
  • Take with or without food.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Gln-apremilastTablet30 mgOralGlenmark Pharmaceuticals, Inc2022-11-14Not applicableCanada flag
OtezlaTablet, film coated30 mgOralAmgen Europe Bv2016-09-08Not applicableEU flag
OtezlaTablet, film coated30 mg/1OralREMEDYREPACK INC.2021-07-14Not applicableUS flag
OtezlaTablet, film coated30 mg/1OralAMGEN INC2020-02-26Not applicableUS flag
OtezlaTablet, film coated30 mgOralAmgen Europe Bv2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-apremilastTablet30 mgOralApotex Corporation2023-09-28Not applicableCanada flag
Apo-apremilast TabletsTablet30 mgOralApotex CorporationNot applicableNot applicableCanada flag
ApremilastTablet, film coated30 mg/1OralCamber Pharmaceuticals, Inc.2023-07-26Not applicableUS flag
ApremilastTablet, film coated30 mg/1OralAmneal Pharmaceuticals NY LLC2021-07-05Not applicableUS flag
Auro-apremilastTablet30 mgOralAuro Pharma Inc2022-12-07Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Apo-apremilastApremilast (10 mg) + Apremilast (20 mg) + Apremilast (30 mg)TabletOralApotex CorporationNot applicableNot applicableCanada flag
Apo-apremilastApremilast (10 mg) + Apremilast (20 mg) + Apremilast (30 mg)TabletOralApotex CorporationNot applicableNot applicableCanada flag
Apo-apremilastApremilast (10 mg) + Apremilast (20 mg) + Apremilast (30 mg)TabletOralApotex CorporationNot applicableNot applicableCanada flag
Apo-apremilast TabletsApremilast (10 mg) + Apremilast (20 mg) + Apremilast (30 mg)TabletOralApotex CorporationNot applicableNot applicableCanada flag
Apo-apremilast TabletsApremilast (10 mg) + Apremilast (20 mg) + Apremilast (30 mg)TabletOralApotex CorporationNot applicableNot applicableCanada flag

Categories

ATC Codes
L04AA32 — Apremilast
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phthalimides. These are aromatic heterocyclic compounds containing a 1,3-dioxoisoindoline moiety. They are imide derivatives of phthalic anhydrides.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Isoindoles and derivatives
Sub Class
Isoindolines
Direct Parent
Phthalimides
Alternative Parents
Isoindoles / N-acetylarylamines / Anisoles / Methoxybenzenes / Phenoxy compounds / Alkyl aryl ethers / N-substituted carboxylic acid imides / Sulfones / Vinylogous amides / Acetamides
show 6 more
Substituents
Acetamide / Alkyl aryl ether / Anisole / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carbonyl group / Carboxamide group / Carboxylic acid derivative / Carboxylic acid imide
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
aromatic ether, sulfone, phthalimides, N-acetylarylamine (CHEBI:78540)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
UP7QBP99PN
CAS number
608141-41-9
InChI Key
IMOZEMNVLZVGJZ-QGZVFWFLSA-N
InChI
InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1
IUPAC Name
N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
SMILES
CCOC1=CC(=CC=C1OC)[C@@H](CS(C)(=O)=O)N1C(=O)C2=CC=CC(NC(C)=O)=C2C1=O

References

General References
  1. Molostvov G, Morris A, Rose P, Basu S, Muller G: The effects of selective cytokine inhibitory drugs (CC-10004 and CC-1088) on VEGF and IL-6 expression and apoptosis in myeloma and endothelial cell co-cultures. Br J Haematol. 2004 Feb;124(3):366-75. [Article]
  2. Abdulrahim H, Thistleton S, Adebajo AO, Shaw T, Edwards C, Wells A: Apremilast: a PDE4 inhibitor for the treatment of psoriatic arthritis. Expert Opin Pharmacother. 2015 May;16(7):1099-108. doi: 10.1517/14656566.2015.1034107. Epub 2015 Apr 11. [Article]
  3. Hoffmann M, Kumar G, Schafer P, Cedzik D, Capone L, Fong KL, Gu Z, Heller D, Feng H, Surapaneni S, Laskin O, Wu A: Disposition, metabolism and mass balance of [(14)C]apremilast following oral administration. Xenobiotica. 2011 Dec;41(12):1063-75. doi: 10.3109/00498254.2011.604745. Epub 2011 Aug 23. [Article]
  4. Suzuki Kurokawa M, Suzuki N: Behcet's disease. Clin Exp Med. 2004 Sep;4(1):10-20. [Article]
  5. Fertig BA, Baillie GS: PDE4-Mediated cAMP Signalling. J Cardiovasc Dev Dis. 2018 Jan 31;5(1). pii: jcdd5010008. doi: 10.3390/jcdd5010008. [Article]
  6. Tong B, Liu X, Xiao J, Su G: Immunopathogenesis of Behcet's Disease. Front Immunol. 2019 Mar 29;10:665. doi: 10.3389/fimmu.2019.00665. eCollection 2019. [Article]
  7. Young M, Roebuck HL: Apremilast, an oral phosphodiesterase 4 (PDE4) inhibitor: A novel treatment option for nurse practitioners treating patients with psoriatic disease. J Am Assoc Nurse Pract. 2016 Dec;28(12):683-695. doi: 10.1002/2327-6924.12428. Epub 2016 Nov 21. [Article]
  8. Liu Y, Zhou S, Nissel J, Wu A, Lau H, Palmisano M: The pharmacokinetic effect of coadministration of apremilast and methotrexate in individuals with rheumatoid arthritis and psoriatic arthritis. Clin Pharmacol Drug Dev. 2014 Nov;3(6):456-465. doi: 10.1002/cpdd.109. Epub 2014 May 8. [Article]
  9. Zerilli T, Ocheretyaner E: Apremilast (Otezla): A New Oral Treatment for Adults With Psoriasis and Psoriatic Arthritis. P T. 2015 Aug;40(8):495-500. [Article]
  10. Cada DJ, Ingram K, Baker DE: Apremilast. Hosp Pharm. 2014 Sep;49(8):752-62. doi: 10.1310/hpj4908-752. [Article]
  11. Afra TP, Razmi TM, Dogra S: Apremilast in Psoriasis and Beyond: Big Hopes on a Small Molecule. Indian Dermatol Online J. 2019 Jan-Feb;10(1):1-12. doi: 10.4103/idoj.IDOJ_437_18. [Article]
  12. FDA approvals, Otezla [Link]
  13. Otezla product information [Link]
  14. FDA Approved Drug Products: Otezla (apremilast) tablets for oral use [Link]
  15. Medsafe NZ [Link]
  16. EMA label, Otezla [Link]
KEGG Drug
D08860
PubChem Compound
11561674
PubChem Substance
310264858
ChemSpider
9736448
BindingDB
50248919
RxNav
1492727
ChEBI
78540
ChEMBL
CHEMBL514800
ZINC
ZINC000030691736
PDBe Ligand
A9L
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Apremilast
PDB Entries
7cbq
MSDS
Download (104 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAlopecia Areata (AA)1
4CompletedTreatmentCardiovascular Disease (CVD) / Psoriasis1
4CompletedTreatmentCentral Centrifugal Cicatricial Alopecia (CCCA)1
4CompletedTreatmentErythema Nodosum Leprosum1
4CompletedTreatmentPalmoplantar Psoriasis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
KitOral
Kit; tablet, film coatedOral
TabletOral
TabletOral30 mg
Tablet, film coatedOral30 mg/1
Tablet, film coatedOral30.0 mg/1
Tablet, coatedOral
Tablet, coatedOral30 mg
Tablet, film coatedOral
Tablet, film coatedOral30 mg
Tablet, film coatedOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8802717No2014-08-122023-03-19US flag
US6962940No2005-11-082023-03-19US flag
US6020358No2000-02-012018-10-30US flag
US7208516No2007-04-242023-03-19US flag
US7659302No2010-02-092023-03-19US flag
US8455536No2013-06-042023-03-19US flag
US9018243No2015-04-282023-03-19US flag
US7427638No2008-09-232024-11-17US flag
US7893101No2011-02-222023-12-09US flag
US9872854No2018-01-232034-05-29US flag
US9724330No2017-08-082023-03-19US flag
US10092541No2018-10-092034-05-29US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)156.1http://www.guildlink.com.au/gc/ws/celgene/pi.cfm?product=cjpaprem
boiling point (°C)741.3±60.0 http://www.chemspider.com/Chemical-Structure.9736448.html
pKa12.58https://pubchem.ncbi.nlm.nih.gov/compound/Apremilast#section=Solubility
Predicted Properties
PropertyValueSource
Water Solubility0.0341 mg/mLALOGPS
logP1.86ALOGPS
logP1.31Chemaxon
logS-4.1ALOGPS
pKa (Strongest Acidic)12.98Chemaxon
pKa (Strongest Basic)-4.2Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count7Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area119.08 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity119.1 m3·mol-1Chemaxon
Polarizability46.71 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0000900000-4fa09deea89e17357555
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-066r-1000900000-cc0757be6053d8d34230
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-02t9-0365900000-a7a9ec2eaa036bfc9807
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0cgi-1001900000-34e03e07eceb3110e43a
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udr-0329300000-fd8a063994b2e7a1c06f
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-2926500000-9f9145b4948f3748e11b
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-199.93428
predicted
DeepCCS 1.0 (2019)
[M+H]+202.32982
predicted
DeepCCS 1.0 (2019)
[M+Na]+208.24236
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Not Available
Specific Function
3',5'-cyclic-nucleotide phosphodiesterase activity
Gene Name
PDE4
Uniprot ID
Q86V67
Uniprot Name
Phosphodiesterase isozyme 4
Molecular Weight
11946.535 Da
References
  1. Baumer W, Hoppmann J, Rundfeldt C, Kietzmann M: Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis. Inflamm Allergy Drug Targets. 2007 Mar;6(1):17-26. [Article]
  2. Abdulrahim H, Thistleton S, Adebajo AO, Shaw T, Edwards C, Wells A: Apremilast: a PDE4 inhibitor for the treatment of psoriatic arthritis. Expert Opin Pharmacother. 2015 May;16(7):1099-108. doi: 10.1517/14656566.2015.1034107. Epub 2015 Apr 11. [Article]
  3. Afra TP, Razmi TM, Dogra S: Apremilast in Psoriasis and Beyond: Big Hopes on a Small Molecule. Indian Dermatol Online J. 2019 Jan-Feb;10(1):1-12. doi: 10.4103/idoj.IDOJ_437_18. [Article]
  4. FDA Approved Drug Products: Otezla (apremilast) tablets for oral use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Hoffmann M, Kumar G, Schafer P, Cedzik D, Capone L, Fong KL, Gu Z, Heller D, Feng H, Surapaneni S, Laskin O, Wu A: Disposition, metabolism and mass balance of [(14)C]apremilast following oral administration. Xenobiotica. 2011 Dec;41(12):1063-75. doi: 10.3109/00498254.2011.604745. Epub 2011 Aug 23. [Article]
  2. Zerilli T, Ocheretyaner E: Apremilast (Otezla): A New Oral Treatment for Adults With Psoriasis and Psoriatic Arthritis. P T. 2015 Aug;40(8):495-500. [Article]
  3. Young M, Roebuck HL: Apremilast, an oral phosphodiesterase 4 (PDE4) inhibitor: A novel treatment option for nurse practitioners treating patients with psoriatic disease. J Am Assoc Nurse Pract. 2016 Dec;28(12):683-695. doi: 10.1002/2327-6924.12428. Epub 2016 Nov 21. [Article]
  4. FDA Approved Drug Products: Otezla (apremilast) tablets for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Zerilli T, Ocheretyaner E: Apremilast (Otezla): A New Oral Treatment for Adults With Psoriasis and Psoriatic Arthritis. P T. 2015 Aug;40(8):495-500. [Article]
  2. FDA Approved Drug Products: Otezla (apremilast) tablets for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Zerilli T, Ocheretyaner E: Apremilast (Otezla): A New Oral Treatment for Adults With Psoriasis and Psoriatic Arthritis. P T. 2015 Aug;40(8):495-500. [Article]
  2. FDA Approved Drug Products: Otezla (apremilast) tablets for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created at November 18, 2007 18:26 / Updated at February 20, 2024 23:55