U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H24N2O7S
Molecular Weight 460.5
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of APREMILAST

SMILES

CCOC1=C(OC)C=CC(=C1)[C@@H](CS(C)(=O)=O)N2C(=O)C3=CC=CC(NC(C)=O)=C3C2=O

InChI

InChIKey=IMOZEMNVLZVGJZ-QGZVFWFLSA-N
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

HIDE SMILES / InChI

Molecular Formula C22H24N2O7S
Molecular Weight 460.5
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://ir.celgene.com/releasedetail.cfm?releaseid=872240; http://www.ncbi.nlm.nih.gov/pubmed/26806620; http://www.ncbi.nlm.nih.gov/pubmed/?term=20525198; http://www.ncbi.nlm.nih.gov/pubmed/20050849

Apremilast (brand name Otezla) selective inhibitor of phosphodiesterase 4 is used for the treatment of patients with moderate to severe plaque psoriasis. OTEZLA is the first and only PDE4 inhibitor approved for the treatment of plaque psoriasis, a chronic inflammatory disease of the skin resulting from an uncontrolled immune response. Apremilast also inhibits spontaneous production of TNF-alpha from human rheumatoid synovial cells. It has anti-inflammatory activity. By inhibiting PDE-4, apremilast increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including PDE-4, TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
74.0 nM [IC50]
0.074 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
OTEZLA

Approved Use

For the treatment of adult patients with active psoriatic arthritis and patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy

Launch Date

2014
Primary
OTEZLA

Approved Use

For the treatment of adult patients with active psoriatic arthritis and patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
527 ng × eq/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
APREMILAST, (+/-)- plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
208 ng/mL
10 mg 2 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
298 ng/mL
20 mg 2 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
637 ng/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6632 ng × eq × h/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
APREMILAST, (+/-)- plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1008 ng × h/mL
10 mg 2 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1591 ng × h/mL
20 mg 2 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3467 ng × h/mL
30 mg 2 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
APREMILAST plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
50.4 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
APREMILAST, (+/-)- plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
50 mg 2 times / day steady, oral
Overdose
Dose: 50 mg, 2 times / day
Route: oral
Route: steady
Dose: 50 mg, 2 times / day
Sources:
healthy, adult
n = 8
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Disc. AE: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Nausea (3%)
Diarrhea (2%)
Headache (2%)
Dizziness (1%)
Vomiting (1%)
Fatigue (1%)
Migraine (<1%)
Abdominal pain upper (<1%)
Decreased appetite (<1%)
Depressed mood (<1%)
Abdominal distension (<1%)
Sources: Page: p. 61
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Disc. AE: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Nausea (1%)
Diarrhea (1%)
Vomiting (<1%)
Fatigue (<1%)
Migraine (<1%)
Abdominal pain upper (<1%)
Decreased appetite (<1%)
Depressed mood (<1%)
Depression (<1%)
Abdominal distension (<1%)
Dyspepsia (<1%)
Sources: Page: p. 61
AEs

AEs

AESignificanceDosePopulation
Dizziness 1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Fatigue 1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Vomiting 1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Diarrhea 2%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Headache 2%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Nausea 3%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Abdominal distension <1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Abdominal pain upper <1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Decreased appetite <1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Depressed mood <1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Migraine <1%
Disc. AE
30 mg 2 times / day steady, oral
Recommended
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Diarrhea 1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Nausea 1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Abdominal distension <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Abdominal pain upper <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Decreased appetite <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Depressed mood <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Depression <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Dyspepsia <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Fatigue <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Migraine <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
Vomiting <1%
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources: Page: p. 61
unhealthy
n = 501
Health Status: unhealthy
Sex: M+F
Population Size: 501
Sources: Page: p. 61
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak [IC50 >10 uM]
weak
weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
no
no
no
no
no
no
no
no
weak
weak
weak
yes
yes
yes
no (co-administration study)
Comment: in vivo bioavailability is more than 70% and DDI study with ketoconazole (CYP3A and P-gp inhibitor) did not reveal the potential of a significant interaction
Page: 5.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
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.
2004 Feb
CC-10004 .
2005 May
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
2009 Mar 26
Disposition, metabolism and mass balance of [(14)C]apremilast following oral administration.
2011 Dec
Novel systemic drugs under investigation for the treatment of psoriasis.
2012 Jul
Novel systemic drugs for psoriasis: mechanism of action for apremilast, a specific inhibitor of PDE4.
2013 Jun
Apremilast: a PDE4 inhibitor for the treatment of psoriatic arthritis.
2015 May
Patents

Sample Use Guides

The recommended initial dosage titration of OTEZLA (apremilast) from Day 1 to Day 5 is from 10 mg till 30 mg corresponding. Following the 5-day titration, the recommended maintenance dosage is 30 mg twice daily taken orally starting on Day 6. This titration is intended to reduce the gastrointestinal symptoms associated with initial therapy.
Route of Administration: Oral
LPS-stimulated human monocytes were treated with concentrations of apremilast ranging from 6.25 nM to 100 nM.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:56:23 GMT 2023
Edited
by admin
on Fri Dec 15 15:56:23 GMT 2023
Record UNII
UP7QBP99PN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
APREMILAST
DASH   INN   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CC-10004
Code English
Apremilast [WHO-DD]
Common Name English
apremilast [INN]
Common Name English
(+)-N-(2-((1S)-1-(3-ETHOXY-4-METHOXYPHENYL)-2-(METHYLSULFONYL)ETHYL)-1,3-DIOXO- 2,3-DIHYDRO-1H-ISOINDOL-4-YL)ACETAMIDE
Systematic Name English
APREMILAST [USAN]
Common Name English
N-[2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide
Systematic Name English
APREMILAST [MI]
Common Name English
APREMILAST [VANDF]
Common Name English
OTEZLA
Brand Name English
APREMILAST [ORANGE BOOK]
Common Name English
Acetamide, N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-
Systematic Name English
APREMILAST [JAN]
Common Name English
CC10004
Code English
Classification Tree Code System Code
NDF-RT N0000182961
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
WHO-ATC L04AA32
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
EMA ASSESSMENT REPORTS OTEZLA (AUTHORIZED: ARTHRITIS, PSORIATIC)
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
NCI_THESAURUS C744
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
EU-Orphan Drug EU/3/13/1180
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
WHO-VATC QL04AA32
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
Code System Code Type Description
EPA CompTox
DTXSID30976289
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
USAN
SS-114
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
IUPHAR
7372
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
NDF-RT
N0000182960
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY Phosphodiesterase 4 Inhibitors [MoA]
INN
8872
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
HSDB
8221
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
MERCK INDEX
m2010
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY Merck Index
MESH
C505730
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
PUBCHEM
11561674
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
LACTMED
Apremilast
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
EVMPD
SUB130837
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
ChEMBL
CHEMBL514800
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
RXCUI
1492727
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY RxNorm
CHEBI
78540
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
CAS
608141-41-9
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
DRUG BANK
DB05676
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
FDA UNII
UP7QBP99PN
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
DAILYMED
UP7QBP99PN
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
SMS_ID
100000156798
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
DRUG CENTRAL
4829
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
NCI_THESAURUS
C147044
Created by admin on Fri Dec 15 15:56:23 GMT 2023 , Edited by admin on Fri Dec 15 15:56:23 GMT 2023
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
RACEMATE -> ENANTIOMER
TARGET -> INHIBITOR
Apremilast is a selective inhibitor of PDE4 that regulates inflammatory mediators.
COMPETITIVE INHIBITOR
IC50
TARGET -> INHIBITOR
INHIBITS PDE4 AND INCREASES cAMP CONCENTRATION
INDIRECT
BINDER->LIGAND
BINDING
Related Record Type Details
METABOLITE -> PARENT
MINOR
PLASMA; URINE
METABOLITE -> PARENT
Metabolites M7 and M17,which were present at trace levels in plasma, did retain some PDE4 and TNF-.alpha. inhibition activity, with IC 50 values similar to those of apremilast.
FECAL
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA; URINE
METABOLITE -> PARENT
MINOR
FECAL
METABOLITE -> PARENT
MINOR
FECAL
METABOLITE -> PARENT
MINOR
FECAL
METABOLITE -> PARENT
Metabolites M7 and M17,which were present at trace levels in plasma, did retain some PDE4 and TNF-.alpha. inhibition activity, with IC 50 values similar to those of apremilast.
FECAL; URINE
METABOLITE -> PARENT
Major fecal
MAJOR
FECAL
METABOLITE -> PARENT
MINOR
PLASMA; URINE
METABOLITE INACTIVE -> PARENT
METABOLITE -> PARENT
MINOR
URINE
METABOLITE -> PARENT
MINOR
FECAL
METABOLITE -> PARENT
MINOR
PLASMA; URINE
METABOLITE -> PARENT
MINOR
FECAL
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC