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

Details

Stereochemistry RACEMIC
Molecular Formula C13H11N3O4
Molecular Weight 273.2441
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POMALIDOMIDE

SMILES

NC1=C2C(=O)N(C3CCC(=O)NC3=O)C(=O)C2=CC=C1

InChI

InChIKey=UVSMNLNDYGZFPF-UHFFFAOYSA-N
InChI=1S/C13H11N3O4/c14-7-3-1-2-6-10(7)13(20)16(12(6)19)8-4-5-9(17)15-11(8)18/h1-3,8H,4-5,14H2,(H,15,17,18)

HIDE SMILES / InChI
Molecular Formula C13H11N3O4
Molecular Weight 273.2441
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/?term=10386948; https://www.ncbi.nlm.nih.gov/pubmed/?term=19009291; http://www.ncbi.nlm.nih.gov/pubmed/?term=12649301; https://www.ncbi.nlm.nih.gov/pubmed/?term=16115943

Pomalidomide is a derivative of thalidomide marketed by Celgene, an analogue of thalidomide, is an immunomodulatory agent with antineoplastic activity. In in vitro cellular assays, pomalidomide inhibited proliferation and induced apoptosis of hematopoietic tumor cells. Additionally, pomalidomide inhibited the proliferation of lenalidomide-resistant multiple myeloma cell lines and synergized with dexamethasone in both lenalidomide-sensitive and lenalidomide-resistant cell lines to induce tumor cell apoptosis. Pomalidomide enhanced T cell- and natural killer (NK) cell-mediated immunity and inhibited production of pro-inflammatory cytokines (e.g., TNF-α and IL-6) by monocytes. Pomalidomide demonstrated anti-angiogenic activity in a mouse tumor model and in the in vitro umbilical cord model.

CNS Activity

CNS Active
3913
Curator's Comment: In vitro cell culture experiments were carried out to further investigate the impact of POM on the biology of macrophages. POM crosses the blood brain barrier with CNS penetration of ~ 39%.

Originator

Approval Year

2013
596
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 13.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8429
POMALYST

Approved Use

Indicated, in combination with dexamethasone, for patients with multiple myeloma who have received at least two prior therapies including lenalidomide and a proteasome inhibitor and have demonstrated disease progression on or within 60 days of completion of the last therapy.

Launch Date

2013
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
75 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204026s019lbl.pdf
4 mg 1 times / day steady-state, oral
dose: 4 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
POMALIDOMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
860 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204026s019lbl.pdf
4 mg 1 times / day steady-state, oral
dose: 4 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
POMALIDOMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204026s019lbl.pdf
4 mg 1 times / day steady-state, oral
dose: 4 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
POMALIDOMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
72%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204026s019lbl.pdf
4 mg 1 times / day steady-state, oral
dose: 4 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
POMALIDOMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
DLT: Diarrhea, Thrombocytopenia...
Dose limiting toxicities:
Diarrhea (grade 3, 3 patients)
Thrombocytopenia (grade 3, 3 patients)
Lung infection (grade 3, 3 patients)
Neutropenia (grade 4, 3 patients)
Lung infection (grade 3, 1 patient)
Thrombocytopenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
2.6 mg/m2 1 times / day steady, oral
MTD
Dose: 2.6 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 2.6 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
10 mg 1 times / day steady, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
unhealthy, 56 years (range: 20–85 years)
n = 2
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 56 years (range: 20–85 years)
Sex: M+F
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
DLT: Dyspnea, Neutropenia...
Dose limiting toxicities:
Dyspnea (grade 3, 2 patients)
Neutropenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Disc. AE: Birth defects, Venous thromboembolism...
Other AEs: Neutropenia, Anemia...
AEs leading to
discontinuation/dose reduction:
Birth defects (grade 5)
Venous thromboembolism (serious, 3%)
Other AEs:
Neutropenia (grade 3-4, 47%)
Anemia (grade 3-4, 22%)
Thrombocytopenia (grade 3-4, 22%)
Dizziness (grade 3-4, 1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
4 mg 1 times / day steady, oral
MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 14
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 14
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
2 mg 1 times / day steady, oral
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 6
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
3 mg 1 times / day steady, oral
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 8
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
5 mg 1 times / day steady, oral
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 10
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 3-4, 4 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204026Orig1s000ClinPharmR.pdf
healthy
n = 30
Health Status: healthy
Population Size: 30
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204026Orig1s000ClinPharmR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204026Orig1s000ClinPharmR.pdf
AEs

AEs

AESignificanceDosePopulation
Lung infection grade 3, 1 patient
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Thrombocytopenia grade 3, 1 patient
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Diarrhea grade 3, 3 patients
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Lung infection grade 3, 3 patients
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Thrombocytopenia grade 3, 3 patients
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Neutropenia grade 4, 3 patients
DLT
3.4 mg/m2 1 times / day steady, oral
Highest studied dose
Dose: 3.4 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 3.4 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Thrombocytopenia grade 4, 1 patient
DLT
2.6 mg/m2 1 times / day steady, oral
MTD
Dose: 2.6 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 2.6 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
unhealthy, 12.3 years (range: 5.8-20.8 years)
n = 29
Health Status: unhealthy
Condition: recurrent, progressive, or refractory CNS tumor
Age Group: 12.3 years (range: 5.8-20.8 years)
Sex: M+F
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/33025730
Dyspnea grade 3, 2 patients
DLT
10 mg 1 times / day steady, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
unhealthy, 56 years (range: 20–85 years)
n = 2
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 56 years (range: 20–85 years)
Sex: M+F
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
Neutropenia grade 4, 1 patient
DLT
10 mg 1 times / day steady, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
unhealthy, 56 years (range: 20–85 years)
n = 2
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 56 years (range: 20–85 years)
Sex: M+F
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/22875080
Dizziness grade 3-4, 1%
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Anemia grade 3-4, 22%
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Thrombocytopenia grade 3-4, 22%
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Neutropenia grade 3-4, 47%
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Birth defects grade 5
Disc. AE
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Venous thromboembolism serious, 3%
Disc. AE
4 mg 1 times / day steady, oral
Recommended|MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
unhealthy, 61 years (range: 37 - 88 years)
n = 107
Health Status: unhealthy
Condition: relapsed multiple myeloma
Age Group: 61 years (range: 37 - 88 years)
Sex: M+F
Population Size: 107
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204026lbl.pdf
Neutropenia grade 4, 2 patients
DLT
4 mg 1 times / day steady, oral
MTD
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 14
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 14
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
Fatigue grade 3, 1 patient
DLT
2 mg 1 times / day steady, oral
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 6
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
Neutropenia grade 4, 1 patient
DLT
3 mg 1 times / day steady, oral
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 8
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
Neutropenia grade 3-4, 4 patients
DLT
5 mg 1 times / day steady, oral
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
unhealthy, 64.7 years (range: 55-72 years)
n = 10
Health Status: unhealthy
Condition: relapsed and refractory multiple myeloma
Age Group: 64.7 years (range: 55-72 years)
Sex: M+F
Population Size: 10
Sources:
https://pubmed.ncbi.nlm.nih.gov/23243282
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737
inhibitor
1767

inducer
389
substrate
1217

inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882

CYP3A4/5
278

P-gp
1461

BCRP
699

OAT1
599

OAT3
642

OCT2
647

OATP1B3
706

OATP1B1
788
CYP1A2
1054

CYP2C19
991

P-gp
1537

UGT
192
CYP1A2
701

CYP2B6
547

CYP2C19
293

CYP3A4/5
124
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no [IC50 >30 uM]
CYP2A6
739
 no [IC50 >30 uM]
CYP2B6
1001
 no [IC50 >30 uM]
CYP2C19
1553
 no [IC50 >30 uM]
CYP2C8
965
 no [IC50 >30 uM]
CYP2C9
1819
 no [IC50 >30 uM]
CYP2D6
1891
 no [IC50 >30 uM]
CYP2E1
970
 no [IC50 >30 uM]
CYP3A4/5
335
 no [IC50 >30 uM]
BCRP
773
 no [Inhibition 20 uM]
OAT1
603
 no [Inhibition 20 uM]
OAT3
644
 no [Inhibition 20 uM]
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C9
1819
 no
CYP3A4/5
335
 no
OATP1B1
803
 no
OATP1B3
715
 no
OCT2
648
 no
P-gp
1650
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1054
 major
unknown
Comment: Clinical DDI studies to assess the influence of CYP3A4, CYP1A2 and P-gp inhibitors on pomalidomide exposure and any metabolites is planned
Page: 4.0
CYP3A4
1737
 major
unknown
Comment: Clinical DDI studies to assess the influence of CYP3A4, CYP1A2 and P-gp inhibitors on pomalidomide exposure and any metabolites is planned
Page: 4.0
CYP2C19
991
 minor
CYP2D6
1217
 minor
UGT
192
 yes
P-gp
1537
 yes
unknown
Comment: Clinical DDI studies to assess the influence of CYP3A4, CYP1A2 and P-gp inhibitors on pomalidomide exposure and any metabolites is planned
Page: 6.0
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:72690
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:72690
ChemicalBook
CB32128749
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32128749
MolPort
MolPort-016-633-239
https://www.molport.com/shop/molecule-link/MolPort-016-633-239
Selleck Chemicals
Pomalidomide(CC-4047)
http://www.selleckchem.com/products/Pomalidomide(CC-4047).html
eMolecules
32278076
https://www.emolecules.com/cgi-bin/more?vid=32278076
PubMed

PubMed

TitleDatePubMed
Immunomodulatory drugs (IMiDs) increase the production of IL-2 from stimulated T cells by increasing PKC-theta activation and enhancing the DNA-binding activity of AP-1 but not NF-kappaB, OCT-1, or NF-AT.
2005 Oct
Thalidomide derivative CC-4047 inhibits osteoclast formation by down-regulation of PU.1.
2006 Apr 15
Primary function analysis of human mental retardation related gene CRBN.
2008 Jun
Identification of a primary target of thalidomide teratogenicity.
2010 Mar 12
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.
2012 Nov
Pomalidomide: a novel drug to treat relapsed and refractory multiple myeloma.
2013
Pomalidomide and its clinical potential for relapsed or refractory multiple myeloma: an update for the hematologist.
2013 Jun
Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide.
2014 Aug 7
Human cytochrome P450 oxidation of 5-hydroxythalidomide and pomalidomide, an amino analogue of thalidomide.
2014 Jan 21
Patents

Patents

07091353
4
07576104
4
08012997
4
20040220144
1

Sample Use Guides

In Vivo Use Guide
Curator's Comment: Should be given in combination with dexamethasone
4 mg per day taken orally on Days 1-21 of repeated 28­ day cycles until disease progression
Route of Administration: Oral
In Vitro Use Guide
When a PBMC population was maintained in IL-2 over a period of 7 days, the addition of pomalidomide 1 μM (IC50) in the incubation significantly decreased the proportion/number of Tregs in the population, compared with untreated controls.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:29:19 GMT 2023
Edited
by admin
on Fri Dec 15 15:29:19 GMT 2023
Record UNII
D2UX06XLB5
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POMALIDOMIDE
DASH   EMA EPAR   INN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
ACTIMID
Brand Name English
POMALIDOMIDE [USAN]
Common Name English
pomalidomide [INN]
Common Name English
IMID 3
Code English
Pomalidomide [WHO-DD]
Common Name English
1H-ISOINDOLE-1,3(2H)-DIONE, 4-AMINO-2-(2,6-DIOXO-3-PIPERIDINYL)-
Systematic Name English
IMNOVID
Brand Name English
POMALIDOMIDE [JAN]
Common Name English
IMID-3
Code English
CC-4047
Code English
4-Amino-2-[(3RS)-2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione
Systematic Name English
POMALIDOMIDE [ORANGE BOOK]
Common Name English
POMALIDOMIDE [MI]
Common Name English
POMALIDOMIDE [VANDF]
Common Name English
3-(3-AMINO)-PHTALAMIDO-GLUTARIMIDE
Common Name English
POMALIDOMIDE [EMA EPAR]
Common Name English
POMALYST
Brand Name English
Classification Tree Code System Code
WHO-VATC QL04AX06
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
FDA ORPHAN DRUG 308610
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
FDA ORPHAN DRUG 635818
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
EU-Orphan Drug EU/3/10/759
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
FDA ORPHAN DRUG 161402
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
FDA ORPHAN DRUG 363212
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
NCI_THESAURUS C129820
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
NCI_THESAURUS C54677
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
WHO-ATC L04AX06
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
NDF-RT N0000184014
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
NCI_THESAURUS C1742
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
Code System Code Type Description
SMS_ID
100000126117
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
IUPHAR
7348
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
MESH
C467566
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
HSDB
8222
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
FDA UNII
D2UX06XLB5
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
EPA CompTox
DTXSID40893458
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
PUBCHEM
134780
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
DRUG BANK
DB08910
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
LACTMED
Pomalidomide
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
EVMPD
SUB33379
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
MERCK INDEX
m8978
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY Merck Index
RXCUI
1369713
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY RxNorm
USAN
SS-115
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
WIKIPEDIA
POMALIDOMIDE
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
NCI_THESAURUS
C72560
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
INN
8873
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
DRUG CENTRAL
4746
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
DAILYMED
D2UX06XLB5
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
ChEMBL
CHEMBL43452
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
CHEBI
72690
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
JAPANESE REVIEW
POMALYST
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY APPROVED MARCH 2015
CAS
19171-19-8
Created by admin on Fri Dec 15 15:29:19 GMT 2023 , Edited by admin on Fri Dec 15 15:29:19 GMT 2023
PRIMARY
Related Record Type Details
Structure of POMALIDOMIDE, (S)-
ENANTIOMER -> RACEMATE
Pomalidomide is a racemic mixture of the S-enantiomer (CC-5083) and the R-enantiomer (CC-6016) which interconvert in plasma via both enzymatic and non-enzymatic pathways.
Structure of POMALIDOMIDE, (R)-
ENANTIOMER -> RACEMATE
Pomalidomide is a racemic mixture of the S-enantiomer (CC-5083) and the R-enantiomer (CC-6016) which interconvert in plasma via both enzymatic and non-enzymatic pathways.
CYTOCHROME P450 1A2
METABOLIC ENZYME -> SUBSTRATE
PROTEIN CEREBLON
TARGET -> INHIBITOR
Dose-dependent interaction with the CRBN-DDB1 complex
IC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of CC-17368
METABOLITE -> PARENT
MINOR
URINE
Structure of CC-17368
METABOLITE -> PARENT
MINOR
PLASMA
Structure of CC-15262
METABOLITE -> PARENT
MINOR
URINE
Structure of CC-15262
METABOLITE -> PARENT
MINOR
URINE
Structure of CC-17368
METABOLITE -> PARENT
MINOR
FECAL
Structure of CC-8017
METABOLITE -> PARENT
MAJOR
FECAL; PLASMA; URINE
Related Record Type Details
Structure of POMALIDOMIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Vdss PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC Elimination
PHARMACOKINETIC
Elimination
PHARMACOKINETIC
NIH
NCATS
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DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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