Identification

Name
Pomalidomide
Accession Number
DB08910
Type
Small Molecule
Groups
Approved
Description

Pomalidomide, an analogue of thalidomide, is an immunomodulatory antineoplastic agent. FDA approved on February 8, 2013.

Structure
Thumb
Synonyms
Not Available
External IDs
CC-4047
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ImnovidCapsule2 mgOralCelgene Europe Limited2013-08-05Not applicableEu
ImnovidCapsule4 mgOralCelgene Europe Limited2013-08-05Not applicableEu
ImnovidCapsule1 mgOralCelgene Europe Limited2013-08-05Not applicableEu
ImnovidCapsule3 mgOralCelgene Europe Limited2013-08-05Not applicableEu
PomalystCapsule4 mgOralCelgene2014-02-24Not applicableCanada
PomalystCapsule1 mgOralCelgene2014-02-24Not applicableCanada
PomalystCapsule4 mg/1OralCelgene2013-02-18Not applicableUs
PomalystCapsule1 mg/1OralCelgene2013-02-18Not applicableUs
PomalystCapsule3 mgOralCelgene2014-02-24Not applicableCanada
PomalystCapsule3 mg/1OralCelgene2013-02-18Not applicableUs
International/Other Brands
Imnovid
Categories
UNII
D2UX06XLB5
CAS number
19171-19-8
Weight
Average: 273.2441
Monoisotopic: 273.074955855
Chemical Formula
C13H11N3O4
InChI Key
UVSMNLNDYGZFPF-UHFFFAOYSA-N
InChI
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)
IUPAC Name
4-amino-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
SMILES
NC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O

Pharmacology

Indication

Pomalidomide is indicated for patients with multiple myeloma who have received at least two prior therapies including lenalidomide and bortezomib and have demonstrated disease progression on or within 60 days of completion of the last therapy.

Associated Conditions
Pharmacodynamics

Pomalidomide is more potent than thalidomide (100-times) and lenalidomide (10-times).

Mechanism of action

Promalidomide is an immunomodulatory agent with antineoplastic activity. It is shown to inhibit the proliferation and induce apoptosis of various tumour cells. Furthermore, promalidomide enhances T cell and natural killer (NK) cell-mediated immunity and inhibited the production of pro-inflammatory cytokines, like TNF-alpha or IL-6, by monocytes. The primary target of promalidomide is thought to be the protein cereblon. It binds to this target and inhibits ubiquitin ligase activity. It is also a transcriptional inhibitor of COX2.

TargetActionsOrganism
AProtein cereblon
inhibitor
Human
ATumor necrosis factor
inhibitor
Human
AProstaglandin G/H synthase 2
inhibitor
Human
Absorption

Pomalidomide is generally well absorbed. The major circulating component is the parent compound. Tmax, single oral dose = 2 -3 hours. When 4 mg of promalidomide is given to patients with multiple myeloma, the steady-state pharmacokinetic parameters are as follows: AUC(T) = 400 ng.hr/mL; Cmax = 75 ng/mL. Promalidomide accumulates following multiple doses.

Volume of distribution

Mean apparent volume of distribution (Vd/F), steady-state = 62 - 138 L

Protein binding

12-44% protein bound. It is not concentration dependent.

Metabolism

Promalidomide is hepatically metabolized by CYP1A2 and CYP3A4. The metabolites are 26-fold less active than the parent compound. Minor contributions from CYP2C19 and CYP2D6 have been observed in vitro.

Route of elimination

When a single oral dose (2mg) is given to healthy subjects, 73% of the dose was eliminated in urine. 15% of the dose was eliminated in feces. 2% and 8% of the dose eliminated unchanged as pomalidomide in urine and feces, respectively.

Half life

Healthy subjects = 9.4 hours; Multiple myeloma patients = 7.5 hours.

Clearance

Total body clearance = 7-10 L/hour

Toxicity

Most common adverse reactions (≥30%) included fatigue and asthenia, neutropenia, anemia, constipation, nausea, diarrhea, dyspnea, upper-respiratory tract infections, back pain and pyrexia.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(4R)-limoneneThe risk or severity of adverse effects can be increased when (4R)-limonene is combined with Pomalidomide.
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Pomalidomide.
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Pomalidomide.
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Pomalidomide.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Pomalidomide is combined with 7-Nitroindazole.
AbirateroneThe serum concentration of Pomalidomide can be increased when it is combined with Abiraterone.
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Pomalidomide.
AcemetacinThe risk or severity of adverse effects can be increased when Acemetacin is combined with Pomalidomide.
AcepromazineThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Aceprometazine.
Food Interactions
Not Available

References

General References
  1. Gertz MA: Pomalidomide and myeloma meningitis. Leuk Lymphoma. 2013 Apr;54(4):681-2. doi: 10.3109/10428194.2012.723708. Epub 2013 Jan 2. [PubMed:22917017]
  2. McCurdy AR, Lacy MQ: Pomalidomide and its clinical potential for relapsed or refractory multiple myeloma: an update for the hematologist. Ther Adv Hematol. 2013 Jun;4(3):211-6. doi: 10.1177/2040620713480155. [PubMed:23730498]
  3. Terpos E, Kanellias N, Christoulas D, Kastritis E, Dimopoulos MA: Pomalidomide: a novel drug to treat relapsed and refractory multiple myeloma. Onco Targets Ther. 2013 May 10;6:531-8. doi: 10.2147/OTT.S34498. Print 2013. [PubMed:23690693]
External Links
KEGG Drug
D08976
PubChem Compound
134780
PubChem Substance
175427148
ChemSpider
118785
BindingDB
65456
ChEBI
72690
ChEMBL
CHEMBL43452
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pomalidomide
ATC Codes
L04AX06 — Pomalidomide
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (292 KB)
MSDS
Download (479 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedTreatmentMultiple Myeloma (MM)1
1Active Not RecruitingOtherMultiple Myeloma (MM)1
1Active Not RecruitingTreatmentB-Cell Lymphoma, Unclassifiable, With Features Intermediate Between Diffuse Large B-Cell Lymphoma and Burkitt Lymphoma / Central Nervous System Lymphoma / Intraocular Lymphoma / Primary Diffuse Large B-Cell Lymphoma of the Central Nervous System / Recurrent Adult Diffuse Large Cell Lymphoma / Retinal Lymphoma1
1Active Not RecruitingTreatmentBlasts 10-19 Percent of Bone Marrow Nucleated Cells / Blasts 20 Percent or More of Bone Marrow Nucleated Cells / Blasts 5-19 Percent of Peripheral Blood White Cells / Blasts More Than 10 Percent of Bone Marrow Nucleated Cells / Chronic Myelomonocytic Leukemia-2 / High Risk Myelodysplastic Syndrome / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome / Myeloproliferative Neoplasms / Previously Treated Myelodysplastic Syndromes / Untreated Adult Acute Myeloid Leukemia1
1Active Not RecruitingTreatmentImpaired Renal Function / Multiple Myeloma (MM)1
1Active Not RecruitingTreatmentMalignant Lymphomas / Plasma Cell Myeloma1
1Active Not RecruitingTreatmentMultiple Myeloma (MM)5
1Active Not RecruitingTreatmentNeurofibromatosis Type 1 / Recurrent Central Nervous System Neoplasm / Recurrent Childhood Brain Stem Glioma / Recurrent Childhood Visual Pathway Glioma / Refractory Central Nervous System Neoplasm1
1CompletedNot AvailableClinical Pharmacology, Healthy Volunteer Study2
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailableHealthy Volunteers / Pharmacology, Clinical1
1CompletedTreatmentBioequivalence1
1CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL) / Other B-cell NHL Subtypes, Including WM / T-cell NHL / Waldenström's Macroglobulinemia (WM)1
1CompletedTreatmentMultiple Myeloma (MM)1
1CompletedTreatmentMultiple Myeloma (MM) / Multiple Myeloma in Relapse / Refractory Multiple Myeloma1
1CompletedTreatmentSickle Cell Disorders1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1Not Yet RecruitingTreatmentMultiple Myeloma (MM)1
1Not Yet RecruitingTreatmentRecurrent Plasma Cell Myeloma1
1RecruitingTreatmentHaematological Malignancies / Plasma Cell Myeloma1
1RecruitingTreatmentHereditary Haemorrhagic Telangiectasia (HHT) / Idiopathic Vascular Ectasia1
1RecruitingTreatmentKaposi s Sarcoma (KS)1
1RecruitingTreatmentMultiple Myeloma (MM)3
1RecruitingTreatmentRelapsed Or Refractory Multiple Myeloma1
1SuspendedTreatmentLight Chain Deposition Disease / Primary Systemic Amyloidosis1
1SuspendedTreatmentRecurrent Plasma Cell Myeloma1
1TerminatedTreatmentMultiple Myeloma (MM)2
1TerminatedTreatmentMultiple Myeloma in Relapse1
1TerminatedTreatmentPlasma Cell Myeloma1
1TerminatedTreatmentWaldenström's Macroglobulinemia (WM)1
1, 2Active Not RecruitingTreatmentAL Amyloidosis1
1, 2Active Not RecruitingTreatmentAdvanced Malignancies / Cancer, Advanced / Metastatic Cancers / Tumors, Solid1
1, 2Active Not RecruitingTreatmentChronic Myeloproliferative Disorders / Secondary Myelofibrosis1
1, 2Active Not RecruitingTreatmentKaposi s Sarcoma (KS)1
1, 2Active Not RecruitingTreatmentMultiple Myeloma (MM)8
1, 2Active Not RecruitingTreatmentPlasma Cell Myeloma1
1, 2Active Not RecruitingTreatmentRecurrent Plasma Cell Myeloma / Refractory Plasma Cell Myeloma1
1, 2Active Not RecruitingTreatmentRefractory Multiple Myeloma1
1, 2CompletedTreatmentMalignant Neoplasm of Pancreas1
1, 2CompletedTreatmentMultiple Myeloma (MM)1
1, 2CompletedTreatmentPlasma Cell Myeloma1
1, 2RecruitingTreatmentLymphoma, Hodgkins / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
1, 2RecruitingTreatmentMultiple Myeloma (MM)4
1, 2RecruitingTreatmentMultiple Myeloma in Relapse1
1, 2RecruitingTreatmentPMF / Post-ET MF / Post-PV MF / Primary Myelofibrosis / Secondary Myelofibrosis / SMF1
1, 2RecruitingTreatmentPlasma Cell Myeloma1
1, 2TerminatedTreatmentCarcinoma, Small Cell1
1, 2TerminatedTreatmentMultiple Myeloma (MM)3
1, 2WithdrawnTreatmentLarge Cell Lymphoma Arising in KSHV-associated Multicentric Castleman Disease / Primary Effusion Lymphomas1
2Active Not RecruitingTreatmentGraft Versus Host Disease (GVHD)1
2Active Not RecruitingTreatmentHigh Grade Squamous Intra-epithelial Lesion (HSIL)1
2Active Not RecruitingTreatmentMultiple Myeloma (MM)7
2Active Not RecruitingTreatmentMultiple Myeloma (MM) / Relapse After Use of Lenalidomide and Bortezomib1
2Active Not RecruitingTreatmentMultiple Myeloma in Relapse / Refractory Multiple Myeloma1
2Active Not RecruitingTreatmentPolycythemia Vera (PV) / Thrombocythemia1
2CompletedTreatmentAgnogenic Myeloid Metaplasia / Myelofibrosis With Myeloid Metaplasia / Myeloid Metaplasia1
2CompletedTreatmentGraft Versus Host Disease (GVHD)1
2CompletedTreatmentMultiple Myeloma (MM)5
2CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1
2CompletedTreatmentPrimary Amyloidosis of Light Chain Type1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentRecurrent Plasma Cell Myeloma / Refractory Plasma Cell Myeloma1
2CompletedTreatmentRelapsed Or Refractory Multiple Myeloma1
2CompletedTreatmentScleroderma, Systemic / Sclerosis, Progressive Systemic1
2Not Yet RecruitingTreatmentGenetic Condition / Multiple Myeloma (MM) / Relapsed and Refractory Multiple Myeloma1
2Not Yet RecruitingTreatmentHuman Immunodeficiency Virus 1 Positive / Skin Kaposi Sarcoma1
2Not Yet RecruitingTreatmentMultiple Myeloma (MM)1
2Not Yet RecruitingTreatmentMultiple Myeloma in Relapse / Multiple Myeloma Progression / Refractory Multiple Myeloma1
2Not Yet RecruitingTreatmentRelapsed/Refractory Multiple Myeloma1
2RecruitingTreatmentCentral Nervous System Neoplasms / Medulloblastomas1
2RecruitingTreatmentLeukemia, Plasma Cell / Plasma Cell Myeloma / Plasmacytoma1
2RecruitingTreatmentMultiple Myeloma (MM)6
2RecruitingTreatmentMultiple Myeloma in Relapse1
2RecruitingTreatmentRecurrent Plasma Cell Myeloma / Refractory Plasma Cell Myeloma1
2RecruitingTreatmentRefractory Multiple Myeloma1
2RecruitingTreatmentRelapsed and/or Refractory Multiple Myeloma1
2TerminatedTreatmentSoft Tissue Sarcoma (STS)1
2Unknown StatusTreatmentMyeloproliferative Neoplasms1
2WithdrawnTreatmentMultiple Myeloma (MM)2
2, 3RecruitingTreatmentRelapsed and/or Refractory Multiple Myeloma1
3Active Not RecruitingTreatmentMultiple Myeloma (MM)4
3Active Not RecruitingTreatmentPlasma Cell Myeloma1
3Active Not RecruitingTreatmentPrimary Myelofibrosis1
3CompletedTreatmentMultiple Myeloma (MM)2
3Not Yet RecruitingTreatmentMultiple Myeloma (MM)2
3RecruitingTreatmentMultiple Myeloma (MM)4
3RecruitingTreatmentRelapse Multiple Myeloma1
Not AvailableApproved for MarketingNot AvailableMultiple Myeloma (MM)1
Not AvailableRecruitingNot AvailableMultiple Myeloma (MM)3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral1 mg
CapsuleOral1 mg/1
CapsuleOral2 mg/1
CapsuleOral2 mg
CapsuleOral3 mg/1
CapsuleOral3 mg
CapsuleOral4 mg/1
CapsuleOral4 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6045501No1998-08-282018-08-28Us
US6315720No2000-10-232020-10-23Us
US6561976No1998-08-282018-08-28Us
US6561977No2000-10-232020-10-23Us
US6755784No2000-10-232020-10-23Us
US6908432No1998-08-282018-08-28Us
US8204763No1998-08-282018-08-28Us
US8315886No2000-10-232020-10-23Us
US8626531No2000-10-232020-10-23Us
US8589188No1998-08-282018-08-28Us
US5635517No1999-10-042019-10-04Us
US6316471No1996-08-102016-08-10Us
US6476052No1996-07-242016-07-24Us
US8198262No2004-10-192024-10-19Us
US8673939No2003-05-152023-05-15Us
US8735428No2003-05-152023-05-15Us
US8828427No2011-06-212031-06-21Us
US8158653No1996-08-102016-08-10Us
US9993467No2010-05-192030-05-19Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.57 mg/mLALOGPS
logP0.02ALOGPS
logP-0.16ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)11.59ChemAxon
pKa (Strongest Basic)1.56ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area109.57 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity69.03 m3·mol-1ChemAxon
Polarizability25.81 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9653
Blood Brain Barrier+0.8304
Caco-2 permeable-0.6419
P-glycoprotein substrateSubstrate0.5264
P-glycoprotein inhibitor INon-inhibitor0.5983
P-glycoprotein inhibitor IINon-inhibitor0.9147
Renal organic cation transporterNon-inhibitor0.847
CYP450 2C9 substrateNon-substrate0.844
CYP450 2D6 substrateNon-substrate0.8882
CYP450 3A4 substrateSubstrate0.5079
CYP450 1A2 substrateNon-inhibitor0.8863
CYP450 2C9 inhibitorNon-inhibitor0.8428
CYP450 2D6 inhibitorNon-inhibitor0.9002
CYP450 2C19 inhibitorNon-inhibitor0.8513
CYP450 3A4 inhibitorNon-inhibitor0.7289
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8686
Ames testNon AMES toxic0.7979
CarcinogenicityNon-carcinogens0.9081
BiodegradationNot ready biodegradable0.9858
Rat acute toxicity2.5862 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9885
hERG inhibition (predictor II)Non-inhibitor0.7765
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-1590000000-a511655f5e07f3ab2179

Taxonomy

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
Alpha amino acids and derivatives / Isoindoles / Piperidinediones / Delta lactams / N-substituted carboxylic acid imides / Benzenoids / Vinylogous amides / N-unsubstituted carboxylic acid imides / Dicarboximides / Azacyclic compounds
show 5 more
Substituents
Phthalimide / Alpha-amino acid or derivatives / Isoindole / Piperidinedione / Delta-lactam / Piperidinone / Benzenoid / Piperidine / Carboxylic acid imide, n-substituted / Carboxylic acid imide
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
dicarboximide, aromatic amine, piperidones, isoindoles (CHEBI:72690)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2. Norma...
Gene Name
CRBN
Uniprot ID
Q96SW2
Uniprot Name
Protein cereblon
Molecular Weight
50545.375 Da
References
  1. McCurdy AR, Lacy MQ: Pomalidomide and its clinical potential for relapsed or refractory multiple myeloma: an update for the hematologist. Ther Adv Hematol. 2013 Jun;4(3):211-6. doi: 10.1177/2040620713480155. [PubMed:23730498]
  2. Ito T, Ando H, Suzuki T, Ogura T, Hotta K, Imamura Y, Yamaguchi Y, Handa H: Identification of a primary target of thalidomide teratogenicity. Science. 2010 Mar 12;327(5971):1345-50. doi: 10.1126/science.1177319. [PubMed:20223979]
  3. Lopez-Girona A, Mendy D, Ito T, Miller K, Gandhi AK, Kang J, Karasawa S, Carmel G, Jackson P, Abbasian M, Mahmoudi A, Cathers B, Rychak E, Gaidarova S, Chen R, Schafer PH, Handa H, Daniel TO, Evans JF, Chopra R: Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35. doi: 10.1038/leu.2012.119. Epub 2012 May 3. [PubMed:22552008]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Tumor necrosis factor receptor binding
Specific Function
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct ac...
Gene Name
TNF
Uniprot ID
P01375
Uniprot Name
Tumor necrosis factor
Molecular Weight
25644.15 Da
References
  1. Gertz MA: Pomalidomide and myeloma meningitis. Leuk Lymphoma. 2013 Apr;54(4):681-2. doi: 10.3109/10428194.2012.723708. Epub 2013 Jan 2. [PubMed:22917017]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Ferguson GD, Jensen-Pergakes K, Wilkey C, Jhaveri U, Richard N, Verhelle D, De Parseval LM, Corral LG, Xie W, Morris CL, Brady H, Chan K: Immunomodulatory drug CC-4047 is a cell-type and stimulus-selective transcriptional inhibitor of cyclooxygenase 2. J Clin Immunol. 2007 Mar;27(2):210-20. Epub 2007 Feb 17. [PubMed:17308870]

Enzymes

Kind
Protein
Organism
Human
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. Li Y, Xu Y, Liu L, Wang X, Palmisano M, Zhou S: Population pharmacokinetics of pomalidomide. J Clin Pharmacol. 2015 May;55(5):563-72. doi: 10.1002/jcph.455. Epub 2015 Feb 4. [PubMed:25556560]
  2. Pomalidomide FDA label [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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

Transporters

Kind
Protein
Organism
Human
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 on June 20, 2013 16:45 / Updated on October 16, 2018 08:40