Details of the Drug

General Information of Drug (ID: DMTGBAX)

Drug Name

Pomalidomide

Synonyms

Actimid (TN); Pomalidomide (Immunomodulator)

Indication

Disease Entry	ICD 11	Status	REF
Plasma cell myeloma	2A83.1	Approved	[1]
Systemic sclerosis	4A42	Approved	[2]

Affected Organisms

Humans and other mammals

ATC Code

L04AX06: Pomalidomide

L04AX: Other immunosuppressants

L04A: IMMUNOSUPPRESSANTS

L04: IMMUNOSUPPRESSANTS

L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

273.24

Logarithm of the Partition Coefficient (xlogp)

0.2

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 400 mcgh/L []
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 75 mcg/L []
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 2-3 h []
Clearance: The total body clearance of drug is 7-10 L/h []
Half-life: The concentration or amount of drug in body reduced by one-half in 9.4 hours [3]
Metabolism: The drug is metabolized via the hepatic []
Vd: The volume of distribution (Vd) of drug is 62 - 138 L []

Chemical Identifiers

Formula: C13H11N3O4
IUPAC Name: 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
Canonical SMILES: C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)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)
InChIKey: UVSMNLNDYGZFPF-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 134780
ChEBI ID: CHEMBL43452
CAS Number: 19171-19-8
UNII: D2UX06XLB5
DrugBank ID: DB08910
TTD ID: D0A3ZU
VARIDT ID: DR00151
INTEDE ID: DR1313
ACDINA ID: D00540

Drug-Molecule Activity Atlas (DMA)^NEW

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Drug Pharmacogenomic Perturbation (DPP)^NEW

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Drug ADMET Endpoint Profile (DAE)^NEW

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Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiogenesis/myeloma cell growth (AMCG)	TTDIBYJ	NOUNIPROTAC	Modulator	[4]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[5]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[6]
Cytochrome P450 1A2 (CYP1A2)_{Main DME}	DEJGDUW	CP1A2_HUMAN	Substrate	[7]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
C-C motif chemokine 2 (CCL2)	OTAD2HEL	CCL2_HUMAN	Protein Interaction/Cellular Processes	[8]
CCAAT/enhancer-binding protein alpha (CEBPA)	OTOM9OE4	CEBPA_HUMAN	Gene/Protein Processing	[8]
CCAAT/enhancer-binding protein delta (CEBPD)	OTNBIPMY	CEBPD_HUMAN	Gene/Protein Processing	[8]
CCAAT/enhancer-binding protein epsilon (CEBPE)	OTKZA25M	CEBPE_HUMAN	Gene/Protein Processing	[8]
Cytochrome P450 2C19 (CYP2C19)	OTFMJYYE	CP2CJ_HUMAN	Biotransformations	[9]
DNA-binding protein inhibitor ID-1 (ID1)	OTKGNZN5	ID1_HUMAN	Gene/Protein Processing	[8]
Endothelial transcription factor GATA-2 (GATA2)	OTBP2QQ2	GATA2_HUMAN	Gene/Protein Processing	[8]
Erythroid transcription factor (GATA1)	OTX1R7O1	GATA1_HUMAN	Gene/Protein Processing	[8]
Krueppel-like factor 1 (KLF1)	OT1FK08U	KLF1_HUMAN	Gene/Protein Processing	[8]
Sal-like protein 4 (SALL4)	OTC08PR5	SALL4_HUMAN	Protein Interaction/Cellular Processes	[10]

Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Pomalidomide (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Pomalidomide due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[11]
Troleandomycin	DMUZNIG	Moderate	Decreased metabolism of Pomalidomide caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[12]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Pomalidomide caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[13]
Tucatinib	DMBESUA	Moderate	Decreased clearance of Pomalidomide due to the transporter inhibition by Tucatinib.	Breast cancer [2C60-2C6Y]	[12]
Lumacaftor	DMCLWDJ	Moderate	Increased metabolism of Pomalidomide caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[14]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Pomalidomide caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[15]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Pomalidomide caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[16]
Cobicistat	DM6L4H2	Moderate	Decreased metabolism of Pomalidomide caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[12]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Pomalidomide caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[17]
Ceritinib	DMB920Z	Moderate	Decreased clearance of Pomalidomide due to the transporter inhibition by Ceritinib.	Lung cancer [2C25]	[12]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Pomalidomide caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[18]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Pomalidomide caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[19]
Idelalisib	DM602WT	Moderate	Decreased metabolism of Pomalidomide caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[12]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Pomalidomide caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[20]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Pomalidomide caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[21]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Pomalidomide and Siponimod.	Multiple sclerosis [8A40]	[12]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Pomalidomide and Ocrelizumab.	Multiple sclerosis [8A40]	[22]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Pomalidomide and Ozanimod.	Multiple sclerosis [8A40]	[21]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Pomalidomide caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[21]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Pomalidomide caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[23]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Pomalidomide caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[24]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Pomalidomide when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[25]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Pomalidomide caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[21]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Pomalidomide caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[12]
Fostamatinib	DM6AUHV	Moderate	Decreased clearance of Pomalidomide due to the transporter inhibition by Fostamatinib.	Thrombocytopenia [3B64]	[26]


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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium stearyl fumarate	E00545	23665634	lubricant

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Pomalidomide 1 mg capsule	1 mg	Oral Capsule	Oral
Pomalidomide 2 mg capsule	2 mg	Oral Capsule	Oral
Pomalidomide 3 mg capsule	3 mg	Oral Capsule	Oral
Pomalidomide 4 mg capsule	4 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Pomalidomide FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7348).
3	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4	Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
5	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB08910)
6	Pomalidomide: evaluation of cytochrome P450 and transporter-mediated drug-drug interaction potential in vitro and in healthy subjects. J Clin Pharmacol. 2015 Feb;55(2):168-78.
7	Population pharmacokinetics of pomalidomide. J Clin Pharmacol. 2015 May;55(5):563-72.
8	Immunomodulatory derivative of thalidomide (IMiD CC-4047) induces a shift in lineage commitment by suppressing erythropoiesis and promoting myelopoiesis. Blood. 2005 May 15;105(10):3833-40. doi: 10.1182/blood-2004-03-0828. Epub 2004 Aug 3.
9	Human cytochrome P450 oxidation of 5-hydroxythalidomide and pomalidomide, an amino analogue of thalidomide. Chem Res Toxicol. 2014 Jan 21;27(1):147-56. doi: 10.1021/tx4004215. Epub 2013 Dec 24.
10	Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. Elife. 2018 Aug 1;7:e38430. doi: 10.7554/eLife.38430.
11	Product Information. Pomalyst (pomalidomide). QLT Phototherapeutics Inc, Vancouver, AZ.
12	Cerner Multum, Inc. "Australian Product Information.".
13	Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
14	Patel S, Robinson R, Burk M "Hypertensive crisis associated with St. John's Wort." Am J Med 112 (2002): 507-8. [PMID: 11959071]
15	Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
16	EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
17	Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
18	Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
19	Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
20	Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
21	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
22	Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
23	Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
24	Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
25	CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
26	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.