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Thalidomide

drug
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Also known as .alpha.-phthalimidoglutarimideCelgeneConterganDistavalK-17KevadonMyrinN-phthalylglutamic acid imideNeurosedynNSC-527179NSC-66847PantosedivPharmionSoftenonTalidexTalidomidaThaledThalidomide lipomedThalomid

Summary

Thalidomide (CHEMBL468) is an approved small molecule (ATC L04AX02) targeting CRBN; indicated across 94 conditions including immune system disorder and plasma cell myeloma.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L04AX02
  • Targets: 1 (CRBN)
  • Indications: 94 conditions
  • Clinical trials: 344
  • Chemistry: 258.23 Da · C13H10N2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL468
NameThalidomide
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5426
ChEBICHEBI:74947
ATCL04AX02
Molecular formulaC13H10N2O4
Molecular weight258.23
InChIKeyUEJJHQNACJXSKW-UHFFFAOYSA-N

SMILES: C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O

IUPAC name: 2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione

ChEBI definition: A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.

Also known as: .alpha.-phthalimidoglutarimide, Celgene, Contergan, Distaval, K-17, Kevadon, Myrin, N-phthalylglutamic acid imide, Neurosedyn, NSC-527179, NSC-66847, Pantosediv

Patent coverage: 25,098 distinct patent families (97,393 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 95,046 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
CRBNcereblonBinding8.070.2%Q96SW2

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Muscarinic acetylcholine receptor M2, Mu-type opioid receptor, Prostaglandin G/H synthase 1, Aldehyde dehydrogenase 1A1, Protein cereblon, Prostaglandin G/H synthase 2, Protein cereblon/DNA damage-binding protein 1, Zinc finger protein Aiolos.

Bioactivity

ChEMBL activities: 27 potent at pChembl ≥ 5 of 32 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
DDB17.44EC5036nMCHEMBL_ACT_24860456
OPRM16.69AC50202.2nMCHEMBL_ACT_25158213
CRBN6.6Kd250nMCHEMBL_ACT_25848527
CRBN6.6Kd250nMCHEMBL_ACT_26133921
DDB16.57IC50268nMCHEMBL_ACT_28440005
DDB16.52IC50301nMCHEMBL_ACT_28439915
IKZF36.48EC50330nMCHEMBL_ACT_25673168
P059796.43IC50370nMCHEMBL_ACT_435711
IKZF36.3EC50500nMCHEMBL_ACT_29220691
P792086.3IC50500nMCHEMBL_ACT_435712
CRBN6.29Kd510nMCHEMBL_ACT_29075682
DDB16.25IC50560nMCHEMBL_ACT_25673120
CRBN6.14IC50720nMCHEMBL_ACT_29075708
DDB16.11IC50770nMCHEMBL_ACT_29220594
CRBN5.89IC501300nMCHEMBL_ACT_29075648
DDB15.86IC501380nMCHEMBL_ACT_24375641
CRBN5.83IC501490nMCHEMBL_ACT_25083005
CRBN5.75Ki1800nMCHEMBL_ACT_25639174
CRBN5.75Ki1800nMCHEMBL_ACT_26016804
CRBN5.57IC502700nMCHEMBL_ACT_25885804
CRBN5.54IC502900nMCHEMBL_ACT_25472085
CRBN5.49IC503260nMCHEMBL_ACT_29103055
CRBN5.36Ki4400nMCHEMBL_ACT_25528464
CRBN5.07Ki8510nMCHEMBL_ACT_22446499
CRBN5.07Ki8500nMCHEMBL_ACT_25589462
CRBN5.07Ki8500nMCHEMBL_ACT_25908410
CRBN5.07Ki8550nMCHEMBL_ACT_26009932

Target pathways

Aggregated over 1 target gene(s): CRBN.

Top Reactome pathways

1 total, by targets touching each:

PathwayTargetsGenes
Potential therapeutics for SARS1CRBN

Dominant GO biological processes

GO termTargets
protein ubiquitination1
positive regulation of Wnt signaling pathway1
negative regulation of protein-containing complex assembly1
positive regulation of protein-containing complex assembly1
negative regulation of monoatomic ion transmembrane transport1
locomotory exploration behavior1
proteasome-mediated ubiquitin-dependent protein catabolic process1
limb development1

Indications & clinical

Indications

94 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
immune system disorder4MONDO:0005046EFO:0000540
plasma cell myeloma4MONDO:0009693EFO:0001378
Crohn disease3MONDO:0005011EFO:0000384
colorectal adenocarcinoma3MONDO:0005008EFO:0000365
neoplasm3MONDO:0005070EFO:0000616
hepatocellular carcinoma3MONDO:0007256EFO:0000182
myelodysplastic syndrome3MONDO:0018881EFO:0000198
diffuse large B-cell lymphoma3MONDO:0018905EFO:0000403
ulcerative colitis3MONDO:0005101EFO:0000729
idiopathic pulmonary fibrosis3MONDO:0800504EFO:0000768
kidney neoplasm3MONDO:0021163EFO:0003865
colorectal neoplasm3MONDO:0005335EFO:0004142
vascular malformation3MONDO:0024291EFO:0006888
colorectal carcinoma3MONDO:0024331EFO:1001951
peritoneal neoplasm3MONDO:0006901MONDO:0002087
fallopian tube neoplasm3MONDO:0021092MONDO:0002158
kidney cancer3MONDO:0002367MONDO:0002367
lung neoplasm3MONDO:0021117MONDO:0008903
nasal cavity and paranasal sinus lethal midline granuloma3MONDO:0006828MONDO:0019472
sarcoidosis3MONDO:0019338MONDO:0019338
hereditary amyloidosis3MONDO:0018634MONDO:0019438
beta thalassemia3MONDO:0019402Orphanet:848
plasma cell neoplasm3MONDO:0004959EFO:0000200
stomatitis3MONDO:0004842EFO:1001904
sarcoma2MONDO:0005089EFO:0000691
primary myelofibrosis2MONDO:0009692EFO:0002430
HIV infectious disease2MONDO:0005109EFO:0000764
ankylosing spondylitis2MONDO:0005306EFO:0003898
B-cell chronic lymphocytic leukemia2MONDO:0004948EFO:0000095
hepatitis C virus infection2MONDO:0005231EFO:0003047
sclerosing cholangitis2MONDO:0018646EFO:0004268
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
neoplasm of mature B-cells2MONDO:0004949EFO:0000096
Hodgkins lymphoma2MONDO:0004952EFO:0000183
MALT lymphoma2MONDO:0007650EFO:0000191
chronic pancreatitis2MONDO:0005003EFO:0000342
cutaneous melanoma2MONDO:0005012EFO:0000389
glioblastoma2MONDO:0018177EFO:0000519
leukemia2MONDO:0005059EFO:0000565
lymphoma2MONDO:0005062EFO:0000574
prostate adenocarcinoma2MONDO:0005082EFO:0000673
psoriasis2MONDO:0005083EFO:0000676
renal cell carcinoma2MONDO:0005086EFO:0000681
melanoma2MONDO:0005105EFO:0000756
AIDS2MONDO:0012268EFO:0000765
medulloblastoma2MONDO:0007959EFO:0002939
non-Hodgkin lymphoma2MONDO:0018908EFO:0005952
head and neck cancer2MONDO:0005627EFO:0006859
autoimmune thrombocytopenic purpura2MONDO:0008558EFO:0007160
HIV wasting syndrome2MONDO:0005797EFO:0007312
pancreatic neuroendocrine tumor2MONDO:0019954EFO:1000045
brainstem neoplasm2MONDO:0021228EFO:1001767
neuroendocrine neoplasm2MONDO:0019496EFO:1001901
thalassemia2MONDO:0000984EFO:1001996
Waldenstrom macroglobulinemia2MONDO:0100280EFO:0009441
neuroblastoma2MONDO:0005072EFO:0000621
oral cavity cancer2MONDO:0005515EFO:0005570
central nervous system neoplasm2MONDO:0006130EFO:1000158
Langerhans cell histiocytosis2MONDO:0018310EFO:1000318
uterine carcinosarcoma2MONDO:0006485EFO:1000613
soft tissue sarcoma2MONDO:0018078EFO:1001968
appendiceal neoplasm2MONDO:0001236MONDO:0003196
breast neoplasm2MONDO:0021100MONDO:0007254
ovarian cancer2MONDO:0008170MONDO:0008170
Castleman disease2MONDO:0015564MONDO:0015564
follicular lymphoma2MONDO:0018906MONDO:0018906
colonic neoplasm2MONDO:0005401MONDO:0021063
proctitis2MONDO:0005538EFO:0005628
mantle cell lymphoma2MONDO:0018876EFO:1001469
discoid lupus erythematosus2MONDO:0019558MONDO:0019558
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
Alzheimer disease2MONDO:0004975MONDO:0004975
amyotrophic lateral sclerosis2MONDO:0004976MONDO:0004976
lymphoid leukemia2MONDO:0005402EFO:0004289
ocular melanoma2MONDO:0006325EFO:1000403
paraganglioma2MONDO:0000448EFO:1000453
syringomyelia2MONDO:0017987MONDO:0017987
systemic sclerosis1MONDO:0005100EFO:0000717
epilepsy1MONDO:0005027EFO:0000474
endometriosis1MONDO:0005133EFO:0001065
amyloidosis1MONDO:0019065EFO:1001875

13 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 344.

Phase distribution

PhaseTrials
PHASE2204
PHASE359
PHASE418
Not specified18
PHASE117
PHASE2/PHASE313
PHASE1/PHASE213
EARLY_PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06276933PHASE4NOT_YET_RECRUITINGA Study of Camrelizumab Combined With Chemotherapy ± Thalidomide in First-line Treatment of Patients With Advanced Non-small Cell Lung Cancer (NSCLC)
NCT00314665PHASE4TERMINATEDUse of Thalidomide in Chronic Uveitis
NCT00390247PHASE4WITHDRAWNThalidomide for the Treatment of Malnutrition Inflammation Syndrome in Peritoneal Dialysis Patients
NCT00652041PHASE4COMPLETEDBortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma
NCT01249690PHASE4UNKNOWNEfficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma
NCT01638078PHASE4UNKNOWNThalidomide fOr the Prevention of Restenosis After Coronary ArtERy Stent Implantation
NCT01640639PHASE4UNKNOWNTHalidomide on Left ventricUlar Morphology aND Function in congEstive heaRt Failure
NCT02401971PHASE4UNKNOWNIrinotecan Plus Thalidomide in Second Line Advanced Gastric Cancer
NCT02559154PHASE4UNKNOWNModified Bortezomib-based Combination Therapy for Multiple Myeloma
NCT02778893PHASE4UNKNOWNConmana Combined With Thalidomide to Treat NSCLC
NCT02844309PHASE4COMPLETEDThe Efficacy of TCD Following by TP Maintenance Therapy in Newly Diagnosed WM
NCT02858804PHASE4COMPLETEDEDOCH Alternating With DHAP for New Diagnosed Younger MCL
NCT03122431PHASE4COMPLETEDRelevance of Monitoring Blood and Salivar Levels of Drugs Used in Rheumatic Autoimmune Diseases
NCT03777930PHASE4UNKNOWNThe Evaluation of Curative Effect on Treatment of Tumor Above Thalidomide Combined With Megestrol
NCT04612582PHASE4UNKNOWNComparison of BTD and BCD Based Regimens in the Treatment of AL Amyloidosis
NCT05525234PHASE4UNKNOWNA Study of Thalidomide in the Treatment of Refractory Uremic Pruritus
NCT05527444PHASE4UNKNOWNThe Clinical Efficacy and the Changes of Immune Cells Subsets With Bioagents in Ankylosing Spondylitis Patients
NCT06299670PHASE4UNKNOWNEfficacy of Combination of Hdroxyurea and Thalidomide Over Either Hydroxyurea or Thalidomide Alone in the Treatment of Transfusion Dependent Thalassemia in Children: A Quasi-Randomised Clinical Trial
NCT00098475PHASE3ACTIVE_NOT_RECRUITINGLenalidomide and Dexamethasone With or Without Thalidomide in Treating Patients With Multiple Myeloma
NCT00572169PHASE3ACTIVE_NOT_RECRUITINGUARK 2006-66, Total Therapy 3B: An Extension of UARK 2003-33 Total Therapy
NCT00602641PHASE3ACTIVE_NOT_RECRUITINGMelphalan, Prednisone, and Thalidomide or Lenalidomide in Treating Patients With Newly Diagnosed Multiple Myeloma
NCT03562169PHASE3RECRUITINGThe Role of Ixazomib in Autologous Stem Cell Transplant in Relapsed Myeloma - Myeloma XII (ACCoRd)
NCT06017284PHASE3RECRUITINGThalidomide to Chemotherapy Related Nausea and Vomiting in Pancreatic Cancer
NCT07309419PHASE2/PHASE3NOT_YET_RECRUITINGA Phase III Randomized Study of TACE Plus an Oral Triple-Agent Cocktail Versus TACE Plus First-Line Targeted Immunotherapy in Unresectable Hepatocellular Carcinoma
NCT00004635PHASE3COMPLETEDThalidomide for the Treatment of Hormone-Dependent Prostate Cancer
NCT00004859PHASE3TERMINATEDCarboplatin, Paclitaxel, and Radiation Therapy With or Without Thalidomide in Patients With Stage III Non-small Cell Lung Cancer
NCT00005834PHASE3TERMINATEDS9922 Combination Chemo Plus Filgrastim With or Without Thalidomide in Refractory Multiple Myeloma
NCT00005966PHASE3COMPLETEDInterferon Alfa-2b With or Without Thalidomide in Treating Patients With Metastatic or Unresectable Kidney Cancer
NCT00028886PHASE3UNKNOWNCombination Chemotherapy With or Without Thalidomide in Treating Patients With Multiple Myeloma
NCT00033254PHASE3COMPLETEDRadiation Therapy With or Without Thalidomide in Treating Patients With Brain Metastases
NCT00033332PHASE3COMPLETEDDexamethasone With or Without Thalidomide in Treating Patients With Newly Diagnosed Multiple Myeloma
NCT00038090PHASE2/PHASE3COMPLETEDThalidomide-Dexamethasone for Multiple Myeloma
NCT00038233PHASE3COMPLETEDThalidomide for Multiple Myeloma
NCT00041080PHASE3COMPLETEDTamoxifen Compared With Thalidomide in Treating Women With Ovarian Epithelial Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer
NCT00049673PHASE3COMPLETEDThalidomide and Prednisone After Autologous Stem Cell Transplantation Multiple Myeloma
NCT00050843PHASE3COMPLETEDA Study to Access the Safety/Efficacy of Thalidomide in the Treatment of Anemia in Patients With Myelodysplastic Syndromes
NCT00075829PHASE3COMPLETEDStem Cell Transplantation in Individuals With Multiple Myeloma (BMT CTN 0102)
NCT00083551PHASE3COMPLETEDUARK 98-026 TT II: Multiple Myeloma Evaluating Anti-Angiogenesis With Thalidomide and Post-Transplant Consolidation Chemotherapy
NCT00083876PHASE3COMPLETEDD.T. PACE Versus High Dose Melphalan and Autologous Transplant in Patients With Previously Treated Multiple Myeloma
NCT00083915PHASE3COMPLETEDDTPACE Followed by Tandem Transplant With Melphalan (MEL) 200 Versus MEL/Dexamethasone/Thalidomide (DT) Platinol/Adriamycin/Etoposide (PACE) Hybrid and DTPACE Consolidation

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 26 clinical and 32 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

18 molecules share ≥1 primary target. Top 18 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)CRBN
POMALIDOMIDEChEMBL + PubChemPhase 4 (approved)CRBN
ASCIMINIBChEMBLPhase 4 (approved)CRBN
BRIGATINIBChEMBLPhase 4 (approved)CRBN
DASABUVIRChEMBLPhase 4 (approved)CRBN
LENALIDOMIDEChEMBLPhase 4 (approved)CRBN
PONATINIBChEMBLPhase 4 (approved)CRBN
IBERDOMIDEChEMBLPhase 3CRBN
MEZIGDOMIDEChEMBLPhase 3CRBN
URACILChEMBLPhase 3CRBN
VEPDEGESTRANTChEMBLPhase 3CRBN
ADAVOSERTIBChEMBLPhase 2CRBN
AVADOMIDEChEMBLPhase 2CRBN
E-7820ChEMBLPhase 2CRBN
FORETINIBChEMBLPhase 2CRBN
INDISULAMChEMBLPhase 2CRBN
FulvestrantPubChemApprovedCRBN
SotorasibPubChemApprovedCRBN

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot