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thalidomide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antineoplastics, thalidomide derivatives	2616	50-35-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: thalidomide (+/-)-Thalidomide thalomid	A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action. Molecular weight: 258.23 Formula: C13H10N2O4 CLOGP: 0.53 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 83.55 ALOGS: -2 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

thalidomide
(+/-)-Thalidomide
thalomid

A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.

Molecular weight: 258.23
Formula: C13H10N2O4
CLOGP: 0.53
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 83.55
ALOGS: -2
ROTB: 1

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	4.70 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	22.13 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.95 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.40 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.05 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
April 16, 2008	EMA	Bristol-Myers Squibb Pharma EEIG
Feb. 24, 2021	PMDA	Fujimoto Pharmaceutical Corporation
July 16, 1998	FDA	CELGENE

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Disease progression	1509.23	14.59	851	28928	121907	63337336
Death	1396.70	14.59	1249	28530	373132	63086111
Plasma cell myeloma	823.28	14.59	380	29399	35525	63423718
Human chorionic gonadotropin increased	663.15	14.59	153	29626	1432	63457811
Neuropathy peripheral	633.44	14.59	481	29298	113186	63346057
Malignant neoplasm progression	322.92	14.59	284	29495	81837	63377406
Osteonecrosis	204.27	14.59	133	29646	24397	63434846
Deep vein thrombosis	202.22	14.59	222	29557	83578	63375665
Renal failure	182.01	14.59	249	29530	117403	63341840
Pneumonia	175.25	14.59	540	29239	456227	63003016

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Disease progression	1894.46	14.85	1243	34486	106834	34814368
Death	1621.73	14.85	1996	33733	396053	34525149
Plasma cell myeloma	731.37	14.85	483	35246	41554	34879648
Neuropathy peripheral	694.38	14.85	617	35112	82646	34838556
Malignant neoplasm progression	345.25	14.85	437	35292	87609	34833593
Osteonecrosis	333.44	14.85	201	35528	14689	34906513
Plasma cell myeloma recurrent	300.19	14.85	127	35602	4338	34916864
Deep vein thrombosis	291.44	14.85	346	35383	64902	34856300
Plasmacytoma	196.19	14.85	89	35640	3602	34917600
Acute myeloid leukaemia	173.15	14.85	146	35583	18124	34903078

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Disease progression	3684.95	13.82	1968	50088	182394	79509938
Death	3215.58	13.82	2761	49295	563753	79128579
Plasma cell myeloma	1345.00	13.82	668	51388	52591	79639741
Neuropathy peripheral	916.06	13.82	749	51307	140556	79551776
Malignant neoplasm progression	815.13	13.82	689	51367	135301	79557031
Plasma cell myeloma recurrent	521.36	13.82	174	51882	4827	79687505
Human chorionic gonadotropin increased	461.19	13.82	115	51941	1069	79691263
Deep vein thrombosis	452.53	13.82	472	51584	120447	79571885
Osteonecrosis	434.14	13.82	264	51792	30831	79661501
Pneumonia	315.19	13.82	1045	51011	659201	79033131

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AX02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Other immunosuppressants
CHEBI has role	CHEBI:35472	anti-inflammatory drugs
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:35705	immunosuppressive agents
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:35816	leprostatic drugs
CHEBI has role	CHEBI:48422	angiogenesis antagonist
CHEBI has role	CHEBI:50905	teratogeno
CHEBI has role	CHEBI:50919	antiemetico

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Crow-Fukase (POEMS) syndrome	indication	79268002	DOID:14039
Multiple myeloma	indication	109989006	DOID:9538
Erythema nodosum leprosum	indication	240411003
Refractory upper gastrointestinal bleeding due to angiodysplasia	off-label use	37372002
Pyoderma gangrenosum	off-label use	74578003	DOID:8553
Discoid lupus erythematosus	off-label use	200938002
Actinic prurigo	off-label use	201015007
Graft-versus-host disease	off-label use	234646005
Erosive oral lichen planus	off-label use	238662007
Subacute cutaneous lupus erythematosus	off-label use	239891002

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.84	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Protein cereblon	Cytosolic other	Q96SW2	CRBN_HUMAN	MODULATOR	EC50	6.39	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN		IC50	6.43	WOMBAT-PK
Tumor necrosis factor	Cytokine	P01375	TNFA_HUMAN		IC50	8	WOMBAT-PK
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN		IC50	6.30	WOMBAT-PK
Prostaglandin G/H synthase 2	Enzyme		PGH2_SHEEP		IC50	6.30	CHEMBL
Cereblon isoform 4	Unclassified		A4TVL0_9PROT		Ki	5.36	CHEMBL
Prostaglandin G/H synthase 1	Enzyme		PGH1_SHEEP		IC50	6.43	CHEMBL

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External reference:

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ID	Source
005933	NDDF
10432	RXNORM
11845	MMSL
4021134	VUID
4021134	VANDF
404878004	SNOMEDCT_US
4Z8R6ORS6L	UNII
5426	PUBCHEM_CID
7327	IUPHAR_LIGAND_ID
7488	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-205	CAPSULE	50 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-205	CAPSULE	50 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-205	CAPSULE	50 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-210	CAPSULE	100 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-210	CAPSULE	100 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-210	CAPSULE	100 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-215	CAPSULE	150 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-215	CAPSULE	150 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-215	CAPSULE	150 mg	ORAL	NDA	30 sections
Thalomid	HUMAN PRESCRIPTION DRUG LABEL	1	59572-220	CAPSULE	200 mg	ORAL	NDA	30 sections

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