Drug/Small Molecule:
thalidomide

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with thalidomide that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105262

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all thalidomide variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs1051685 *451A>G, 101357A>G, 217070376A>G, 67279794A>G
A > G
3' UTR
No VIP available CA VA
rs12418 *4785G>A, 24577478G>A, 53895G>A, 73773014G>A, CHST3:rs12418 A>G, NM_004273.3:c.*4785G>A
G > A
3' UTR
No VIP available CA VA
rs12960 1180945G>A, 2063G>A, 50524G>A, 89620328G>A, Arg688Gln, NM_003119.2:c.2063G>A, NP_003110.1:p.Arg688Gln, SPG7:rs12960 A>G
G > A
Missense
Arg688Gln
No VIP available CA VA
rs1402467 108994808C>G, 13668637C>G, 15C>G, Asp5Glu, NM_006588.2:c.15C>G, NP_006579.2:p.Asp5Glu, SULT1C2:rs1402467 C>G
C > G
Missense
Asp5Glu
No VIP available CA VA
rs1799931 14616G>A, 18258370G>A, 6116516G>A, 857G>A, NAT2:857G>A, NAT2:GLY286GLU, NAT2:rs1799931 A>G, NM_000015.2:c.857G>A, NP_000006.2:p.Gly286Glu, included in NAT2*7B. A allele defines "M3", signature SNP for NAT2*7 allelic group
G > A
Missense
Gly286Glu
No VIP available CA VA
rs1871450 *3785G>A, 24576478G>A, 52895G>A, 73772014G>A, CHST3:rs1871450 A>G, NM_004273.3:c.*3785G>A
G > A
3' UTR
No VIP available CA VA
rs1883322 -101-8958C>T, -102+4436C>T, 14-18098C>T, 35309806C>T, 35369806C>T, 64472C>T, PPARD:rs1883322 A>G
C > T
Intronic
No VIP available CA VA
rs2016520 -87C>T, 14-9126C>T, 35318778C>T, 35378778C>T, 73444C>T, NM_006238.3:c.-87C>T, PPARD:rs2016520 A>G
C > T
5' UTR
No VIP available CA VA
rs2227291 107309G>C, 2299G>C, 564810G>C, 77268502G>C, ATP7A:rs2227291 C>G, NM_000052.4:c.2299G>C, NP_000043.3:p.Val767Leu, Val767Leu
G > C
Missense
Val767Leu
No VIP available CA VA
rs2238472 16191599C>T, 16251599C>T, 3803G>A, 70730G>A, ABCC6:rs2238472 A>G, Arg1268Gln, NM_001171.5:c.3803G>A, NP_001162.4:p.Arg1268Gln
C > T
Missense
Arg1268Gln
No VIP available CA VA
rs2292954 1173740A>G, 1507A>G, 43319A>G, 89613123A>G, NM_003119.2:c.1507A>G, NP_003110.1:p.Thr503Ala, SPG7:rs2292954 C>T, Thr503Ala
A > G
Missense
Thr503Ala
No VIP available CA VA
rs2301159 *755C>T, 103697728G>A, 16787404G>A, 26469C>T, NM_000452.2:c.*755C>T, SLC10A2:rs2301159 C>T
G > A
3' UTR
No VIP available CA VA
rs3734254 *1154C>T, 35335010C>T, 35395010C>T, 89676C>T, PPARD:rs3734254 C>T
C > T
3' UTR
No VIP available CA VA
rs4148943 *1278C>T, 24573971C>T, 50388C>T, 73769507C>T, CHST3:rs4148943 C>T, NM_004273.3:c.*1278C>T
C > T
3' UTR
No VIP available CA VA
rs4148945 *1361C>T, 24574054C>T, 50471C>T, 73769590C>T, CHST3:rs4148945 C>T, NM_004273.3:c.*1361C>T
C > T
3' UTR
No VIP available CA VA
rs4148947 *1888T>C, 24574581T>C, 50998T>C, 73770117T>C, CHST3:rs4148947 C>T, NM_004273.3:c.*1888T>C
T > C
3' UTR
No VIP available CA VA
rs4148950 *3477G>A, 24576170G>A, 52587G>A, 73771706G>A, CHST3:rs4148950 A>G, NM_004273.3:c.*3477G>A
G > A
3' UTR
No VIP available CA VA
rs4630 *101C>T, 24376322G>A, 3766891G>A
G > A
3' UTR
No VIP available CA VA
rs4646487 17251093C>T, 19506C>T, 47279175C>T, 517C>T, Arg173Trp, CYP4B1:rs4646487 C>T, NM_000779.3:c.517C>T, NP_000770.2:p.Arg173Trp
C > T
Missense
Arg173Trp
No VIP available CA VA
rs6922548 -101-25241A>G, -197-11752A>G, 14-34381A>G, 35293523A>G, 35353523A>G, 48189A>G, PPARD:rs6922548 A>G
A > G
Intronic
No VIP available CA VA
rs730720 *4533C>T, 24577226C>T, 53643C>T, 73772762C>T, CHST3:rs730720 A>G, NM_004273.3:c.*4533C>T
C > T
3' UTR
No VIP available CA VA
rs735482 *931T>G, 18180220A>C, 45912002A>C, 75085T>G, 776A>C, Lys259Thr
A > C
Missense
Lys259Thr
No VIP available CA VA
rs7769719 -101-16239G>A, -197-2750G>A, 14-25379G>A, 35302525G>A, 35362525G>A, 57191G>A, PPARD:rs7769719 A>G
G > A
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • N-Phthalimidoglutamic acid imide
  • N-Phthaloylglutamimide
  • N-Phthalylglutamic acid imide
  • Thalidomine USP26
  • alpha-phthalimidoglutarimide
  • thalidomide
Trade Names
  • Algosediv
  • Asidon 3
  • Asmadion
  • Asmaval
  • Bonbrain
  • Bonbrrin
  • Calmore
  • Calmorex
  • Contergan
  • Corronarobetin
  • Distaval
  • Distaxal
  • Distoval
  • Ectiluran
  • Enterosediv
  • Gastrinide
  • Glupan
  • Glutanon
  • Grippex
  • Hippuzon
  • Imida-Lab
  • Imidan
  • Imidene
  • Isomin
  • Kedavon
  • Kevadon
  • Lulamin
  • Neaufatin
  • Neo
  • Neosedyn
  • Neosydyn
  • Nerosedyn
  • Neufatin
  • Neurodyn
  • Neurosedin
  • Neurosedym
  • Neurosedyn
  • Nevrodyn
  • Nibrol
  • Noctosediv
  • Noxodyn
  • Pangul
  • Pantosediv
  • Poly-Giron
  • Polygripan
  • Predni-Sediv
  • Pro-ban M
  • Profarmil
  • Psycholiquid
  • Psychotablets
  • Quetimid
  • Quietoplex
  • Sandormin
  • Sedalis
  • Sedalis sedi-lab
  • Sedimide
  • Sedin
  • Sedisperil
  • Sedoval
  • Shin-naito S
  • Shinnibrol
  • Sleepan
  • Slipro
  • Softenil
  • Softenon
  • Talargan
  • Talimol
  • Talismol
  • Telagan
  • Telargan
  • Telargean
  • Tensival
  • Thalin
  • Thalinette
  • Thalomid
  • Theophilcholine
  • Valgis
  • Valgraine
  • Yodomin
Brand Mixture Names

PharmGKB Accession Id:
PA451644

Description

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 immunosuppresive and anti-angiogenic activity. It inhibits release of tumor necrosis factor-alpha from monocytes, and modulates other cytokine action.

Source: Drug Bank

Indication

For the acute treatment of the cutaneous manifestations of moderate to severe erythema nodosum leprosum (ENL). Also for use as maintenance therapy for prevention and suppression of the cutaneous manifestations of ENL recurrence.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

In patients with erythema nodosum leprosum (ENL) the mechanism of action is not fully understood. Available data from in vitro studies and preliminary clinical trials suggest that the immunologic effects of this compound can vary substantially under different conditions, but may be related to suppression of excessive tumor necrosis factor-alpha (TNF-a) production and down-modulation of selected cell surface adhesion molecules involved in leukocyte migration. For example, administration of thalidomide has been reported to decrease circulating levels of TNF-a in patients with ENL, however, it has also been shown to increase plasma TNF-a levels in HIV-seropositive patients. As a cancer treatment, the drug may act as a VEGF inhibitor.

Source: Drug Bank

Pharmacology

Thalidomide is an immunomodulatory agent with a spectrum of activity that is not fully characterized. Thalidomide is racemic — it contains both left and right handed isomers in equal amounts: one enantiomer is effective against morning sickness, and the other is teratogenic. The enantiomers are converted to each other in vivo. That is, if a human is given D-thalidomide or L-thalidomide, both isomers can be found in the serum. Hence, administering only one enantiomer will not prevent the teratogenic effect in humans.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Thalidomide itself does not appear to be hepatically metabolized to any large extent, but appears to undergo non-enzymatic hydrolysis in plasma to multiple metabolites. Thalidomide may be metabolized hepatically by enzymes of the cytochrome P450 enzyme system. The end product of metabolism, phthalic acid, is excreted as a glycine conjugate.

Source: Drug Bank

Protein Binding

55% and 66% for the (+)R and (−)S enantiomers, respectively.

Source: Drug Bank

Absorption

The absolute bioavailability has not yet been characterized in human subjects due to its poor aqueous solubility. In studies of both healthy volunteers and subjects with Hansen's disease, the mean time to peak plasma concentrations (Tmax) ranged from 2.9 to 5.7 hours indicating that thalidomide is slowly absorbed from the gastrointestinal tract.

Source: Drug Bank

Half-Life

The mean half-life of elimination ranges from approximately 5 to 7 hours following a single dose and is not altered upon multiple dosing.

Source: Drug Bank

Toxicity

The R-configuration and the S-configuration are more toxic individually than the racemic mixture. The LD 50 could not be established in mice for racemic thalidomide, whereas LD 50 values for the R and S configurations are reported to be 0.4 to 0.7 g/kg and 0.5 to 1.5 g/kg, respectively.

Source: Drug Bank

Route of Elimination

Thalidomide itself has less than 0.7% of the dose excreted in the urine as unchanged drug.

Source: Drug Bank

Chemical Properties

Chemical Formula

C13H10N2O4

Source: Drug Bank

Isomeric SMILES

c1ccc2c(c1)C(=O)N(C2=O)C3CCC(=O)NC3=O

Source: OpenEye

Canonical SMILES

O=C1N(C2CCC(=O)NC2=O)C(=O)C2=CC=CC=C12

Source: Drug Bank

Average Molecular Weight

258.2295

Source: Drug Bank

Monoisotopic Molecular Weight

258.064056818

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
FGFR2 (source: Drug Bank)
NFKB1 (source: Drug Bank)
PTGS2 (source: Drug Bank)
TNF (source: Drug Bank)

Drug Interactions

Drug Description
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
abatacept Thalidomide may increase the adverse effects of Abatacept. Increased risk of serious infection. Concomitant therapy should be avoided. (source: Drug Bank)
amikacin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
anakinra Thalidomide may increase the adverse effects of Anakinra. Increased risk of serious infection. Concomitant therapy should be avoided. (source: Drug Bank)
dexamethasone Increased risk of dermatologic adverse effects and venous thromboembolic events (VTE). Consider VTE prophylaxis during concomitant therapy and monitor for adverse dematologic effects. (source: Drug Bank)
gentamicin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
gentamicin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
natalizumab Thalidomide may increase the adverse effects of Natalizumab. Concurrent administration should be avoided due to increased risk of infection. (source: Drug Bank)
netilmicin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
tobramycin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
tobramycin Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Thalidomide increases the renal toxicity of the aminoglycoside (source: Drug Bank)
thalidomide Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank)
thalidomide The CNS depressants, Triprolidine and Thalidomide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
thalidomide The CNS depressants, Triprolidine and Thalidomide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to thalidomide: 9

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact on response and survival of DNA repair single nucleotide polymorphisms in relapsed or refractory multiple myeloma patients treated with thalidomide. Leukemia research. 2011. Cibeira MarĂ­a Teresa, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A pharmacogenetic study of docetaxel and thalidomide in patients with castration-resistant prostate cancer using the DMET genotyping platform. The pharmacogenomics journal. 2010. Deeken J F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Identification of a primary target of thalidomide teratogenicity. Science (New York, N.Y.). 2010. Ito Takumi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Systematic evaluation of drug-disease relationships to identify leads for novel drug uses. Clinical pharmacology and therapeutics. 2009. Chiang A P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug discovery. Repurposing with a difference. Science (New York, N.Y.). 2009. Boguski Mark S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic associations with thalidomide mediated venous thrombotic events in myeloma identified using targeted genotyping. Blood. 2008. Johnson David C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP450 pharmacogenetics for personalizing cancer therapy. Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy. 2008. van Schaik Ron H N. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Thalidomide and lenalidomide extend survival in a transgenic mouse model of amyotrophic lateral sclerosis. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2006. Kiaei Mahmoud, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphisms of the tumor necrosis factor-alpha gene promoter predict for outcome after thalidomide therapy in relapsed and refractory multiple myeloma. Blood. 2002. Neben Kai, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
59572-205-14
DrugBank:
DB01041
KEGG Compound:
C07910
KEGG Drug:
D00754
PubChem Compound:
5426
PubChem Substance:
10112
46505665
BindingDB:
50070114
ChemSpider:
5233
Therapeutic Targets Database:
DAP000865
FDA Drug Label at DailyMed:
2eda833b-1357-4ed4-a093-194524fcb061

Clinical Trials

These are trials that mention thalidomide and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.