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Thalidomide

Immunosuppressant · Treatment of Leprosy Reactions

ImmunosuppressantTreatment of Leprosy Reactions
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Teratogenic; contraindicated in pregnancy
FDA category + note
Top interactionssee all 12
  • AdalimumabSevereDatabaseDDInter
  • AldesleukinSevereDatabaseDDInter
  • AltretamineSevereDatabaseDDInter
  • AnastrozoleSevereDatabaseDDInter

Mechanism

Thalidomide inhibits TNF-α production from activated monocytes and has anti-angiogenic activity by inhibiting basic fibroblast growth factor (bFGF)-induced neovascularization. Its mechanism involves binding to cereblon (CRBN), a component of the E3 ubiquitin ligase complex, redirecting its substrate specificity to target transcription factors (IKZF1, IKZF3) for proteasomal degradation. Its notorious teratogenicity is now understood to involve cereblon-mediated degradation of the transcription factor SALL4, which is essential for limb development.

Indications

Severe type II reactions (erythema nodosum leprosum) in corticosteroid-dependent patientserythema nodosum leprosumnewly diagnosed MMheavily pretreated relapsed/refractory MMENL (erythema nodosum leprosum, as an alternative to prednisolone)multiple myelomavarious conditions where cytokines play an important roleCancer associated cachexiaErythema nodosum leprosum (ENL)

Dosing

Adult
programme. Increased doses of clofazimine are also useful. Paucibacillary leprosy should be treated with rifampicin and dapsone for 6 months. If treatment is interrupted the regimen should be recommenced where it was left off to complete the full course. Neither the multibacillary nor the paucibacillary antileprosy regimen is sufficient to treat tuberculosis.…

Pharmacokinetics

Half-life
about 6 h (enantiomers)
Bioavailability
slow absorption (oral), highly variable
Protein binding
without significant binding to plasma proteins
Metabolism
spontaneous hydrolysis in all body fluids (main elimination path for enantiomers); inactive hydrolysis products undergo CYP-mediated metabolism
Excretion
in the urine (thalidomide and metabolites), unchanged in feces (non-absorbed portion)

Contraindications

  • Pregnancy
  • Women of child-bearing potential unless they comply with a pregnancy prevention programme
  • pregnancy (highly teratogenic)

Side effects

Common
sedationconstipationfatiguenumbness of toes and feetmuscle crampsweaknesssigns of pyramidal tract involvementcarpal tunnel syndrome
Serious
  • Teratogenicity
  • peripheral sensory neuropathy (10%–30% of patients, dose- and time-dependent)
  • thromboembolic events (deep vein thrombosis, stroke, myocardial infarction)
  • phocomelia (teratogenic)
  • multiple defects of internal organs (teratogenic)
  • highly teratogenic
  • Teratogenic effect

Pregnancy & lactation

Pregnancy

Teratogenic; contraindicated in pregnancy

Drug interactions

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Aldesleukin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Altretamine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anastrozole
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Asparaginase Erwinia Chrysanthemi
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Asparaginase Escherichia Coli
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Atezolizumab
Severe
Database

Drug interaction classified as: others

Source: DDInter

Avelumab
Severe
Database

Drug interaction classified as: others

Source: DDInter

Axitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Azacitidine
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Betamethasone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Immunosuppressant drugs

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team