Drug/Small Molecule:
levamisole

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

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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?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • L-Tetramisole
  • Levamisol [INN-Spanish]
  • Levamisole hydrochloride
  • Levamisolum [INN-Latin]
  • Phenyl imidothiazole
  • dl-Tetramisol
  • dl-Tetramisole
Trade Names
  • Ergamisol
  • Ketrax
  • LEVOMYSOL
  • Lepuron
  • Levamisol
  • Nilverm base
  • Tetramisol
  • Tetramisole
  • Tramisol
  • Vermisol 150
  • Wormicid
Brand Mixture Names

PharmGKB Accession Id:
PA450205

Description

An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)

Source: Drug Bank

Indication

For adjuvant treatment in combination with fluorouracil after surgical resection in patients with Dukes' stage C colon cancer. Also used to treat malignant melanoma and head/neck cancer.
Levamisole was originally used as an antihelminthic to treat worm infestations in both humans and animals.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The mechanism of action of levamisole as an antiparasitic agent appears to be tied to its agnositic activity towards the L-subtype nicotinic acetylcholine receptors in nematode muscles. This agonistic action reduces the capacity of the males to control their reproductive muscles and limits their ability to copulate. The mechanism of action of Levamisole as an anticancer drug in combination with fluorouracil is unknown. The effects of levamisole on the immune system are complex. The drug appears to restore depressed immune function rather than to stimulate response to above-normal levels. Levamisole can stimulate formation of antibodies to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis and chemotaxis, and increase neutrophil mobility, adherence, and chemotaxis.

Source: Drug Bank

Pharmacology

Levamisole is a synthetic imidazothiazole derivative that has been widely used in treatment of worm infestations in both humans and animals. As an anthelmintic, it probably works by targeting the nematode nicotinergic acetylcholine receptor. As an immunomodulator, it appears that Levamisole is an immunostimulant which has been shown to increase NK cells and activated T-cells in patients receiving this adjuvantly along with 5FU for Stage III colon cancer.

Source: Drug Bank

Food Interaction

Take on an empty stomach.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Primarily hepatic (extensive) with both active and inactive metabolites.

Source: Drug Bank

Protein Binding

20-25%

Source: Drug Bank

Absorption

Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.

Source: Drug Bank

Half-Life

4.4-5.6 hours (biphasic)

Source: Drug Bank

Toxicity

LD 50 = 40 mg/kg (Pigs, subcutaneous); LD 50 = 180 mg/kg (rat, oral)

Source: Drug Bank

Chemical Properties

Chemical Formula

C11H12N2S

Source: Drug Bank

Isomeric SMILES

c1ccc(cc1)[C@H]2CN3CCSC3=N2

Source: OpenEye

Canonical SMILES

C1CN2C[C@@H](N=C2S1)C1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

204.291

Source: Drug Bank

Monoisotopic Molecular Weight

204.072119084

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.

Drug Targets

Gene Description
ALB (source: Drug Bank)
ALPPL2 (source: Drug Bank)
CHRNA3 (source: Drug Bank)

Drug Interactions

Drug Description
acenocoumarol The agent increases the anticoagulant effect (source: Drug Bank)
acenocoumarol Levamisole may increase the anticoagulant effect of acenocoumarol. (source: Drug Bank)
anisindione Levamisole may increase the anticoagulant effect of anisindione. (source: Drug Bank)
dicumarol The agent increases the anticoagulant effect (source: Drug Bank)
dicumarol Levamisole may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
warfarin The agent increases the anticoagulant effect (source: Drug Bank)
warfarin Levamisole may increase the anticoagulant effect of warfarin. (source: Drug Bank)

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

May Treat
Contraindicated With

Publications related to levamisole: 3

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug hypersensitivity and human leukocyte antigens of the major histocompatibility complex. Annual review of pharmacology and toxicology. 2012. Bharadwaj Mandvi, 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
Human leukocyte antigens and drug hypersensitivity. Current opinion in allergy and clinical immunology. 2007. Chung Wen-Hung, 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
Cancer and leukemia group B gastrointestinal cancer committee. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Goldberg Richard M, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00848
ChEBI:
30524
KEGG Compound:
C07070
KEGG Drug:
D08114
PubChem Compound:
26879
PubChem Substance:
46509052
9282
Drugs Product Database (DPD):
645699
BindingDB:
50241179
ChemSpider:
25037
Therapeutic Targets Database:
DAP000570

Clinical Trials

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

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