Drug/Small Molecule:
dapsone

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 gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.


last updated 10/25/2013

FDA Label for dapsone and G6PD

This label is on the FDA Biomarker List
Actionable PGx

Summary

The FDA-approved label for dapsone gel provides a precautionary warning that G6PD deficient individuals may be at an increased risk of hemolytic adverse reactions, as oral dapsone treatment is associated with dose-related hemolysis and hemolytic anemia in these individuals. This enzyme deficiency is due to underlying genetic variants in the G6PD gene and can be tested for by enzyme activity or genetic tests.

Annotation

Dapsone gel (Aczone) is indicated for the topical treatment of acne vulgaris. Although the Dapsone drug label does not specifically mention genetic testing, the drug label highlights that G6PD deficient individuals may be more at risk of hematological adverse effects, though no evidence of hemolysis or anemia was observed when treated with the gel form of dapsone. Oral dapsone is associated with hemolysis and hemolytic anemia in G6PD deficient individuals. G6PD deficiency is a condition caused by variants in the G6PD gene that can be determined by enzymatic or genetic tests (see the G6PD VIP summary).

Excerpts from the dapsone gel (Aczone) drug label:

Oral dapsone treatment has produced dose-related hemolysis and hemolytic anemia. Individuals with glucose-6-phosphate dehydrogenase (G6PD) deficiency are more prone to hemolysis with the use of certain drugs...There was no evidence of clinically relevant hemolysis or anemia in patients treated with ACZONE Gel, 5%, including patients who were G6PD deficient. Some subjects with G6PD deficiency using ACZONE Gel developed laboratory changes suggestive of mild hemolysis.

WARNINGS AND PRECAUTIONS
Hematological Effects: Some subjects with G6PD deficiency using ACZONE Gel developed laboratory changes suggestive of mild hemolysis. (5.1)(8.6)

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the and Dapsone gel drug label.

Please note that the drug label for dapsone tablets available on the DailyMed website also precautions use of dapsone in patients with methemoglobin reductase (CYB5R3) deficiency or Hemoglobin M, both caused by underlying genetic variants, see the Dapsone tablet drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • Acne Vulgaris
    • Indications & usage section, Dosage & administration section
    • source: FDA Label
  • Anemia, Hemolytic
    • Information for patients section, Use in specific populations section, Warnings and precautions section, toxicity
    • source: FDA Label
  • G6PD
    • Information for patients section, Use in specific populations section, Warnings and precautions section, toxicity
    • source: FDA Label

Clinical Variants that meet the highest level of criteria, manually curated by PharmGKB, are shown below.

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?
Molecular Genetics Laboratory ARUP Laboratories, Glucose-6-Phosphate Dehydrogenase (G6PD) 2 Mutations G6PDA-202A_376G , rs1050829 , rs1050828

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.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA G6PD A-202A_376G N/A N/A N/A
No VIP available CA VA HLA-B *13:01:01 N/A N/A N/A
No VIP available CA VA
rs1050828 153764217C>T, 16571G>A, 202G>A, 292G>A, 4682155C>T, Asahi, G6PD:202G>A, Val68Met, Val98Met
C > T
Not Available
Val68Met
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Acedapsone
  • DADPS
  • DDS
  • DSS
  • Dapson
  • Dapsonum
  • Dds, Diaphenylsulfone
  • Dds, Pharmaceutical
  • Diamino-diphenyl sulphone
  • Diaminodifenilsulfona
  • Diaminodiphenyl Sulfone
  • Diaphenylsulfon
  • Diaphenylsulfone
  • Diaphenylsulphon
  • Diaphenylsulphone
  • Diphenasone
  • Metabolite C
  • N, N'-Diphenyl Sulfondiamide
  • P, P'-Sulfonyldianiline
  • P,P'-Diaminodiphenyl Sulfone
  • P,P-Diaminodiphenyl Sulphone
  • P,P-Sulfonylbisbenzamine
  • P,P-Sulfonylbisbenzenamine
  • P,P-Sulphonylbisbenzamine
  • P,P-Sulphonylbisbenzenamine
  • P,P-Sulphonyldianiline
  • P-Aminophenyl Sulfone
  • Sulfonyldianiline
  • Sulphadione
  • Sulphonyldianiline
  • dapsone
Trade Names
  • Araldite Ht
  • Avlosulfon
  • Avlosulfone
  • Avlosulphone
  • Croysulfone
  • Croysulphone
  • Dimitone
  • Diphone
  • Dubronax
  • Dumitone
  • Eporal
  • ICI
  • Normet
  • Novophone
  • Recolip
  • Sulfadione
  • Sulfanona-Mae
  • Sulfon-Mere
  • Sulfona
  • Sulfona-Mae
  • Sulfone Ucb
  • Sulphon-Mere
  • Sumicure S
  • Tarimyl
  • Udolac
Brand Mixture Names

PharmGKB Accession Id:
PA449211

Description

A sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae. Its mechanism of action is probably similar to that of the sulfonamides which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with pyrimethamine in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)

Source: Drug Bank

Indication

For the treatment and management of leprosy and dermatitis herpetiformis.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Dapsone acts against bacteria and protozoa in the same way as sulphonamides, that is by inhibiting the synthesis of dihydrofolic acid through competition with para-amino-benzoate for the active site of dihydropteroate synthetase. The anti-inflammatory action of the drug is unrelated to its antibacterial action and is still not fully understood.

Source: Drug Bank

Pharmacology

Dapsone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Dapsone is the principal drug in a multidrug regimen recommended by the World Health Organization for the treatment of leprosy. As an anti-infective agent, it is also used for treating malaria and, recently, for Pneumocystic carinii pneumonia in AIDS patients. Dapsone is absorbed rapidly and nearly completely from the gastrointestinal tract. Dapsone is distributed throughout total body water and is present in all tissues. However, it tends to be retained in skin and muscle and especially in the liver and kidney: traces of the drug are present in these organs up to 3 weeks after therapy cessation.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, mostly CYP2E1-mediated.

Source: Drug Bank

Protein Binding

70 to 90%

Source: Drug Bank

Absorption

Bioavailability is 70 to 80% following oral administration.

Source: Drug Bank

Half-Life

28 hours (range 10-50 hours)

Source: Drug Bank

Toxicity

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.

Source: Drug Bank

Route of Elimination

Renal

Source: Drug Bank

Chemical Properties

Chemical Formula

C12H12N2O2S

Source: Drug Bank

Isomeric SMILES

c1cc(ccc1N)S(=O)(=O)c2ccc(cc2)N

Source: OpenEye

Canonical SMILES

NC1=CC=C(C=C1)S(=O)(=O)C1=CC=C(N)C=C1

Source: Drug Bank

Average Molecular Weight

248.301

Source: Drug Bank

Monoisotopic Molecular Weight

248.061948328

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
DHFR (source: Drug Bank)

Drug Interactions

Drug Description
dapsone Formation of non-absorbable complexes (source: Drug Bank)
dapsone Formation of non-absorbable complexes (source: Drug Bank)
aluminium Formation of non-absorbable complexes (source: Drug Bank)
Calcium Formation of non-absorbable complexes (source: Drug Bank)
Calcium Formation of non-absorbable complexes (source: Drug Bank)
Magnesium Formation of non-absorbable complexes (source: Drug Bank)
Magnesium Formation of non-absorbable complexes (source: Drug Bank)
magnesium oxide Formation of non-absorbable complexes (source: Drug Bank)
rifabutin Decreased levels of dapsone (source: Drug Bank)
rifabutin Decreased levels of dapsone (source: Drug Bank)
rifampin Decreased levels of dapsone (source: Drug Bank)
rifampin Decreased levels of dapsone (source: Drug Bank)
trimethoprim Increased toxicity of both products (source: Drug Bank)
trimethoprim Increased toxicity of both products (source: Drug Bank)
dapsone Decreased levels of dapsone (source: Drug Bank)
dapsone Decreased levels of dapsone (source: Drug Bank)
dapsone Decreased levels of dapsone (source: Drug Bank)
dapsone Decreased levels of dapsone (source: Drug Bank)
dapsone Telithromycin may reduce clearance of Dapsone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dapsone if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
dapsone Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Dapsone. Consider alternate therapy or monitor for changes in Dapsone therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
dapsone Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Dapsone. Consider alternate therapy or monitor for changes in Dapsone therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
dapsone Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of dapsone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of dapsone if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

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

May Treat
May Prevent
Contraindicated With

Publications related to dapsone: 25

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Humanized mouse model of glucose 6-phosphate dehydrogenase deficiency for in vivo assessment of hemolytic toxicity. Proceedings of the National Academy of Sciences of the United States of America. 2013. Rochford Rosemary, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
HLA-B*13:01 and the dapsone hypersensitivity syndrome. The New England journal of medicine. 2013. Zhang F-R, 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
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, 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
Malaria pharmacogenomics: return to the future. Pharmacogenomics. 2013. Gil Jp. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Clinical spectrum and severity of hemolytic anemia in glucose 6-phosphate dehydrogenase-deficient children receiving dapsone. Blood. 2012. Pamba Allan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for G6PD. Pharmacogenetics and genomics. 2012. McDonagh Ellen M, 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
Prospective-retrospective biomarker analysis for regulatory consideration: white paper from the industry pharmacogenomics working group. Pharmacogenomics. 2011. Patterson Scott D, 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 review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, 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
Medications and glucose-6-phosphate dehydrogenase deficiency: an evidence-based review. Drug safety : an international journal of medical toxicology and drug experience. 2010. Youngster Ilan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The rise and fall of the antimalarial Lapdap: a lesson in pharmacogenetics. Lancet. 2010. Luzzatto Lucio. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria. European journal of clinical pharmacology. 2009. Miller Ann K, 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
Application of pharmacogenomics to malaria: a holistic approach for successful chemotherapy. Pharmacogenomics. 2009. Mehlotra Rajeev K, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Chlorproguanil-dapsone-artesunate versus artemether-lumefantrine: a randomized, double-blind phase III trial in African children and adolescents with uncomplicated Plasmodium falciparum malaria. PloS one. 2009. Premji Zul, 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
Glucose-6-phosphate dehydrogenase deficiency. Lancet. 2008. Cappellini M D, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
High risk of severe anaemia after chlorproguanil-dapsone+artesunate antimalarial treatment in patients with G6PD (A-) deficiency. PloS one. 2008. Fanello Caterina I, 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
G6PD deficiency: the genotype-phenotype association. Blood reviews. 2007. Mason Philip J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Comparison of chlorproguanil-dapsone with sulfadoxine-pyrimethamine for the treatment of uncomplicated falciparum malaria in young African children: double-blind randomised controlled trial. Lancet. 2004. Alloueche A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Chlorproguanil-dapsone versus sulfadoxine-pyrimethamine for sequential episodes of uncomplicated falciparum malaria in Kenya and Malawi: a randomised clinical trial. Lancet. 2002. Sulo J, 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
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott 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
Meta-analysis of phenotype and genotype of NAT2 deficiency in Chinese populations. Pharmacogenetics. 1997. Xie H G, 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
Concise review: methemoglobinemia. American journal of hematology. 1993. Mansouri A, 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
Genetically determined drug-metabolizing activity and desipramine-associated cardiotoxicity: a case report. Clinical pharmacology and therapeutics. 1993. Bluhm R E, 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
Glucose-6-phosphate dehydrogenase deficiency. WHO Working Group. Bulletin of the World Health Organization. 1989. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
N-acetylation pharmacogenetics. Pharmacological reviews. 1985. Weber W W, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0469-5005-03
DrugBank:
DB00250
ChEBI:
4325
KEGG Compound:
C07666
KEGG Drug:
D00592
PubChem Compound:
2955
PubChem Substance:
46505300
7847658
Drugs Product Database (DPD):
2041510
BindingDB:
50029764
ChemSpider:
2849
Therapeutic Targets Database:
DAP000637
FDA Drug Label at DailyMed:
aa249ecd-afd3-4800-b196-d4f7b8c8fc6e

Clinical Trials

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

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