Description

Simple

A drug used in medical imaging to help healthcare providers detect bladder cancer.

Clinical

An optical imaging agent used to perform Blue Light Cystoscopy (BLC™) in order to detect carcinoma of the bladder.

Overview

Hexaminolevulinate is an optical imaging drug. In solution form it is instilled intravesically for use with photodynamic blue light cystoscopy as an adjunct to white light cystoscopy. On May 28, 2010, the U.S. Food and Drug Administration (FDA) granted approval for hexaminolevulinate hydrochloride (Cysview for Intravesical Solution, Photocure ASA), as an optical imaging agent for use in combination with the Karl Storz Photodynamic Diagnostic D-Light C (PDD) System for cystoscopic detection of non-muscle invasive papillary cancer of the bladder for patients suspected or known to have lesion(s) on the basis of a prior cystoscopy. Hexaminolevulinate is manufactured under the brand Cysview® by Photocure ASA. In Europe, Hexaminolevulinate is marketed under the brand Hexvix®.

Pharmacology

Indication

Hexaminolevulinate is indicated for use in the cystoscopic detection of non-muscle invasive papillary cancer of the bladder among patients suspected or known to have lesion(s) on the basis of a prior cystoscopy.

Pharmacodynamic

In vitro studies have shown increased porphyrin fluorescence in normal urothelium after exposure to hexaminolevulinate hydrochloride intravesical solution. In the human bladder, a greater accumulation of porphyrins is proposed in neoplastic or inflamed cells, compared to normal urothelium. After bla... Read more

Mechanism of action

Hexaminolevulinate is an ester of the heme precursor, aminolevulinic acid. After bladder instillation, hexaminolevulinate enters the bladder mucosa and is proposed to enter the intracellular space of mucosal cells where it is used as a precursor in the formation of the photoactive intermediate proto... Read more

Absorption

Absolute bioavailability 7% (90% confidence interval [CI]: 5%-10%)

Protein binding

No evidence of significant binding.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Biphasic elimination, with an initial elimination half-life of 39 minutes, followed by a terminal half-life of approximately 76 hours.

Route of elimination

Information currently not available.

Toxicity

No studies in animals have been conducted to evaluate the carcinogenic potential of hexaminolevulinate hydrochloride.

Hexaminolevulinate hydrochloride was not mutagenic in in-vitro reverse mutation tests in bacteria, or in chromosome aberration tests in human peripheral blood lymphocytes, and wa... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Intravesical chemotherapy
      • Drugbank Id: DBCOND0108433
  • Regions: US
  • Patient Conditions:
      • Name: Porphyria
      • Drugbank Id: DBCOND0008396
  • Regions: US
  • Patient Conditions:
      • Name: BCG immunotherapy
      • Drugbank Id: DBCOND0108432
  • Regions: US
  • Patient Conditions:
      • Name: Gross hematuria
      • Drugbank Id: DBCOND0095751

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
BCG vaccine
BCG vaccine may decrease effectiveness of Hexaminolevulinate as a diagnostic agent.
Porfimer sodium
Hexaminolevulinate may increase the photosensitizing activities of Porfimer sodium.
Verteporfin
Hexaminolevulinate may increase the photosensitizing activities of Verteporfin.
3 References
  1. 1 . Yang LP: Hexaminolevulinate blue light cystoscopy: a review of its use in the diagnosis of bladder cancer. Mol Diagn Ther. 2014 Feb;18(1):105-16. doi: 10.1007/s40291-013-0068-x.PubMed: 24248555
  2. 2 . O'Brien T, Thomas K: Bladder cancer: Photodynamic diagnosis can improve surgical outcome. Nat Rev Urol. 2010 Nov;7(11):598-9. doi: 10.1038/nrurol.2010.183.PubMed: 21068759
  3. 3 . Hillemanns P, Wang X, Hertel H, Andikyan V, Hillemanns M, Stepp H, Soergel P: Pharmacokinetics and selectivity of porphyrin synthesis after topical application of hexaminolevulinate in patients with cervical intraepithelial neoplasia. Am J Obstet Gynecol. 2008 Mar;198(3):300.e1-7. doi: 10.1016/j.ajog.2007.07.045. Epub 2008 Feb 21.PubMed: 18177838