Hycanthone

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Hycanthone

Hycanthone is a anthelmintic drug that was previously used in the treatment of schistosomiasis. It is a derivative of lucanthone and is a DNA intercalator that causes single and double strand DNA breaks.

History

Hycanthone was first synthesized in the 1960s as a potential anticancer drug. However, it was found to be effective against Schistosoma mansoni, a parasitic worm that causes schistosomiasis. It was used extensively in the 1970s for the treatment of this disease, especially in Egypt and Brazil.

Mechanism of Action

Hycanthone works by intercalating into the DNA of the parasite, causing single and double strand breaks. This leads to the death of the parasite. It is also thought to inhibit the enzyme topoisomerase II, which is necessary for the replication of DNA.

Side Effects and Contraindications

The use of hycanthone is associated with several side effects, including nausea, vomiting, abdominal pain, and dizziness. It is also known to cause hepatotoxicity and neurotoxicity. Due to these side effects and its potential to cause mutagenesis, it is no longer used in the treatment of schistosomiasis.

Hycanthone is contraindicated in pregnant women due to its potential to cause teratogenesis. It is also contraindicated in individuals with liver disease due to its hepatotoxic effects.

Resistance

Resistance to hycanthone has been reported in Schistosoma mansoni. This is thought to be due to mutations in the parasite's DNA that prevent the drug from intercalating.

See Also

• Schistosomiasis
• Anthelmintic
• Lucanthone
• Topoisomerase II