Nifurtimox
Encyclopedia
Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosome
Trypanosoma
Trypanosoma is a genus of kinetoplastids , a monophyletic group of unicellular parasitic flagellate protozoa. The name is derived from the Greek trypano and soma because of their corkscrew-like motion. All trypanosomes are heteroxenous and are transmitted via a vector...

s including Chagas disease
Chagas disease
Chagas disease is a tropical parasitic disease caused by the flagellate protozoan Trypanosoma cruzi. T. cruzi is commonly transmitted to humans and other mammals by an insect vector, the blood-sucking insects of the subfamily Triatominae most commonly species belonging to the Triatoma, Rhodnius,...

 and sleeping sickness. It is given by mouth and not by injection.

Indications

Nifurtimox has been used to treat Chagas disease
Chagas disease
Chagas disease is a tropical parasitic disease caused by the flagellate protozoan Trypanosoma cruzi. T. cruzi is commonly transmitted to humans and other mammals by an insect vector, the blood-sucking insects of the subfamily Triatominae most commonly species belonging to the Triatoma, Rhodnius,...

, when it is given for 30 to 60 days, but gastrointestinal and neurological side effects have meant that benznidazole
Benznidazole
Benznidazole is an antiparasitic medication used in the treatment of Chagas disease. Its mechanism of action is thought to be inhibition of protein and ribonucleic acid synthesis...

 is now preferred for that indication.

Nifurtimox has also been used to treat African trypanosomiasis (sleeping sickness), and is active in the second stage of the disease (CNS
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...

 involvement). When nifurtimox is given on its own, about half of all patients will relapse, but the combination of melarsoprol
Melarsoprol
Melarsoprol is a medicinal drug used in the treatment of human African trypanosomiasis. It is also sold under the trade names “Mel B” and “Melarsen Oxide-BAL.”...

 with nifurtimox appears to be efficacious. Trials are awaited comparing melarsoprol/nifurtimox against melarsoprol alone for African sleeping sickness.

Combination therapy with eflornithine
Eflornithine
Eflornithine is a drug found to be effective in the treatment of facial hirsutism as well as in African trypanosomiasis...

 and nifurtimox is safer and easier than treatment with eflornithine alone, and appears to be equally or more effective. It has been recommended as first-line treatment for second-stage African trypanosomiasis.

Investigational

Nifurtimox is in a Phase II clinical trial for the treatment of pediatric neuroblastoma
Neuroblastoma
Neuroblastoma is the most common extracranial solid cancer in childhood and the most common cancer in infancy, with an annual incidence of about 650 cases per year in the US , and 100 cases per year in the UK . Close to 50 percent of neuroblastoma cases occur in children younger than two years old...

 and medulloblastoma
Medulloblastoma
Medulloblastoma is a highly malignant primary brain tumor that originates in the cerebellum or posterior fossa.Previously, medulloblastomas were thought to represent a subset of primitive neuroectodermal tumor of the posterior fossa...

.

Dosing

Nifurtimox is dosed as 15 mg/kg/day in two to three divided doses. It is given by mouth. Refer to the articles on Chagas disease
Chagas disease
Chagas disease is a tropical parasitic disease caused by the flagellate protozoan Trypanosoma cruzi. T. cruzi is commonly transmitted to humans and other mammals by an insect vector, the blood-sucking insects of the subfamily Triatominae most commonly species belonging to the Triatoma, Rhodnius,...

 and sleeping sickness for more detailed information on dosing for these diseases.

Manufacturing and availability

Nifurtimox is sold as Lampit by Bayer. It was previously known as Bayer 2502.

Nifurtimox is only licensed for use in Argentina
Argentina
Argentina , officially the Argentine Republic , is the second largest country in South America by land area, after Brazil. It is constituted as a federation of 23 provinces and an autonomous city, Buenos Aires...

 and Germany
Germany
Germany , officially the Federal Republic of Germany , is a federal parliamentary republic in Europe. The country consists of 16 states while the capital and largest city is Berlin. Germany covers an area of 357,021 km2 and has a largely temperate seasonal climate...

, where it is sold as 120 mg tablets.
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