Stibophen is an
anthelmintic
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them without causing significant damage to the host. They may also ...
originally developed by
Bayer
Bayer AG (English: , commonly pronounced ; ) is a German multinational pharmaceutical and biotechnology company and is one of the largest pharmaceutical companies and biomedical companies in the world. Headquartered in Leverkusen, Bayer' ...
that is used as a treatment for
schistosomiasis
Schistosomiasis, also known as snail fever, bilharzia, and Katayama fever is a neglected tropical helminthiasis, disease caused by parasitism, parasitic Schistosoma, flatworms called schistosomes. It affects both humans and animals. It affects ...
by
intramuscular injection
Intramuscular injection, often abbreviated IM, is the medical injection, injection of a substance into a muscle. In medicine, it is one of several methods for parenteral, parenteral administration of medications. Intramuscular injection may be ...
. It is classified as a trivalent
antimony
Antimony is a chemical element; it has chemical symbol, symbol Sb () and atomic number 51. A lustrous grey metal or metalloid, it is found in nature mainly as the sulfide mineral stibnite (). Antimony compounds have been known since ancient t ...
compound. Brand names include Fouadin/Fuadin (named in honor of
Fuad I
Fuad I ( ''Fu’ād al-Awwal''; 26 March 1868 – 28 April 1936) was the Sultan and later King of Egypt and the Sudan. The ninth ruler of Egypt and Sudan from the Muhammad Ali dynasty, he became Sultan in 1917, succeeding his elder brother Hus ...
of Egypt, who had enthusiastically supported its research and development).
Mechanism of action
Stibophen inhibits the enzyme
phosphofructokinase
Phosphofructokinase (PFK) is a kinase enzyme that phosphorylates fructose 6-phosphate in glycolysis.
Function
The enzyme-catalysed transfer of a phosphoryl group from ATP is an important reaction in a wide variety of biological processe ...
, which the worms need for glycolysis, at least partly by binding to the
sulfhydryl
In organic chemistry, a thiol (; ), or thiol derivative, is any organosulfur compound of the form , where R represents an alkyl or other organic substituent. The functional group itself is referred to as either a thiol group or a sulfhydryl grou ...
(–SH) group of the enzyme.
Inhibiting glycolysis paralyzes the worms, which lose their hold on the wall of
mesenteric veins and undergo
hepatic shift, die, and are
phagocytose
Phagocytosis () is the process by which a cell uses its plasma membrane to engulf a large particle (≥ 0.5 μm), giving rise to an internal compartment called the phagosome. It is one type of endocytosis. A cell that performs phagocytosis is c ...
d by liver cells.
References
Antiparasitic agents
Sulfonates
Antimony(III) compounds
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