Small molecule
PubChem CID 6435110
Ivermectin
Stromectol
- Mechanism of action
- Glutamate-gated chloride channel agonist
- In plain language
- Locks onto a chloride channel found only in parasite nerve and muscle cells, letting chloride ions rush in and paralyze the parasite — a channel human cells don't have, so the drug spares the person while killing the worm.
- How it works
- Ivermectin is a semisynthetic avermectin derivative that binds selectively and with high affinity to glutamate-gated chloride ion channels found in invertebrate nerve and muscle cells. This binding increases cell membrane permeability to chloride ions, causing hyperpolarization of the nerve or muscle cell that results in paralysis and death of the parasite. Ivermectin's selectivity for parasites over the mammalian host arises because mammals lack glutamate-gated chloride channels; the drug also has low affinity for mammalian ligand-gated chloride channels and does not readily cross the blood-brain barrier in humans, limiting central nervous system exposure at therapeutic doses.
- Therapeutic applications
- Per FDA-approved labeling, STROMECTOL (ivermectin) is indicated for the treatment of intestinal (nondisseminated) strongyloidiasis caused by the nematode Strongyloides stercoralis, and for the treatment of onchocerciasis caused by the nematode Onchocerca volvulus; the drug has no activity against adult O. volvulus parasites, only against microfilariae.
- Class
- Small molecule
- Therapeutic area
- Antiparasitic
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