Preclinical and Clinical Characteristics of the Trichuricidal Drug Oxantel Pamoate and Clinical Development Plans: A Review

AbstractSoil-transmitted helminths (Ascaris lumbricoides, hookworm andTrichuris trichiura) infect about one-fifth of the world ’s population. The currently available drugs are all highly efficacious againstA. lumbricoides. However, they are only moderately efficacious against hookworm and poorly efficacious againstT. trichiura. Oxantel, a tetrahydropyrimidine derivative discovered in the 1970s, has recently been brought back to our attention given its high efficacy againstT. trichiura infections (estimated 76% cure rate and 85% egg reduction rate at a 20 mg/kg dose). This review summarizes the current knowledge on oxantel pamoate and its use againstT. trichiura infections in humans. Oxantel pamoate acts locally in the human gastrointestinal tract and binds to the parasite ’s nicotinic acetylcholine receptor (nAChR), leading to a spastic paralysis of the worm and subsequent expulsion. The drug is metabolically stable, shows low permeability and low systemic bioavailability after oral use. Oxantel pamoate was found to be safe in humans, with only a few mild adverse e vents reported. Several clinical trials have investigated the efficacy of this drug againstT. trichiura and suggest that oxantel pamoate is more efficacious againstT. trichiura than the currently recommended drugs, which makes it a strong asset to the depleted drug armamentarium and could help delay or even prevent the development of resistance to existing drugs. We highlight existing data to support the use o...
Source: Drugs - Category: Drugs & Pharmacology Source Type: research