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PubMed1976

Hycanthone dose-response in treatment of schistosomiasis mansoni in St. Lucia.

Clinical trials of hycanthone (single intramuscular dose) were undertaken in schistosomiasis mansoni patients in St. Lucia at five dose levels: 3.0, 2.5, 2.0, 1.5, and 1.0 mg/kg body weight. The most common side effect, vomiting, decreased in frequency from 51% at the highest dose to 3% at the lowest; minor side effects showed a similar trend. Three fecal specimens were examined before and at 6 months after treatment by qualitative, quantitative, and hatching techniques. All dose levels caused reductions in egg excretion of 89 to 98%. Rates of cure (absence of eggs by all three methods) according to dose (descending), pretreatment egg output (0-19, 20-49, 50-399, 400+ eggs/ml feces), and age (0-7, 8-14, 15-29, 30+ years) were analyzed to estimate the effect of each variable if the others had been constant. For dose, the standardized percentage success rates were 53.9%, 62.0%, 51.2% 54.0%, and 27.4%; for egg output, 67.0%, 51.8%, 43.2%, and 21.7%; and for age, 25.2%, 34.5%, 59.3% and 57.4%. Logit regression analysis shows a significant difference in cure rate (a) between the lowest dose and all others, among which latter there was no difference, (b) between patients excreting 0 to 49 eggs/ml before treatment and those excreting 50+ eggs/ml, and (c) between the age groups 0 to 14 and 15+ years. All dose levels caused some regression in enlargement of liver or spleen. A dose of 1.5 to 2.0 mg/kg body weight is considered to be as effective as one of 3.0 mg/kg and more acceptable for a control program because of the marked reduction in side effects.

Adolescent↗
PubMed1976

Hycanthone in the treatment of Egyptian bilharzial patients.

Hycanthone has a schistosomicidal effect against S. haematobium and S. mansoni present singly or combined in the patient. It is effective in all age groups but better in old and adults than in children and better in females than in males. It gave a cure rate of 60.6% after single intramuscular dose of 3 mg/kg body weight. Second dose after three months gave 94.4% cure rate and a third injection after further two months gave 100% cure rate. So, the drug cannot be used in the treatment of bilharziasis as a single dose course.

Adult↗
PubMed1978

Phase I study of hycanthone.

Hycanthone was given to 15 patients with metastatic cancer in order to determine the maximum tolerable dose. The drug was administered in 5-day courses at 3-week intervals. The starting dose was 30 mg/m2/day and the highest dose level reached was 90 mg/m2/day. The most common (13 patients) side effect was nausea and/or vomiting. The dose-limiting toxicity was toxic hepatitis manifested as elevation in serum transaminases in eight of 15 patients and an increase in serum bilirubin in three patients. Hepatotoxicity was dose-related and was observed in two of 25 courses given at the dose level of less than or equal to 70 mg/m2 compared to seven of nine courses given at the dose level of greater than or equal to 80 mg/m2. Because of an unacceptable incidence of hepatotoxicity at higher doses, 70 mg/m2/day x 5 appears to be a safe dose for phase II studies.

Adult↗
PubMed1986

Lack of correlation between schistosomicidal and anticholinergic properties of hycanthone and related drugs.

Visual observation of the motor activity of Schistosoma mansoni kept in vitro showed an increase of activity in the presence of hycanthone (HC). In addition, HC caused a delay in the paralytic effects of carbachol. Similar results were observed in the presence of oxamniquine (OXA). The same pattern of motor activity, however, was shown by HC-resistant worms, by Schistosoma japonicum, and by worms exposed to drug precursors (lucanthone and UK-3883), which are not schistosomicidal in vitro. Other analogs with in vitro killing activity (IA-4 and IA-4 N-oxide) showed minimal anticholinergic effects. The anticholinergic effects of HC and OXA were quickly reversible in vitro and in vivo, whereas their antischistosomal effects are irreversible and delayed. Incubation of schistosomes with high concentrations of carbachol or with anticholinergic drugs failed to compete with the schistosomicidal effects of HC. These results are viewed as contradictory to the hypothesis that HC kills schistosomes by blocking their acetylcholine receptors.

Animals↗
PubMed1977

Biochemical studies on beta-glucuronidase in the urinary bladder of normal and Schistosoma mansoni infected mice treated with hycanthone.

beta-Glucuronidase activity is elevated in the urine of patients with bilharziasis hematobium. In the present study the enzyme level was estimated in whole urinary bladder tissue homogenates of mice experimentally infected with Schistosoma mansoni. In the infected mice the enzyme activity is significantly higher than in the controls. The effect of the schistosomicidal drug hycanthone was also evaluated. Treatment with the drug did not affect the level of the enzyme activity in the infected mice; it induced an increase in the enzyme activity of the controls.

Animals↗
PubMed1980

Genetic analysis of adenine-3 mutants induced by hycanthone, lucanthone and their indazole analogs in Neurospora crassa.

Ad-3 mutants induced by hycanthone, lucanthone and their indazole analogs, IA-3, IA-4 and IA-5 were studied to characterize the genetic alterations produced by these agents in Neurospora crassa. The results of genetic analysis indicate that, in marked contrast to past experiments with chemical mutagens on heterokaryon 12, all of these antischistosomal agents induce a very high frequency of multilocus deletions.

Adenine↗
PubMed1980

Development of a cell-free protein-synthesizing system from Schistosoma mansoni and a comparison of the effects of hycanthone and praziquantel on this system.

A cell-free, protein-synthesizing system was developed using polysomes and pH 5 fractions isolated from Schistosoma mansoni. Under optimal conditions, the system incorporated 35-S methionine into TCA-precipitable protein at a rate of approximately 1.8 pmoles/hr/microgram polysomal RNA. Praziquantel had no significant effect on the rate of protein synthesis, whereas hycanthone, at concentrations of 0.125 and 0.5 mM, caused a 136% and 515% stimulation, respectively. The mechanism of the stimulation is unknown. This S. mansoni--cell-free system for protein synthesis has been standardized so that new drugs can now be screened with relative ease for their effects on in vitro protein synthesis or charging of tRNA.

Animals↗
PubMed1974

Hycanthone analogs: dissociation of mutagenic effects from antischistosomal effects.

N-Oxidation at the diethylamino group of hycanthone, of lucanthone, and of two chlorobenzothiopyranoindazoles resulted in a marked reduction in mutagenic activity, while antischistosomal activity was retained or even enhanced. Introduction of chlorine into the 8-position of benzothiopyranoindazoles reduced acute toxicity but had no effect on chemnotherapeutic potency. These dissociations of biological activities indicate that safer antischistosomal compounds of this class can be developed.

Animals↗
PubMed1974

Two-year follow-up of hycanthone-treated schistosomiasis mansoni patients in St. Lucia.

Of 433 schistosomiasis mansoni patients in St. Lucia who were treated with hycanthone (3 mg/kg of body weight), 190 were seen 2 years after treatment and 143 of these had attended all follow-up examinations at 6 weeks, 6 months, 1 year and 2 years. Viable eggs were not detected in 86% at 1 year nor in 76% at 2 years. The reinfection rate, as judged by a significant increase in egg excretion, was 15% and was related to the geographic area to which the patient returned. Extremely high total reduction in egg excretion (98%) was achieved through 1 year, and even with reinfections this fell only to 87% at 2 years. Liver and spleen enlargement was related to intensity of infection and responded to treatment in 92% and 83% of instances, respectively. Among patients with hepatosplenomegaly, those 15 years or older showed less clinical response than younger patients but were too few for statistical comparison.

Adolescent↗
PubMed1970

The uptake of tritiated hycanthone by male and female Schistosoma mansoni worms and distribution of the drug in plasma and whole blood of mice following a single intramuscular injection.

Mice infected with Schistosoma mansoni were given an intramuscular injection of a single 80 mg/kg dose of randomly tritiated hycanthone. The uptake of the drug in male and female worms, as well as its concentration in the red blood cells and plasma of the mice, was followed for a period of 24 hours.Blood and plasma drug levels reached maximum values within 30 minutes. During the postmedication period, plasma concentrations were consistently higher than red blood cell concentrations. At 2-6 hours, when blood levels were declining, peak uptake was reached in the female schistosome worms; the concentration in the female worm was 5 times higher than in the male worm. At 24 hours the schistosomes contained appreciably more drug than was present in the blood.

Animals↗