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Phase 1 tolerability and searching dose studies with 4‐isothiocyanato‐ 4′‐nitrodiphenylamine (C.9333‐Go/CGP 4540), a new anthelmintic.
Author(s) -
Vaidya AB,
Sen HG,
Mankodi NA,
Paul T,
Sheth UK
Publication year - 1977
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1977.tb00763.x
Subject(s) - tolerability , anthelmintic , adverse effect , medicine , pharmacology , veterinary medicine
1 Phase 1 and 2 studies were carried out in thirteen volunteers and thirty patients with hookworm anaemia with a new anthelmintic, 4‐ isothiocyanato‐4′‐nitrodiphenylamine (C.9333‐Go/CGP 4540). Single and multiple doses were administered by mouth under careful supervision by the staff of the clinical pharmacology unit. 2 4‐Isothiocyanato‐4′‐ nitrodiphenylamine (C.9333‐Go/CGP 4540) was well tolerated in volunteers up to a single dose of 1750 mg and in patients up to 3000 mg in divided doses. Side effects were rare, transient and mild. One patient had moderate giddiness for 24 h after the compound. The laboratory investigations did not show any adverse effects on organ functions. Transient non‐specific changes in the T‐wave were occasionally observed in the e.c.g. 3 Multiple doses (125 mg, 250 mg or 1000 mg X 3) of the compound were highly effective in eradicating hookworm infection, as judged by almost 100% reduction in faecal egg counts and significant recovery of parasites from 24 h stool samples. The compound also showed activity against A. lumbricoides, T. trichiura and E. vermicularis. The compound appears to be promising and more studies, in a field situation, are desirable.