¹⁴C-labeled cyoctol (I) was applied in an ethanolic solution to the forearm of four young healthy volunteers for 8 h under non-occluding conditions, to investigate its absorption, disposition, and excretion after a single dermal application.I was absorbed by human skin at levels of approx. 10% of the applied dose and appeared to penetrate at a relatively fast rate.Radioactivity accumulated neither in the skin nor in any other site in the body as total recovery values were close to 100% at 120 h after removal of the dose.Radioactivity was eliminated primarily through the kidneys (>99%) in the form of polar metabolismsAnother interesting phenomenon was that I was completely metabolized when passing through the skin as no unchanged I could be detected in ipsilateral plasma samples.This may eliminate the occurrence of adverse systemic effects after dermal application.

01 Jan 1990·Pharmaceutical ResearchQ3 · MEDICINE

Metabolic conversion of cyoctol during skin passage in humans.

Q3 · MEDICINE

Article

Author: Ben F. H. Drenth ; Johann W. Wiechers ; Renella E. Herder ; Rokus A. de Zeeuw

Upon application of 14C-labeled cyoctol to the forearm of healthy volunteers, no parent cyoctol was detectable in ipsilateral blood plasma. The 14C activity was largely accounted for by a component with higher lipophilicity than the parent compound, as justified from their HPLC retention. Thus, this study suggests that human skin is capable of nearly complete cutaneous first-pass metabolism, resulting in negligible systemic availability of cyoctol. In a comparable experiment, rabbits were also able to convert cyoctol during skin absorption to a more lipophilic metabolite, which was identified as the palmitoleic acid ester of O-demethylated cyoctol by GC/MS. However, chromatographic evidence indicates that the human ipsilateral metabolite differs from the rabbit cyoctol metabolite.

01 May 1987·American Journal of Obstetrics and GynecologyQ1 · MEDICINE

Determination of estrogen and androgen receptors in Trichomonas vaginalis and the effects of antihormones

Q1 · MEDICINE

Article

Author: Hunter A. Hammill ; Robert J. DeLange ; Larry C. Ford ; Kristina L. Mickus ; Thomas B. Lebherz ; David A. Bruckner ; Fusako Suzuki-Chavez

Trichomonas vaginalis, a common genital pathogen, was found to possess both specific estrogen and specific androgen receptors. These 4.3 S macromolecules were proteinaceous in nature. Both metronidazole-resistant and metronidazole-sensitive strains possessed both types of sex hormone-binding proteins. The estrogen receptor binding was competitively inhibited by the antiestrogen tamoxifen citrate, and the androgen binding was competitively inhibited by the antiandrogen cyoctol. The presence of these specific receptors may allow the use of hormonal and antihormonal manipulation in the treatment of infections caused by these organisms.

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Indication	Highest Phase	Country/Location	Organization	Date
Acne Vulgaris	Phase 3	United States	Chantal Pharmaceutical Corp.	-
Acne Vulgaris	Phase 3	-	Cbd Pharmaceutical	-
Alopecia	Phase 3	United States	Chantal Pharmaceutical Corp.	-
Keloid	Phase 3	United States	Chantal Pharmaceutical Corp.	-
Mycoses	Phase 3	United States	Chantal Pharmaceutical Corp.	-
Prostatic Hyperplasia	Phase 3	United States	Chantal Pharmaceutical Corp.	-

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