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

01 Jan 1985·ChemotherapyQ4 · MEDICINE

Antiandrogen and Antineoplastic Effects of a Novel Drug, CPC10997

Q4 · MEDICINE

Article

Author: DeLange, Robert J. ; Ford, Larry C. ; Kasha, Walter ; Chang, Norman H. C.

CPC10997 was found to be effective in vitro as an antiandrogen without effects on either the estrogen or the progesterone receptors in carcinomas of the breast, ovary and prostate as well as in malignant melanomas. Using the clonogenic assay of Salmon et al. [Cancer Treat. Rep. 65: 1-12, 1981], CPC10997 was found to be more effective against carcinomas of the breast, the kidney, the ovary and the prostate than conventional antineoplastic agents in the majority of tumors tested. In view of the very favorable toxicology profiles and in vitro efficacy, further trials using CPC10997 as an antineoplastic agent are indicated.

100 Deals associated with Cioteronel

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

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