Liarozole

Drugs & Aging
H M Bryson, A J Wagstaff

Abstract

Liarozole prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid-sparing and retinoid-mimetic effects in vivo. Liarozole is also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17, 20-lyase). Although testosterone levels decrease in vivo after single dose administration of liarozole, testosterone levels normalise as a result of pituitary feedback after multiple doses. Liarozole reduced the tumour size of androgen-dependent and -independent prostatic carcinomas in animal models. Liarozole also demonstrated chemopreventive activity in vivo. In phase I and II trials in patients with relapsed prostate cancer, liarozole achieved a complete response (assessed using prostate specific antigen levels) in 4% and a partial response in 26% of patients. Cutaneous adverse events, similar to those associated with excess levels of retinoic acid, were the most frequently reported events associated with liarozole.

Citations

Jun 19, 2001·Molecular and Cellular Endocrinology·G Séralini, S Moslemi
Nov 6, 2007·Expert Opinion on Emerging Drugs·M A M van Steensel
Jan 15, 2005·Journal of the European Academy of Dermatology and Venereology : JEADV·V SchleyerR-M Szeimies
Oct 19, 2007·Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG·Christel J VerfailleMaurice A M van Steensel
Mar 10, 2017·The Journal of Pharmacology and Experimental Therapeutics·Jing JingNina Isoherranen

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