PMID- 9270551 OWN - NLM STAT- MEDLINE DCOM- 19970915 LR - 20141120 IS - 0190-9622 (Print) IS - 0190-9622 (Linking) VI - 37 IP - 2 Pt 3 DP - 1997 Aug TI - Tazarotene: the first receptor-selective topical retinoid for the treatment of psoriasis. PG - S12-7 AB - Tazarotene belongs to a novel, nonisomerizable class of retinoic acid receptor (RAR)-specific retinoids, the acetylenic retinoids, and is the first topical retinoid developed for the treatment of psoriasis. Tazarotene targets the keratinocyte and modulates the major causes of psoriasis. Tazarotene is rapidly metabolized by esterase to the active free acid tazarotenic acid, which is rapidly eliminated in animal species. Tazarotene selectively transactivates RAR beta and RAR gamma subtypes and is inactive at retinoid X receptors (RXRs). This receptor selectivity could contribute to an optimized therapeutic index. Tazarotene has low systemic absorption after topical administration. In preclinical toxicity studies, high topical doses produced reversible topical irritation, and lower doses were well tolerated. Topical doses were neither teratogenic nor carcinogenic and were not sensitizing, phototoxic, or photosensitizing. The topical delivery of tazarotene and limited systemic exposure apparently result in a very low potential for systemic effects. FAU - Chandraratna, R A AU - Chandraratna RA AD - Allergan, Inc., Irvine CA 92713, USA. LA - eng PT - Journal Article PT - Review PL - United States TA - J Am Acad Dermatol JT - Journal of the American Academy of Dermatology JID - 7907132 RN - 0 (Dermatologic Agents) RN - 0 (Nicotinic Acids) RN - 0 (Prodrugs) RN - 0 (Receptors, Retinoic Acid) RN - 0 (Retinoids) RN - 81BDR9Y8PS (tazarotene) SB - IM CIN - J Am Acad Dermatol. 1999 Dec;41(6):1049-50. PMID: 10570404 MH - Administration, Topical MH - Animals MH - Dermatologic Agents/pharmacology/*therapeutic use/toxicity MH - Humans MH - Nicotinic Acids/pharmacology/*therapeutic use/toxicity MH - Prodrugs/pharmacology/*therapeutic use/toxicity MH - Psoriasis/*drug therapy MH - Receptors, Retinoic Acid/*drug effects MH - Retinoids/pharmacology/*therapeutic use/toxicity RF - 34 EDAT- 1997/08/01 00:00 MHDA- 1997/08/01 00:01 CRDT- 1997/08/01 00:00 PHST- 1997/08/01 00:00 [pubmed] PHST- 1997/08/01 00:01 [medline] PHST- 1997/08/01 00:00 [entrez] AID - S0190-9622(97)80395-7 [pii] PST - ppublish SO - J Am Acad Dermatol. 1997 Aug;37(2 Pt 3):S12-7.