Tamibarotene

Abstract

An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (AT RA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than AT RA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to AT RA. In addition, this agent may exhibit a lower toxicity profile than AT RA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. Qeios · Definition, February 7, 2020