Drug intelligence / Profile preview

tamibarotene

Development stage
Phase 3
Lead developer
Nippon Shinyaku
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tamibarotene is an orally active synthetic retinoid developed to overcome resistance to all-trans retinoic acid (ATRA), with antineoplastic activity. It acts as a specific agonist for the retinoic acid receptor alpha and beta (RARα/β), and may also bind to retinoid X receptors (RXR). Tamibarotene is more chemically stable than ATRA and has greater potency in inducing differentiation of promyelocytic leukemia cells. It sustains plasma levels better than ATRA due to lower affinity for cellular binding proteins and generally causes milder side effects. Tamibarotene was first approved in Japan in 2005 for relapsed or refractory acute promyelocytic leukemia (APL) and has been investigated for other hematological malignancies such as myelodysplastic syndromes and acute myeloid leukemia with RARA positivity. The drug was developed by Nippon Shinyaku.

Brand names
Amnolake
Other names
retinobenzoic acid4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl)benzoic acid
02

Targets

RARA (Retinoic acid receptor alpha)RARB (Retinoic acid receptor beta)

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