Difference between revisions of "Tamibarotene (Amnoid)"
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==Mechanism of action== | ==Mechanism of action== | ||
| − | From the [ | + | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=571791 NCI Drug Dictionary]: An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than ATRA 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 ATRA. In addition, this agent may exhibit a lower toxicity profile than ATRA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
Latest revision as of 20:21, 27 June 2024
Mechanism of action
From the NCI Drug Dictionary: An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than ATRA 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 ATRA. In addition, this agent may exhibit a lower toxicity profile than ATRA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium.
Diseases for which it is used
History of changes in PMDA indication
- 2005-04-11: Initial approval for the treatment of Acute promyelocytic leukemia.
Also known as
- Brand names: Amnoid, Amnolake