Tamibarotene
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
Catalog ID80071764
CAS NO.94497-51-5
Purity 98%
MDL NumberMFCD00866188
Molecular Formula C22H25NO3
Molecular Weight 351.444
Melting point: 190~195°C
| Item | Information |
|---|---|
| Mechanism of Action | Tamibarotene is a specific agonist for retinoic acid receptor alpha/beta (RARα/β) and may also bind to retinoid X receptors (RXR). It induces differentiation and inhibits proliferation of promyelocytic leukemia cells, overcoming resistance to all-trans retinoic acid (ATRA) . |
| Indications | Approved in Japan for the treatment of relapsed or refractory acute promyelocytic leukemia (APL) . |
| Dosage Forms | Available as tablets (e.g., 2 mg) . |
| Clinical Use | – Induction Therapy: 6 mg/m² per day, divided into two doses (morning and evening), until bone marrow remission is achieved. Treatment duration should not exceed 8 weeks . |
| Advantages over ATRA | – Chemically more stable than ATRA.<br>- Sustains plasma levels better due to lower affinity for cellular retinoic acid-binding protein.<br>- Milder adverse effects compared to ATRA . |
| Pharmacokinetics | – Highly protein-bound (over 99%), primarily to serum albumin . |
| Side Effects | Generally milder than those of ATRA, but may include retinoic acid syndrome, hyperlipidemia, and other retinoid-related effects . |
| Development and Approval | Developed by Toko Pharmaceutical Industrial Co., Ltd., and first approved in Japan in 2005 under the brand name Amnolake . |
| Research and Development | Investigated for overcoming ATRA resistance and improving outcomes in patients with APL who have relapsed or are refractory to standard treatments |
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