tamibarotene
Tamibarotene, also called retinobenzoic acid, is orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity against acute promyelocytic leukaemia (APL). It is currently marketed only in Japan and early trials have demonstrated that it tends to be better tolerated than ATRA. Tamibarotene has been tested in many other cancer types, including Acute Myeloid Leukemia where it shows no benefit, and lung cancer, where it accelerated the cancer growth and increased mortality. — Wikipedia
Clinical trial activity
11 trials · 19 clinical orgs · 0 marketing orgs
Earliest trial started Dec 1, 2006 (NCT00417391)
Timeline
Indications
Studied for
- Alzheimer Disease · Phase 2
- Carcinoma, Hepatocellular · Phase 1/Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Transitional Cell · Phase 2
- Crohn Disease · Phase 2
- Leukemia, Myeloid, Acute · Phase 2
- Leukemia, Promyelocytic, Acute · Phase 2
- Lupus Nephritis · Phase 2
- Myelodysplastic Syndromes · Phase 2
- Pancreatic Neoplasms · Phase 1/Phase 2
- Paraparesis, Tropical Spastic · Phase 2/Phase 3
Mechanism of action
- Retinoic acid receptorAGONIST
Retinoic acid receptor agonist
- Retinoic acid receptor alphaAGONIST
Retinoic acid receptor alpha agonist
- Retinoic acid receptor betaAGONIST
Retinoic acid receptor beta agonist
Chemistry & pharmacology
SMILES
CC1(C)CCC(C)(C)c2cc(NC(=O)c3ccc(C(=O)O)cc3)ccc21- Mol. weight
- 351.45 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaTamibarotene ↗
- ChEMBLCHEMBL25202 ↗
Also known as
- 4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl)benzoic acid
- am80
- am80
- am 80
- am-80
- amnolake
- benzoic acid, 4-(((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)amino)carbonyl)-
- retinobenzoic acid
- retinobenzoic acid
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- tamibarotene
- z-208
- z-208
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06983210 | Phase 2 | May 1, 2025 | Chiba University, Japan Agency for Medical Research and Development, Kyoto University, Kyushu University, Nagoya University, University of Tsukuba |
| NCT05064618 | Phase 1/Phase 2 (Phase 2) | Aug 23, 2021 | Japan Agency for Medical Research and Development, Nagoya University |
| NCT02807558 | Phase 2 | Aug 1, 2016 | Syros Pharmaceuticals |
| NCT01337154 | Phase 2 | Apr 1, 2011 | CytRx, Government of Colombia |
| NCT01343355 | Phase 2/Phase 3 (Phase 3) | Jan 1, 2011 | St. Marianna University School of Medicine |
| NCT01226147 | Phase 2 | Sep 1, 2010 | Kindai University |
| NCT01120002 | Phase 2 | May 1, 2010 | Osaka City University |
| NCT00985530 | Phase 1 | Oct 1, 2009 | Cephalon, CytRx, Northwestern University |
| NCT00731445 | Phase 1/Phase 2 (Phase 2) | Jul 1, 2008 | University of Tokyo, Zeria Pharmaceutical |
| NCT00520208 | Phase 2 | Sep 1, 2007 | CytRx, University of Texas at Houston |
| NCT00417391 | Phase 2 | Dec 1, 2006 | Keio University, R&R Inc. |
Organizations
Research & Development (19)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| CytRx | For profit | 3 | 2 | 2 | 2007 |
| Japan Agency for Medical Research and Development | Government | 2 | 0 | 1 | 2021 |
| Nagoya University | Academic/Hospital | 2 | 2 | 1 | 2021 |
| Cephalon | For profit | 1 | 0 | 1 | 2009 |
| Chiba University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Government of Colombia | Government | 1 | 0 | 1 | 2011 |
| Keio University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Kindai University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Kyoto University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Kyushu University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Northwestern University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Osaka City University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| R&R Inc. | For profit | 1 | 1 | 1 | 2006 |
| St. Marianna University School of Medicine | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Syros Pharmaceuticals | For profit | 1 | 1 | 1 | 2016 |
| University of Texas at Houston | Academic/Hospital | 1 | 0 | 1 | 2007 |
| University of Tokyo | Academic/Hospital | 1 | 0 | 1 | 2008 |
| University of Tsukuba | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Zeria Pharmaceutical | For profit | 1 | 1 | 1 | 2008 |