Motesanib
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| Preferred IUPAC name
N-(3,3-Dimethyl-2,3-dihydro-1H-indol-6-yl)-2-{[(pyridin-4-yl)methyl]amino}pyridine-3-carboxamide | |
| Other names
AMG 706
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| Identifiers | |
3D model (JSmol)
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| E number | Lua error in Module:Wikidata at line 880: attempt to index field 'wikibase' (a nil value). |
PubChem CID
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CompTox Dashboard (EPA)
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| Properties | |
| C22H23N5O | |
| Molar mass | 373.460 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Motesanib (AMG 706) is an experimental drug candidate originally developed by Amgen[1] but later investigated by the Takeda Pharmaceutical Company. It is an orally administered small molecule belonging to angiokinase inhibitor class which acts as an antagonist of VEGF receptors, platelet-derived growth factor receptors, and stem cell factor receptors.[2] It is used as the phosphate salt motesanib diphosphate. After clinical trials in thyroid cancer, non-small cell lung cancer, gastrointestinal stromal cancer, colorectal cancer, and breast cancer, the drug was not found to show sufficient efficacy for further development, and development was abandoned by Takeda.[3]
Clinical trials
[edit | edit source]Motesanib was originally investigated for effectiveness against advanced nonsquamous non-small-cell lung cancer (NSCLC), with Phase II trials indicating an effectiveness comparable to bevacizumab when they were both used in combination with paclitaxel/carboplatin.[4] However a later and more detailed Phase III trial failed to show any benefit for the treatment of NSCLC.[2][5] A second Phase III trial was started in 2012,[6] which focused on patients from Asian backgrounds (performed on the basis of subgroup analysis)[7] however this also failed to meet its primary endpoint.[8]
The drug has undergone a Phase II evaluation as first-line therapy for breast cancer[2] however this study found no evidence to support further investigation.[9] Phase II testing against persistent or recurrent ovarian, fallopian tube and primary peritoneal carcinomas was also unsuccessful.[10] Two phase II clinical trials for thyroid cancer showed promising results.[11][12][13]
References
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- ^ Motesanib Diphosphate Provides Anticancer Activity Among Patients with Progressive Thyroid Cancer, CancerConnect.com
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