 | |
| Names | |
|---|---|
| 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 | |
| Identifiers | |
3D model (JSmol) | |
| ChEMBL | |
| ChemSpider | |
| UNII | |
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| |
| Properties | |
| C22H23N5O | |
| Molar mass | 373.460 g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
Motesanib (AMG 706) is an experimental drug candidate originally developed byAmgen[1] but later investigated by theTakeda Pharmaceutical Company. It is an orally administered small molecule belonging toangiokinase inhibitor class which acts as anantagonist ofVEGF receptors,platelet-derived growth factor receptors, andstem cell factor receptors.[2] It is used as thephosphatesalt 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]
Motesanib was originally investigated for effectiveness against advanced nonsquamousnon-small-cell lung cancer (NSCLC), withPhase II trials indicating an effectiveness comparable tobevacizumab when they were both used in combination withpaclitaxel/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 ofsubgroup analysis)[7] however this also failed to meet itsprimary endpoint.[8]
The drug has undergone a Phase II evaluation as first-line therapy forbreast 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 forthyroid cancer showed promising results.[11][12][13]
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