![]() | |
Names | |
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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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|
ChEMBL | |
ChemSpider | |
PubChem
CID
|
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UNII | |
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).
|
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]
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]
{{
cite book}}
: |first1=
has generic name (
help)CS1 maint: multiple names: authors list (
link)
![]() | |
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 | |
PubChem
CID
|
|
UNII | |
CompTox Dashboard (
EPA)
|
|
| |
| |
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).
|
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]
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]
{{
cite book}}
: |first1=
has generic name (
help)CS1 maint: multiple names: authors list (
link)