Motesanib

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Motesanib
Motesanib.svg
Names
IUPAC name
N-(3,3-Dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide
Other names
AMG 706
Identifiers
453562-69-1 YesY
ChEMBL ChEMBL572881
ChemSpider 9842625
5660
Jmol 3D model Interactive image
PubChem 11667893
UNII U1JK633AYI YesY
  • InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
  • O=C(c2cccnc2NCc1ccncc1)Nc3ccc4c(c3)NCC4(C)C
Properties
C22H23N5O
Molar mass 373.46 g·mol−1
Vapor pressure {{{value}}}
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Motesanib (AMG 706) is an experimental drug candidate originally developed by Amgen[1] but is now being 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.

Clinical trials

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.[3] However a later and more detailed Phase III trial failed to show any benefit for the treatment of NSCLC.[2][4] A second Phase III trial was started in 2012,[5] which focused on patients from Asian backgrounds (performed on the bases of subgroup analysis)[6] however this also failed to meet its primary endpoint.[7]

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.[8] Phase II testing against persistent or recurrent ovarian, fallopian tube and primary peritoneal carcinomas was also unsuccessful.[9]

There have also been 2 separate Phase II clinical trials for thyroid cancer which have both shown promising results.[10][11][12]

References

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  10. Motesanib Diphosphate Provides Anticancer Activity Among Patients with Progressive Thyroid Cancer, CancerConnect.com
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External links