Details
Stereochemistry | ACHIRAL |
Molecular Formula | C26H24N8O2 |
Molecular Weight | 480.5212 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(OC2=CC3=NC=NN3C=C2)C=CC(NC4=C5C=C(NC6=NC(C)(C)CO6)C=CC5=NC=N4)=C1
InChI
InChIKey=SDEAXTCZPQIFQM-UHFFFAOYSA-N
InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31)
Molecular Formula | C26H24N8O2 |
Molecular Weight | 480.5212 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
TUCATINIB (ONT-380 or ARRY-380) is an orally active, reversible and selective small-molecule HER2 inhibitor invented by Array and licensed to Cascadian Therapeutics (previously named Oncothyreon) for development, manufacturing and commercialization. HER2, a growth factor receptor that is over-expressed in multiple cancers, including breast, ovarian, and stomach cancer. HER2 mediates cell growth, differentiation and survival, and tumors that overexpress HER2 are more aggressive and historically have been associated with poorer overall survival compared with HER2-negative cancers. ONT-380 is highly active as a single agent and in combination with both chemotherapy and Herceptin® (trastuzumab) in xenograft models of HER2+ breast cancer, including models of CNS metastases that were refractory to Tykerb® (lapatinib) or neratinib treatment. In a Phase 1 single agent clinical study, ONT-380 administered orally twice a day was well tolerated and demonstrated anti-tumor activity in heavily pre-treated HER2+ breast cancer patients with metastatic disease. Based on the strength of these preclinical and clinical trials, ONT-380 is advancing in one Phase 2 and three Phase 1b combination trials in patients with metastatic breast cancer. A second study reported the CNS activity of ONT-380 in combination with either T-DM1 or trastuzumab or capecitabine. Patients with brain metastases assessable for response were included in the combined analysis. Responses and clinical benefit in the CNS were reported with the three combinations tested, supporting future development of the drug for this particular indication.
CNS Activity
Originator
Approval Year
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Oct 21 23:01:16 UTC 2019
by
admin
on
Mon Oct 21 23:01:16 UTC 2019
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Record UNII |
234248D0HH
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Record Status |
Validated (UNII)
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Record Version |
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-
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
570716
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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NCI_THESAURUS |
C2167
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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FDA ORPHAN DRUG |
571216
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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FDA ORPHAN DRUG |
603217
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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Code System | Code | Type | Description | ||
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CHEMBL3545380
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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9997
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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937263-43-9
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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C77896
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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SUB177913
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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C77896
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY | |||
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51039094
Created by
admin on Mon Oct 21 23:01:16 UTC 2019 , Edited by admin on Mon Oct 21 23:01:16 UTC 2019
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
SELECTIVE
Ki
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Related Record | Type | Details | ||
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ACTIVE MOIETY |