Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H22N8O2 |
Molecular Weight | 466.4955 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NN(C(=O)\C1=N/NC2=C(O)C(=CC=C2)C3=CC(=CC=C3)C4=NN=NN4)C5=CC(C)=C(C)C=C5
InChI
InChIKey=IIBBJCNVTRCTDV-QYQHSDTDSA-N
InChI=1S/C25H22N8O2/c1-14-10-11-19(12-15(14)2)33-25(35)22(16(3)30-33)27-26-21-9-5-8-20(23(21)34)17-6-4-7-18(13-17)24-28-31-32-29-24/h4-13,26,34H,1-3H3,(H,28,29,31,32)/b27-22-
Molecular Formula | C25H22N8O2 |
Molecular Weight | 466.4955 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
Totrombopag is an orally bioavailable, nonpeptide, small-molecule thrombopoietin receptor agonist. It induces proliferation and differentiation of megakaryocytes and progenitor cells, ultimately increasing the production of platelets. Totrombopag has been investigated in healthy volunteers in a phase 1, single-blind, randomized fashion to cause a dosedependent increase in platelet count with demonstrated safety. There were no serious adverse events, no significant changes in laboratory or cardiovascular safety parameters and there was no observed relationship between the incidence or severity of adverse events and dose. Most adverse events were mild in intensity and self-limiting. Totrombopag was developed for the treatment of immune thrombocytopenic purpura.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1864 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20188141 |
170.0 nM [IC50] |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.bloodjournal.org/content/108/11/1072
Once-daily at doses of 160 to 640 mg
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:18:08 GMT 2025
by
admin
on
Mon Mar 31 18:18:08 GMT 2025
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Record UNII |
83D6475CAW
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Record Status |
FAILED
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NCI_THESAURUS |
C2459
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C152703
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TARGET -> AGONIST |
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SALT/SOLVATE -> PARENT |
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