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Details

Stereochemistry ACHIRAL
Molecular Formula C20H16ClN5O3.CH4O3S
Molecular Weight 505.931
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TELATINIB MESYLATE

SMILES

CS(O)(=O)=O.CNC(=O)C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1

InChI

InChIKey=LCMLACPWPXITHP-UHFFFAOYSA-N
InChI=1S/C20H16ClN5O3.CH4O3S/c1-22-19(27)16-10-12(6-8-23-16)11-29-20-17-15(7-9-28-17)18(25-26-20)24-14-4-2-13(21)3-5-14;1-5(2,3)4/h2-10H,11H2,1H3,(H,22,27)(H,24,25);1H3,(H,2,3,4)

HIDE SMILES / InChI

Molecular Formula C20H16ClN5O3
Molecular Weight 409.826
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula CH4O3S
Molecular Weight 96.106
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Telatinib (Bay-579352) developed by Bayer is an orally available and highly potent inhibitor of tyrosine kinases VEGFR2,VEGFR3, PDGFR and c-Kit. Telatinib is a potent inhibitor of angiogenesis. Telatinib caused a significant decrease in endothelium-dependent and endothelium-independent vasodilation. Telatinib demonstrates anti-tumor activity in various cancer models. Telatinib is ready for phase III clinical trials for the treatment of gastric cancer. In 2010, it has been granted orphan drug status by the FDA. Most frequent adverse events were pain, nausea, voice changes and fatigue.

Originator

Curator's Comment: # Bayer

Approval Year

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Gateways to clinical trials.
2007 Jan-Feb
Gateways to clinical trials.
2007 Jun
Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.
2008 Jun 1
Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours.
2008 Nov 18
Gateways to clinical trials.
2008 Oct
Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors.
2009 Sep 1
Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors.
2010 Apr 1
A model of hypertension and proteinuria in cancer patients treated with the anti-angiogenic drug E7080.
2010 Aug
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.
2010 May 5
Gateways to clinical trials.
2010 Sep
Patents

Sample Use Guides

twice-daily continuously, 450-900 mg
Route of Administration: Oral
Telatinib inhibits VEGF-dependent proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 of 26 nM and PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:26:27 GMT 2023
Edited
by admin
on Fri Dec 15 16:26:27 GMT 2023
Record UNII
571LVA9UMS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TELATINIB MESYLATE
Common Name English
2-PYRIDINECARBOXAMIDE, 4-(((4-((4-CHLOROPHENYL)AMINO)FURO(2,3-D)PYRIDAZIN-7-YL)OXY)METHYL)-N-METHYL-, METHANESULPHONATE (1:1)
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1742
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
NCI_THESAURUS C129825
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
NCI_THESAURUS C1967
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
Code System Code Type Description
FDA UNII
571LVA9UMS
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
PRIMARY
NCI_THESAURUS
C87837
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
PRIMARY
CAS
332013-26-0
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
PRIMARY
PUBCHEM
9870815
Created by admin on Fri Dec 15 16:26:27 GMT 2023 , Edited by admin on Fri Dec 15 16:26:27 GMT 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
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ACTIVE MOIETY