TELATINIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H16ClN5O3
Molecular Weight	409.826
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CNC(=O)C1=CC(COC2=C3OC=CC3=C(NC4=CC=C(Cl)C=C4)N=N2)=CC=N1

InChI

InChIKey=QFCXANHHBCGMAS-UHFFFAOYSA-N

InChI=1S/C20H16ClN5O3/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/h2-10H,11H2,1H3,(H,22,27)(H,24,25)

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 | https://www.ncbi.nlm.nih.gov/pubmed/18519779 | https://www.ncbi.nlm.nih.gov/pubmed/21378200

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

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vascular endothelial growth factor receptor 2 112 Target ID: CHEMBL279 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8504	6.0 nM [IC50]
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8504	4.0 nM [IC50]
Platelet-derived growth factor receptor alpha 33 Target ID: P26618 Gene ID: 18595.0 Gene Symbol: Pdgfra Target Organism: Mus musculus (Mouse) Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8504	15.0 nM [IC50]
Stem cell growth factor receptor 57 Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8504	1.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Gastric cancer 53 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28052652 http://www.news-medical.net/news/20110228/ACT-Biotech-files-SPA-with-FDA-for-telatinib-combination-Phase-3-trial-for-stomach-cancer.aspx	Primary		Phase III 665	Unknown Approved Use Unknown
Solid tumors 147 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19002179	Primary		Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
1.275 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	900 mg 2 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.964 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	1500 mg 2 times / day steady-state, oral dose: 1500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
7.3 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	900 mg 2 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.29 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	1500 mg 2 times / day steady-state, oral dose: 1500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
5.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	900 mg 2 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19002179/	1500 mg 2 times / day steady-state, oral dose: 1500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TELATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY105440	https://www.001chemical.com/chem/search?q=DY105440
1PlusChem LLC	1P00C70M	https://www.1pchem.com/search?query=1P00C70M
AK Scientific	X7508	https://aksci.com/item_detail.php?cat=X7508
ApexBio Technology	A8550	https://www.apexbt.com/catalogsearch/result/?q=A8550
AstaTech	42291	http://astatechinc.com/CPSResult.php?CRNO=42291
BLD Pharm	BD152516	http://www.bldpharm.com/search/Search.html?keyword=BD152516
Capot Chemical	22596	https://www.capotchem.com/search.do?q=22596
Chem Scene	CS-3722	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-3722
ChemShuttle	101248	https://www.chemshuttle.com/catalogsearch/result/?q=101248
eMolecules	36516863	https://orderbb.emolecules.com/search/#?query=36516863
eMolecules	85163657	https://orderbb.emolecules.com/search/#?query=85163657
eNovation Chemicals	D210767	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D210767&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A007	http://www.excenen.com/searchresultlist.php?id=EX-A007
Hairui	HR144656	http://www.hairuichem.com/en/product/search.do?q=HR144656
Matrix Scientific	125102	http://www.matrixscientific.com/125102.html
mcule	MCULE-2706634959	https://mcule.com/MCULE-2706634959/
mcule	MCULE-6157972879	https://mcule.com/MCULE-6157972879/
MedChem Express	HY-10527	https://www.medchemexpress.com/search.html?q=HY-10527&ft=&fa=&fp=
Molcore	MC105440	http://www.molcore.com/CatMC105440.html
Molnova	M14115	https://www.molnova.com/en/serch-list.html?keywords=M14115
MolPort	MolPort-016-633-360	https://www.molport.com/shop/molecule-link/MolPort-016-633-360
MuseChem	I003199	https://www.musechem.com/product/I003199.html
Selleck Chemicals	S2231	http://www.selleckchem.com/search.html?searchDTO.searchParam=S2231
ShangHai Biochempartner	BCP000350	http://www.biochempartner.com/search_BCP000350
ShangHai Biochempartner	BCP02409	http://www.biochempartner.com/search_BCP02409
Synthonix	13822	https://synthonix.com/catalogsearch/result/?q=13822
TargetMol	T6166	https://www.targetmol.com/search?keyword=T6166
Toronto Research Chemicals	T015700	https://www.trc-canada.com/product-detail/?CatNum=T015700

PubMed

Title	Date	PubMed
Gateways to clinical trials.	2010-09	21069103
A model of hypertension and proteinuria in cancer patients treated with the anti-angiogenic drug E7080.	2010-08	20652729
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.	2010-05-05	20351338
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.	2010-04-01	20233884
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.	2009-09-01	19636022
Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours.	2008-11-18	19002179
Gateways to clinical trials.	2008-10	19088949
Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.	2008-06-01	18519779
Gateways to clinical trials.	2007-06	17805439
Gateways to clinical trials.	2007-03-09	17344945

Patents

Sample Use Guides

In Vivo Use Guide

twice-daily continuously, 450-900 mg

Route of Administration: Oral

In Vitro Use Guide

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 `Wed Apr 02 09:43:16 GMT 2025` Edited by `admin` on `Wed Apr 02 09:43:16 GMT 2025`
Record UNII	18P7197Q7J
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BAY 57-9352

Preferred Name

English

TELATINIB

Official Name

English

4-(((4-((4-CHLOROPHENYL)AMINO)FURO(2,3-D)PYRIDAZIN-7-YL)OXY)METHYL)-N-METHYLPYRIDINE-2-CARBOXAMIDE

Systematic Name

English

Telatinib [WHO-DD]

Common Name

English

telatinib [INN]

Common Name

English

BAY-579352

Code

English

Classification Tree Code System Code

FDA ORPHAN DRUG

307410