U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C23H21Cl2FN4O3
Molecular Weight 491.342
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POZIOTINIB

SMILES

COC1=CC2=NC=NC(NC3=CC=C(Cl)C(Cl)=C3F)=C2C=C1OC4CCN(CC4)C(=O)C=C

InChI

InChIKey=LPFWVDIFUFFKJU-UHFFFAOYSA-N
InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29)

HIDE SMILES / InChI

Molecular Formula C23H21Cl2FN4O3
Molecular Weight 491.342
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Poziotinib is an inhibitor of EGFR tyrosine kinase family. The drug is being tested in phase II of clinical trials for different cancers: breast cancer, lung adenocarcinoma, head and neck squamous cell carcinoma, HER-2 positive advanced gastric cancer (in combination with Paclitaxel and Trastuzumab).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
3.2 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

Head and Neck Squamous Cell Carcinoma: Take 45 mg orally, daily and continuously. Lung Adenocarcinoma: patients should receive poziotinib at dose of 16 mg orally once daily in a 28-day cycle.
Route of Administration: Oral
HCC827 cells were inhibited on 50% at 1.2 nM of poziotinib; NCI-H358 cells - at 4.8 nM; NCI-H1975 cells - at 5.7 nM; Calu-3 cells - at 2.1 nM; NCI-H1781 cells - at 4 nM; SK-Br3 cells - at 1 nM; NCI-N87 cells - at 0.6 nM.
Substance Class Chemical
Created
by admin
on Sat Dec 16 16:05:19 GMT 2023
Edited
by admin
on Sat Dec 16 16:05:19 GMT 2023
Record UNII
OEI6OOU6IK
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POZIOTINIB
INN   WHO-DD  
USAN   INN  
Official Name English
Poziotinib [WHO-DD]
Common Name English
NOV-1201
Code English
2-PROPEN-1-ONE, 1-(4-((4-((3,4-DICHLORO-2-FLUOROPHENYL)AMINO)-7-METHOXY-6-QUINAZOLINYL)OXY)-1-PIPERIDINYL)-
Systematic Name English
1-(4-((4-(3,4-DICHLORO-2-FLUOROANILINO)-7-METHOXYQUINAZOLIN-6-YL)OXY(PIPERIDIN-1-YL)PROP-2-EN-1-ONE
Common Name English
HM-781-36B
Code English
NOV-120101
Code English
poziotinib [INN]
Common Name English
HM-781-36
Code English
POZIOTINIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C1742
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
NCI_THESAURUS C2167
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
Code System Code Type Description
DRUG BANK
DB12114
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
CAS
1092364-38-9
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
WIKIPEDIA
Poziotinib
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
ChEMBL
CHEMBL3545154
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
PUBCHEM
25127713
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
EPA CompTox
DTXSID80148853
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
NCI_THESAURUS
C98838
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
SMS_ID
100000177756
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
USAN
JK-195
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
FDA UNII
OEI6OOU6IK
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
INN
9736
Created by admin on Sat Dec 16 16:05:20 GMT 2023 , Edited by admin on Sat Dec 16 16:05:20 GMT 2023
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY