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Details

Stereochemistry ACHIRAL
Molecular Formula C23H21Cl2FN4O3.ClH
Molecular Weight 527.803
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POZIOTINIB HYDROCHLORIDE

SMILES

Cl.COC1=CC2=C(C=C1OC3CCN(CC3)C(=O)C=C)C(NC4=CC=C(Cl)C(Cl)=C4F)=NC=N2

InChI

InChIKey=OMYSOLOMWJFVNK-UHFFFAOYSA-N
InChI=1S/C23H21Cl2FN4O3.ClH/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);1H

HIDE SMILES / InChI

Molecular Formula C23H21Cl2FN4O3
Molecular Weight 491.342
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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).

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
3.2 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
0.869 ng/mL
32 mg 1 times / day multiple, oral
POZIOTINIB plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
0.989 ng × h/mL
32 mg 1 times / day multiple, oral
POZIOTINIB plasma
Homo sapiens

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer





Drug as perpetrator​

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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
Record UNII
X4Z7U6JL1C
Record Status Validated (UNII)
Record Version