This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Nazartinib
DrugBank Accession Number
DB16250
Background

Nazartinib is under investigation in clinical trial NCT03529084 (Phase III Study of Nazartinib (EGF816) Versus Erlotinib/gefitinib in First-line Locally Advanced / Metastatic NSCLC With EGFR Activating Mutations).

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 495.02
Monoisotopic: 494.219702
Chemical Formula
C26H31ClN6O2
Synonyms
  • Nazartinib
External IDs
  • EGF-816
  • EGF816
  • NVP-EGF816-NX

Pharmacology

Indication

Not Available

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Darbepoetin alfaThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Nazartinib.
ErythropoietinThe risk or severity of Thrombosis can be increased when Erythropoietin is combined with Nazartinib.
Methoxy polyethylene glycol-epoetin betaThe risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Nazartinib.
PeginesatideThe risk or severity of Thrombosis can be increased when Peginesatide is combined with Nazartinib.
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
KE7K32EME8
CAS number
1508250-71-2
InChI Key
IOMMMLWIABWRKL-WUTDNEBXSA-N
InChI
InChI=1S/C26H31ClN6O2/c1-18-16-19(12-13-28-18)25(35)30-26-29-22-10-6-9-21(27)24(22)33(26)20-8-4-5-15-32(17-20)23(34)11-7-14-31(2)3/h6-7,9-13,16,20H,4-5,8,14-15,17H2,1-3H3,(H,29,30,35)/b11-7+/t20-/m1/s1
IUPAC Name
N-{7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]-1H-1,3-benzodiazol-2-yl}-2-methylpyridine-4-carboxamide
SMILES
CN(C)C\C=C\C(=O)N1CCCC[C@H](C1)N1C(NC(=O)C2=CC=NC(C)=C2)=NC2=C1C(Cl)=CC=C2

References

General References
Not Available
ChemSpider
35308229
ChEMBL
CHEMBL3787344
ZINC
ZINC000210610738

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3WithdrawnTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2Active Not RecruitingTreatmentLung Cancers1
2RecruitingTreatmentAdvanced Solid Tumors Which Are cMET-dependent1
2TerminatedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1Active Not RecruitingTreatmentEGFR-Mutated Non-Small-Cell Lung Carcinoma1
1CompletedTreatmentColorectal Cancer, Triple Negative Breast Cancer, NSCLC - Adenocarcinoma1
1RecruitingTreatmentAdvanced EGFRmutant NonSmallSellLungCancer (NSCLC),KRAS G12-mutant NSCLC,Esophageal SquamousCellCancer (SCC),Head/Neck SCC,Melanoma1
1RecruitingTreatmentNeoplasm, Bronchial1
1, 2Active Not RecruitingTreatmentAdvanced Non Small Cell Lung Cancer (NSCLC)1
1, 2RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.02 mg/mLALOGPS
logP3.78ALOGPS
logP3.5ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)13.62ChemAxon
pKa (Strongest Basic)8.81ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area83.36 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity140.04 m3·mol-1ChemAxon
Polarizability54.2 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at December 15, 2020 18:16 / Updated at February 21, 2021 18:55