NAV

Nazartinib

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
3D
Similar Structures
Weight
Average: 495.02
Monoisotopic: 494.219702
Chemical Formula
C26H31ClN6O2
Synonyms
  • Nazartinib
External IDs
  • EGF-816
  • EGF816
  • NVP-EGF816-NX
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Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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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
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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
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interactions in your software
AmbroxolThe risk or severity of methemoglobinemia can be increased when Nazartinib is combined with Ambroxol.
ArticaineThe risk or severity of methemoglobinemia can be increased when Nazartinib is combined with Articaine.
BenzocaineThe risk or severity of methemoglobinemia can be increased when Nazartinib is combined with Benzocaine.
Benzyl alcoholThe risk or severity of methemoglobinemia can be increased when Nazartinib is combined with Benzyl alcohol.
BupivacaineThe risk or severity of methemoglobinemia can be increased when Nazartinib is combined with Bupivacaine.
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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
3WithdrawnTreatmentNon-Small Cell Lung Carcinoma1
2Active Not RecruitingTreatmentLung Cancer1
2RecruitingTreatmentAdvanced Solid Tumors Which Are cMET-dependent1
2TerminatedTreatmentNon-Small Cell Lung Cancer (NSCLC)1
1Active Not RecruitingTreatmentEGFR Positive Non-small Cell Lung Cancer1

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
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-1900100000-f9b71ff575e50731bebf
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000x-6000900000-8f3fddbad96e62e9b395
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9165600000-36fcc276976ec2c0d084
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0uk9-0200900000-7e0b519213d014761271
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001l-9510200000-89f55da8853f0c483ddd
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-014m-9102300000-88515e7c3bed85ab861b
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

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