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Tigozertinib

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Identification

Generic Name
Tigozertinib
DrugBank Accession Number
DB19239
Background

Tigozertinib (BLU-945) is currently under investigation in clinical trial NCT04862780 (Phase 1/​2 Study Targeting EGFR Resistance Mechanisms in NSCLC) for the treatment of NSCLC.

Type
Small Molecule
Groups
Investigational
Structure
3D
Similar Structures
Weight
Average: 556.7
Monoisotopic: 556.263188412
Chemical Formula
C28H37FN6O3S
Synonyms
  • 3-ISOQUINOLINAMINE, N-(2-((3S,4R)-3-FLUORO-4-METHOXY-1-PIPERIDINYL)-4-PYRIMIDINYL)-5-(1-METHYLETHYL)-8-((2R,3S)-2-METHYL-3-((METHYLSULFONYL)METHYL)-1-AZETIDINYL)-
  • EGFR MUTANT-SELECTIVE INHIBITOR BLU-945
  • N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-5-(propan-2-yl)-8-[(2R,3S)-2-methyl-3-[(methanesulfonyl)methyl]azetidin-1-yl]isoquinolin-3-amine
  • Tigozertinib
External IDs
  • BLU-945
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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
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.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
PA4PTH5HL9
CAS number
2660250-10-0
InChI Key
LIMFPAAAIVQRRD-BCGVJQADSA-N
InChI
InChI=1S/C28H37FN6O3S/c1-17(2)20-6-7-24(35-14-19(18(35)3)16-39(5,36)37)22-13-31-27(12-21(20)22)32-26-8-10-30-28(33-26)34-11-9-25(38-4)23(29)15-34/h6-8,10,12-13,17-19,23,25H,9,11,14-16H2,1-5H3,(H,30,31,32,33)/t18-,19+,23+,25+/m0/s1
IUPAC Name
SMILES
CO[C@@H]1CCN(C[C@@H]1F)C1=NC=CC(NC2=CC3=C(C=CC(N4C[C@H](CS(C)(=O)=O)[C@H]4C)=C3C=N2)C(C)C)=N1

References

General References
Not Available
ChemSpider
115010209
ChEMBL
CHEMBL5095169

Clinical Trials

Clinical Trials
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
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1, 2Active Not RecruitingTreatmentAdenocarcinomas / Antineoplastic Agents / Bronchial Neoplasm / Bronchogenic Carcinoma / Carcinoma / EGFR Activating Mutation / EGFR C797S / EGFR Exon 19 Deletion Mutation / EGFR Gene Mutations / EGFR L858R / EGFR Mutation Resulting in Tyrosine Kinase Inhibitor Resistance / EGFR Positive Non-small Cell Lung Cancer / EGFR T790M / Lung Disorder / Lung Neoplasm / Neoplasm / Neoplasms by Histologic Type / Neoplasms by Site / Neoplasms, Nerve Tissue / Non-Small Cell Lung Carcinoma / Protein Kinase Inhibitors / Respiratory Tract Diseases / Respiratory Tract Neoplasms / Thoracic Neoplasms1somestatusstop reasonjust information to hide

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
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at July 10, 2024 13:51 / Updated at July 11, 2024 07:56