Abivertinib

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

Identification

Generic Name
Abivertinib
DrugBank Accession Number
DB15327
Background

Abivertinib is a tyrosine kinase inhibitor targeted against mutant forms of both human epidermal growth factor receptor (EGFR) and Bruton's tyrosine kinase (BTK).1 It has been investigated for use in the treatment of non-small cell lung cancer (NSCLC) and B-cell malignancies. In binding to and inhibiting EGFR and BTK receptors, abivertinib exerts immunomodulatory effects by preventing the production and release of pro-inflammatory cytokines (e.g. TNF-alpha, interleukins).2

Abivertinib's potential to depress cytokine production has led to its investigation in the treatment of hospitalized patients with moderate-to-severe COVID-19.2,3 The cytokine storm associated with COVID-19 is thought to contribute to disease progression and is associated with poor outcomes in patients - as abivertinib inhibits the release of multiple cytokines at once, it may provide more pronounced clinical benefits as compared to agents targeting single pathways (e.g. interleukin-6 inhibitors). The study is expected to be completed in March 2021.4

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 487.539
Monoisotopic: 487.213201268
Chemical Formula
C26H26FN7O2
Synonyms
  • Abivertinib
External IDs
  • A610
  • AC-0010
  • AC0010
  • ACEA100610
  • EX-ACEA0010

Pharmacology

Indication

Not Available

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Avoid life-threatening adverse drug events & improve clinical decision support.
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
AEpidermal growth factor receptor
inhibitor
Humans
ATyrosine-protein kinase BTK
inhibitor
Humans
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
Adverseeffects
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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

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Abivertinib maleateY50131AMFJ1822357-78-7QITOONQVTOGMOJ-IUJXYRIYSA-N

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
CER0OPG92L
CAS number
1557267-42-1
InChI Key
UOFYSRZSLXWIQB-UHFFFAOYSA-N
InChI
InChI=1S/C26H26FN7O2/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32)
IUPAC Name
N-{3-[(2-{[3-fluoro-4-(4-methylpiperazin-1-yl)phenyl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]phenyl}prop-2-enamide
SMILES
CN1CCN(CC1)C1=C(F)C=C(NC2=NC(OC3=CC=CC(NC(=O)C=C)=C3)=C3C=CNC3=N2)C=C1

References

General References
  1. Sorrento Therapeutics: Abivertinib [Link]
  2. Sorrento Therapeutics: Abivertinib COVID-19 Trial [Link]
  3. NCT04440007: Study of the Efficacy and Safety of STI-5656 (Abivertinib Maleate) With SOC Versus SOC in Subjects With COVID-19 (SOC) [Link]
  4. Targeted Oncology: FDA Clears Phase 2 Study of Abivertinib in Hospitalized Patients With COVID-19 [Link]
ChemSpider
57490375
BindingDB
294480
ChEMBL
CHEMBL4297865
ZINC
ZINC000142081723

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Not Yet RecruitingTreatmentAdvanced Non Small Cell Lung Cancer (NSCLC)1
3WithdrawnTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2Active Not RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
2RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
2RecruitingTreatmentMetastatic Non-Small Cell Lung Cancer1
2RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)2
1RecruitingTreatmentB Cell Lymphoma (BCL)1
1TerminatedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1, 2Active Not RecruitingTreatmentMetastatic 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 Solubility0.0276 mg/mLALOGPS
logP4.33ALOGPS
logP4.82ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)12.6ChemAxon
pKa (Strongest Basic)7.25ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area98.41 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity138.95 m3·mol-1ChemAxon
Polarizability52.34 Å3ChemAxon
Number of Rings5ChemAxon
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

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Ubiquitin protein ligase binding
Specific Function
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TG...
Gene Name
EGFR
Uniprot ID
P00533
Uniprot Name
Epidermal growth factor receptor
Molecular Weight
134276.185 Da
References
  1. Sorrento Therapeutics: Abivertinib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately le...
Gene Name
BTK
Uniprot ID
Q06187
Uniprot Name
Tyrosine-protein kinase BTK
Molecular Weight
76280.71 Da
References
  1. Sorrento Therapeutics: Abivertinib [Link]

Drug created on May 20, 2019 15:15 / Updated on February 21, 2021 18:55