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

Identification

Generic Name
Almonertinib
DrugBank Accession Number
DB16640
Background

Almonertinib is a third-generation EGFR tyrosine kinase inhibitor targeting EGFR-sensitizing and T790M resistance mutations.1,2,3 It is being investigated against advanced or metastatic EGFR-mutated non-small cell lung cancer (NSCLC).3

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 525.657
Monoisotopic: 525.285223395
Chemical Formula
C30H35N7O2
Synonyms
  • Almonertinib
  • HS-10296
External IDs
  • HS 10296
  • HS-10296

Pharmacology

Indication

Not Available

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

Not Available

Mechanism of action

Almonertinib inhibits EGFR tyrosine kinase targeting EGFR-sensitizing and T790M resistance mutations.1,2,3

TargetActionsOrganism
AReceptor protein-tyrosine kinase
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
Improve decision support & research outcomes
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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

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International/Other Brands
Ameile (Hansoh Pharma)

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
T4RS462G19
CAS number
1899921-05-1
InChI Key
DOEOECWDNSEFDN-UHFFFAOYSA-N
InChI
InChI=1S/C30H35N7O2/c1-6-29(38)32-24-17-25(28(39-5)18-27(24)36(4)16-15-35(2)3)34-30-31-14-13-23(33-30)22-19-37(20-11-12-20)26-10-8-7-9-21(22)26/h6-10,13-14,17-20H,1,11-12,15-16H2,2-5H3,(H,32,38)(H,31,33,34)
IUPAC Name
N-(5-{[4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl]amino}-2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxyphenyl)prop-2-enamide
SMILES
COC1=CC(N(C)CCN(C)C)=C(NC(=O)C=C)C=C1NC1=NC(=CC=N1)C1=CN(C2CC2)C2=C1C=CC=C2

References

General References
  1. Yang JC, Camidge DR, Yang CT, Zhou J, Guo R, Chiu CH, Chang GC, Shiah HS, Chen Y, Wang CC, Berz D, Su WC, Yang N, Wang Z, Fang J, Chen J, Nikolinakos P, Lu Y, Pan H, Maniam A, Bazhenova L, Shirai K, Jahanzeb M, Willis M, Masood N, Chowhan N, Hsia TC, Jian H, Lu S: Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial. J Thorac Oncol. 2020 Dec;15(12):1907-1918. doi: 10.1016/j.jtho.2020.09.001. Epub 2020 Sep 9. [Article]
  2. Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F, Ou SI: Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2020 Dec 15. pii: S1556-0864(20)31105-9. doi: 10.1016/j.jtho.2020.11.028. [Article]
  3. Jiang T, Luo Y, Wang B: Almonertinib-induced interstitial lung disease: A case report. Medicine (Baltimore). 2021 Jan 22;100(3):e24393. doi: 10.1097/MD.0000000000024393. [Article]
ChemSpider
75535991

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4RecruitingTreatmentAdenocarcinomas / Carcinoma / Non-Small Cell Lung Carcinoma (NSCLC)1
3Active Not RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)2
3Enrolling by InvitationTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
3Not Yet RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)5
3RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2Active Not RecruitingTreatmentMetastatic Non-Small Cell Lung Cancer1
2Enrolling by InvitationOtherSafety of Almonertinib1
2Not Yet RecruitingTreatmentAdvanced Non Small Cell Lung Cancer (NSCLC)1
2Not Yet RecruitingTreatmentEGF-R Positive Non-Small Cell Lung Cancer / Tumors Metastatic to Brain1
2Not Yet RecruitingTreatmentEGFR Gene Mutations / EGFR T790M / Non-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
logP4.95ChemAxon
pKa (Strongest Acidic)13.64ChemAxon
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area87.55 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity157.53 m3·mol-1ChemAxon
Polarizability58.07 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Atp binding
Gene Name
EGFR
Uniprot ID
Q504U8
Uniprot Name
Receptor protein-tyrosine kinase
Molecular Weight
120691.33 Da
References
  1. Yang JC, Camidge DR, Yang CT, Zhou J, Guo R, Chiu CH, Chang GC, Shiah HS, Chen Y, Wang CC, Berz D, Su WC, Yang N, Wang Z, Fang J, Chen J, Nikolinakos P, Lu Y, Pan H, Maniam A, Bazhenova L, Shirai K, Jahanzeb M, Willis M, Masood N, Chowhan N, Hsia TC, Jian H, Lu S: Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial. J Thorac Oncol. 2020 Dec;15(12):1907-1918. doi: 10.1016/j.jtho.2020.09.001. Epub 2020 Sep 9. [Article]
  2. Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F, Ou SI: Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2020 Dec 15. pii: S1556-0864(20)31105-9. doi: 10.1016/j.jtho.2020.11.028. [Article]
  3. Jiang T, Luo Y, Wang B: Almonertinib-induced interstitial lung disease: A case report. Medicine (Baltimore). 2021 Jan 22;100(3):e24393. doi: 10.1097/MD.0000000000024393. [Article]

Drug created at March 18, 2021 18:30 / Updated at March 21, 2021 02:08