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Details

Stereochemistry MIXED
Molecular Formula C29H31N7O3
Molecular Weight 525.6015
Optical Activity UNSPECIFIED
Defined Stereocenters 0 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SELPERCATINIB

SMILES

COC1=NC=C(CN2C3CC2CN(C3)C4=CC=C(C=N4)C5=CC(OCC(C)(C)O)=CN6N=CC(C#N)=C56)C=C1

InChI

InChIKey=XIIOFHFUYBLOLW-UHFFFAOYSA-N
InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3

HIDE SMILES / InChI
Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor that was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P07949
Gene ID: 5979.0
Gene Symbol: RET
Target Organism: Homo sapiens (Human)
0.56 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
RETEVMO

Approved Use

RETEVMO is a kinase inhibitor indicated for the treatment of: Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)1. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate)
Primary
RETEVMO

Approved Use

RETEVMO is a kinase inhibitor indicated for the treatment of: Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)1. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate)
Primary
RETEVMO

Approved Use

RETEVMO is a kinase inhibitor indicated for the treatment of: Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC)1. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy. Adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate)

Sample Use Guides

Less than 50 kg: 120 mg; 50 kg or greater: 160 mg. Take it orally twice daily (approximately every 12 hours) until disease progression or unacceptable toxicity.
Route of Administration: Oral
Name Type Language
SELPERCATINIB
INN   USAN  
Official Name English
LOXO-292
Code English
SELPERCATINIB [JAN]
Common Name English
SELPERCATINIB [MI]
Common Name English
SELPERCATINIB [USAN]
USAN  
Common Name English
6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO(3.1.1)HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO(1,5-A)PYRIDINE-3-CARBONITRILE
Systematic Name English
SELPERCATINIB [ORANGE BOOK]
Common Name English
RET INHIBITOR LOXO-292
Common Name English
RETEVMO
Brand Name English
Selpercatinib [WHO-DD]
Common Name English
LY-3527723
Code English
LY3527723
Code English
PYRAZOLO(1,5-A)PYRIDINE-3-CARBONITRILE, 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXY-3-PYRIDINYL)METHYL)-3,6-DIAZABICYCLO(3.1.1)HEPT-3-YL)-3-PYRIDINYL)-
Systematic Name English
selpercatinib [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 675218
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
EU-Orphan Drug EU/3/18/2071
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
FDA ORPHAN DRUG 653118
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
FDA ORPHAN DRUG 652318
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
FDA ORPHAN DRUG 849621
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
Code System Code Type Description
PUBCHEM
134436906
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
NCI_THESAURUS
C134987
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
DRUG BANK
DB15685
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
INN
10967
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
LACTMED
Selpercatinib
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
DAILYMED
CEGM9YBNGD
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
FDA UNII
CEGM9YBNGD
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
USAN
GH-184
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
CAS
2152628-33-4
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
MERCK INDEX
M12205
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
EPA CompTox
DTXSID901026442
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
RXCUI
2370147
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY
WIKIPEDIA
Selpercatinib
Created by admin on Sun Dec 18 21:19:01 UTC 2022 , Edited by admin on Sun Dec 18 21:19:01 UTC 2022
PRIMARY