Selpercatinib, marketed under the brand name Retevmo, is a selective RET (Rearranged during Transfection) kinase inhibitor approved for the treatment of certain cancers that harbor RET gene alterations. It is a targeted cancer therapy used to treat:
∙ Non-small cell lung cancer (NSCLC) with RET fusion-positive tumors
∙ Medullary thyroid cancer (MTC) with RET mutations
∙ Other thyroid cancers with RET fusions or mutations
Selpercatinib is taken orally, typically twice daily, and is part of a class of precision oncology drugs that work by inhibiting abnormal RET signaling, which promotes uncontrolled cancer cell growth.
![Tert-Butyl 3-(5-(3-Cyano-6-(2-Hydroxy-2-Methylpropoxy)Pyrazolo[1,5-A]Pyridin-4-Yl)Pyridin-2-Yl)-3,6-Diazabicyclo[3.1.1]Heptane-6-Carboxylate](https://veeprho.com/wp-content/uploads/2024/01/Selpercatinib-Impurity-1-VE0017826.png "Tert-Butyl 3-(5-(3-Cyano-6-(2-Hydroxy-2-Methylpropoxy)Pyrazolo[1,5-A]Pyridin-4-Yl)Pyridin-2-Yl)-3,6-Diazabicyclo[3.1.1]Heptane-6-Carboxylate")
Parent: Selpercatinib
Parent: Selpercatinib
![4-(6-(3,6-Diazabicyclo[3.1.1]Heptan-3-Yl)Pyridin-3-Yl)-6-(2-Hydroxy-2-Methylpropoxy)Pyrazolo[1,5-A]Pyridine-3-Carbonitrile](https://veeprho.com/wp-content/uploads/2024/01/VE0017827-Selpercatinib-Impurity.png "4-(6-(3,6-Diazabicyclo[3.1.1]Heptan-3-Yl)Pyridin-3-Yl)-6-(2-Hydroxy-2-Methylpropoxy)Pyrazolo[1,5-A]Pyridine-3-Carbonitrile")
Parent: Selpercatinib
Parent: Selpercatinib
Due to the complex nature of its synthesis and stability considerations, impurities in selpercatinib must be controlled per ICH Q3A/B and regulatory authority guidelines to ensure drug safety, efficacy, and purity.
Process-Related Impurities
Degradation Impurities
Elemental Impurities
Analytical Techniques for Impurity Detection
Selpercatinib is used to treat:
Selpercatinib inhibits RET tyrosine kinase, which is abnormally activated in certain cancers. This inhibition:
Common side effects include:
Regular monitoring of blood pressure, liver function, and heart rhythm is recommended.
Yes.
