General Information

Osimertinib Impurities and Osimertinib  

Daicel Pharma synthesizes high-quality Osimertinib impurities such as Osimertinib Impurity N, Osimertinib N desmethyl impurity, Osimertinib N-Oxide, Osimertinib N, N’-Dioxide, Osimertinib Impurity-J, and Osimertinib Impurity-I, crucial in the analysis of the quality, stability, and biological safety of the active pharmaceutical ingredient, Osimertinib. Moreover, Daicel Pharma offers custom synthesis of Osimertinib impurities and delivers them globally.

 Osimertinib [CAS: 1421373-65-0] is a small molecule, tyrosine kinase receptor inhibitor, and antineoplastic agent. It treats certain forms of advanced non-small cell lung cancer (NSCLC).

Osimertinib: Use and Commercial Availability  

Osimertinib is an oral medication sold under the brand name Tagrisso. It treats adults with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive NSCLC that has progressed on or after EGFR TKI therapy. Further, Tagrisso is the first treatment for patients having ‘activating mutations’ whose cancer has advanced or spread.

Osimertinib Structure and Mechanism of Action

The chemical name of Osimertinib is N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide. Its formula for Osimertinib is C₂₈H₃₃N₇O_2, and its molecular weight is approximately 499.6 g/mol.

 Osimertinib is an EGFR kinase inhibitor, and it irreversibly binds to certain mutant forms of EGFR (T790M, L858R, exon 19 deletion). It binds at approximately 9-fold lower concentrations than wild-type EGFR.

Osimertinib Impurities and Synthesis 

Osimertinib may contain related substances and process impurities that impact its final purity, yield, and quality. It is crucial to regulate impurity levels in Osimertinib to maintain the drug’s safety and effectiveness.

Daicel offers a Certificate of Analysis (CoA) from a cGMP-compliant analytical facility for Osimertinib impurity standards, including Osimertinib Impurity N, Osimertinib N-desmethyl impurity, Osimertinib N-Oxide, Osimertinib N, N’-Dioxide, Osimertinib Impurity-J, and Osimertinib Impurity-I. The CoA includes complete characterization data, such as 1H NMR, 13C NMR, IR, MASS¹, and HPLC purity². We also provide 13C-DEPT and CHN on request. We also give a complete characterization report on delivery.

Daicel has the technology and expertise to prepare any unknown Osimertinib impurity or degradation product. Daicel also provides labeled compounds to quantify the efficacy of generic Osimertinib. Daicel offers Osimertinib-D6, a deuterium-labeled standard of Osimertinib for bioanalytical research and BA/BE studies.

Osimertinib