1421373-66-1

Product Details:

CasNo： 1421373-66-1

Molecular Formula： C29H37N7O5S

Appearance： White to almost white Powder

Packing： Aluminium bag

Throughput： 100KG/Month

Purity： 99%

Brief Summary

Osimertinib mesylate (CAS 1421373-65-0, AZD9291) is an oral, irreversible third-generation EGFR tyrosine kinase inhibitor (EGFR-TKI). It selectively targets EGFR activating mutations including Exon 19 deletion and L858R, as well as the common acquired resistance mutation T790M, with limited activity against wild-type EGFR. Developed by AstraZeneca under the brand name Tagrisso®, it exhibits robust penetration across the blood-brain barrier and is a cornerstone therapy for EGFR-mutant non-small cell lung cancer (NSCLC). This API is widely supplied for generic formulation development, CMC documentation and preclinical oncology research.

Product Overview

Osimertinib mesylate is the marketed methanesulfonate salt form of osimertinib, a landmark covalent EGFR-TKI discovered and developed by AstraZeneca with the internal code AZD9291. Distinct from first‑ and second‑generation reversible EGFR inhibitors, osimertinib is rationally designed for mutant EGFR selectivity. It potently suppresses both primary sensitizing mutations and the T790M gatekeeper mutation, the major resistance mechanism after prior EGFR‑TKI treatment. It achieves high exposure in central nervous system lesions and is highly effective for brain metastases, a frequent complication of EGFR‑mutant lung cancer. The mesylate salt is the crystal form adopted for the commercial Tagrisso® tablet formulation and is the standard API grade for generic development worldwide.

Mechanism of Action

EGFR activating mutations (Ex19del, L858R) drive sustained downstream RAS‑RAF‑MEK‑ERK and PI3K‑AKT signalling, leading to uncontrolled tumour cell proliferation and survival. Osimertinib binds covalently and irreversibly to the ATP-binding pocket of mutant EGFR kinase domain, blocking receptor autophosphorylation and shutting off oncogenic signalling cascades. It shows much weaker affinity for wild-type EGFR, which reduces classic skin and gastrointestinal toxicities associated with earlier EGFR-TKIs. Osimertinib also readily crosses the blood-brain barrier, delivering therapeutic concentrations to intracranial tumour lesions and suppressing the growth of EGFR-mutant brain metastases.

Research & Clinical Background

Osimertinib received accelerated FDA approval in 2015 for T790M-positive metastatic NSCLC, based on the AURA trial programme. Subsequent pivotal trials including FLAURA, ADAURA and LAURA expanded its clinical landscape dramatically, and it is now approved across major global markets including EU, China and Japan. Core approved indications:

• First-line treatment of locally advanced or metastatic NSCLC harbouring EGFR Exon 19 deletion or L858R activating mutations;
• Treatment of locally advanced or metastatic T790M mutation-positive NSCLC progressing after prior EGFR-TKI therapy;
• Adjuvant therapy for resected IB‑IIIA stage EGFR-mutant NSCLC to lower recurrence risk;
• Consolidation therapy for unresectable stage III EGFR-mutant NSCLC without progression after platinum-based chemoradiotherapy. Active clinical pipelines continue to explore osimertinib in combination regimens, neoadjuvant settings and for overcoming secondary resistance mechanisms such as C797S, MET amplification and HER2 bypass signalling.

Research & Commercial Applications

Our Osimertinib Mesylate API is available for generic drug development and preclinical lung cancer research:

• Tagrisso® generic formulation development, process scale-up and complete CMC dossier preparation
• Polymorph control, impurity profiling, analytical method validation and long-term stability testing
• In vitro kinase screening, cell-based proliferation assays and EGFR signalling pathway mechanistic research
• In vivo xenograft and PDX tumour models, including intracranial brain metastasis efficacy evaluation
• SAR and lead optimisation for next-generation EGFR inhibitors addressing C797S resistance
• Combination studies with chemotherapy, anti‑angiogenic agents, MET inhibitors and other targeted agents

Product Statement & Disclaimer

This product is Osimertinib Mesylate API for pharmaceutical R&D and generic formulation. Batches manufactured under full GMP conditions can be used for clinical trial material production. It is not a finished medicinal product. End users must comply with local pharmaceutical regulatory requirements, complete quality audits and relevant registrations before clinical use. All technical data provided is for reference only.