Delving into the Latest Updates on XHL-11 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

EGFR T790M

Mechanism

EGFR T790M inhibitors(EGFR T790M inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

Non-Small Cell Lung Cancer

Inactive Indication-

Originator Organization

Yantai Institute of Materia Medica

Active Organization

Yantai Institute of Materia Medica

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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The first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), gefitinib and erlotinib significantly improved the therapeutic effect in non-small cell lung cancer (NSCLC) patients with EGFR mutation. However, the EGFR^T790M mutation occurs and results in acquired resistance. Consequently, mutant selective third-generation EGFR TKIs represented by AZD9291 (Osimertinib) have been developed to offer more effective therapeutic treatment, but the clinical application is limited by the acquired resistance and the high costs. A series of 5-chloropyrimidine-2,4-diamine derivatives were synthesized and screened for in vitro antitumor activity on H1975 and A431 cells. XHL11 showed the strongest antineoplastic activity. Compared to AZD9291, XHL11 suppressed cellular proliferation and colony formation and induced apoptosis in H1975 cells with EGFR^L858R/T790M mutation. In addition, XHL11 caused expression changes in EGFR and apoptosis-related pathways. Moreover, oral administration of XHL11 suppressed tumor progression in vivo in a H1975 subcutaneous xenograft model. These data demonstrated that XHL11 might be developed as a promising EGFR TKI for the therapeutic use of NSCLC patients.

100 Deals associated with XHL-11

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