Delving into the Latest Updates on HJM-561 with Synapse

Overview

Basic Info

Drug Type

Proteolysis-targeting chimeras (PROTAC)

Synonyms

Target

EGFR C797S

Mechanism

EGFR C797S inhibitors(Epidermal Growth Factor Receptor C797S inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

EGFR C797S Mutation Non-small Cell Lung Cancer

Inactive Indication-

Originator Organization

Jing Medicine Technology Shanghai Ltd.

Active Organization

Jing Medicine Technology Shanghai Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

AbstractThe EGFR C797S mutation is the most common on-target resistance mechanism to osimertinib in patients with advanced non–small cell lung cancer (NSCLC). Currently there are no effective treatment options for patients with NSCLC harboring EGFR C797S triple mutants (Del19/T790M/C797S and L858R/T790M/C797S). Herein, we report an orally bioavailable EGFR PROTAC, HJM-561, which selectively degrades the EGFR C797S-containing triple mutants. HJM-561 potently inhibits the proliferation of Del19/T790M/C797S and L858R/T790M/C797S Ba/F3 cells while sparing cells expressing wild-type EGFR. Oral administration of HJM-561 shows robust antitumor activity in EGFR Del19/T790M/C797S-driven Ba/F3 CDX and PDX models that were resistant to osimertinib treatment. Taken together, our results suggest that HJM-561 is a promising therapeutic option for overcoming EGFR triple mutation-mediated drug resistance in NSCLC.Watch the interview with George Zhang, PhD, recipient of the 2024 Molecular Cancer Therapeutics Award for Outstanding Journal Article: https://vimeo.com/992990122

100 Deals associated with HJM-561

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