EGFR Exon 20 NSCLC - October 2020

EGFR Exon 20 NSCLC - October 2020

Preclinical data of DS-2087b in an NSCLC patient-derived xenograft (PDX) model with EGFR ins.ASV demonstrated antitumor effects

17 Sep 2020

DS-2087b (Selective inhibitor of EGFR/HER2 exon 20 insertions) – Daiichi Sankyo

  • Daiichi Sankyo presented the preclinical data of DS-2087b at ESMO2020
  • Results:
    • DS-2087b inhibited the proliferation of Ba/F3 cells expressing EGFR ins.ASV, EGFR ins.SVD, and HER2 ins.YVMA with GI50 values of 23.5, 21.3, and 29.0 nM, respectively
    • The GI50 value for Ba/F3 cells expressing EGFR WT was 368.9 nM
    • Similar GI50 values between EGFR/HER2 Exon 20 and WT EGFR were observed for poziotinib
    • Antitumor effects were observed in Ba/F3 allograft models with EGFR ins.ASV, EGFR ins.SVD, and HER2 ins.YVMA and the PDX model with EGFR ins.ASV in a dose-dependent manner
    • DS-2087b was effective against EGFR/HER2 Exon 20 and also showed selectivity over WT EGFR in in vitro and in vivo preclinical assays

Daiichi Sankyo’s DS-2087 demonstrated preclinical antitumor activity in EGFR/HER2 Exon 20 mutated NSCLC patients

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CI Scientists Remarks: 

  • DS-2087b is engineered to be an oral effective treatment to selectively inhibit EGFR/HER2 Exon 20 in mutated NSCLC patients and avoid the inhibition of WT EGFR
  • Daiichi Sankyo is looking to out-license (global) this molecule
  • Company has a wide range of portfolio targeting NSCLC

    Molecule

    MOA

    Patient segment

    Phase

    Trastuzumab deruxtecan

    (DS-8201)

    Anti HER2-ADC

    HER2+ mutated

    Phase 2

    Patritumab deruxtecan

    (U3-1402)

    Anti HER3-ADC

    EGFR mutated

    Phase 1

    DS-1062

    Anti TROP2-ADC

    —

    Phase 1

    DS-1205

    AXL inhibitor

    EGFR mutated

    Phase 1

– Tarun, CI Scientists

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