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    DRUG:

    BAY 2927088

    i
    Other names: BAY 2927088, BAY2927088, BAY-2927088
    Company:
    Bayer, Broad Institute
    Drug class:
    EGFR inhibitor, HER2 inhibitor, HER2 exon 20 mutation inhibitor
    Related drugs:
    3ms
    SOHO-02: A Study to Learn More About How Well BAY 2927088 Works and How Safe it is Compared With Standard Treatment, in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P3, N=278, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    Keytruda (pembrolizumab) • cisplatin • carboplatin • pemetrexed • BAY 2927088
    3ms
    SOHO-01: First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1/2, N=370, Recruiting, Bayer | Trial completion date: Nov 2027 --> Dec 2026 | Trial primary completion date: Nov 2027 --> Dec 2025
    Trial completion date • Trial primary completion date • HER2 exon 20 • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    BAY 2927088
    5ms
    A Study to Learn About How BAY2927088 Affects the Level of Dabigatran or Rosuvastatin in the Blood When These Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Completed, Bayer | Recruiting --> Completed
    Trial completion
    |
    BAY 2927088
    5ms
    A Study to Learn About How Food and Esomeprazole Affect the Level of BAY2927088 in the Blood When Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=21, Completed, Bayer | Recruiting --> Completed
    Trial completion
    |
    BAY 2927088
    5ms
    A Study to Learn About How BAY2927088 Affects the Level of Midazolam in the Blood When Both Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Completed, Bayer | Active, not recruiting --> Completed
    Trial completion
    |
    BAY 2927088 • midazolam hydrochloride
    5ms
    A Study to Learn About How Itraconazole and Carbamazepine Affect the Level of BAY2927088 in the Blood When These Drugs Are Taken Together by Healthy Participants (clinicaltrials.gov)
    P1, N=30, Completed, Bayer | Recruiting --> Completed
    Trial completion
    |
    itraconazole • BAY 2927088
    5ms
    A Study to Learn More About How Well BAY 2927088 Works and How Safe it is Compared With Standard Treatment, in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P3, N=278, Not yet recruiting, Bayer
    New P3 trial • Metastases
    |
    Keytruda (pembrolizumab) • cisplatin • carboplatin • pemetrexed • BAY 2927088
    6ms
    A Study to Learn About How BAY2927088 Affects the Level of Midazolam in the Blood When Both Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Active, not recruiting, Bayer | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    BAY 2927088 • midazolam hydrochloride
    7ms
    A Study to Learn About How Itraconazole and Carbamazepine Affect the Level of BAY2927088 in the Blood When These Drugs Are Taken Together by Healthy Participants (clinicaltrials.gov)
    P1, N=30, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    itraconazole • BAY 2927088
    7ms
    Safety and anti-tumor activity of BAY 2927088 in patients with HER2-mutant NSCLC: Results from an expansion cohort of the SOHO-01 phase I/II study. (ASCO 2024)
    BAY 2927088 led to rapid, substantial, and durable responses in pts with pretreated HER2-mutant NSCLC. The safety profile was consistent with previously reported data. These data support the further clinical development of BAY 2927088 in pts with HER2-mutant NSCLC.
    Late-breaking abstract • P1/2 data • Clinical
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    Oncomine Precision Assay
    |
    BAY 2927088
    7ms
    A Study to Learn About How BAY2927088 Affects the Level of Midazolam in the Blood When Both Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    BAY 2927088 • midazolam hydrochloride
    7ms
    A Study to Learn About How Food and Esomeprazole Affect the Level of BAY2927088 in the Blood When Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=21, Recruiting, Bayer
    New P1 trial
    |
    BAY 2927088
    7ms
    A Study to Learn About How BAY2927088 Affects the Level of Dabigatran or Rosuvastatin in the Blood When These Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    BAY 2927088
    7ms
    A Study to Learn About How BAY2927088 Affects the Level of Midazolam in the Blood When Both Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, Bayer
    New P1 trial
    |
    BAY 2927088 • midazolam hydrochloride
    7ms
    A Study to Learn How BAY2927088 is Taken up and Handled by the Body in Healthy Male Participants (clinicaltrials.gov)
    P1, N=8, Completed, Bayer | Active, not recruiting --> Completed
    Trial completion
    |
    BAY 2927088
    8ms
    A Study to Learn About How Itraconazole and Carbamazepine Affect the Level of BAY2927088 in the Blood When These Drugs Are Taken Together by Healthy Participants (clinicaltrials.gov)
    P1, N=30, Not yet recruiting, Bayer
    New P1 trial
    |
    itraconazole • BAY 2927088
    8ms
    A Study to Learn About How BAY2927088 Affects the Level of Dabigatran or Rosuvastatin in the Blood When These Drugs Are Taken Together in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, Bayer
    New P1 trial
    |
    BAY 2927088
    8ms
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1/2, N=460, Recruiting, Bayer | Trial completion date: Jul 2028 --> Nov 2027 | Trial primary completion date: Jul 2028 --> Nov 2027
    Trial completion date • Trial primary completion date • HER2 exon 20 • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088
    9ms
    A Study to Learn How BAY2927088 is Taken up and Handled by the Body in Healthy Male Participants (clinicaltrials.gov)
    P1, N=8, Active, not recruiting, Bayer | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    BAY 2927088
    10ms
    A Study to Learn How BAY2927088 is Taken up and Handled by the Body in Healthy Male Participants (clinicaltrials.gov)
    P1, N=8, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    BAY 2927088
    10ms
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1/2, N=460, Recruiting, Bayer | Phase classification: P1 --> P1/2 | N=340 --> 460
    Phase classification • Enrollment change • HER2 exon 20 • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088
    10ms
    A Study to Learn How BAY2927088 is Taken up and Handled by the Body in Healthy Male Participants (clinicaltrials.gov)
    P1, N=8, Not yet recruiting, Bayer
    New P1 trial
    |
    BAY 2927088
    1year
    Mechanisms of resistance to BAY 2927088, the first reversible inhibitor targeting EGFR exon 20 insertion mutations in non-small cell lung cancer. (AACR-NCI-EORTC 2023)
    No abstract available
    EGFR exon 20
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
    |
    BAY 2927088
    over1year
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1, N=340, Recruiting, Bayer | Trial completion date: Dec 2025 --> Jul 2028 | Trial primary completion date: Dec 2025 --> Jul 2028
    Trial completion date • Trial primary completion date • HER2 exon 20 • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088
    over1year
    Early evidence of efficacy in patients (pts) with non-small cell lung cancer (NSCLC) with HER2 exon20 insertion (ex20ins) mutations treated in a phase I study with BAY 2927088 (ESMO 2023)
    In pts with HER2 ex20ins mutant disease, BAY 2927088 showed encouraging preliminary anti-tumour activity. These results warrant further investigation of BAY 2927088 in pts with NSCLC.
    Clinical • P1 data
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation • HER-2 exon 20 insertion • HER-2 exon 20 mutation • HER-2 exon 23 mutation
    |
    BAY 2927088
    over1year
    Preclinical activity of BAY 2927088 in HER2 mutant non-small cell lung cancer (AACR 2023)
    With the recent approval of fam-trastuzumab deruxtecan-nxki, the first targeted treatment option became available for HER2 mutant NSCLC patients. In addition, the compound was active in a subset of endogenously HER2 mutant cancer cell lines. The in vitro activity of BAY 2927088 was validated in vivo in a patient-derived xenograft model carrying the HER2 exon20 insertion mutation A775insYVMA.The strong preclinical activity of BAY 2927088 in HER2 mutant NSCLC supports clinical evaluation in this indication and might offer a novel targeted therapy option for NSCLC patients that carry HER2 mutations.
    Preclinical
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation • HER-2 exon 20 insertion • HER-2 L755S • HER-2 S310F • HER-2 exon 20 mutation • HER-2 A775 • HER-2 S335C • HER-2 YVMA • HER-2 exon 23 mutation
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • BAY 2927088
    over1year
    An open-label, first-in-human study of BAY2927088 in patients with advanced non-small cell lung cancer (NSCLC) harboring an EGFR and/or HER2 mutation (AACR 2023)
    Key exclusion criteria include presence of serious cardiac conditions, interstitial lung disease, active CNS metastasis, or leptomeningeal disease. The trial is currently enrolling patients in dose-escalation and backfill parts (NCT05099172).
    Clinical • P1 data • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation • EGFR exon 20 insertion • EGFR wild-type • EGFR C797S • AR mutation • EGFR exon 20 mutation
    |
    BAY 2927088
    over1year
    Mechanisms of resistance to BAY 2927088, the first reversible inhibitor targeting EGFR exon 20 insertion mutations in non-small cell lung cancer (AACR 2023)
    Agents such as amivantamab and mobocertinib have been approved for treatment of lung cancer patients with exon 20 insertions, but agents with an improved selectivity profile versus wild-type EGFR are still needed. As a parallel approach, we are developing a deep-scanning mutagenesis assay of the EGFR kinase domain to identify mutations that could cause resistance. Understanding these resistance mechanisms will help to identify second-line treatments for exon 20 insertion patients who develop resistance to EGFR inhibition.
    EGFR exon 20
    |
    EGFR (Epidermal growth factor receptor) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    EGFR mutation • NRAS mutation • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • EGFR wild-type • EGFR exon 20 mutation
    |
    Rybrevant (amivantamab-vmjw) • Exkivity (mobocertinib) • BAY 2927088
    over1year
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1, N=340, Recruiting, Bayer | N=250 --> 340
    Enrollment change • HER2 exon 20 • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088
    2years
    BAY 2927088: The first non-covalent, potent, and selective tyrosine kinase inhibitor targeting EGFR exon 20 insertions and C797S resistance mutations in NSCLC (AACR-NCI-EORTC 2022)
    Despite the recent advances with the approval of amivantamab and mobocertinib, there remains a high unmet need for more effective and better tolerated agents targeting exon 20 insertions that can improve response rates and response durability. The strong potency and improved selectivity of BAY 2927088 offer the prospect of a wider therapeutic window in the clinic and potentially a favorable safety profile with improved combinability compared to available EGFR exon 20 insertion targeted therapies. BAY 2927088 is currently being evaluated in a first-in-human, phase I clinical trial in patients with EGFR mutant NSCLC (NCT05099172). The study will evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary anti-tumor activity of BAY 2927088.
    EGFR exon 20
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • EGFR wild-type • EGFR C797S • EGFR exon 20 mutation
    |
    Rybrevant (amivantamab-vmjw) • Exkivity (mobocertinib) • BAY 2927088
    almost3years
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1, N=250, Recruiting, Bayer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088
    3years
    First in Human Study of BAY2927088 in Participants Who Have Advanced Non-small Cell Lung Cancer (NSCLC) With Mutations in the Genes of Epidermal Growth Factor Receptor (EGFR) and/or Human Epidermal Growth Factor Receptor 2 (HER2) (clinicaltrials.gov)
    P1, N=250, Not yet recruiting, Bayer
    Clinical • New P1 trial
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation
    |
    BAY 2927088