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    DRUG CLASS:

    HER2 exon 20 mutation inhibitor

    Related drugs:
    20h
    A Phase 1/2, Open-label, Multicenter, FIH Study to Evaluate Safety, Tolerability, PK and Anti-tumor Activity of YH42946 (clinicaltrials.gov)
    P1/2, N=161, Recruiting, Yuhan Corporation | Not yet recruiting --> Recruiting
    Enrollment open
    |
    YH42946
    18d
    A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body (clinicaltrials.gov)
    P1, N=16, Completed, Boehringer Ingelheim | Active, not recruiting --> Completed
    Trial completion
    |
    zongertinib (BI 1810631) • midazolam hydrochloride • omeprazole
    1m
    BEAMION-Lung 1: A Study to Test Different Doses of Zongertinib in People With Different Types of Advanced Cancer (Solid Tumours With Changes in the HER2 Gene) (clinicaltrials.gov)
    P1, N=554, Recruiting, Boehringer Ingelheim | Trial primary completion date: Dec 2025 --> Mar 2026
    Trial primary completion date • Metastases
    |
    NRG1 (Neuregulin 1)
    |
    EGFR mutation • HER-2 overexpression • HER-2 amplification • HER-2 mutation
    |
    zongertinib (BI 1810631)
    1m
    A Study in Healthy Men to Test Whether Zongertinib Influences the Amount of 4 Other Medicines (Dabigatran, Rosuvastatin, Metformin, and Furosemide) in the Blood (clinicaltrials.gov)
    P1, N=32, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    zongertinib (BI 1810631) • metformin
    2ms
    A Phase 1/2, Open-label, Multicenter, FIH Study to Evaluate Safety, Tolerability, PK and Anti-tumor Activity of YH42946 (clinicaltrials.gov)
    P1/2, N=161, Recruiting, Yuhan Corporation
    New P1/2 trial • EGFR exon 20 • Metastases
    |
    YH42946
    2ms
    Beamion PANTUMOR-1: A Study to Test Whether Zongertinib Helps People With Advanced Cancers With HER2 Alterations (clinicaltrials.gov)
    P2, N=200, Recruiting, Boehringer Ingelheim | Not yet recruiting --> Recruiting
    Enrollment open • Pan tumor • Metastases
    |
    zongertinib (BI 1810631)
    2ms
    Zongertinib (BI 1810631), an irreversible HER2 TKI, spares EGFR signaling and improves therapeutic response in preclinical models and patients with HER2-driven cancers. (PubMed, Cancer Discov)
    Zongertinib potently and selectively blocks HER2, while sparing EGFR, and inhibits the growth of cells dependent on HER2 oncogenic driver events, including HER2-dependent human cancer cells resistant to trastuzumab deruxtecan. Zongertinib displays potent anti-tumor activity in HER2-dependent human NSCLC xenograft models and enhances the activities of antibody-drug conjugates and KRASG12C inhibitors, without causing obvious toxicities. The preclinical efficacy of zongertinib translates in objective responses in patients with HER2-dependent tumors, including cholangiocarcinoma (SDC4-NRG1 fusion) and breast cancer (V777L HER2 mutation) thus supporting the ongoing clinical development of zongertinib.
    Preclinical • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • NRG1 (Neuregulin 1) • SDC4 (Syndecan 4)
    |
    HER-2 mutation • NRG1 fusion • HER-2 V777L • NRG1 fusion • SDC4-NRG1 fusion
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • zongertinib (BI 1810631)
    2ms
    Beamion PANTUMOR-1: A Study to Test Whether Zongertinib Helps People With Advanced Cancers With HER2 Alterations (clinicaltrials.gov)
    P2, N=200, Not yet recruiting, Boehringer Ingelheim
    New P2 trial • Pan tumor • Metastases
    |
    zongertinib (BI 1810631)
    3ms
    A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body (clinicaltrials.gov)
    P1, N=16, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    zongertinib (BI 1810631) • midazolam hydrochloride • omeprazole
    3ms
    A Study in Healthy Men to Test Whether Zongertinib Influences the Amount of 4 Other Medicines (Dabigatran, Rosuvastatin, Metformin, and Furosemide) in the Blood (clinicaltrials.gov)
    P1, N=32, Recruiting, Boehringer Ingelheim | Not yet recruiting --> Recruiting
    Enrollment open
    |
    zongertinib (BI 1810631) • metformin
    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
    4ms
    A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body (clinicaltrials.gov)
    P1, N=16, Recruiting, Boehringer Ingelheim | Not yet recruiting --> Recruiting
    Enrollment open
    |
    zongertinib (BI 1810631) • midazolam hydrochloride • omeprazole
    4ms
    A Study in Healthy Men to Test Whether Zongertinib Influences the Amount of 4 Other Medicines (Dabigatran, Rosuvastatin, Metformin, and Furosemide) in the Blood (clinicaltrials.gov)
    P1, N=32, Not yet recruiting, Boehringer Ingelheim
    New P1 trial
    |
    zongertinib (BI 1810631) • metformin
    4ms
    A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body (clinicaltrials.gov)
    P1, N=16, Not yet recruiting, Boehringer Ingelheim
    New P1 trial
    |
    zongertinib (BI 1810631) • midazolam hydrochloride • omeprazole
    4ms
    A Study in Healthy People to See How Zongertinib is Taken up Into the Blood When Given as Tablets Made by Two Different Manufacturers (clinicaltrials.gov)
    P1, N=56, Completed, Boehringer Ingelheim | Active, not recruiting --> Completed
    Trial completion
    |
    zongertinib (BI 1810631)
    4ms
    BEAMION-Lung 1: A Study to Test Different Doses of Zongertinib in People With Different Types of Advanced Cancer (Solid Tumours With Changes in the HER2 Gene) (clinicaltrials.gov)
    P1, N=554, Recruiting, Boehringer Ingelheim | N=371 --> 554
    Enrollment change • Metastases
    |
    NRG1 (Neuregulin 1)
    |
    zongertinib (BI 1810631)
    4ms
    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
    4ms
    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
    4ms
    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
    5ms
    A Study in Healthy People to See How Zongertinib is Taken up Into the Blood When Given as Tablets Made by Two Different Manufacturers (clinicaltrials.gov)
    P1, N=56, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    zongertinib (BI 1810631)
    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
    6ms
    Beamion BCGC-1: A Study to Find a Suitable Dose of Zongertinib in Combination With Trastuzumab Deruxtecan or With Trastuzumab Emtansine and to Test Whether it Helps People With Different Types of HER2+ Cancer That Has Spread (clinicaltrials.gov)
    P1/2, N=240, Recruiting, Boehringer Ingelheim | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • zongertinib (BI 1810631)
    6ms
    A Study in Healthy People to See How Zongertinib is Taken up Into the Blood When Given as Tablets Made by Two Different Manufacturers (clinicaltrials.gov)
    P1, N=56, Recruiting, Boehringer Ingelheim | Not yet recruiting --> Recruiting
    Enrollment open
    |
    zongertinib (BI 1810631)
    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 in Healthy People to See How Zongertinib is Taken up Into the Blood When Given as Tablets Made by Two Different Manufacturers (clinicaltrials.gov)
    P1, N=56, Not yet recruiting, Boehringer Ingelheim
    New P1 trial
    |
    zongertinib (BI 1810631)
    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
    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, Not yet recruiting, Bayer
    New P1 trial
    |
    itraconazole • BAY 2927088
    8ms
    IAM1363-01: A Phase 1/1b Study of IAM1363 in HER2 Cancers (clinicaltrials.gov)
    P1, N=287, Recruiting, Iambic Therapeutics, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Herceptin (trastuzumab)
    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
    Beamion BCGC-1: A Study to Find a Suitable Dose of Zongertinib in Combination With Trastuzumab Deruxtecan or With Trastuzumab Emtansine and to Test Whether it Helps People With Different Types of HER2+ Cancer That Has Spread (clinicaltrials.gov)
    P1/2, N=240, Not yet recruiting, Boehringer Ingelheim
    New P1/2 trial • Combination therapy • Metastases
    |
    Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • zongertinib (BI 1810631)
    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
    9ms
    A Phase 1/1b Study of IAM1363 in HER2 Cancers (clinicaltrials.gov)
    P1, N=287, Not yet recruiting, Iambic Therapeutics, Inc
    New P1 trial
    |
    Herceptin (trastuzumab)
    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