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    DRUG CLASS:

    Topoisomerase I inhibitor

    Related drugs:
    1d
    Pilot Study of IT Topotecan and Maintenance Chemotherapy for HR-EBTs in Children < 6 Years, Post Consolidation (clinicaltrials.gov)
    P1, N=15, Recruiting, C17 Council | Not yet recruiting --> Recruiting
    Enrollment open
    |
    cisplatin • carboplatin • temozolomide • tamoxifen • cytarabine • cyclophosphamide • etoposide IV • vincristine • topotecan • mesna • thiotepa • Neupogen (filgrastim) • celecoxib oral
    1d
    A Study of GSK5764227 in Participants With. Advanced Solid Tumors (EMBOLD PanTumor-101) (clinicaltrials.gov)
    P1, N=590, Recruiting, GlaxoSmithKline | N=316 --> 590
    Enrollment change • Pan tumor
    |
    Keytruda (pembrolizumab) • Avastin (bevacizumab) • Erbitux (cetuximab) • cisplatin • Tecentriq (atezolizumab) • carboplatin • Imfinzi (durvalumab) • risvutatug rezetecan (GSK5764227)
    1d
    A Study of SHR-A2009 Combined With Aumolertinib Versus Aumolertinib for First-line Treatment in EGFR-mutated, Advanced or Metastatic NSCLC (clinicaltrials.gov)
    P3, N=576, Recruiting, Suzhou Suncadia Biopharmaceuticals Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Ameile (aumolertinib) • ruzaltatug rezetecan (SHR-A2009)
    1d
    JSKN022 in Subjects With Advanced Malignant Solid Tumors (clinicaltrials.gov)
    P1, N=225, Recruiting, Jiangsu Alphamab Biopharmaceuticals Co., Ltd
    New P1 trial
    2d
    DESTINY-Breast08: A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=138, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2025 --> Jun 2026
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor)
    |
    HER-2 expression • HER-2 underexpression • PGR positive
    |
    Imfinzi (durvalumab) • paclitaxel • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • fulvestrant • Truqap (capivasertib) • anastrozole
    2d
    A Study to Assess Adverse Events and Change in Disease Activity of Intravenous (IV) Telisotuzumab Adizutecan Compared to Standard of Care in Adult Participants With Locally Advanced or Metastatic EGFR-Mutated Non-Squamous Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2/3, N=430, Recruiting, AbbVie | Not yet recruiting --> Recruiting | Trial completion date: Aug 2031 --> Sep 2030 | Trial primary completion date: Aug 2031 --> Sep 2030
    Enrollment open • Trial completion date • Trial primary completion date • Adverse events
    |
    telisotuzumab adizutecan (ABBV-400)
    2d
    HS-20089 for Injection in Patients With Platinum-Resistant Recurrent Epithelial Ovarian Cancer (clinicaltrials.gov)
    P3, N=468, Recruiting, Hansoh BioMedical R&D Company | Not yet recruiting --> Recruiting
    Enrollment open • Platinum resistant
    |
    paclitaxel • doxorubicin hydrochloride • topotecan • mocertatug rezetecan (GSK5733584)
    2d
    A Study to Assess Adverse Events and Change in Disease Activity in Participants 12 Years of Age or Older With Locally Advanced or Metastatic Solid Tumors That Harbor MET Amplification Receiving Intravenously Infused Telisotuzumab Adizutecan (clinicaltrials.gov)
    P2, N=125, Recruiting, AbbVie | Not yet recruiting --> Recruiting
    Enrollment open • Adverse events
    |
    telisotuzumab adizutecan (ABBV-400)
    2d
    RAINFOL-05: Study to Assess the Efficacy and Safety of Rina-S in Participants With Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=240, Not yet recruiting, Genmab
    New P2 trial
    |
    Rina-S (rinatabart sesutecan)
    3d
    A Study to Investigate GSK5733584 Compared With Chemotherapy in Participants With Platinum-resistant Ovarian Cancer (BEHOLD-Ovarian01) (clinicaltrials.gov)
    P3, N=450, Not yet recruiting, GlaxoSmithKline
    New P3 trial • Platinum resistant
    |
    gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan • mocertatug rezetecan (GSK5733584)
    3d
    Stepwise DNA damage and repair mechanisms at replication forks in response to topoisomerase I inhibition. (PubMed, DNA Repair (Amst))
    Camptothecin (CPT) and its derivative irinotecan inhibit DNA topoisomerase I (TOP1), inducing replication stress by stabilizing the TOP1 cleavage complex...Furthermore, we explain some of the contrasting effects of the replication fork dynamics and DDR activation triggered by TOP1 inhibition. Finally, we identify cancer genetic vulnerabilities, such as HR deficiency, that may be exploitable with low-dose TOP1 inhibitors.
    Journal
    |
    RAD51 (RAD51 Homolog A)
    |
    irinotecan
    3d
    Sequencing antibody-drug conjugates in metastatic breast cancer: A systematic review. (PubMed, Cancer Treat Rev)
    Emerging evidence indicates that sequential ADC use can be effective despite some cross-resistance, especially when distinct payload mechanisms are employed. Clinical use should consider payload type, timing, and breast cancer subtype, but toxicities remain critical for decision-making. Research providing insights into resistance mechanisms and biomarkers is needed for personalized approaches.
    Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 negative
    |
    Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki)