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    DRUG CLASS:

    HER3-targeted antibody-drug conjugate

    Related drugs:
    7d
    A Phase I Study of AK138D1 in the Treatment of Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=100, Not yet recruiting, Akeso
    New P1 trial • Metastases
    15d
    Patritumab Deruxtecan in Patients with Solid Tumor Harboring an NRG1 Fusion (clinicaltrials.gov)
    P2, N=30, Recruiting, Samsung Medical Center | Not yet recruiting --> Recruiting
    Enrollment open • Pan tumor
    |
    patritumab deruxtecan (U3-1402)
    19d
    The Era of Antibody Drug Conjugates in Lung Cancer: Trick or Threat? (PubMed, Cancer Res Treat)
    Antibody Drug Conjugates (ADCs) are a novel class of therapeutics that structurally are composed by an antibody directed to a tumour epitope connected via a linker to a cytotoxic payload, and that have shown significant antitumor activity across a range of malignancies including lung cancer. In this article we review the pharmacology and design of ADCs, as well as we describe the results of different studies evaluating ADCs in lung cancer directed to several targets including HER2, HER3, TROP2, MET, CEACAM5 and DLL3, among others.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • CEACAM5 (CEA Cell Adhesion Molecule 5) • DLL3 (Delta Like Canonical Notch Ligand 3)
    23d
    Study of HRS-8080 or SHR-A2009 Combined With Anti-tumor Therapy in Patients With Unresectable or Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2, N=350, Recruiting, Shandong Suncadia Medicine Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    trastuzumab rezetecan (SHR-A1811) • Ariely (adebrelimab) • SHR-A2009
    27d
    PARAMETer: A Window of Opportunity Study of Patritumab Deruxtecan in Patients With Brain Metastases (clinicaltrials.gov)
    P1, N=15, Not yet recruiting, Mustafa Khasraw, MBChB, MD, FRCP, FRACP | Trial completion date: Jan 2027 --> Apr 2027 | Trial primary completion date: Jan 2025 --> Apr 2026
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    patritumab deruxtecan (U3-1402)
    1m
    A Phase 2 Study to Evaluate the Efficacy, Safety and Pharmacokinetics of YL202 in Patients With BC (clinicaltrials.gov)
    P2, N=180, Recruiting, MediLink Therapeutics (Suzhou) Co., Ltd. | Active, not recruiting --> Recruiting
    Enrollment open • Metastases
    |
    BNT326
    1m
    Study of ORM-5029 in Subjects with HER2-Expressing Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=87, Active, not recruiting, Orum Therapeutics USA, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    ORM-5029
    1m
    A Study of YL202 in Selected Patients with Advanced Solid Tumors (clinicaltrials.gov)
    P2, N=200, Recruiting, MediLink Therapeutics (Suzhou) Co., Ltd. | Active, not recruiting --> Recruiting
    Enrollment open • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    BNT326
    1m
    Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009) (clinicaltrials.gov)
    P1/2, N=81, Not yet recruiting, Merck Sharp & Dohme LLC
    New P1/2 trial
    |
    Perjeta (pertuzumab) • Tukysa (tucatinib) • patritumab deruxtecan (U3-1402) • Herzuma (trastuzumab-pkrb) • Trazimera (trastuzumab-qyyp)
    1m
    A Multicenter, Open-label, Phase II Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of YL202 in Subjects With Locally Advanced or Metastatic Breast Cancer Who Are TNBC and HR Positive, HER2 Zero, or HER2 Hypoactive (ChiCTR2400089158)
    P2, N=180, Recruiting, Fudan University Shanghai Cancer Center; Fudan University Shanghai Cancer Center
    New P2 trial • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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    HR positive • HER-2 negative • HER-2 expression • HER-2 underexpression • PGR expression • HER-2 negative + HR negative
    |
    BNT326
    1m
    A Phase I Clinical Study Evaluating the Safety, Tolerability, Pharmacokinetic Profiles, and Preliminary Efficacy of SYS6023 in Patients with Advanced Solid Tumors (ChiCTR2400089836)
    P1, N=388, Recruiting, Shanghai Chest Hospital; CSPC Megalith Biopharmaceutical Co., Ltd
    New P1 trial • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ER (Estrogen receptor) • ALK (Anaplastic lymphoma kinase) • PGR (Progesterone receptor) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • EGFR mutation • KRAS G12C • BRAF mutation • HER-2 amplification • HER-2 negative • BRAF V600 • HER-2 expression • ALK positive • MET amplification • ALK fusion • ERBB3 expression • RET mutation • ROS1 fusion • MET mutation • NRG1 fusion • RET rearrangement • KRAS G12 • KRAS amplification • ER expression • PGR expression • ALK-ROS1 fusion • NRG1 fusion • NTRK fusion
    1m
    ICARUS-BREAST01: Patritumab Deruxtecan (U3-1402) in Unresectable Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=99, Active, not recruiting, Gustave Roussy, Cancer Campus, Grand Paris | Recruiting --> Active, not recruiting | N=170 --> 99 | Trial completion date: Jun 2026 --> Apr 2028 | Trial primary completion date: Jan 2024 --> Apr 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    patritumab deruxtecan (U3-1402)
    1m
    A Study of SHR-A2009 Versus Platinum-based Chemotherapy in EGFR-mutated, Advanced or Metastatic NSCLC (clinicaltrials.gov)
    P3, N=500, Not yet recruiting, Suzhou Suncadia Biopharmaceuticals Co., Ltd.
    New P3 trial • Metastases
    |
    cisplatin • carboplatin • SHR-A2009
    1m
    HERTHENA-Lung02: A Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced EGFRm NSCLC After Failure of EGFR TKI Therapy (clinicaltrials.gov)
    P3, N=586, Active, not recruiting, Daiichi Sankyo | Trial primary completion date: Aug 2024 --> May 2024
    Trial primary completion date • Metastases
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    cisplatin • carboplatin • patritumab deruxtecan (U3-1402)
    2ms
    Characterization of patritumab deruxtecan activity in breast cancer (BC) patient-derived xenograft (PDX) models (SABCS 2024)
    The antitumor activity of HER3-DXd (10 mg/kg or 3 mg/kg dosed once weekly, 4 doses in total; Q1W x 4) was assessed in 30 BC PDX models (21 ER+/HER2- and 9 triple negative [TNBC]) and compared to the antitumor activity of the clinically approved TOP1 inhibitor irinotecan (50 mg/kg dosed once weekly; Q1W). HER3-DXd exerts a potent antitumor response in BC PDXs across baseline levels of HER3/ERBB3 expression in ER+/HER2- and TNBC models. Based on our data, basal-like PDX models were more likely to show long-term responses to HER3-DXd than luminal B PDX models. Results also suggest that BRCA1/2-altered PARPi-resistant tumors will show high benefit with HER3-DXd treatment.
    Clinical • BRCA Biomarker • PARP Biomarker
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • RB1 (RB Transcriptional Corepressor 1) • RPA2 (Replication Protein A2)
    |
    HER-2 negative • HER-2 expression • ERBB3 expression • ERBB3 overexpression
    |
    MSK-IMPACT • Prosigna™ Breast Cancer Prognostic Gene Signature Assay
    |
    irinotecan • patritumab deruxtecan (U3-1402)
    2ms
    Primary results of SOLTI VALENTINE: neoadjuvant randomized phase II trial of HER3-DXd alone or in combination with letrozole for high-risk hormone receptor positive (HR+)/HER2-negative (neg) early breast cancer (EBC). (SABCS 2024)
    Pts were randomized 2:2:1 to: (A) HER3-DXd 5.6 mg/kg every (Q) 21 days (D) for 6 cycles; (B) HER3-DXd plus QD LET (+/- LHRH agonist); (C) CT with 4 cycles of EC/AC (epirubicin 90 mg/m2 or doxorubicin 60 mg/m2 and cyclophosphamide 600 mg/m2 Q14 or 21 D) followed by weekly paclitaxel 80mg/m2 for 12 weeks. In SOLTI VALENTINE, treatment with HER3-DXd, with or without LET, resulted in similar pCR rates to CT, while exhibiting a lower incidence of grade ≥3 TEAEs. CelTIL score at C2D1 correlated with response to HER3-DXd, but not to CT. The ongoing translational analysis, as well as the survival outcomes of VALENTINE, will provide further insights into the activity of HER3-DXd in EBC and clarify its potential role as a treatment strategy for high-risk HR+/HER2-neg breast cancer.
    Clinical • P2 data • Late-breaking abstract • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    Prosigna™ Breast Cancer Prognostic Gene Signature Assay
    |
    paclitaxel • doxorubicin hydrochloride • cyclophosphamide • letrozole • epirubicin • patritumab deruxtecan (U3-1402)
    2ms
    A Study of BL-B01D1 in Patients With Recurrent Glioblastoma (clinicaltrials.gov)
    P2, N=20, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    izalontamab brengitecan (BL-B01D1)
    2ms
    A Study of BL-B01D1, SI-B003 and BL-B01D1+SI-B003 in Patients With Recurrent or Metastatic Cervical Cancer and Other Gynecological Malignancies (clinicaltrials.gov)
    P2, N=130, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=98 --> 130
    Enrollment change • Combination therapy • Metastases
    |
    HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset)
    |
    HRD • BRCA mutation
    |
    izalontamab brengitecan (BL-B01D1) • danvilostomig (SI-B003)
    2ms
    Study of Patritumab Deruxtecan in Participants With Gastrointestinal Cancers (MK-1022-011) (clinicaltrials.gov)
    P1/2, N=130, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting
    Enrollment open
    |
    patritumab deruxtecan (U3-1402)
    2ms
    A Clinical Trial of SIBP-A13 Injection in the Treatment of Advanced Malignant Solid Tumor Patients. (clinicaltrials.gov)
    P1, N=144, Recruiting, Shanghai Institute Of Biological Products | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    2ms
    BL-B01D1-204-05: A Study of BL-B01D1+PD-1 Monoclonal Antibody in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer, Nasopharyngeal Carcinoma and Other Solid Tumors (clinicaltrials.gov)
    P2, N=332, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=126 --> 332
    Enrollment change • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    2ms
    A Study of BL-B01D1 in Patients With Locally Advanced or Metastatic Urological Tumors and Other Solid Tumors (clinicaltrials.gov)
    P1, N=26, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Trial completion date: Aug 2024 --> Jun 2025 | Trial primary completion date: Aug 2024 --> Jun 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    A Study to Evaluate the Safety, Tolerability, Drug Levels, and Preliminary Efficacy of BMS-986507 Combinations in Adult Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=218, Not yet recruiting, Bristol-Myers Squibb
    New P1/2 trial
    |
    Keytruda (pembrolizumab) • Tagrisso (osimertinib) • izalontamab brengitecan (BL-B01D1)
    3ms
    A Study of SI-B003, BL-B01D1+SI-B003 and BL-B01D1+PD-1 Monoclonal Antibody in Patients With Locally Advanced or Metastatic Esophageal Cancer, Gastric Cancer, Colorectal Cancer and Other Gastrointestinal Tumors (clinicaltrials.gov)
    P2, N=376, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=268 --> 376
    Enrollment change • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 negative
    |
    izalontamab brengitecan (BL-B01D1) • danvilostomig (SI-B003)
    3ms
    BL-B01D1-204-01: A Study of BL-B01D1+PD-1 Monoclonal Antibody in Patients With Extensive-stage Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=66, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=36 --> 66
    Enrollment change
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    YL202-INT-101-01: A Study of YL202 in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer and Breast Cancer (clinicaltrials.gov)
    P1, N=80, Recruiting, MediLink Therapeutics (Suzhou) Co., Ltd. | Active, not recruiting --> Recruiting | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
    Enrollment open • Trial completion date • Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HR positive • HER-2 negative • EGFR L858R • EGFR exon 19 deletion • HR positive + HER-2 negative • PTEN mutation + HR positive
    |
    BNT326
    3ms
    A Study of BL-B01D1 in Patients With Multiple Solid Tumors, Including Locally Advanced or Metastatic Urinary System Tumors (clinicaltrials.gov)
    P2, N=76, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=32 --> 76
    Enrollment change • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    DB-1310-O-1001: A Study of DB-1310 in Advanced/Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=1000, Recruiting, DualityBio Inc. | N=287 --> 1000
    Enrollment change
    |
    ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    Herceptin (trastuzumab) • Tagrisso (osimertinib) • DB-1310
    3ms
    A Study of BL-B01D1 in Patients With Recurrent Glioblastoma (clinicaltrials.gov)
    P2, N=20, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    TUXEDO-3: HER3-DXd in Breast Cancer and NSCLC Brain Metastases and Solid Tumor Leptomeningeal Disease (clinicaltrials.gov)
    P2, N=63, Active, not recruiting, MedSIR | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
    |
    HER-2 positive • EGFR mutation • HER-2 expression • EGFR T790M • ERBB3 expression • TROP2 expression • ER expression • PGR expression
    |
    patritumab deruxtecan (U3-1402)
    3ms
    To Evaluate the Phase I Clinical Study of JSKN016 in Chinese Patients With Advanced Malignant Solid Tumors (clinicaltrials.gov)
    P1, N=140, Recruiting, Jiangsu Alphamab Biopharmaceuticals Co., Ltd
    New P1 trial • Metastases
    3ms
    A Study of BL-B01D1 in Patients With Locally Advanced or Metastatic Gastrointestinal Tumor and Other Solid Tumor (clinicaltrials.gov)
    P1, N=96, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Trial completion date: Aug 2024 --> Dec 2024 | Trial primary completion date: Aug 2024 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    Study of Patritumab Deruxtecan in Participants With Gastrointestinal Cancers (MK-1022-011) (clinicaltrials.gov)
    P1/2, N=130, Not yet recruiting, Merck Sharp & Dohme LLC
    New P1/2 trial
    |
    patritumab deruxtecan (U3-1402)
    3ms
    BL-B01D1-101: A Study of BL-B01D1 in Patients With Locally Advanced or Metastatic Solid Tumor (clinicaltrials.gov)
    P1, N=96, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Trial completion date: Aug 2024 --> Dec 2024 | Trial primary completion date: Aug 2024 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    3ms
    A Study of BL-B01D1 in Patients With Unresectable Locally Advanced or Metastatic Breast Cancer and Other Solid Tumors (clinicaltrials.gov)
    P1, N=36, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Trial completion date: Aug 2024 --> Dec 2024 | Trial primary completion date: Aug 2024 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    4ms
    U31402-A-U103: HER3-DXd (Patritumab Deruxtecan; U3-1402) in Combination With Osimertinib in Subjects With Locally Advanced or Metastatic EGFR-mutated Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=280, Active, not recruiting, Daiichi Sankyo | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy • Metastases
    |
    Tagrisso (osimertinib) • patritumab deruxtecan (U3-1402)
    4ms
    A Study of BL-B01D1+PD-1 Monoclonal Antibody in Patients With Unresectable Locally Advanced or Recurrent Metastatic Triple-negative Breast Cancer (clinicaltrials.gov)
    P2, N=52, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    4ms
    BL-B01D1-304: A Study Comparing BL-B01D1 With Topotecan in Patients With Recurrent Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=652, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    topotecan • izalontamab brengitecan (BL-B01D1)
    4ms
    BL-B01D1-204-02: A Study of BL-B01D1+PD-1 Monoclonal Antibody in Patients With Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma and Other Solid Tumors (clinicaltrials.gov)
    P2, N=52, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    4ms
    HERTHENA-Lung01: Patritumab Deruxtecan in Subjects With Metastatic or Locally Advanced EGFR-mutated Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=277, Active, not recruiting, Daiichi Sankyo | Trial completion date: Nov 2024 --> Jan 2026
    Trial completion date • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    patritumab deruxtecan (U3-1402)
    4ms
    A Study of BL-B01D1 in Combination With Osimertinib Mesylate Tablets in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=40, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    Tagrisso (osimertinib) • izalontamab brengitecan (BL-B01D1)
    4ms
    A Study of BL-B01D1 and BL-B01D1 in Combination With Osimertinib Mesylate Tablets in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=114, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=42 --> 114
    Enrollment change • Combination therapy • Metastases
    |
    EGFR (Epidermal growth factor receptor)
    |
    Tagrisso (osimertinib) • izalontamab brengitecan (BL-B01D1)