^
    20d
    Antibody-Drug Conjugates Targeting the EGFR Ligand Epiregulin Elicit Robust Anti-Tumor Activity in Colorectal Cancer. (PubMed, bioRxiv)
    While the efficacy of clinically approved anti-EGFR mAbs are largely limited by RAS mutational status, EREG ADCs may show promise for both RAS mutant and wildtype patients, thus improving existing treatment options. Significance: EREG-targeting antibody-drug conjugates demonstrate acceptable safety and robust therapeutic efficacy in RAS mutant and wildtype colorectal cancer, suggesting their potential as an alternative to EGFR-targeted therapy to benefit a broader patient population.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • EREG (Epiregulin)
    |
    RAS mutation • RAS wild-type
    22d
    A Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK), and Antitumor Activity of ALK202 in Participants with Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=234, Not yet recruiting, Shanghai Allink Biotherapeutics Co., Ltd.
    New P1 trial • Metastases
    22d
    Trial to Assess the Safety, Tolerability, Pharmacokinetics (PK) and Antitumor Activity of GEN1286 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=214, Recruiting, Genmab | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    24d
    IBI3001 in Participants With Unresectable, Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=250, Recruiting, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Recruiting | Phase classification: P1/2 --> P1 | N=180 --> 250 | Trial completion date: May 2027 --> Dec 2027 | Initiation date: May 2024 --> Dec 2024 | Trial primary completion date: May 2026 --> Dec 2026
    Enrollment open • Phase classification • Enrollment change • Trial completion date • Trial initiation date • Trial primary completion date • Metastases
    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
    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
    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
    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
    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
    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
    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
    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
    Study of Intravenous (IV) ABBV-637 Alone or in Combination With IV Docetaxel/Osimertinib to Assess Adverse Events and Change in Disease Activity in Adult Participants With Relapsed/Refractory (R/R) Solid Tumors (clinicaltrials.gov)
    P1, N=81, Active, not recruiting, AbbVie | Trial completion date: Aug 2024 --> Feb 2025 | Trial primary completion date: Aug 2024 --> Feb 2025
    Trial completion date • Trial primary completion date • Adverse events • Combination therapy
    |
    Tagrisso (osimertinib) • docetaxel • ABBV-637
    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)
    5ms
    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=36, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting | N=60 --> 36
    Enrollment open • Enrollment change
    |
    izalontamab brengitecan (BL-B01D1)
    5ms
    A Study of DM005 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=136, Not yet recruiting, Doma Biopharmaceutical（Suzhou）Co., Ltd.
    New P1 trial • Metastases
    |
    DM005
    5ms
    Study to Evaluate BL-B01D1 in Patients With Metastatic or Unresectable Non-Small Cell Lung Cancer (NSCLC) and Other Solid Tumors (clinicaltrials.gov)
    P1, N=260, Recruiting, SystImmune Inc. | Trial completion date: Sep 2025 --> Mar 2028 | Trial primary completion date: Jul 2024 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    5ms
    A Study Comparing BL-B01D1 With Topotecan in Patients With Recurrent Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=652, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P3 trial
    |
    topotecan • izalontamab brengitecan (BL-B01D1)
    5ms
    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, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial • Combination therapy • Metastases
    |
    Tagrisso (osimertinib) • izalontamab brengitecan (BL-B01D1)
    5ms
    BL-B01D1-204-03: A Study of BL-B01D1 + PD-1 in Patients With Locally Advanced or Metastatic Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=52, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    6ms
    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=126, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    6ms
    A Study Comparing BL-B01D1 With Chemotherapy of Physician's Choice in Patients With Unresectable Locally Advanced or Metastatic Triple-Negative Breast Cancer (clinicaltrials.gov)
    P3, N=436, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    gemcitabine • capecitabine • Halaven (eribulin mesylate) • vinorelbine tartrate • izalontamab brengitecan (BL-B01D1)
    6ms
    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=268, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | N=190 --> 268
    Enrollment change • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    izalontamab brengitecan (BL-B01D1) • danvilostomig (SI-B003)
    6ms
    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=126, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    6ms
    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, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial • Combination therapy • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    6ms
    Safety, Efficacy, and Pharmacokinetics of SHR-A1811, a Human Epidermal Growth Factor Receptor 2-Directed Antibody-Drug Conjugate, in Human Epidermal Growth Factor Receptor 2-Expressing or Mutated Advanced Solid Tumors: A Global Phase I Trial. (PubMed, J Clin Oncol)
    SHR-A1811 exhibited acceptable tolerability, promising antitumor activity, and a favorable pharmacokinetic profile in heavily pretreated advanced solid tumors. The recommended phase II dose of 4.8 or 6.4 mg/kg was selected for various tumor types.
    P1 data • PK/PD data • Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Herceptin (trastuzumab) • trastuzumab rezetecan (SHR-A1811)
    6ms
    Study of Intravenous (IV) ABBV-637 Alone or in Combination With IV Docetaxel/Osimertinib to Assess Adverse Events and Change in Disease Activity in Adult Participants With Relapsed/Refractory (R/R) Solid Tumors (clinicaltrials.gov)
    P1, N=81, Active, not recruiting, AbbVie | Trial completion date: Feb 2024 --> Aug 2024 | Trial primary completion date: Feb 2024 --> Aug 2024
    Trial completion date • Trial primary completion date • Adverse events • Combination therapy
    |
    Tagrisso (osimertinib) • docetaxel • ABBV-637
    7ms
    A Study Comparing BL-B01D1 With Docetaxel in Patients With Unresectable Locally Advanced or Metastatic EGFR Wild-type Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=558, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    docetaxel • izalontamab brengitecan (BL-B01D1)
    7ms
    A Study of BL-B01D1+PD-1 Monoclonal Antibody in Patients With Extensive-stage Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=60, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial
    |
    izalontamab brengitecan (BL-B01D1)
    7ms
    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, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial • Metastases
    |
    izalontamab brengitecan (BL-B01D1)
    7ms
    A Study Comparing BL-B01D1 With Platinum Based Chemotherapy in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=428, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    cisplatin • carboplatin • pemetrexed • izalontamab brengitecan (BL-B01D1)
    7ms
    A Study Comparing BL-B01D1 With Chemotherapy of Physician's Choice in Patients With Unresectable Locally Advanced, Recurrent, or Metastatic HR+HER2- Breast Cancer (clinicaltrials.gov)
    P3, N=382, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    gemcitabine • capecitabine • Halaven (eribulin mesylate) • vinorelbine tartrate • izalontamab brengitecan (BL-B01D1)
    7ms
    Bystander effects, pharmacokinetics, and linker-payload stability of EGFR-targeting antibody-drug conjugates Losatuxizumab vedotin and Depatux-M in glioblastoma models. (PubMed, Clin Cancer Res)
    EGFR-targeting ADCs are promising therapeutic options for GBM when delivered intra-tumorally by CED. However, the linker and payload for the ADC must be carefully considered to maximize the therapeutic window.
    PK/PD data • Journal
    |
    CD68 (CD68 Molecule)
    |
    EGFR amplification
    |
    depatuxizumab mafodotin (ABT-414) • losatuxizumab vedotin (ABBV-221)
    7ms
    A Study of BL-B01D1 + PD-1 in Patients With Locally Advanced or Metastatic Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=52, Not yet recruiting, Sichuan Baili Pharmaceutical Co., Ltd.
    New P2 trial • Combination therapy • Metastases
    |
    izalontamab brengitecan (BL-B01D1)