OQY-3258 / Escugen Biotechnology, Sorrento, Oqory - LARVOL DELTA

Updated Efficacy of anti-TROP2 ADC ESG401 for first-line metastatic TNBC (ESMO 2025) - P1/2 | "Conclusions ESG401 monotherapy demonstrated promising antitumor activity in 1L mTNBC pts, with a high response rate and potential for prolonged PFS compared with standard chemotherapy. These findings support further clinical development."

Clinical • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Triple Negative Breast Cancer • PD-L1

A Phase III Study of ESG401 for Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer (clinicaltrials.gov) - P3 | N=504 | Recruiting | Sponsor: Qilu Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

ESG401-101: Study of ESG401 in Adults With Solid Tumors (clinicaltrials.gov) - P1/2 | N=156 | Completed | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | Recruiting ➔ Completed | Trial completion date: Dec 2025 ➔ Jun 2025 | Trial primary completion date: Oct 2025 ➔ Jun 2025

Trial completion • Trial completion date • Trial primary completion date • Bladder Cancer • Breast Cancer • Colorectal Cancer • Gastric Cancer • Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor

A Phase III Study of ESG401 for Locally Advanced or Metastatic HR+/HER2- Breast Cancer (clinicaltrials.gov) - P3 | N=378 | Recruiting | Sponsor: Qilu Pharmaceutical Co., Ltd. | Trial completion date: Dec 2026 ➔ Jul 2028 | Trial primary completion date: Jul 2026 ➔ Jun 2027

Trial completion date • Trial primary completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

Comprehensive results of ESG401, a TROP2-targeting ADC: Updated phase 1 analysis in advanced solid tumors. (ASCO 2025) - P1/2 | "ESG401 demonstrated favorable safety and efficacy benefits due to its enhanced linker, showing good safety and promising antitumor activity in advanced solid tumors across settings. These results warrant further clinical investigation. aThe actual value for these two patients is listed."

Metastases • P1 data • Adenoid Cystic Carcinoma • Anemia • Endometrial Cancer • Leukopenia • Neutropenia • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

Anti-TROP2 ADC ESG401 in a master protocol clinical trial for salivary gland cancer based on molecular typing. (ASCO 2025) - P2 | "ESG401 demonstrated promising efficacy in Trop2-positive SGC, providing a rationale for molecular subtype-based targeted therapy in this population and warranting further investigation in larger studies."

Clinical • Adenoid Cystic Carcinoma • Oncology • Salivary Gland Cancer • HER-2 • NTRK

A Phase III Study of ESG401 for Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer (clinicaltrials.gov) - P3 | N=504 | Not yet recruiting | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | Initiation date: Feb 2025 ➔ Sep 2025

Trial initiation date • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

ESG401-101: Study of ESG401 in Adults With Solid Tumors (clinicaltrials.gov) - P1/2 | N=177 | Recruiting | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | Trial completion date: Apr 2025 ➔ Dec 2025 | Trial primary completion date: Feb 2025 ➔ Oct 2025

Trial completion date • Trial primary completion date • Bladder Cancer • Breast Cancer • Colorectal Cancer • Gastric Cancer • Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor

Novel TROP2 antibody-drug conjugates for treatment of HER2-negative metastatic breast cancer patients with brain metastases: a promising option☆. (PubMed, ESMO Open) - P1/2 | "These findings suggest that ESG401 is a promising and well-tolerated treatment option for BMs."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Vincerx Pharma, Inc. and Oqory, Inc. Highlight Promising Data for Oqory’s TROP2 Antibody Drug Conjugate, OQY-3258 (GlobeNewswire) - P1a/1b | N=177 | NCT04892342 | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | "As of August 2024, the Phase 1a/1b study had enrolled approximately 150 patients...A recent data cut from January 2025, with ten additional patients (n=35) evaluable for efficacy, showed an improved confirmed ORR of 80%, with median DOR and PFS still not reached...Additionally, in patients with brain metastases, PFS (95% confidence interval) was 4.6 (2.0-9.8) months with OQY-3258 compared with 2.8 (1.5-3.9) months for historical data with Trodelvy. OQY-3258 has demonstrated a favorable safety profile, with the most common Grade ≥3 adverse events being manageable hematologic toxicities, such as neutropenia and leukopenia, that did not lead to treatment discontinuation. Notably, no Grade ≥3 rash or interstitial lung disease/pneumonitis was observed..."

P1 data • Breast Cancer • Solid Tumor • Triple Negative Breast Cancer

About Proposed Merger (GlobeNewswire) - "'With its optimized serum-stable linker design, OQY-3258 has shown a markedly lower incidence of severe off-target toxicity compared with other marketed TROP2 therapies, positioning it as a differentiated late-stage ADC for metastatic breast cancer and other TROP2-expressing cancers. Our proposed merger with Vincerx represents a pivotal step toward advancing this asset into global Phase 3 trials and driving innovation in next-generation ADCs.'...Vincerx and Oqory are parties to a binding term sheet, as amended, pursuant to which Oqory would merge into Vincerx, with Oqory equity holders expected to own approximately 95% of the combined entity and Vincerx equity holders expected to hold approximately 5%. The proposed merger provides for a minimum fully diluted equity value of $13.66 million for existing Vincerx stockholders at closing and, as a condition to the closing of the merger, completion of a concurrent private offering of Vincerx equity securities of at least $20 million."

M&A • Breast Cancer • Solid Tumor • Triple Negative Breast Cancer

Precision Treatment of Recurrent/Metastatic Salivary Gland Carcinoma Guided by Molecular Typing (clinicaltrials.gov) - P2 | N=10 | Recruiting | Sponsor: Peking Union Medical College | N=30 ➔ 10

Enrollment change • Metastases • Oncology • Salivary Gland Cancer

Case report: Prolonged benefit of ESG401, a Trop2 antibody-drug conjugate, in endocrine-refractory hormone receptor-positive, HER-2 negative metastatic breast cancer. (PubMed, Front Oncol) - "We report a case of a 61-year-old female with HR+HER2- metastatic breast cancer (MBC) who developed resistance to fulvestrant and subsequent chemotherapy but achieved a durable partial response (PR) lasting more than 22.5 months following ESG401 treatment. Furthermore, the patient's exceptionally long clinical benefit distinguishes her from other patients receiving ESG401 treatment. Further exploration of the use of ESG401 in HR+HER2- MBC patients, as well as a deeper understanding of the characteristics of patients that may impact sustained efficacy, in expanded clinical trials is warranted."

Journal • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

A Phase III Study of ESG401 for Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer (clinicaltrials.gov) - P3 | N=504 | Not yet recruiting | Sponsor: Shanghai Escugen Biotechnology Co., Ltd

Metastases • New P3 trial • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Pharmaceutical Valley News | Shijian Biopharma’s ESG401 was included in the Breakthrough Therapy category by CDE [Google translation] (bydrug.pharmcube.com) - "On November 2, the official website of the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) announced that Shijian Bio's core product ESG401 (recombinant humanized anti-Trop2 monoclonal antibody-SN38 conjugate) was included in the breakthrough therapy category , with the proposed indication being inoperable locally advanced, recurrent or metastatic PD-L1-negative triple-negative breast cancer (TNBC) that has not been previously treated with systemic therapy."

Breakthrough therapy • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Results from a phase Ia/Ib Study of ESG401, a novel Trop2 antibody-drug conjugate, in patients with different subtypes of metastatic breast cancer (ESMO 2024) - P1/2 | "ESG401 demonstrates promising and durable therapeutic efficacy in various subtypes of mBC. Despite the limited sample size, there was no significant difference in efficacy observed among the three types of late-line and heavily treated BC patients. These findings warrant further clinical evaluation."

Clinical • Metastases • P1 data • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

ESG401, a novel Trop2 antibody-drug conjugate (ADC), and its efficacy evidence in HER2-negative metastatic breast cancer with brain metastases (ESMO 2024) - P1/2 | "ESG401 demonstrates encouraging therapeutic efficacy in both heavily pretreated and first-line HER2-negative mBC-BMs pts, with responses in brain metastatic and systemic lesions being consistent. These findings warrant further clinical evaluation."

Clinical • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

Phase 1a study of ESG401, a Trop2 antibody-drug conjugate, in patients with locally advanced/metastatic solid tumors. (PubMed, Cell Rep Med) - P1/2 | "ESG401 demonstrates a favorable safety profile and promising antitumor activity in this heavily treated population. The trial is registered at ClinicalTrials.gov (NCT04892342)."

Journal • Metastases • P1 data • Breast Cancer • Hematological Disorders • Leukopenia • Neutropenia • Oncology • Solid Tumor

Updated efficacy of anti-TROP2 ADC ESG401 for first-line metastatic TNBC in phase 1b study. (ASCOBT 2024) - P1/2 | "ESG401 monotherapy demonstrates promising antitumor activity in 1L mTNBC pts, characterized by a high response rate and durable response. The ORR numerically exceeded that reported in the BEGONIA Study arm 7 in which pts with the same indication were treated with TROP-2 ADC and PD-L1 combination therapy. Additionally, ESG401 shows clear potential for treating HER2-negative breast cancer with brain metastases, including mTNBC and HR+/HER2- BC."

Clinical • Metastases • P1 data • CNS Disorders • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Triple Negative Breast Cancer • HER-2

A Phase III Study of ESG401 for Locally Advanced or Metastatic HR+/HER2- Breast Cancer (clinicaltrials.gov) - P3 | N=378 | Recruiting | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor

ESG401, a trophoblast cell-surface antigen 2 (TROP2) antibody drug conjugate (ADC), for the treatment of first-line metastatic triple negative breast cancer (mTNBC). (ASCO 2024) - P1/2 | "ESG401 demonstrates promising antitumor activity in the first-line mTNBC pts, with efficacy comparable to the combination therapy reported by the BEGONIA Study. Additionally, the efficacy of ESG401 in brain metas in the first-line mTNBC pts is in alignment with our previous observations made in the late-line mTNBC and HR+/HER2- BC pts. These results warrant further clinical investigation of ESG401."

Clinical • Metastases • Anemia • Breast Cancer • CNS Disorders • Fatigue • Hematological Disorders • Interstitial Lung Disease • Leukopenia • Neutropenia • Oncology • Pulmonary Disease • Respiratory Diseases • Solid Tumor • Triple Negative Breast Cancer • HER-2

Sijian Biologics Announces Positive Phase I Clinical Trial Data of Trop 2 ADC “ESG401“ (min.news) - P1/2 | N=177 | NCT04892342 | Sponsor: Shanghai Escugen Biotechnology Co., Ltd | "The study enrolled 35 patients, including 1 patient with endometrial cancer, 16 patients with triple-negative breast cancer, 16 patients with HR+/HER2- breast cancer and 2 patients with HR-/HER2+ breast cancer...The incidence rate of study drug-related adverse events (TRAEs) was 94.3% (33/35), and the incidence rate of grade 3 and above TRAEs was 34.3% (12/35)...The incidence of SAEs related to the study drug was 5.7% (2/35)...Among the 33 subjects whose efficacy could be evaluated, 12 subjects achieved PR, the objective response rate (ORR) was 36.4%, and 9 subjects achieved SD...DCR is 63.6%."

P1 data • Breast Cancer • Endometrial Cancer • Gynecologic Cancers • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

A Phase III Study of ESG401 for Locally Advanced or Metastatic HR+/HER2- Breast Cancer (clinicaltrials.gov) - P3 | N=378 | Not yet recruiting | Sponsor: Shanghai Escugen Biotechnology Co., Ltd

Metastases • New P3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor

No. 3: Shijian Biotech’s TROP2 ADC launches Phase III clinical trial [Google translation] (163.com) - "On April 25, the Clinicaltrials website showed that the TROP2 ADC (ESG401) developed by Shijian Biotech launched Phase III clinical trials, becoming the third domestically produced TROP2 ADC to enter the Phase III stage....The study is a multi-center, randomized, open-label phase III clinical trial that intends to enroll 378 patients with unresectable locally advanced or metastatic HR+/HER2- breast cancer who have received at least one prior chemotherapy treatment to evaluate ESG401 To compare the safety and effectiveness of physician choice (TPC) in this population of patients. The primary endpoint of the study is progression-free survival (PFS) at 24 months."

Trial status • Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

Precision Treatment of Recurrent/Metastatic Salivary Gland Carcinoma Guided by Molecular Typing (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Peking Union Medical College | Initiation date: Dec 2023 ➔ May 2024

Metastases • Trial initiation date • Oncology • Salivary Gland Cancer