risvutatug rezetecan (GSK5764227) / Jiangsu Hansoh Pharma, GSK - LARVOL DELTA

ARTEMIS-002: A phase II study of HS-20093 in patients with relapsed or refractory sarcomas (ESMO 2025) - P2 | "Table: 2684O Efficacy Osteosarcoma (39 Adults and 5 adolescents) Other Sarcomas 8.0 mg/kg (N=15) 12.0 mg/kg (N=29) 12.0 mg/kg (N=20) ORR, % 6.7 17.2 25.0 DCR, % 66.7 86.2 85.0 mDoR, months NA NA 5.7 mPFS, months 4.0 8.4 8.2 6 months PFS, % 33.3 59.7 62.3 Median F/U, months 16.4 10.8 15.4 * Cut-off date: 3 March, 2025; ORR=Objective response rate; DCR=Disease control rate; F/U=Follow-up; mDoR=Median duration of response; mPFS=Median progression-free survival; mOS=Median overall survival; NA=Not available. Conclusions HS-20093 demonstrated promising emerging efficacy with manageable safety profile in heavily pretreated R/R sarcomas pts, supporting further clinical development."

Clinical • P2 data • Oncology • Osteosarcoma • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

HS-20093, a B7-H3-targeted antibody-drug conjugate in lung cancer: Results from the ARTEMIS-001 phase 1a/b trial. (PubMed, Cancer Cell) - P1 | "Among response-evaluable patients, the confirmed objective response rate was 52.3% (95% CI: 39.5, 64.9) for extensive-stage SCLC (ES-SCLC, N = 65) and 22.4% (95% CI: 16.0, 29.8) for non-small cell lung cancer (NSCLC, N = 152) patients, with comparable rates between 8.0 mg/kg and 10.0 mg/kg dose cohorts across both groups. These results support further development of HS-20093, with 8.0 mg/kg selected for phase 3 trials."

Journal • P1 data • Hematological Disorders • Interstitial Lung Disease • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pulmonary Disease • Respiratory Diseases • Small Cell Lung Cancer • Solid Tumor

First-Time-in-Human Study of GSK4381562 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=152 | Active, not recruiting | Sponsor: GlaxoSmithKline | Recruiting ➔ Active, not recruiting

Enrollment closed • Monotherapy • Breast Cancer • Colorectal Cancer • Endometrial Cancer • Gastric Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck

GSK plc…announced today that risvutatug rezetecan, its B7-H3-targeted antibody-drug conjugate, received Orphan Drug Designation from Japan’s Ministry of Health, Labour and Welfare for the treatment of small-cell lung cancer. (Investing.com) - "The designation was supported by preliminary clinical data from the phase I ARTEMIS-001 trial showing responses in patients with extensive-stage small-cell lung cancer who were treated with the drug, according to a company press release statement."

Orphan drug • Small Cell Lung Cancer

Combination of risvutatug rezetecan and adebrelimab in previously treated advanced nsq-NSCLC without actionable genomic alterations: Results from ARTEMIS-101, a phase 1 study (AACR 2026) - "Abstract is embargoed at this time."

Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Non-clinical characterization of GSK5764227, a novel B7-H3-directed antibody-drug conjugate (ADC) (AACR 2026) - "Importantly, the strong antitumor activity in SCLC models align with early phase clinical data (ARTEMIS-001), where GSK5764227 demonstrated >60% ORR in extensive stage SCLC patients [Wang, 2025]. Collectively, these non-clinical observations, in tandem with emerging clinical data, support GSK5764227 as a promising cancer therapy and its rapidly progressing global clinical development."

ADC • Clinical • Bladder Cancer • Genito-urinary Cancer • Hematological Malignancies • Lung Cancer • Oncology • Osteosarcoma • Sarcoma • Small Cell Lung Cancer • Solid Tumor • CD276 • TOP1

Studying the mechanism of action and bystander effect of the GSK5764227 antibody-drug conjugate in patient-derived cancer organoids (AACR 2026) - "Altogether, this work characterises how GSK5764227 induces cell cycle arrest and tumour apoptosis directly in B7-H3 positive cells and indirectly in neighbouring B7-H3 negative cells via bystander effect. Combining clinical, molecular and imaging data, this study enhances our understanding of the drug's mechanism of action and provides a foundation for optimising its use in difficult-to-treat-cancers, ultimately guiding personalised therapeutic strategies for patients."

ADC • Clinical • Oncology • CD276 • TOP1

Exploring both targeted and untargeted (bystander) effects of GSK5764227 antibody‑drug conjugate in patient‑derived tumor explants (PDEs) (AACR 2026) - "Our results potentially aid in mechanistic understanding of the inter-play between ADC binding and payload deposition, bystander effect and heterogeneity of tumor response, which will support the future design of clinical trials with GSK5764227."

ADC • Clinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CAFs • CASP3 • CD276 • CD68 • TOP1

B7-H3 targeting ADC GSK5764227 demonstrates broad and varied anti-tumor activity across solid tumor translational models (AACR 2026) - "These findings underscore the promise of B7-H3 targeting ADCs with topoisomerase payloads for treating a broad range of cancers, while highlighting the need for further exploration of patient population and/or predictive biomarkers to elucidate determinants of response. Together, this work supports GSK5764227 ongoing clinical development as an innovative therapeutic strategy to address unmet patient needs."

ADC • Gastric Cancer • Oncology • Solid Tumor • TOP1

ARTEMIS-003: A phase 2 study of HS-20093 (GSK5764227) in patients with metastatic castration-resistant prostate cancer (mCRPC). (ASCO-GU 2026) - P2 | "HS-20093 monotherapy showed encouraging anti-tumor activity and was generally well-tolerated with a manageable safety profile in pts with mCRPC. Efficacy. *Patients had target lesion at baseline."

Clinical • Metastases • P2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

223674: Phase 3, Multicenter, Randomized, Open-label Clinical Study of GSK5764227, a B7-H3 Antibody Drug Conjugate (ADC), compared with Topotecan in Participants with Relapsed Small Cell Lung Cancer (SCLC) (clinicaltrialsregister.eu) - P2/3 | N=161 | Recruiting | Sponsor: Glaxosmithkline Research & Development Limited

New P2/3 trial • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • PD-L1

300148: A Phase 1b/2 study of GSK5764227 in combination with Standard of Care (SoC) or other agents in participants with advanced solid tumors (clinicaltrialsregister.eu) - P1/2 | N=15 | Recruiting | Sponsor: Glaxosmithkline Research & Development Limited

New P1/2 trial • Colon Adenocarcinoma • Colon Cancer • Oncology • Solid Tumor • BRAF • CD276 • HER-2 • KRAS • MSI

223054: A Phase 1 study of GSK5764227 in participants with advanced solid tumors (clinicaltrialsregister.eu) - P1 | N=152 | Recruiting | Sponsor: Glaxosmithkline Research & Development Limited | N=112 ➔ 152

Enrollment change • Oncology • Solid Tumor

A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer (clinicaltrials.gov) - P2 | N=218 | Recruiting | Sponsor: Jiangsu HengRui Medicine Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

HS-20093 in Patients With Advanced Gastric and Gastroesophageal Junction Adenocarcinoma (clinicaltrials.gov) - P1 | N=40 | Recruiting | Sponsor: Hansoh BioMedical R&D Company

New P1 trial • Esophageal Cancer • Gastric Cancer • Gastroesophageal Junction Adenocarcinoma • Oncology • Solid Tumor

A Phase III Study of HS-20093 Injection Combined With Adebrelimab Versus Docetaxel in Previously Treated Patients With Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer Without Actionable Genomic Alterations (clinicaltrials.gov) - P3 | N=450 | Not yet recruiting | Sponsor: Hansoh BioMedical R&D Company

New P3 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

223675: Evaluation of efficacy and safety of GSK5764227 (alone and in combination) in participants with previously treated advanced unresectable or metastatic gastrointestinal solid tumors (clinicaltrialsregister.eu) - P1/2 | N=176 | Recruiting | Sponsor: Glaxosmithkline Research & Development Limited

New P1/2 trial • Colon Adenocarcinoma • Colon Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

A Study of GSK5764227 in Participants With Relapsed Small Cell Lung Cancer (SCLC) (clinicaltrials.gov) - P3 | N=420 | Recruiting | Sponsor: GlaxoSmithKline | N=300 ➔ 420

Enrollment change • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor

Cancer Cell Publishes Phase 1 Lung Cancer Results of Risvutatug Rezetecan (Hansoh Pharma Press Release) - "ARTEMIS-001 evaluated the safety, pharmacokinetics, and antitumor activity of risvutatug rezetecan in 306 patients with previously treated advanced solid tumors, including 259 patients with lung cancer.... In ES-SCLC (N=65), the cORR was 52.3% in a population in which approximately 60% had received ≥2 prior lines of therapy; median duration of response (DoR) was 7.1 months, median progression-free survival (PFS) was 6.2 months and median overall survival (OS) was 13.0 months. In NSCLC (N=152), the cORR was 22.4%, with over 60% having received ≥2 prior lines of systemic therapy; median DoR was 9.7 months, median PFS was 5.5 months and median OS was 13.7 months."

P1 data • Non Small Cell Lung Cancer • Small Cell Lung Cancer

ASCO GU 2026 | Hansoh Pharma Presented Phase 2 Data of Risvutatug Rezetecan in Metastatic Castration-Resistant Prostate Cancer (Hansoh Pharma Press Release) - "Risvutatug Rezetecan demonstrated encouraging antitumor activity in both taxane-pretreated and taxane-naïve patients with metastatic castration-resistant prostate cancer (mCRPC). In taxane-pretreated patients, the cORR was 38.9%, with a cPSA50 response rate of 40.7%. Among taxane-naïve patients, the uORR was 41.7% and uPSA50 rate 23.8%; enrollment in this cohort remains ongoing as of the data cutoff date, with updated results pending....The safety profile is in line with previous reports in other solid tumors."

P2 data • Castration-Resistant Prostate Cancer

A Phase 0/1 Clinical Trial With an Expansion Phase of GSK5764227, a B7-H3-Targeted Antibody-Drug Conjugate (ADC), in Patients With Recurrent Grade 4 Glioma and Patients With Brain Metastases (clinicaltrials.gov) - P1 | N=15 | Recruiting | Sponsor: Nader Sanai | Not yet recruiting ➔ Recruiting

Enrollment open • Brain Cancer • Glioblastoma • Glioma • Oncology • Solid Tumor

A Study of GSK5764227 in Participants With Relapsed Small Cell Lung Cancer (SCLC) (clinicaltrials.gov) - P3 | N=300 | Recruiting | Sponsor: GlaxoSmithKline | Trial completion date: Sep 2028 ➔ Sep 2029 | Trial primary completion date: Sep 2026 ➔ Oct 2027

Trial completion date • Trial primary completion date • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor

R&D momentum further strengthens growth prospects: (GSK Press Release) - "Further pipeline acceleration expected in 2026:...Pivotal readouts: Jemperli (rectal cancer)....10 pivotal trial starts, including for ADCs B7-H3 (ris-rez) & B7-H4 (mocertatug rezetecan, mo-rez) to treat multiple cancer types."

Clinical data • New trial • Rectal Cancer

Jiangsu Hengrui Pharmaceuticals…announced that SHR‑7877 has received National Medical Products Administration (NMPA) approval to enter clinical trials in combination with HS‑20093 (with or without adebelisib) for the treatment of extensive‑stage small cell lung cancer (SCLC) (flcube.com) - "Next Steps: Phase I/II trial initiation expected Q2 2026; data may support breakthrough therapy designation and expedited NMPA review."

New P1/2 trial • Small Cell Lung Cancer

BeeHive: A Comprehensive Multiomic Biomarker Evaluation Across Two Single-arm Cohorts to Elucidate Mechanisms of Response and Resistance in Recurrent/Metastatic (R/M) Head and Neck Squamous Cell Carcinoma (HNSCC) (clinicaltrials.gov) - P2 | N=30 | Not yet recruiting | Sponsor: University Health Network, Toronto

Biomarker • IO biomarker • Monotherapy • New P2 trial • Head and Neck Cancer • Oncology • Oropharyngeal Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck