cobolimab (TSR-022) / AnaptysBio, GSK - LARVOL DELTA

Randomized phase II study of neoadjuvant (neoadj) anti-PD-1 dostarlimab (D) vs. D + anti-TIM-3 cobolimab (C) in high-risk resectable melanoma (mel) (NEO-MEL-T): Primary analysis. (ASCO 2025) - P2 | "Neoadj D+C was safe and efficacious. The 1-year EFS of 92% in Arm B was significantly improved relative to adjuvant anti-PD-1, and this combination warrants further investigation. Clinical trial information: NCT04139902."

Clinical • Late-breaking abstract • P2 data • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HAVCR2

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=475 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Oct 2024 ➔ Jul 2025 | Trial primary completion date: Oct 2023 ➔ Dec 2024

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Phase 1 trial of TIM-3 inhibitor cobolimab monotherapy and in combination with PD-1 inhibitors nivolumab or dostarlimab (AMBER). (ASCO 2022) - P1 | "Funded by: Pharmaceutical/Biotech Company. Cobolimab + dostarlimab was well tolerated and showed preliminary anti-tumor activity, warranting further investigation of the RP2D + docetaxel in a randomized, phase 2 study. Funding: GSK (213348)."

Combination therapy • Monotherapy • P1 data • Fatigue • Lung Cancer • Melanoma • Mesothelioma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HAVCR2

COSTAR Lung: Efficacy Comparison of Cobolimab + Dostarlimab + Docetaxel to Dostarlimab + Docetaxel to Docetaxel Alone in Participants With Advanced Non-small Cell Lung Cancer Who Have Progressed on Prior Anti-PD-(L)1 Therapy and Chemotherapy (clinicaltrials.gov) - P2/3 | N=758 | Active, not recruiting | Sponsor: GlaxoSmithKline | Phase classification: P3 ➔ P2/3

Phase classification • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=475 | Recruiting | Sponsor: GlaxoSmithKline

Metastases • New P1 trial • Hepatocellular Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=475 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Jul 2025 ➔ Apr 2027 | Trial primary completion date: Dec 2024 ➔ Apr 2025

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=369 | Recruiting | Sponsor: Tesaro, Inc. | N=873 ➔ 369 | Trial completion date: Jun 2022 ➔ Jul 2023

Enrollment change • First-in-human • Trial completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=369 | Recruiting | Sponsor: Tesaro, Inc. | Trial primary completion date: Jul 2021 ➔ Apr 2022

First-in-human • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=369 | Recruiting | Sponsor: Tesaro, Inc. | Trial primary completion date: Apr 2022 ➔ Jul 2021

First-in-human • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=369 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Oct 2023 ➔ Jun 2024 | Trial primary completion date: Oct 2021 ➔ Jun 2023

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=369 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Jun 2024 ➔ Oct 2024 | Trial primary completion date: Jun 2023 ➔ Oct 2023

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=819 | Recruiting | Sponsor: Tesaro, Inc. | N=627 ➔ 819 | Trial completion date: Jun 2020 ➔ Jun 2022 | Trial primary completion date: Dec 2019 ➔ Dec 2020

Enrollment change • First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=819 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Jun 2022 ➔ Jun 2020 | Trial primary completion date: Dec 2020 ➔ Dec 2019

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=873 | Recruiting | Sponsor: Tesaro, Inc. | Trial completion date: Jun 2020 ➔ Jun 2022 | Trial primary completion date: Dec 2019 ➔ Jun 2021

First-in-human • Trial completion date • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TSR-022 (Anti-TIM-3 Antibody) and TSR-042 (Anti-PD-1 Antibody) in Patients With Liver Cancer (clinicaltrials.gov) - P2 | N=42 | Active, not recruiting | Sponsor: University of Hawaii | Trial primary completion date: Oct 2025 ➔ Mar 2026

Trial primary completion date • Hepatocellular Cancer • Liver Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=402 | Not yet recruiting | Sponsor: Tesaro, Inc.

First-in-human • New P1 trial • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=402 | Recruiting | Sponsor: Tesaro, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • First-in-human • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=463 | Active, not recruiting | Sponsor: Tesaro, Inc. | Recruiting ➔ Active, not recruiting | Trial primary completion date: Apr 2025 ➔ Mar 2027

Enrollment closed • First-in-human • Trial primary completion date • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study of TSR-022 in Participants With Advanced Solid Tumors (AMBER) (clinicaltrials.gov) - P1 | N=627 | Recruiting | Sponsor: Tesaro, Inc. | N=447 ➔ 627

Enrollment change • First-in-human • Colorectal Cancer • Hepatocellular Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Dostarlimab and Cobolimab in Advanced Cervical Cancer (clinicaltrials.gov) - P2 | N=66 | Active, not recruiting | Sponsor: Meghan Shea | Recruiting ➔ Active, not recruiting

Enrollment closed • Cervical Cancer • Oncology • Solid Tumor • HAVCR2

Results from COSTAR lung: cobolimab + dostarlimab + docetaxel and dostarlimab + docetaxel versus docetaxel alone in patients with previously treated advanced/metastatic (A/M) non-small cell lung cancer (NSCLC) (ESMO-IO 2025) - P3 | "Safety and immune-related toxicity were comparable across the applicable arms. Table: 241MO Arms A B C n 305 301 152 Median OS, mo (95% CI) 11.9 (10.6–14.2) 11.8 (10.3–12.9) 11.3 (9.5–13.9) Confirmed ORR, n (%) [95% CI] 57 (18.7) [14.5–23.5] 55 (18.3) [14.1–23.1] 22 (14.5) [9.3–21.1] Median duration of response, mo (95% CI) 8.3 (6.2–9.9) 7.1 (6.3–9.4) 8.8 (5.1–11.0) Median PFS, mo (95% CI) 4.4 (4.2–5.5) 4.2 (4.0–5.4) 4.1 (2.9–4.8) n 302 295 144 TEAEs, n (%) 296 (98) 294 (>99) 142 (99) ≥Grade 3 TEAEs, n (%) 223 (74) 223 (76) 102 (71) ≥Grade 3 immune-mediated AEs, n (%) 23 (8) 17 (6) N/A Permanent discontinuation due to cobolimab- and/or dostarlimab-related TEAEs, n (%) 24 (8) 29 (10) N/A Treatment ongoing, n (%) 24 (8) 13 (4) 1 (<1) AE, adverse event; mo, months; N/A, not applicable; TE, treatment emergentConclusions In COSTAR Lung, cobolimab + dostarlimab + docetaxel and dostarlimab + docetaxel did not meet the planned primary endpoint of survival (OS)..."

Clinical • IO biomarker • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HAVCR2

A Study of Cobolimab Plus Dostarlimab in Pediatric and Young Adult Participants With Cancer (clinicaltrials.gov) - P1/2 | N=83 | Active, not recruiting | Sponsor: GlaxoSmithKline | Trial completion date: Jan 2032 ➔ Oct 2026 | Trial primary completion date: Jan 2032 ➔ Oct 2026

Trial completion date • Trial primary completion date • Brain Cancer • Diffuse Intrinsic Pontine Glioma • Ependymoma • Glioblastoma • Glioma • Hematological Malignancies • Hepatoblastoma • Hepatocellular Cancer • Liver Cancer • Lymphoma • Melanoma • Oncology • Osteosarcoma • Pediatrics • Rhabdomyosarcoma • Sarcoma • Solid Tumor

Lysine-specific demethylase 1 (LSD1) inhibition modulates tumor progression and immunotherapeutic priming effects in triple-negative breast cancers (SITC 2025) - "Importantly, cell-derived xenograft humanized mice models treated with immunotherapy combinations (nivolumab, ipilimumab, cobolimab)-coupled LSD1 inhibitor significantly reduced tumor size compared to control group.Conclusions Our study underscores the clinical potential of LSD1-targeted epigenetic drugs to sensitize TNBC tumors to immunotherapies. Additionally, our findings suggest LSD1 cooperates with the AP-1 transcriptional complex to drive oncogenic gene expression programs that promote tumor progression and immune evasion in TNBC, defining a novel LSD1-AP-1 transcriptional axis in TNBC. These findings support combination strategies incorporating LSD1 inhibitors with immune checkpoint blockade for improved therapeutic outcomes in TNBC.Ethics Approval Ethics approval was obtained from The Centralized Institutional Review Board of Singhealth, Singapore.Consent Consent was waived for this study from The Centralized Institutional Review Board of Singhealth, Singapore."

IO biomarker • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • KDM1A • PD-L1

Study of Niraparib, TSR-022, Bevacizumab, and Platinum-Based Doublet Chemotherapy in Combination With TSR-042 (clinicaltrials.gov) - P1 | N=60 | Completed | Sponsor: Tesaro, Inc. | Active, not recruiting ➔ Completed | Trial completion date: Aug 2024 ➔ Dec 2024

Trial completion • Trial completion date • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Study of the Safety and Effectiveness of GSK6097608 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=107 | Active, not recruiting | Sponsor: GlaxoSmithKline | Trial completion date: Dec 2025 ➔ Dec 2026 | Trial primary completion date: Dec 2025 ➔ Dec 2026

Monotherapy • Trial completion date • Trial primary completion date • Colorectal Cancer • Endometrial Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck