BGB-10188 / BeOne Medicines - LARVOL DELTA

BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2 | N=97 | Completed | Sponsor: BeiGene | Active, not recruiting ➔ Completed

Combination therapy • Monotherapy • Trial completion • Breast Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • MSI

A highly selective PI3Kδ inhibitor BGB-10188 shows superior preclinical anti-tumor activities and decreased on-target side effects on colon. (PubMed, Neoplasia) - "BGB-10188 showed significant antitumor effects in human B cell lymphoma xenograft models as single agent or in combination with the BTK inhibitor zanubrutinib. BGB-10188 showed significant Treg inhibition in blood but not in colon, along with less drug accumulation in colon compared with idelalisib, which is an approved PI3Kdelta inhibitor with high incidence of gastrointestinal side effects in clinic. In summary, BGB-10188 is a novel PI3Kδ inhibitor with high selectivity, potency and improved safety profile shown in preclinical studies, which is showing the potential as a best-in-class PI3Kδ inhibitor."

Adverse events • Journal • Preclinical • Colon Cancer • Gastrointestinal Disorder • Hematological Disorders • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • PIK3CD

BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2 | N=97 | Active, not recruiting | Sponsor: BeiGene | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2025 ➔ Sep 2024 | Trial primary completion date: May 2025 ➔ Sep 2024

Combination therapy • Enrollment closed • Monotherapy • Trial completion date • Trial primary completion date • Breast Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • MSI

BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2 | N=113 | Recruiting | Sponsor: BeiGene | Trial completion date: Feb 2025 ➔ Dec 2025

Combination therapy • Monotherapy • Trial completion date • Breast Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • MSI

A first‑in‑human, phase 1a, dose‑escalation study of BGB‑10188, a phosphatidylinositol 3‑kinase delta (PI3Kδ) inhibitor, + tislelizumab (anti-PD-1) in patients with solid tumors (AACR 2024) - P1/2 | "The plasma exposure to BGB-10188 exhibited a dose-dependent increase across a range of 20 mg to 540 mg. BGB‑10188 + tislelizumab showed preliminary antitumor activity and was generally safe and tolerable across doses in this heavily pretreated population of patients with solid tumors. BGB‑10188 + tislelizumab will be further evaluated in dose expansion (Part E)."

Clinical • P1 data • Oncology • Solid Tumor • CD8 • PIK3CD

BeiGene to Present Clinical and Preclinical Data from Broad Portfolio and Pipeline at AACR Annual Meeting 2024 (Businesswire) - "An additional clinical presentation includes the first data from a Phase 1a dose escalation study of BGB-10188, a phosphatidylinositol 3 kinase delta (PI3Kδ) inhibitor, plus tislelizumab in patients with solid tumors. BeiGene will also be presenting preclinical characterizations of several novel molecules from its internal discovery engine, including a CEA x 4-1BB bispecific antibody and a chimeric degradation activation compound (CDAC) targeting BTK, BGB-16673....An additional preclinical presentation highlights the therapeutic potential of the triple-combination of tislelizumab with anti-LAG-3 (LBL-007) and anti-TIM-3 (surzebiclimab)..."

Preclinical • Head and Neck Cancer • Hematological Malignancies • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck

BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2 | N=126 | Recruiting | Sponsor: BeiGene | Trial completion date: Nov 2025 ➔ Feb 2025

Combination therapy • Monotherapy • Trial completion date • Breast Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • MSI

BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2 | N=150 | Recruiting | Sponsor: BeiGene | Trial completion date: Apr 2025 ➔ Nov 2025

Combination therapy • Monotherapy • Trial completion date • Breast Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Neuroendocrine Tumor • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • MSI • PD-L1

PI3K Inhibitors for the Treatment of Chronic Lymphocytic Leukemia: Current Status and Future Perspectives. (PubMed, Cancers (Basel)) - "The dual PI3Kδ/γ inhibitor duvelisib is approved for use in CLL patients but with similar toxicities to idelalisib. Umbralisib, a highly selective inhibitor of PI3Kδ and casein kinase-1ε (CK1ε), was found to be efficient and safe in monotherapy and in combination regimens in phase 3 trials in patients with CLL. Novel PI3Kis are under evaluation in early phase clinical trials. In this paper we present the mechanism of action, efficacy and toxicities of PI3Ki approved in the treatment of CLL and developed in clinical trials."

Journal • Review • Chronic Lymphocytic Leukemia • Gastroenterology • Gastrointestinal Disorder • Hematological Malignancies • Immunology • Infectious Disease • Inflammation • Leukemia • Oncology • Pneumonia • IGH • PIK3CA • PIK3CB • PIK3CD • PIK3CG • TP53

BeiGene announces clinical and preclinical data to be presented at the 2020 American Association for Cancer Research (AACR) Virtual Annual Meeting II (GlobeNewswire) - "BeiGene, Ltd…announced that clinical data on its investigational anti-PD-L1 antibody BGB-A333 and preclinical data on three early-stage drug candidates will be presented at the 2020 American Association for Cancer Research (AACR) Virtual Annual Meeting II, taking place on June 22-24, 2020."

P1/2 data • Preclinical • Oncology • Solid Tumor

[VIRTUAL] BGB-10188, a highly selective PI3Kδ inhibitor with improved safety profile and superior anti-tumor activities in vivo (AACR-II 2020) - "The elimination half-life (t1/2) of BGB-10188 in plasma was 12.6 hours and 10.4 hours in rats and dogs, respectively.BGB-10188 showed significant antitumor effects in different types of B cell Lymphoma xenograft models. The liver toxicities of BGB-10188 were evaluated in mice and significantly improved safety margin was observed for BGB-10188 in comparison with other PI3Kδ inhibitors.In summary, BGB-10188 is a novel PI3Kδ inhibitor with high selectivity, potency and improved safety profile shown in preclinical studies, which is promising and warrants the testing of the compound in human."

Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor

Brief Title: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2; N=150; Recruiting; Sponsor: BeiGene; Not yet recruiting ➔ Recruiting

Clinical • Combination therapy • Enrollment open • Monotherapy • Bladder Cancer • Breast Cancer • Cervical Cancer • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Endometrial Cancer • Esophageal Cancer • Follicular Lymphoma • Gastric Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • Head and Neck Cancer • Hematological Disorders • Hematological Malignancies • Hepatocellular Cancer • Leukemia • Liver Cancer • Lung Cancer • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Melanoma • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • Thoracic Cancer • Triple Negative Breast Cancer • Urothelial Cancer • Uterine Cancer • MSI-H • PD-L1

Brief Title: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov) - P1/2; N=150; Not yet recruiting; Sponsor: BeiGene

Clinical • Combination therapy • Monotherapy • New P1/2 trial