BeiGene (Beijing) Co., Ltd
Oncology Drug Pipeline Analysis – June 2021

Molecule	Target	Phase	Indication	NCT Number	Mol Type
Zanubrutinib / BGB-3111	BTK	III	Chronic Lymphocytic Leukemia	NCT03734016	Small Molecule
			Small Lymphocytic Lymphoma
Tislelizumab / BGB-A317	PD1	III	Diffuse Large B-Cell Lymphoma	NCT04789434	Monoclonal Antibody
		III	Metastatic Nasopharyngeal Cancer	NCT03924986
		III	Small Cell Lung Cancer	NCT04005716
		III	Esophageal Squamous Cell Carcinoma	NCT03783442
		III	Gastric Cancer	NCT03777657
		III	Hepatocellular Carcinoma	NCT03412773
		II	R/R Acute Myeloid Leukemia	NCT04541277
		II	Cervical Cancer	NCT04693234
		II	Esophagus Cancer	NCT04776590
		II	Triple-negative Breast Cancer	NCT04501523
Pamiparib/ BGB-290	PARP	II	Advanced Gastric Cancer	NCT03427814	Small Molecule
		II	Advanced Ovarian Cancer	NCT03933761
		II	Renal Cell Carcinoma	NCT04603365
		I/II	Triple Negative Breast Cancer	NCT03333915
		I	Glioblastoma	NCT04614909
Lifirafenib / BGB-283	RAF	I/II	Advanced Solid Tumor	NCT02610361	Small Molecule
BGB-A333	PD-L1	I/II	Advanced Solid Tumor	NCT03379259	Monoclonal Antibody
BGB-A425	TIM-3	I/II	Advanced Solid Tumor	NCT03744468	Monoclonal Antibody
Ociperlimab / BGB-A1217	TIGIT	I	Metastatic Solid Tumors	NCT04047862	Monoclonal Antibody
BGB-A445	OX40	I	Advanced Solid Tumor	NCT04215978	Monoclonal Antibody
BGB-11417	Bcl-2	I/II	Acute Myeloid Leukemia	NCT04771130	Small Molecule
			Myelodysplastic Syndromes
BGB-10188	PI3-Kδ	I/II	Chronic Lymphocytic Leukemia	NCT04282018	Small Molecule
			Small Lymphocytic Lymphoma
			Follicular Lymphoma
			Marginal Zone Lymphoma
			Mantle Cell Lymphoma
			Diffuse Large B Cell Lymphoma
			Non-small Cell Lung Cancer
			Metastatic Melanoma
			Advanced Solid Tumor
BGB-15025	HPK1	I	Advanced Solid Tumor	NCT04649385	Small Molecule

BeiGene’s  Active Oncology Pipeline Drug Description

• Tislelizumab is an anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. In pre-clinical studies, binding to FcγR on macrophages has been shown to compromise the anti-tumor activity of PD-1 antibodies through activation of antibody-dependent macrophage-mediated killing of T effector cells.
• Pamiparib is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP), with potential antineoplastic activity. Upon administration, pamiparib selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis.
• Lifirafenib (BGB-283) is an investigational novel small molecule inhibitor of the RAF protein. As opposed to other agents which inhibit RAF in its monomeric form, lifirafenib was designed to inhibit both monomeric and dimeric RAF inhibition activities.
• BGB-A333 is a humanized IgG1-variant monoclonal antibody against programmed cell death 1-ligand 1 (PD-L1).
• BGB-A425 is an investigational IgG1-variant monoclonal antibody against TIM-3.
• Ociperlimab (BGB-A1217) is an investigational humanized monoclonal antibody designed to bind to TIGIT with high specificity and affinity. Ociperlimab is one of the most advanced anti-TIGIT antibodies in development with an intact IgG Fc binding region for optimal antibody-mediated anti-tumor activity.
• BGB A445 is an anti OX40 agonist monoclonal antibody being developed by BeiGene for the treatment of solid tumours.
• BGB 11417 is an orally administered, small molecule Bcl-2 inhibitor, being developed by BeiGene for the treatment of B-cell malignancies.
• BGB-10188 is a novel PI3Kδ inhibitor with high selectivity, potency and improved safety profile shown in preclinical studies.
• BGB-15025 is designed to be a potent and highly selective small molecule oral inhibitor of HPK1, a kinase downstream of the T cell receptor.