Bristol-Myers Squibb
Oncology Drug Pipeline Insights – June 2021

Molecule	Target	Phase	Indication	NCT Number	Mol Type
Relatlimab / BMS 986016	LAG 3	II/III	Advanced Melanoma	NCT03470922	Monoclonal Antibody
		II	Head and Neck Cancer (HNSCC)	NCT04080804
		II	Colorectal Adenocarcinoma	NCT03642067
		II	Hepatocellular Carcinoma	NCT04567615
BMS-986012	fucosyl-GM1	II	R/R Small Cell Lung Cancer	NCT04702880	Monoclonal Antibody
BMS-813160	CCR 2/5	II	Non-small Cell Lung Cancer Hepatocellular Carcinoma	NCT04123379	Small Molecule
		I/II	Colorectal Cancer	NCT03184870
			Pancreatic Cancer
Iberdomide /CC220	Aiolos, Ikaros	II	R/R Multiple Myeloma	NCT04392037	Small Molecule
CC 90011	LSD1	I/II	Non Small Cell Lung Cancer	NCT04350463	Small Molecule
		I	Small Cell Lung Cancer
			R/R Acute Myeloid Leukemia	NCT04748848
		I/II	Non-Hodgkin Lymphoma	NCT02875223
CC-90010	BET	I	Astrocytoma	NCT04047303	Small Molecule
			Glioblastoma Non-Hodgkin Lymphoma	NCT03220347
BMS-986179	CD73	I/II	Malignant Solid Tumor	NCT02754141	Monoclonal Antibody
BMS-986249	CTLA-4	I/II	Advanced Solid Tumors	NCT03369223	Monoclonal Antibody
BMS-986288	CTLA-4	I/II	Advanced Solid Cancers	NCT03994601	Monoclonal Antibody
BMS-986218	CTLA-4	I/II	Metastatic Liver Carcinoma Metastatic Lung Carcinoma	NCT04785287	Monoclonal Antibody
			Metastatic Lung Cancer
BMS-986315	NKG2A	I/II	Renal Cell Carcinoma	NCT04349267	Monoclonal Antibody
			Clear Cell Renal Cell Carcinoma
BMS-986178	OX40	I/II	Advanced Cancers	NCT02737475	Monoclonal Antibody
BMS 986258 / ONO 7807	TIM-3	I/II	Advanced Solid Tumors	NCT03446040	Monoclonal Antibody
BMS-986253 / HuMax-IL8	IL-8	I/II	Metastatic Solid Tumors	NCT03400332	Monoclonal Antibody
BMS-986226	CD278	I/II	Advance Cancer	NCT03251924	Monoclonal Antibody
BMS-986207	TIGIT	I/II	Advanced Solid Tumors	NCT02913313	Monoclonal Antibody
BMS-986299	NLRP3	I	Advanced Solid Tumors	NCT03444753	Monoclonal Antibody
CC-95251	SIRPα	I	Advanced Solid Cancers Hematologic Cancers	NCT03783403	Monoclonal Antibody
BMS-986148	Mesothelin	I/II	Advanced Solid Tumors	NCT02341625	Antibody Drug Conjugate
CC-99712	BCMA	I	R/R Multiple Myeloma	NCT04036461	Antibody Drug Conjugate
CC-93269	BCMA x CD3	I	R/R Multiple Myeloma	NCT03486067	Bispecific Antibody
CC-90009	GSPT1	I	Acute Myeloid Leukemia	NCT02848001	Small Molecule
CC-92480	E3 ligase	I/II	R/R Multiple Myeloma	NCT03374085	Small Molecule
CC-99282	E3 ligase	I	Non-Hodgkin Lymphoma	NCT03930953	Small Molecule
BMS 986301	STING	I	Advanced Solid Tumors	NCT03956680	Small Molecule
BMS-986158	BET	I/II	Advance Cancer	NCT02419417	Small Molecule
CC-95775	BET	I	Non-Hodgkin Lymphoma	NCT04089527	Small Molecule
BMS-986310 / ONO-4578	Prostaglandin E2 receptor 4 (EP4)	I/II	Advanced Cancer	NCT03661632	Small Molecule
CC-94676	Androgen Receptor	I	Castration-Resistant Prostate Cancer	NCT04428788	Small Molecule
Motolimod / VTX-2337	TLR8	I	Head and Neck Squamous Cell Carcinoma	NCT04272333	Small Molecule

BMS Active Oncology Pipeline Drug Description

• Relatlimab is a LAG-3–blocking antibody that binds to LAG-3 on T cells, restoring effector function of exhausted T cells.
• BMS-986012 is a first-in-class, fully human mAb with enhanced antibody-dependent cell-mediated cytotoxicity that binds to fucosyl-GM1, a ganglioside highly expressed on SCLC.
• BMS-813160 is an antagonist of both human C-C chemokine receptor types 2 (CCR2; CD192) and 5 (CCR5; CD195), with potential immunomodulating and antineoplastic activities.
  Iberdomide is an investigational cereblon E3 ligase modulator (CELMoD®) compound that induces degradation of transcription factors Aiolos and Ikaros, thereby inhibiting growth of myeloma cells in vitro.
  In pre-clinical models, iberdomide has demonstrated ability to destroy tumor cells, stimulate an immune response, overcome resistance to immunomodulatory drugs, and synergize with dexamethasone, daratumumab and bortezomib.
• CC-90011 is a potent and selective reversible inhibitor of Lysine Specific Demethylase 1 (LSD1).
• CC-90010 is a novel, oral, reversible, small-molecule inhibitor of Bromodomain and extra-terminal (BET) proteins.
• BMS-986179 is a high-affinity antibody that inhibits CD73 enzymatic activity and downregulates its expression on tumor cells.
• CytomX’s BMS-986249 is an engineered probody derived from Yervoy, which works as an inhibitor of the protein receptor CTLA-4, stimulating T-cells to remain active and destroy cancer cells. CTLA4, is an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.
• BMS-986288 is a Probody of a nonfucosylated version of ipilimumab (anti-CTLA-4 NF).
• Anti-CTLA4 monoclonal antibody BMS-986218 targets and binds to CTLA4 expressed on T cells and inhibits the CTLA4-mediated downregulation of T-cell activation.
• BMS-986178 is a fully human IgG1 agonist mAb that binds with high affinity to the OX40 receptor.
• BMS 986258 (also known as ONO 7807) is a fully-human monoclonal antibody targeting T-cell immunoglobulin and mucin domain-3 (TIM-3).
• HuMax-IL8 (now known as BMS-986253) is a novel, fully human monoclonal antibody that inhibits interleukin-8 (IL-8), a chemokine that promotes tumor progression, immune escape, epithelial-mesenchymal transition, and recruitment of myeloid-derived suppressor cells.
• BMS-986226 is an agonistic monoclonal antibody that recognizes inducible T-cell co-stimulator (ICOS; CD278) and binds to ICOS expressed on certain T-cells.
• BMS-986207 is an anti-TIGIT monoclonal antibody that binds to TIGIT expressed on several types of immune cells, including tumor-infiltrating T lymphocytes. This prevents TIGIT from interacting with its ligands, CD112 and CD155.
• BMS-986299 is an NLRP3 agonist that induces IL8 release to activate natural killer (NK) cells.
• CC-95251 is a anti-SIRPa monoclonal antibody which targets and binds to SIRPa, a cell surface protein expressed on macrophages, thereby blocking the interaction between SIRPa and cluster of differentiation 47 (CD47) expressed on tumor cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of phagocytosis.
• BMS-986148 is a fully human IgG1 anti-mesothelin monoclonal antibody conjugated to tubulysin to promote selective cytotoxic delivery to tumor cells.
• CC-99712 is an antibody-drug conjugate (ADC) targeting B-cell maturation antigen (BCMA) for the treatment of multiple myeloma (MM).
• CC 93269 (also known as EM 901) is a T-cell bi-specific antibody (TCB) targeting B-cell maturation antigen (BCMA).
• CC-90009 is a novel protein degrader and the first CEreblon E3 Ligase MoDulator, or CELMoD agent to enter clinical development that specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
• CC-92480 is a novel CEreblon E3 Ligase MoDulator, or CELMoD agent, designed to induces rapid degradation of the transcription factors Ikaros and Aiolos, which leads to apoptosis of the myeloma cells.
• BMS 986301 is a small molecule stimulator of interferon genes (STING) agonist (MPYS-protein-stimulant).
• BMS-986158 is an inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins and binds to the acetyl-lysine binding site in the BRD of BET proteins, thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth.
• BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that bind to acetylated lysines on the tails of histones H3 and H4, and regulate chromatin structure and function.
• BMS-986310 / ONO-4578, Ono’s Phase 1 selective Prostaglandin E 2 (PGE 2 ) receptor 4 (EP 4 ) antagonist.
• CC-94676 is an orally bioavailable androgen receptor (AR) degrader, which prevents AR-mediated signaling and inhibits the proliferation of AR-overexpressing tumor cells. AR plays a key role in tumor cell proliferation in castration-resistant prostate cancer (CRPC).
• Motolimod (VTX-2337), a selective small-molecule agonist of TLR8, stimulates natural killer (NK) cells, dendritic cells, and monocytes.