The mainly selective, but also bispecific new molecular entities inhibit the negative immune checkpoints, including
- CTLA-4 (Cytotoxic T-Lymphocyte-Associated Protein-4; CD152)
- LAG-3 (Lymphocyte Activation Gene 3; CD223)
- TIM-3 (T-cell Immunoglobulin domain and Mucin domain 3; HAVCR2)
- TIGIT (T-cell Immunoreceptor with Ig and ITIM domains)
- B7-H3 (CD276)
- Others (VISTA: V-region Ig-containing Suppressor of T-cell Activation; BTLA: B- and T-Lymphocyte Attenuator; GARP: Glycoprotein A Repetitions Predominant; PVRIG; B7-H4
Immune checkpoint pathways are often activated to inhibit the nascent anti-tumor immune response. Immune checkpoint therapies act by blocking or stimulating these pathways and enhance the body’s immunological activity against tumors. Cytotoxic T lymphocyte-associated molecule-4 (CTLA-4), PD-1, and PD-L1 are the most widely studied and recognized inhibitory checkpoint pathways. Drugs blocking these pathways are currently utilized for a wide variety of malignancies and have demonstrated durable clinical activities in a subset of cancer patients.
This approach is rapidly extending beyond CTLA-4 and PD-1/PD-L1. New inhibitory pathways are under investigation, and drugs blocking LAG-3, TIM-3, TIGIT, VISTA, or B7/H3 are being investigated.
At least 35 new molecular entities (NMEs), mostly selective or increasingly bispecific antibodies, inhibiting negative immune checkpoints are in clinical development as monotherapy or in combination with other checkpoint modulators. At least further 19 NMEs are undergoing IND-enabling studies and numerous preclinical approaches are under evaluation.
The report includes a compilation of currently active projects in research and development of mostly recombinant antibodies, targeting negative immune checkpoints, such as CTLA-4, LAG-3, TIM-3, TIGIT, B7-H3, CTLA-4, LAG-3, TIM-3, TIGIT, B7-H3, VISTA, B7-H4, PVRIG, GARP, BTLA. In addition, the report lists company-specific R&D pipelines of inhibitors of negative immune checkpoints.
Competitor projects are listed in a tabular format providing information on:
- Drug Codes
- Target/Mechanism of Action
- Class of Compound
- Product Category
- R&D Stage
- Additional comments with a hyperlink leading to the source of information.
About Competitor Analysis Series:
The Competitor Analysis Series delivers NO-FRILLS, but concise information about the pipeline of R&D projects for targets, diseases, technologies and companies at low prices. The information is provided in a tabular format and fully referenced.
Table of Contents
1. CTLA-4, LAG-3, TIM-3, TIGIT & Other Immune Checkpoint Inhibitors 2018
1.1 CTLA-4 Receptor Antagonists:
- Selective CTLA-4 Antagonist in Clinical Development in Regulated Markets
- Selective CTLA-4 Antagonist in Clinical Development in Less Regulated Markets
- Bispecific CTLA-4 Antagonist in Clinical Development
- Selective or Bispecific CTLA-4 Antagonists in Non-Clinical Development
- Selective or Bispecific CTLA-4 Antagonist in Preclinical R&D
1.2 LAG-3 Antagonists:
- Relatlimab Pipeline
- Selective LAG-3 Antagonists in Clinical Development
- Bispecific LAG-3 Antagonists in Clinical Development
- LAG-3 Antagonists in Non-Clinical Development
- LAG-3 Antagonists in Preclinical R&D
1.3 TIM-3 Antagonists:
- Selective and Bispecific TIM-3 Antagonists in Clinical Development
- Selective and Bispecific TIM-3 Antagonists in Non-Clinical Development
- TIM-3 Antagonists in Preclinical R&D
1.4 TIGIT Antagonists:
- TIGIT Antagonists in Clinical Development
- TIGIT Antagonists in Non-Clinical Development
- TIGIT Antagonists in Preclinical R&D
1.5 Other Inhibitors of Negative Immune Checkpoints
- B7-H3 Targeted Immune Checkpoint Inhibitors
- Inhibitors of Other Immune Checkpoints
2. Corporate Inhibitors of Negative Immune Checkpoints R&D Pipelines