ArticleCancer discovery2022
Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor.
Article in Cancer discovery, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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Who cites it
59 citing papers in PubMed, 107 citations in OpenAlex.
- Integrated Machine Learning and Molecular Simulation-Guided Discovery of Novel Small-Molecule PD-L1 Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Phase I safety, efficacy, and biomarker response evaluations of three oral PD-L1 inhibitors: INCB086550, INCB099280, and INCB099318.Journal for immunotherapy of cancer · 2026Article
- In silico discovery of novel small-molecule PD-L1 inhibitors through a multi-stage computational workflow integrating machine learning and molecular dynamics.Journal of computer-aided molecular design · 2026Article
- Immune Checkpoint-Based Therapies in Colorectal Cancer-Current Approaches and Future Perspectives.International journal of molecular sciences · 2026Review
- Design, Synthesis and Biological Evaluation of Oxadiazole-Biphenyl Derivatives as Small Molecule Inhibitors Targeting PD-1/PD-L1 Immune Checkpoint.ACS medicinal chemistry letters · 2026Article
- ZBTB21 Is a Dual Suppressor of Pyroptosis and MHC-I Antigen Presentation That Promotes Tumor Immune Evasion.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Strategies to target PD-1/PD-L1 in the tumor microenvironment.Cellular oncology (Dordrecht, Netherlands) · 2026Review
- Proanthocyanidins enhance antitumor immunity by promoting ubiquitin-proteasomal PD-L1 degradation via stabilization of LKB1 and SYVN1.The Journal of clinical investigation · 2026Article
- Small molecules targeting the PD-1/PD-L1 axis for cancer immunotherapy.Theranostics · 2026Review
- Therapeutic Alternatives to Recombinant Biologics: Mechanistic Framework, Clinical Evidence, and Selection Guidance.Drug design, development and therapy · 2026Review
- Novel PD-L1 Small-Molecule Inhibitors Advancing Cancer Immunotherapy.Anti-cancer agents in medicinal chemistry · 2026Review
- Preclinical ex vivo and in vivo models to study immunotherapy agents and their combinations as predictive tools toward the clinic.Journal for immunotherapy of cancer · 2025Review
- Novel GPU Engines for Virtual Screening of Giga-Sized Libraries Identify Inhibitors of Challenging Targets.Journal of chemical information and modeling · 2025Article
- Computational identification and evaluation of novel PD-L1 inhibitors for cancer immunotherapy.Scientific reports · 2025Article
- Discovery of Pyrazole-Containing 4‑Arylindolines as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction.ACS medicinal chemistry letters · 2025Article
- Antineuroblastoma Activity Evaluation and Mechanism of Novel PD-L1 Small Molecule Inhibitors through Immune and Non-Immune Pathways.ACS pharmacology & translational science · 2025Article
- Impact of the PD-1/PD-L1 inhibitor SCL-1 on MDA-MB231 tumor growth in a humanized MHC-double knockout NOG mouse model.Scientific reports · 2025Article
- Characterization of Clinically Evaluated Small-Molecule Inhibitors of PD-L1 for Immunotherapy.ACS medicinal chemistry letters · 2025Article
- Immune checkpoint inhibitors in cancer therapy: what lies beyond monoclonal antibodies?Medical oncology (Northwood, London, England) · 2025Review
- Negative Immune Checkpoint Inhibitors.Pharmaceutics · 2025Review
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Authors and funding
35 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Blocking the activity of the programmed cell death protein 1 (PD-1) inhibitory receptor with therapeutic antibodies against either the ligand (PD-L1) or PD-1 itself has proven to be an effective treatment modality for multiple cancers. Contrasting with antibodies, small molecules could demonstrate increased tissue penetration, distinct pharmacology, and potentially enhanced antitumor activity. Here, we describe the identification and characterization of INCB086550, a novel, oral, small-molecule PD-L1 inhibitor. In vitro, INCB086550 selectively and potently blocked the PD-L1/PD-1 interaction, induced PD-L1 dimerization and internalization, and induced stimulation-dependent cytokine production in primary human immune cells. In vivo, INCB086550 reduced tumor growth in CD34+ humanized mice and induced T-cell activation gene signatures, consistent with PD-L1/PD-1 pathway blockade. Preliminary data from an ongoing phase I study confirmed PD-L1/PD-1 blockade in peripheral blood cells, with increased immune activation and tumor growth control. These data support continued clinical evaluation of INCB086550 as an alternative to antibody-based therapies. SIGNIFICANCE: We have identified a potent small-molecule inhibitor of PD-L1, INCB086550, which has biological properties similar to PD-L1/PD-1 monoclonal antibodies and may represent an alternative to antibody therapy. Preliminary clinical data in patients demonstrated increased immune activation and tumor growth control, which support continued clinical evaluation of this approach. See related commentary by Capparelli and Aplin, p. 1413. This article is highlighted in the In This Issue feature, p. 1397.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.