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BXCL701 + pembrolizumab
- Development stage
- Unknown
- Lead developer
- BioXcel Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
BXCL701 + pembrolizumab is an investigational combination therapy for cancer. BXCL701 (talabostat) is an oral small molecule inhibitor of dipeptidyl peptidases DPP8, DPP9, DPP4, and fibroblast activation protein (FAP). It acts as an innate immune activator by triggering the inflammasome and inducing proinflammatory cytokines such as IL-18 and IL-1β. This mechanism bridges innate and adaptive immunity by inflaming the tumor microenvironment to enhance immune cell infiltration. Pembrolizumab (Keytruda) is a monoclonal antibody that targets programmed cell death protein 1 (PD-1), blocking its interaction with PD-L1/PD-L2 to promote T-cell mediated anti-tumor activity. The combination aims to convert immunologically "cold" tumors into "hot" ones that are more responsive to immunotherapy. The regimen has shown promising results in phase 2 trials for metastatic castration-resistant prostate cancer with small cell neuroendocrine features (mCRPC SCNC) and metastatic pancreatic ductal adenocarcinoma refractory to chemotherapy[1][3][4][5][6].
- Brand names
- Keytruda
- Other names
- talabostatKeytruda
02
Targets
PDCD1 (Programmed cell death protein 1 receptor)DPP9 (Dipeptidyl Peptidase 9)DPP-4 (Dipeptidyl Peptidase-IV)DPP8 (Dipeptidyl peptidase 8)
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