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talabostat + gemcitabine
- Development stage
- Unknown
- Lead developer
- Biodexa Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral (talabostat), Intravenous (gemcitabine)
01
Overview
Talabostat + gemcitabine is a **combination therapy** composed of two agents: - **Talabostat** is an orally administered small molecule inhibitor of dipeptidyl peptidases, including fibroblast activation protein (FAP), DPP8, DPP9, and DPPIV. By inhibiting FAP and related enzymes highly expressed in certain tumors, talabostat remodels the tumor microenvironment, upregulates cytokines and chemokines, activates T-cell and NK-cell responses, and potentially reverses tumor-induced immunosuppression. - **Gemcitabine** is a nucleoside analog and chemotherapeutic agent that is incorporated into DNA during replication, causing chain termination, blockade of DNA synthesis, and apoptosis in rapidly dividing tumor cells. The combination has been specifically investigated in **metastatic pancreatic cancer**, with Phase 2 clinical trials showing some encouraging response rates and survival outcomes[1][4]. Preclinical studies indicate that talabostat may sensitize tumors to cytotoxic agents like gemcitabine by targeting the tumor stroma and immune evasion pathways[1][4].
- Other names
- talabostatVal-boroProGemzar
02
Targets
DPP-4 (Dipeptidyl Peptidase-IV)FAP (Fibroblast activation protein alpha)DPP8 (Dipeptidyl peptidase 8)DPP9 (Dipeptidyl Peptidase 9)
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