Drug intelligence / Profile preview

talabostat + pemetrexed

Development stage
Phase 3
Lead developer
BioXcel Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Talabostat + pemetrexed is a combination therapy of two small molecules: **talabostat** (PT-100), an oral dipeptidyl peptidase (DPP) inhibitor targeting DPP4 and DPP8/9, and **pemetrexed**, a multi-targeted antifolate chemotherapy agent. Talabostat's mechanism aims to enhance anti-tumor immune responses and potentially synergize with chemotherapy. The combination was developed primarily for the treatment of non-small cell lung cancer (NSCLC) after progression following platinum-based chemotherapy. Clinical trials reached phase 3 but did not result in an approval. The drugs are not known to have unique combination-therapy branding. Talabostat was developed by Point Therapeutics, while pemetrexed (brand: Alimta) is a product of Eli Lilly.

Brand names
Alimta (for pemetrexed)
Other names
talabostat mesylatePT-100PT100PT 100pemetrexed disodiumLY231514LY-231514LY 231514
02

Targets

ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DPP-4 (Dipeptidyl Peptidase-IV)DPP8 (Dipeptidyl peptidase 8)DPP9 (Dipeptidyl Peptidase 9)DHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)

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