Drug intelligence / Profile preview

MM-129

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

MM-129 is a novel, chemically synthesized small molecule based on a 1,2,4-triazine scaffold, structurally related to roscovitine. It acts as a multi-target inhibitor with both cytostatic and chemosensitizing properties, demonstrating preclinical antitumor efficacy against colon cancer. Its mechanism of action involves inhibition of the PI3K/Akt/mTOR signaling pathway and Bruton’s tyrosine kinase (BTK), as well as downregulation of programmed death ligand 1 (PD-L1), which can suppress tumor growth and immune evasion. MM-129 shows synergistic activity with 5-fluorouracil and can overcome chemoresistance in colorectal cancer models. Toxicology studies indicate favorable pharmacokinetics and good tolerability at effective doses in zebrafish and rodents, with a safe profile observed at 10 μmol/kg by intraperitoneal administration.

Other names
pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine sulfonamide
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)mTOR (Mammalian target of rapamycin kinase)CD274 (Programmed cell death protein 1 ligand 1)CDK2 (Cyclin-dependent kinase 2)

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