Delving into the Latest Updates on Metalmeta analogue(Sapienza Università di Roma) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Compound 5(Sapienza Università di Roma)

Target

DNMTS

Mechanism

DNA methyltransferase inhibitors

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

Sapienza University of Rome

Active Organization

Sapienza University of Rome

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

A series of 1,2,3-triazole derivatives targeting the PD-1/PD-L1 pathway were designed, synthesized, and evaluated both in vitro and in vivo. Among them, compound III-4 demonstrated exceptional inhibitory activity against the interaction of PD-1/PD-L1 and showed great binding affinity with hPD-L1, with an IC₅₀ value of 2.9 nM and a K_D value of 3.33 nM. In the co-culture of Hep3B/OS-8/hPD-L1 cells and CD3⁺ T cells assay, III-4 relieved the inhibition of PD-L1 on PD-1 and promoted the expression of IFN-γ, which shared a comparable effect to that of the PD-1 monoclonal antibody Pembrolizumab (5 μg/mL). Moreover, compound III-5, an ester prodrug derived from III-4, demonstrated significant antitumor effects in the hPD-L1-MC38 C57BL/6 mouse model (TGI: 49.6 %) by oral administration. These findings suggest that compound III-5 holds promise as an inhibitor of the PD-1/PD-L1 interaction for cancer immunotherapy.

100 Deals associated with Metalmeta analogue(Sapienza Università di Roma)

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