Drug intelligence / Profile preview

T-2143

Development stage
Preclinical
Lead developer
Tarveda Therapeutics
Modality
Small Molecules, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

**T-2143** is an investigational HSP90-targeted miniature drug conjugate being developed by Tarveda Therapeutics for solid tumors, especially PI3K-mutant breast cancer. It is designed to accumulate in tumors through binding to activated HSP90 and to release the pan-PI3K inhibitor payload **T-2026** preferentially within tumor tissue, producing sustained PI3K pathway inhibition while reducing systemic exposure and toxicity associated with non-targeted PI3K inhibition. Preclinical reports describe superior antitumor activity versus free copanlisib-like PI3K inhibition in xenograft models, along with mitigation of dose-limiting hyperglycemia through payload masking and tumor-selective delivery.

02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)HSP90 (Heat shock protein 90 chaperone complex)

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