Drug intelligence / Profile preview

T-SA1-DM1

Development stage
Preclinical
Lead developer
Genentech
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

T-SA1-DM1 is an investigational **antibody-drug conjugate (ADC)** targeting **HER2-positive cancer cells**. It consists of a humanized single-chain variable fragment (**scFv**) antibody fused to human serum albumin (HSA) for half-life extension (**T-SA1**), conjugated to the cytotoxic agent **DM1** (a maytansinoid microtubule inhibitor) via a **non-cleavable maleimidomethyl cyclohexane-1-carboxylate (MCC) linker**. The drug selectively binds HER2 on tumor cells, is internalized, and—after lysosomal degradation—releases the cytotoxic payload to inhibit microtubule assembly, leading to cell cycle arrest and apoptosis. Preclinical studies demonstrated potent anti-proliferative and anti-tumor activity of T-SA1-DM1 in HER2-positive cancer cell lines and xenograft models, comparable to T-DM1.

02

Targets

TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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