Science & Technology

Mechanism of action, in vitro validation, and the scientific foundation of the TBDS platform

Mechanism of Action
01
Systemic Administration
TBDS complex is injected IV — pharmacologically inert with neutralized systemic toxicity to healthy tissue
02
Tumor Microenvironment
MMP-2/9 enzymes — overexpressed 5–10× in solid tumors — cleave the delivery module linker
03
CTP Activation
Cleavage releases CTP and exposes multiple tumor-targeting motifs, concentrating activity at tumor
04
Cancer Cell Destruction
CTP perforates the cancer cell membrane — irreversible physical disruption, independent of MDR
Activation is MMP-dependent — confined to the tumor microenvironment — eliminating off-target effects in healthy tissue

Bispecific Architecture

Each TBDS construct is a single recombinant fusion protein combining three functional modules: the PS14 tumor-targeting delivery module (TDM), an MMP-2/9 cleavable linker, and the cytotoxic payload (CTP).

In the unactivated state, the TDM shields the CTP — preventing off-target toxicity. Upon encountering the tumor microenvironment's elevated MMP-2/9, the linker is cleaved and CTP is released to physically destroy the cancer cell membrane through pore formation.

Why Physical Lysis Wins

MDR-Proof: Membrane disruption is independent of drug efflux pumps, P-glycoprotein, or other resistance mechanisms
Irreversible: Physical membrane perforation cannot be repaired — unlike molecular targets that can be mutated
Immunostimulatory: Tumor cell lysis releases DAMPs, priming anti-tumor immune responses and synergizing with checkpoint inhibitors
Broad applicability: Any tumor overexpressing MMP-2/9 is a target — applicable across multiple solid tumor types
In Vitro Efficacy Potent, selective cytotoxicity in triple-negative breast cancer (MDA-MB-231)

Key Results

Free CTP — IC50
~ 0.2 μM Cytotoxicity endpoint (24h)
Potent free CTP confirms cytotoxic payload activity
PS14-CTP + MMP-2 — IC50
~ 0.3 μM Activated complex (24h)
Activated complex restores cytotoxic potency to ~0.3 μM
✓ PS14-CTP complex: ZERO toxicity until MMP-2 cleavage — confirming selective activation
Study Design
Untreated Control
Baseline — normal cell growth, no intervention
Free CTP
Confirms potent cytotoxicity. IC50 ~0.2 μM
PS14-CTP complex
Shielded complex — Confirms NO cytotoxicity
PS14-CTP + MMP-2 pretreat
Confirms activation: IC50 restored to ~0.3 μM
Assays: CelTox Green (cytotoxicity) + RealTime-Glo MT (viability) · 96-well · 24h serum-free · live cells

MMP-2/9 Cleavage Validation

Gel electrophoresis and cytotoxic bioassay confirm efficient MMP-2/9-mediated proteolytic cleavage of the TBDS linker — the molecular mechanism underlying selective tumor activation.

Safety Profile

Zero Toxicity

The unactivated PS14-CTP complex demonstrates zero toxicity in the absence of MMP-2/9. This is not merely reduced toxicity — it is complete abolition, confirmed by both CelTox and RealTime-Glo assays. Healthy tissue, lacking elevated MMP-2/9, would remain completely protected.

In Vivo Tolerability

Xenograft studies show no body weight loss across TBDS-treated groups (ISB-20, ISB-21 at 5 mg/kg), in contrast to the systemic toxicity profile typical of chemotherapeutic agents at comparable doses. See Pipeline & Data for full in vivo results.

Ready to See the Pipeline?

Explore the full pipeline — four constructs, in vivo validation of efficacy in breast and prostate cancers, and the EGFR-targeted modular expansion.