Drug intelligence / Profile preview

PIP-CpG

Development stage
Unknown
Lead developer
TwoStep Therapeutics
Modality
MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Peptides
Administration
Intravenous
01

Overview

PIP-CpG is a synthetic conjugate composed of a **polyspecific integrin-binding peptide** (PIP) linked to a **CpG oligonucleotide**. The PIP moiety targets integrins overexpressed on the surface of many solid tumor cells, enabling tumor-specific delivery. The CpG component is an immunostimulatory oligonucleotide that acts as a **Toll-like receptor 9 (TLR9) agonist**, promoting potent activation of innate and adaptive anti-tumor immunity. The conjugate is designed for **systemic (intravenous) administration**, thereby overcoming the need for direct tumor injections. In preclinical murine models of aggressive breast and pancreatic cancers, intravenous PIP-CpG induced **strong infiltration of lymphocytes** (including CD8+ and CD4+ T cells and B cells), transformed the tumor microenvironment from immunosuppressive to immune-active, and resulted in notable tumor regression and durable cures in some cases. The approach leverages targeted delivery to maximize immune activation at tumor sites while minimizing off-target effects[1][2][4][5][6].

Other names
PIP + CpGPIP CpGPIP conjugated to CpGPIP-CpG conjugate
02

Targets

αVβ5 (Integrin αVβ5)ITGA5:ITGB1 (Integrin α5β1)TLR9 (Toll-like receptor 9)αVβ3 (Integrin αVβ3)αVβ1 (Integrin alpha-V beta-1)αVβ6 (Integrin αVβ6)

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