PIPELINE

Antapodia Nanotherapeutics uses state-of-the-art and tissue-customarized lipid nanoparticles (LNPs) to deliver highly specific small interfering (siRNA) to inhibit the expression of the Master Invadopodial Regulator (MIR) of invasive cancer cells. The company develops two siRNA projects, AP-01 and AP-02, which inhibits the expression of MIR-1 and MIR-2, respectively (Figure 1). The company also developed AP-03, a monoclonal antibodies (mAb) that blocks the function of MIR-2 on invadopodia. The company has completed a series of POM/POC studies to demonstrate the remarkable anti-tumor and anti-metastasis efficacy of these novel, powerful and first-in-class invadopodia-targeted therapies.

PIPELINE

Product (target diseases)

AP-01 (LNP-siRNA)

(TNBC, HCC)

Molecular target/biomarker

MIR-1

                                                            

POC/POM studies > In vitro testing > In vivo testing > Toxicity > IND enabling

Product (target diseases)

AP-02 (LNP-siRNA)

(GAC)

Molecular target

MIR-2

 

POC/POM studies > In vitro testing > In vivo testing > Toxicity > IND enabling

Product (target diseases)

AP-03 (mAb)

(CRPC, GAC)

Molecular target

MIR-2

 

POC/POM studies > In vitro testing > In vivo testing > Toxicity > IND enabling

LNP: lipid nanoparticle; MIR: master invadopodial regulator; TNBC: triple-negative breast cancer; HCC: hepatocellular carcinoma; GAC: gastric adenocarcinoma; mAb: monoclonal antibody; CRPC: castration-resistant prostate cancer

 

Figure 1. The MOA of the invadopodia-targeted siRNA therapy AP-01 and AP-02

Composite siRNAs that target MIR-1 or MIR-2 are encapsulated in tissue-customarized LNPs to make the nano/gene-therapy agent AP-01 and AP-02, respectively. When delivered to tumors through intratumor (IT), intraperitoneal (IP) or intravenous injections (IV), AP-01 or AP-02 is internalized by invasive cancer cells to inhibit the expression of MIR-1 or MIR-2, thereby inhibiting the invadopodia biogenesis and functions.

figure-1-png1.png

AP-01

AP-01 is a LNP-formulated composite siRNAs targeting the master regulator of invadopodia biogenesis, MIR-1. Since invadopodia regulates the invasive growth of tumor cells in the three-dimensional microenvironment in vivo, and that MIR-1 also critically coregulates Wnt signaling, the downregulation of MIR-1 expression mediated by AP-01 is expected to simultaneously inhibit tumor growth and spreading as well as distant metastases. Systemic administration of AP-01 has been shown to induce a dual blockade of tumor growth and metastasis and significantly lengthens survival. Systemic and/or localized administrations of AP-1 lead to a remarkable tumor shrinkage in ovarious rthotopic and/or PDX models of TNBC and HCC. These compelling POC data underscore the immense therapeutic potential of AP-01 in aggressive and metastatic cancers.

AP-02

AP-02 is a LNP-formulated composite siRNAs targeting the invadopodia-specific membrane receptor MIR-2, thereby inhibiting multiple downstream signaling and the invasiveness and pro-metastatic potential of invasive cancer cells. Systemic administration of AP-02 substantially inhibits distant metastasis in several animal tumor models. These POC data underscore the therapeutic potential of AP-02 in these types of metastatic cancers. AP-02 may synergize with AP-01 to offer a complete blockade of invadopodia and tumor aggressiveness.                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                

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