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KDDF-201712-09 Development of nano-sized anti-cancer prodrug capable of tumor enzyme-specific activation(Oncology, Chemical) [2019-11-28]

Ongoing Project
Section Lead
Preclinical Phase I Phase II Phase III

Development and Market Objectives

The goals are to figure out candidate of anticancer precursors for the development of nano-formulated tumor enzyme-specific anticancer prodrug, optimize nano-formulations, evaluate in vitro / in vivo efficacy and pharmacokinetics, optimize mass production processes and establishing the CMC of the formulation for future preclinical testing.

Unmet Medical Need & Target Patients

The target patient group is defined as patients with cancer diseases that overexpress biomarker (cathepsin B). In the case of colorectal cancer and metastatic colorectal cancer, the activity of cathepsin B has been reported to be greatly increased. Specifically, colorectal cancer, metastatic colorectal cancer, and colorectal cancer that fail in primary chemotherapy are the target diseases. We further aim to expand target patients to cancer diseases such as pancreatic cancer and breast cancer related to cathepsin B.


Doxorubicin is a cytotoxic drug used in the treatment of most cancers due to its excellent anticancer effect. It is approved by FDA to be used in 14 different kinds of cancer diseases. However, it is not capable of tumor-targeting effect, and thus has many side effects. Especially, doxorubicin is a cytotoxic anticancer agent that is increasing limited in its use because it is life threatening to the patient. In order to solve the problems of doxorubicin, we are developing a novel low molecular weight prodrug-based nano-formulation that is selectively activated by cancer cell-specific biomarker (cathepsin B). The anticancer drug candidate itself constitutes the formation of self-assembly nanoparticles without any nano-carriers, thereby achieving both advantages of targeting and cytotoxic anticancer drug. This novel prodrug is a doxorubicin-based low molecular weight cytotoxic drug with a biomarker, which have advantages of nano-formulation. Considering its low toxicity, simple synthetic scheme and the value of nano-formulations, it is expected to be of the effective drug candidates which can be practically used in clinical practice in the future.


- Lead optimization of anticancer drug candidates

- Establishment of simple 1 step synthesis method and scale-up production

- Confirmation of the anticancer efficacy in various tumors (colon cancer, pancreatic cancer, breast cancer) based on biomarkers.

- Optimization of self-assembled nanoformulation.

- Prodrug-based low toxicity validation

Intellectual Property

Completed application for domestic / overseas (including USA and Europe)

Competitive Advantages

- It presents a new anticancer drug paradigm through low molecular prodrug-based tumor specific nano-formulation

- Long term administration due to low toxicity

- Cancer tissue specific delivery by passive accumulation effect of nanoparticle

- Simple synthesis and a clear biomarker

- Acquired all the advantages of cytotoxic anticancer agent and target anticancer agent

Contact & Company Overview

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