Aptocine™

Development Pipeline

LSO is focusing on a number of cancers for the initial development of Aptocine™: Hepatoma, Metastatic Colorectal Cancer, Prostate Cancer, Pancreatic Cancer, Lung Cancer, Nasopharyngeal Cancer, Head and Neck Cancer, Kidney Cancer, and Glioma/Glioblastoma. Aptocine is also in Phase 2 development for treatment of Benign Prostatic Hyperplasia (BPH), and preclinical development for other non-cancer indications.

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Current Clinical Trials

LSO has completed Aptocine treatment in a Phase 3 trial in hepatocellular carcinoma and in a Phase 3 trial in colorectal cancer metastatic to the liver. LSO is also conducting clinical trials in benign prostatic hyperplasia (BPH).

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Aptocine is a water-soluble drug targeted inside a tumor or other tissue by a small, single-use, disposable drug activator included with the drug. The drug activator contains a tiny array of LEDs, located at the end of a very narrow (only 1.2 mm wide) flexible coated micro-wire, that emits red light at a discrete frequency and intensity, for a fixed time period, to activate Aptocine and create a “treatment region” around the LED array. Administering physicians insert the LED array into the targeted tumor or tissue, inject Aptocine intravenously and then energize the drug activator. Constant illumination with the LEDs’ low-intensity light can activate each molecule of Aptocine many times, resulting in a continuous supply of singlet oxygen molecules that can kill target tissues with minimal side effects through vascular closure, apoptosis, and an induced immune response.

Unlike radiation therapy, cytotoxic chemotherapy, biologic therapies, laser-based light-activated therapies, or thermal tissue destruction methods, Aptocine does not require the use of expensive equipment.

There is no evidence that Aptocine causes the serious toxicities associated with traditional cancer treatments such as bone marrow suppression, immune system suppression, marked fatigue, mucositis, and hair loss. A lower risk of skin photosensitivity is anticipated based on the shorter half-life and greater water solubility of Aptocine compared to other light-activated drugs.

Aptocine attacks tumors from the inside-out, rather than outside-in, the method used in many standard treatments. It is not tumor cell-cycle dependent, and targets all tumor cells in the treatment region, rather than only the minority of cells undergoing rapid division. The treatment closes tumor blood supply vessels, starving remaining cancer cells of oxygen and nutrients. The use of multiple drug activators and multiple treatments is common and treatment regimens can be tailored based on the number, size, shape, and location of the target tumors.

Additionally, Aptocine may have a systemic effect. Data from several published preclinical and human studies suggests that the production of large apoptotic masses in tumors using light-activated drugs yields tumor-specific clones of CD8+ T-cells which infiltrate distant, untreated tumors and destroys them or reduces their size. Results from a study showing that Aptocine produces a powerful T-cell anti-tumor response were presented at the 2009 Annual Meeting of the American Society of Clinical Oncology (Bromley 2009).

Aptocine is a pure, semi-synthetic compound developed in Japan by Meiji Seika and Eneos under the Laserphyrin® brand name. Laserphyrin® was approved for commercial use in Japan in October 2003 for the laser-activated treatment of early-stage bronchopulmonary lung cancer. LSO subsequently developed a proprietary synthetic method for the production of Aptocine.

References

• Bromley E, Owczarczak, Keltner L, Wang S, Gollnick SO: Characterization of an anti-tumor immune response after light-activated drug therapy using talaporfin sodium in a spontaneously metastasizing mammary tumor model. 2009 ASCO Annual Meeting. J Clin Oncol. May 20 suppl: abstract 3052.