Tolecine et Apatone

TOLECINE™:
Tolecine™ is a pre-clinical LCP which has demonstrated safety and efficacy in vitro and in vivo. Conceived and synthesized initially at Kent State University, Tolecine regulates gene transcription factor NFkB. The compound is produced at the commercial scale by Materia-Inc of Pasadena, CA using a state-of-the-art metathesis platform developed at Caltech. (Grubbs et al, Noble Prize for Chemistry, 2005). Tolecine is under development for treatment of solid tumors and herpes virus. Animal data suggest Tolecine may be safer and ten times more effective than the guanine analog antiviral pro-drug valacyclovir. Tolecine is tumor cell selective and exhibits strong anti-neoplastic activity.

RESVATOL™:
(Experimental Drug KST-301) is a biologically functional liquid crystal developed using a bioinformatic LCP™ drug discovery platform central to IC-MedTech's cell treatment rationale. KST-301, together with several related compounds in-licensed to the company in 2007, Resvatol has applications in oncology and microbiology for the treatment of cancer and other diseases.
LCP™ and Liquid Crystal Pharmaceuticals™ are trademarks of IC-MedTech which designate products of therapeutic value within the company's family of biologically functional liquid crystals and liquid crystal applications.
IC-MedTech is headquartered in San Diego, CA and has strategic alliances, collaborations and sponsored research agreements with universities and pharma's in the US, Canada and Europe.

ANNIAHLASE™:
Anniahlase™ (Experimental Drug KST-213) is a biologically functional liquid crystal developed using a bioinformatic LCP™ drug discovery platform central to IC-MedTech’s cell treatment rationale. KST-213, together with several related compounds in-licensed to the company in 2007, Anniahlase has application for the treatment of melanoma and other cancers.
LCP™ and Liquid Crystal Pharmaceuticals™ are trademarks of IC-MedTech which designate products of therapeutic value within the company’s family of biologically functional liquid crystals and liquid crystal applications.
IC-MedTech is headquartered in San Diego, CA and has strategic alliances, collaborations and sponsored research agreements with universities and pharma’s in the US, Canada and Europe.

KSS/KSA/KSI:
KSA, KSS and KSI all represent experimental families of LCP’s currently under development by IC-MedTech. These proprietary molecules and applications involve rationale design of liquid crystal compounds for use at the cellular level.
Ongoing research includes products for treatment of a wide range of diseases.

In a significant advancement in the ongoing battle against cancer, a group of researchers from Summa Health System, IC-MedTech and other institutions have completed the first ever FDA-approved human clinical trial of Apatone.

Dans une avancée significative dans la bataille contre le cancer, un groupe de chercheur ont complété le premier test clinique (chez les humains) de Apatone


Demonstrating promising results, Apatone exploits a new strategy to selectively lower the level of compounds within tumor cells that assist in energy production and protect against chemotherapy. This non-toxic approach weakens and kills cancers in a novel way.

Ce médicament démontre des résultats prometteurs et exploite une nouvelle stratégie pour abaisser le niveau des molécules dans les cellules cancéreuses qui assistent la production d'énergie et la protège contre la chimio. Cette approche non-toxique affaiblit et tue les cellules cancéreuses d'une nouvelle manière.

Apatone was discovered by Dr. Henryk Taper from the Catholic University of Leuven in Brussels, Belgium and was developed by Dr. James Jamison and Dr. Jack Summers, both of Summa Health System, and Dr. Jacques Gilloteaux, now with the American University of the Caribbean in St. Maarten. Their groundbreaking discovery found that moderate doses of Apatone eliminate many types of cancer cells, including prostate, bladder, renal and ovarian.

Apatone a été découvert par Henryk Taper et développé par James Jamison et Jack Summers. Ils ont découvert que des doses modérées d'Apatone éliminent plusieurs types de cellules cancéreuses incluant celles de la de la vessie du et de l' .

"This strategy targets cancer cells by their inflammatory response," explains Dr. Jamison. "It's a different approach than most other anti-tumor drugs, which target dividing cells or the development of blood vessels within the tumor. Since normal cells use sugars or fats for energy and cancer cells rely on glucose, the real key here is that Apatone resembles glucose. As Apatone preferentially accumulates in cancer cells, it also supplies quinone that weakens and can destroy the cancer cell from within.

"Cette stratégie cible les cellules cancéreuses par leur réponse inflammatoire" explique le docteur Jamison. "C'est une approche différente des thérapies actuelles qui ciblent la division des cellules et le développement de vaisseaux sanguins de la tumeur." Parce que les cellules saines utilisent les sucres ou les gras pour l'énergie et les cellules cancéreuse dépendent du glucose, la clé ici c'est que l'Apatone ressemble au glucose. Comme l'Apatone s'accumule de façcon préférentielle dans les cellules, il remplace la quinone ce qui affaiblit et peut détruire les cellules cancéreuses de l'intérieur.


"The bottom line is: Apatone selectively targets and kills tumor cells using non-toxic biochemistry that protects surrounding healthy tissue."
Licensed in 2004 to IC-MedTech, Inc., a California-based biotechnology company, the first clinical trial began in 2005 to evaluate the drug in prostate cancer patients. The clinical studies, which were conducted at Summa Health System in Akron, Ohio and with Dr. Ananias Diokno at William Beaumont Hospital in Royal Oak, Mich., examined the safety and effectiveness in 17 end-stage prostate cancer patients for 12 weeks. These patients took Apatone orally each day. The trials were supported by the Beaumont Foundation, Summa Health System and IC-MedTech.
Throughout the trial, investigators monitored prostate-specific antigen (PSA) levels, PSA velocity and PSA doubling times. Although PSA is a protein normally produced by the prostate gland, individuals with prostate cancer have increased levels. PSA velocity is the change of PSA levels over time and PSA doubling time is the time it takes for a patient's PSA level to double.

"The results of the trial are very promising," said Dr. Jamison. "Sixteen of the 17 patients responded positively to the Apatone and 13 showed a decrease in PSA velocity and an increase in PSA doubling time. At the end of the treatment period, 15 patients opted to continue treatment."

"Les résultats de l'essai sont très prometteurs" dit le docteur Jamison "16 des 17 patients ont répondu positivement à l'Apatone et 13 ont montré une décroissance du psa et du temps de doublement du psa. À la fin de la période de traitement 15 patients ont opté pour continuer ce traitement."

Showing delays in the biochemical progression in end-stage prostate cancer patients, the trial successfully demonstrated the safety and efficacy of orally administered Apatone. Research is continuing and insights into how this drug works have lead to collaborations and discoveries in the field of liquid crystal compounds. Apatone is a Liquid Crystal PharmaceuticalTM and has resulted in research sponsored at Summa and with Dr. Chun-che Tsai at Kent State University. This work shows great promise for cancer and other diseases.

Ce travail montre de grandes promesses pour le cancer et d'autres maladies.

"Ultimately, Apatone is intended to be administered intravenously prior to chemotherapy so it can break down the substances in a tumor that protect it from the chemotherapy and allow a greater cell kill," continued Dr. Jamison. "Between cycles and following completion of chemotherapy, Apatone will be taken orally to help prevent or slow tumor regrowth."

Although the researchers are still working to receive FDA approval for chemotherapy in conjunction with Apatone, the FDA granted orphan drug status to IC-MedTech this year for the use of Apatone as treatment for metastatic, or locally advanced, stage III and IV bladder cancer. An orphan drug designation grants special status to a product to treat a rare disease or condition.

La FDA a donné son accord pour que l'Apatone aie le statut de médicament orphelin pour le cancer de la vessie.

The American Cancer Society estimates that nearly 1.5 million new cases of cancerwill be diagnosed this year. This crisis has caused the National Cancer Institute to establish a goal of eliminating suffering and death due to cancer by the year 2015.

Le National Cancer institute s'est fixé le but d'éliminer le cancer pour l'année 2015.

Kent State University, Summa Health System and IC-MedTech Inc. have taken steps toward that goal. Their collaborative efforts have yielded an innovative liquid crystal technology that offers the promise of new drugs which may more effectively manage cancer and other diseases.

Les chercheurs font des pas vers ce but. Il y a une nouvelle technologie (liquid crystal technlogy) qui promet de nouveaux médicaments pour s'occuper plus efficacement du cancer et de d'autres maladies.

Dr. Chun-che Tsai, Kent State professor of chemistry; Dr. Jim Jamison, manager of Urology, Obstetrics and Gynecology Core Basic Research Laboratory for Summa Health System; and Mr. Tom Miller, president of IC-MedTech Inc., a California-based biotechnology company, have developed a new paradigm in drug discovery based on the pharmacologic properties of liquid crystals called Liquid Crystal Pharmaceuticals™ or LCPs.

Recently, the team gathered at Kent State University’s Office of Technology Transfer to file applications for two new patents: one for a new LCP-based anti-tumor drug called Tolecine™ and another for a formulation that combines Tolecine™ and another LCP, Apatone®.

“The path-breaking discoveries of Dr. Tsai and his colleagues offer compelling proof of the value of university research and the enormous good that can come from collaborations between universities and the private sector,” says Kent State President Lester A. Lefton. “As Kent State researchers tackle cancer and a host of other real-world ills and issues, they are bringing their leading-edge knowledge and creativity to our students and playing a significant role in economic development.”

Though best known for their use in laptops, televisions and cell phones, liquid crystals also include families of organic substances that are essential for all life called lyotropic liquid crystals. Examples of lyotropic liquid crystals include DNA, proteins and cholesterol. LCPs are a unique class of lyotropic liquid crystals that represent novel drug candidates for the treatment of a wide range of diseases.

Même si les plus connus de leurs usages sont les ordinateurs portables, télévisions et téléphones portables, les cristaux liquides incluent également des familles des substances organiques qui sont essentielles pendant toute la vie appelée les cristaux liquides lyotropic.

“Mother nature is the ultimate chemist,” says Tsai. “Although we use creative and sophisticated computer modeling techniques to screen for our candidate compounds, I’m always amazed at how nature puts it all together.”

The most recent research involving LCPs has yielded a new investigational anti-tumor drug called Tolecine™, a compound that also has antiviral and antibacterial applications. Created by Tsai, it has been shown to be even more effective than the current standard of care for herpes.

The team’s second patent application involves a formulation that combines Tolecine™ and another LCP, Apatone®, which attacks cancer cells via multiple pathways to offer improved efficacy. Apatone® has been successfully tested in more than 30 human tumor cell lines at Summa and in a Phase I/IIa clinical trial, which demonstrated a delaying effect in the progression of end-stage cancer patients. In addition, the FDA granted Apatone® orphan-drug status for the treatment of metastatic, or locally advanced, inoperable bladder cancer in August 2007.

L'équipe du second patient a emploé une combinaison de Tolecine et un autre LCP Apatonequi attaque les cellules cancéreuses par de multiples chemins pour améliorer son efficacité. L'Apatone a été employé avec succès dans plus de 30 tumeurs humaines.

Unlike other chemotherapy drugs, TolecineTM and Apatone®have low toxicity and do not target dividing cells. Instead, they are activated by inflammation that occurs in and around tumor cells, sparing healthy cells. “We want to kill cancer cells specifically without killing surrounding tissues,” says Jamison.

Tolecine et Apatone, au contraire des autres médicaments, ont de bas taux de toxicité et ne cible pas la division des cellules. Ils sont activés par l'inflammation qui se produit autour des celllules cancéreuses, épargant ainsi les cellules saines.

Innovative, low-toxicity drugs such as Tolecine™ and Apatone®provide new hope in the battle against cancer and other diseases in the next few years. “Research on LCPs provides a solid scientific foundation for generations of new drugs,” says Miller. Adds Tsai: “LCPs are an untapped frontier from which many new, exciting treatments are now emerging.