3.- R&D DIVISION

Propagation of native plants in vitroThe R&D Division is the raison d´être of CEAMED S.A., and its objective is to produce new drugs, focusing on anticancer compounds, although depicting interest in other fields such as antiparasitic molecules.

The aim product of CEAMED S.A. R&D Division is an active compound that would have completed all preclinical studies, and would be ready to enter clinical studies.

The main focus of the activity of the R&D Division lies on anticancer compounds directed to specific therapeutic targets i.e. topoisomerase-II, SERMs, SARMS and protein-kinase inhibitors.

The market of such products is the international pharmaceutical industry.

 

3.1.-  R&D DIVISION STRATEGY

Interaction with ERß CEAMED S.A. TriterpenoquinonaCEAMED S.A. R&D Division maintains narrow relationships with university and hospital research groups but also has got its own scientific staff that gives autonomy for:

  • Obtaining natural products from the rich biodiversity of the Macaronesian archipelagos (Canarias, Madeira, Azores), together with determining their structure elucidation, as well as the formation of more active derivatives by semisynthesis of natural structures.
  •  Obtaining new chemical entities by plant biotechnology means, including genetic engineering of metabolic pathways in in vitro culture systems, to thus improve yields of pharmaceutical interesting products.
  • In silico rational design of new products, based on the interaction among designed molecules and the active sites of enzymes, receptors or other therapeutic targets for cancer; therefore, in CEAMED S.A. we are able to tailor make an inhibitor o blocker of the active site of a target centre.
  • Total synthesis of new chemical entities, generally small sized organic or organometallic molecules, employing different chemistries, producing them in the right degree of purity required by the pharmaceutical industry.
  • Pharmacological activity bioassays of the newly synthesized or modified compounds run in different systems such as in vivo as well as ex vivo and/or in vitro, with a broad range of state-of-the-art technologies providing results with high efficacy and speed.
  •  To study synergies between radiation (radiotherapy) and cytotoxicity, this being an originality of CEAMED S.A. R&D, which allows rapid progress in the knowledge and development of new compounds improving the efficacy of the radiation on the tumours.

 

3.2.-  PRODUCTS AND DEGREE OF DEVELOPMENT

3.2.1.-  CEAMED S.A. patents

CEAMED S.A. has filed three patents of its products with high interest for the pharmaceutical industry.

- FENBUNAFIDE, an anticancer compound of the Amonafide family, a drug invented by Prof. Fernández-Braña (a shareholder of CEAMED S.A. and member of the Board of Directors), designed for the treatment of various cancer types, including prostate and leukaemia, and already in the latest stages prior to its clinical launch.  FENBUNAFIDE is a DNA intercalant agent as well as topoisomerase-II inhibitor; currently, under development in CEAMED S.A. in a study funded by Consejería de Industria of the Canary Government.  New data on its in vitro activity suggest a better activity than Amonafide.  Assays employing nude mice are also being conducted.  Furthermore, it has been demonstrated that Fenbunafide acts synergistically with radiation, inducing cytotoxicity in tumour cell lines.  In order to obtain an appropriate formulation, CEAMED S.A. has synthesized the needed amount of FENBUNAFIDE to begin its galenic development.  The preclinical studies with Fenbunafide are estimated to be complete in 2011.

- VALPENTIN, is a product designed to combat and treat neurogenic pain often suffered by cancer patients.  At present, its pharmacodynamics is being investigated and CEAMED S.A. has already established the analytical protocols needed.  Furthermore, experiments for determining its biological efficacy have already being initiated in collaboration with University of Las Palmas de Gran Canaria.  There is not an estimated date of accomplishing the preclinical studies of Valpentin. In order to carry out these studies and to obtain the necessary fundings, a project entitled "Preclinical Development of the antitumor diphenylbutyrate of amonafide (Fenbunafide)" was submitted for its evaluation.  The project was funded by the Department of Employment, Industry and Commerce of the Canary Islands Government within the FEDER Operational Programme Canary Islands 2007 -2013, with a FEDER contribution rate of 85% of the obtained grant.

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- CEAMED S.A. also filed another patent in 2009 of an invention for the continuous production of 22ß-hydroxytingenone, tingenone and derived nortriterpene methylen quinones by biotechnological methods. 

 

3.2.2.- New anticancer compounds

CEAMED S.A. possesses a growing number of candidates as new drugs under different stages of development, some of them already filed as patents or about to be submitted.

jak-stat inhibitorsThe majority of the products under investigation are organic products of low molecular weight, obtained mainly from the rich Canary biodiversity or inspired from them.  The candidate products are based on solid preclinical data demonstrating their anticancer activities, and are currently being further investigated by multidisciplinary teams.

From the most advanced projects we can stand out the following inhibitors:

  • JAK-STAT pathway
  • Topoisomerase-II
  • SERMs & SARMs

 

3.2.1.1. TOPINIB CEAMED

The objective of this project is the design of new Topoisomerase-II inhibitor products, departing from the technology developed for Fenbunafide already patented.

Nowadays, CEAMED S.A. studies two families of Topoisomerase-II inhibitors. One is based on synthetic structures, and the other on natural product and derivatives that were demonstrated to possess attractive Topoisomerase-II inhibitory activity.

            3.2.1.2.            JAKINIB CEAMED

This project is based on the design of new inhibitory drugs of the JAK-STAT intracellular pathway.  The JAK-STAT pathway is very important since it is involved in cancer, inflammation and diabetes.  Nowadays, we are in the phase of rational in silico design of specific inhibitory molecules, we are studying the in silico interactions between the new virtual molecules and the crystal structure of JAK enzymes.

            3.2.1.3.            PARASITICKILL CEAMED

CEAMED S.A. maintains a collaboration with University of Las Palmas de Gran Canaria Vet School developing new antiparasitic products to treat cattle parasitic infections.

In February 2010, CEAMED submitted a patent describing Canarian endemic plant extracts as vermifuge, antiseptic and insecticide product to the Spanish Patent and Trademark Office (OEPM)

In order to carry out these studies and to obtain the necessary fundings, a project entitled "Development of an antiparasitic natural compound  for livestock use " was submitted for its evaluation.  The project was funded by the Department of Employment, Industry and Commerce of the Canary Islands Government (ref EBT-TF-09/001) within the FEDER Operational Programme Canary Islands 2007 -2013, with a FEDER contribution rate of 85% of the obtained grant.

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3.3       EXPANSION OF THE R&D DIVISION ON NEW DRUGS

Docking genisteína en ERalfaIn order to assure that the first CEAMED S.A. products, which had completed the required preclinical studies, would have time to enter the market, the R&D Division on new drugs requires a continuous supply of funds during a minimum of three additional years (2012)

The funds will come from contributions from the Generic Drugs Division, our proper funds, as well as public funds gained through competitive calls (Spanish Government, Canary Islands Government, Tenerife Local Council, and Universities)

The Board of Directors estimates that the Division of New Drugs will have a positive cash flow from 2013 onwards, and would be able to recover the invested funds in 2015.