For your information, in Nortran's most recent quarterly report the following scientific update can be found:
SCIENTIFIC UPDATE
The Company has continued to focus its scientific efforts on research and development of new antiarrhythmic drugs to treat life-threatening malfunctions known as ventricular arrhythmias. These electrical malfunctions occur during or following a myocardial infarction.
From its research and development programme the Company has identified compounds with unique characteristics which offer a potentially superior therapeutic method of treating arrhythmias, thus preventing Sudden Cardiac Death. The "unique characteristics" that the Company has focussed on developing include; ischaemia selectivity, greater selectivity for cardiac ion channels, greater safety margins over currently available treatments and suitability for oral and/or intravenous administration.
The search for these specific attributes have led to the identification of three classes of antiarrhythmics that the Company has brought to different stages of development:
1. AAA (acute antiarrhythmic) - Preclinical
This series of compounds has been developed for the acute treatment of arrhythmias in emergency situations (i.e. following a heart attack). This compound has a short duration of action, blocks sodium and potassium channels and is selective for ischaemic tissue.
2. AAC (chronic antiarrhythmic) - Preclinical
This series of compounds has been developed as a drug for administration over a longer period of time than the AAA. This drug may be used intravenously in the acute stages of the heart attack and orally in the later stages (0-3 months post-myocardial infarction).
3. AAP (prophylactic antiarrhythmic) - Research
The AAP series under research by the Company are compounds having all the attributes of the AAC series, but has an even greater degree of pathology targeting, conferring upon the agent the high therapeutic index needed for a drug to be used chronically as a prophylactic against SCD. This drug will be orally active and will persist long enough after each dose to allow a once or twice daily dosing regimen.
RSD921
The Company is continuing preparation of its local anesthetic, RSD921, for Phase II clinical trials. The trial will be conducted in Malaysia in association with Nortran's partner, the Chemical Company of Malaysia. It is anticipated that the trials will begin in the period late May to early June.
A clinical trials batch has been synthesized and is currently being prepared for formulation. The clinical trials site and investigators have been confirmed at the University of Malaysia, Kuala Lumpur, Malaysia, and the necessary ethical approvals have been granted. CCM has filed with the Malaysian Ministry of Health for government approval to import and use RSD921 in the above clinical trials. Governmental approval is expected in the immediate future.
AAA
The novel AAA series of compounds have shown exciting results in a laboratory setting and promise to create a new standard for treatment of arrhythmias in the acute setting. These studies indicate that this fast-acting and intravenous drug also offers potential use for patients at risk from arrhythmias during surgery. The clinical development plan has been completed under contract by Premier Research Worldwide. Discussions with potential licensees continue.
AAC
The company continues to concentrate on improving the profile of its orally-active ischaemia-selective ventricular antiarrhythmics. Significant advances have been made in improvements to the therapeutic index and in the bioavailability after oral administration. These are key factors to a successful chronic drug therapy for ventricular arrhythmias. The company expects to advance a clinical candidate through preclinical toxicology towards an IND filing in 1999.
AAP
The AAP series under research by the Company are compounds having all the attributes of the AAC series, but has an even greater degree of pathology targeting, conferring upon the agent the high therapeutic index needed for a drug to be used chronically as a prophylactic against SCD. This drug will be orally active and will persist long enough after each dose to allow a once or twice daily dosing regimen. Currently, the Company's scientists are concentrating on solving the problem of combining these attributes in a single compound .
Nociblocker
In addition to the antiarrhythmic project, the Company is collaborating with scientists to research a new class of analgesic drugs called "Nociblockers". These compounds selectively block the generation of the electrical signal of pain at its source at fine nerve endings. As such, nociblockers may have significant advantages over drugs which act on other targets in the periphery of the body and in the brain. The initial area in which the Company anticipates that the lead nociblocker would be most effectively utilized is in the area of severe or intractable pain.
In November, 1997, the Company acquired rights to a series of peripheral analgesic drugs ("Nociblockers"). The Nociblocker agreement provides that Nortran will pay to each of Drs. MacLeod and Quastel $25,000 in each of the first five years as a University grant-in-aid, commencing April 1, 1997. Nortran will also pay to each of Drs. MacLeod and Quastel, $250,000 upon commencement of Phase III clinical trial on a Nociblocker acquired by Nortran under this agreement, and a further $1,000,000 upon the filing of a new drug application in the United States of America or Canada for a Nociblocker acquired by Nortran under this agreement. The Nociblocker agreement further provides that Nortran will spend a minimum of $200,000 per year on the research and development for the research of Nociblocker drugs. The company is currently planning to initiate preclinical toxicology with its 1st generation nociblocker in 1998.
Dermal Anesthetic
Nortran Pharmaceuticals has signed an agreement with Bridge Pharma Inc. a private pharmaceutical research and development company to collaborate on the research and development of a series of novel dermal anaesthetic compounds. These dermal anaesthetic compounds being developed in collaboration with Bridge Pharma are simple, small molecule indanamine compounds. The lead compound was found to have greater potency and longer duration of action than lidocaine and tetracaine as a topical anaesthetic. It also displayed reduced toxicity compared to tetracaine. Nortran and Bridge Pharma are currently screening a series of compounds derived from the lead compound.
Libido Enhancers
Nortran has discovered compounds that have pro-erectile/libido enhancing (LE) effects in pre-clinical assays. Current erectile dysfunction therapy consists of intra-eurethral suppositories (Vivus MUSE) or intra-cavernosal injectables (e.g. Caverject). An orally active drug has just been marketed by Pfizer (Viagra), which is expected to open up the market for sexual dysfunction. Nortran's pro-erectile compounds offer the possibility of oral dosing with a very positive compliance profile. An extensive preclinical efficacy package has been completed for Nortran's lead compound. While Nortran's management appreciates the commercial potential for its LE compounds, it is recognized that this area of research lies outside the Company's major focus. As such, Nortran's strategy is to licence out its LE compounds in 1998.
|
