Antibiotic list supplied in Dr. Kenny DeMeirleir's patent

8. oktober 2003 22:17

The National CFIDS Foundation has received many requests for the antibiotic
list supplied in Dr. Kenny DeMeirleir's patent.  Our medical director, Alan
Cocchetto, has given us the information to distribute.  Patients should
understand that this is not saying a "cure" will come from any of these but
that we are only supplying the patent information.


This following is taken from:  

World Patent # WO03061605 issued to K. DeMeirleir et.al.; 
Issued on 7/31/03; Filed on 1/10/03; Priority data on 1/17/02

TREATMENT METHODS
As summarized above, the subject invention provides methods for treating a
host suffering from a chronic immune disease. Specifically, the subject
invention provides methods of treating a host suffering from MS or CFS, as
well as other chronic immune diseases.

In practicing the subject methods, an effective amount of a protease
inhibitor, more specifically a serine protease inhibitor, is administered
to the patient in need thereof, i. e. , the patient suffering from the
chronic immune disease. More specifically, an effective amount of an
elastase inhibitor is administered to the patient in need thereof.
By"inhibit"is meant that these agent at least reduces, if not
substantially or complete stops, the protease, e. g., elastase, mediated
cleavage of RNase L protein. RNase L protein cleavage-inhibitory agents of
interest typically reduce the cleavage or RNase L by at least about 2
fold, usually at least about 3 fold and more usually at least about 5
fold. Any suitable protease, e. g., elastase, inhibitor may be employed.

Of particular interest in certain embodiments are beta-lactam containing
agents including, but not limited to: penicillins, nocardins, ampicillin,
cloxacillin, oxacillin, and piperacillin, cephalosporins and other cephems
including, e. g., cefaclor, cefamandole, cefazolin, cefoperazone,
cefotaxime, cefoxitin, ceftazidime, ceftriaxone, and cephalothin ; and the
like. As such, agents of interest include, but are not limited to:
Amifloxacin ; Amifloxacin Mesylaté ; Amikacin; Amikacin Sulfate ;
Aminosalicylic acid; Aminosalicylate sodium ; Azlocillin ; Aziocillin
Sodium; Bacampicillin Hydrochloride ; Carbenicillin Disodium;
Carbenicillin Indanyl Sodium; Carbenicillin Phenyl Sodium; Carbenicillin
Potassium ; Carumonam Sodium; Cefaclor ; Cefadroxil ; Cefamandole ;
Cefamandole Nafate; Cefamandole Sodium; Cefaparole ; Cefatrizine;
Cefazaflur Sodium; Cefazolin ; Cefazolin Sodium; Cefbuperazone; Cefdinir;
Cefepime; Cefepime Hydrochloride ; Cefetecol ; Cefixime; Cefmenoxime
Hydrochloride ; Cefmetazole ; Cefmetazole Sodium; Cefonicid Monosodium;
Cefonicid Sodium; Cefoperazone Sodium; Ceforanide; Cefotaxime Sodium;
Cefotetan; Cefotetan Disodium; Cefotiam Hydrochloride ; Cefoxitin;
Cefoxitin Sodium; Cefpimizole ; Cefpimizole Sodium; Cefpiramide;
Cefpiramide Sodium; Cefpirome Sulfate ; Cefpodoxime Proxetil ; Cefprozil ;
Cefroxadine; Cefsulodin Sodium; Ceftazidime; Ceftibuten; Ceftizoxime
Sodium; Ceftriaxone Sodium; Cefuroxime; Cefuroxime Axetil ; Cefuroxime
Pivoxetil ; Cefuroxime Sodium; Cephacetrile Sodium; Cephalexin ;
Cephalexin Hydrochloride ; Cephaloglycin ; Cephaloridine ; Cephalothin
Sodium; Cephapirin Sodium; Cephradine; Cetocycline Hydrochloride ;
Cetophenicol ; Chlortetracycline Bisulfate ; Chlortetracycline
Hydrochloride ; Ciprofloxacin ; Ciprofloxacin Hydrochloride ; Colistin
Sulfate ; Coumermycin; Coumermycin Sodium; Doxycycline ; Doxycycline
Calcium ; Doxycycline Fosfatex; Doxycycline Hyclate ; Droxacin Sodium;
Enoxacin; Epicillin ; Epitetracycline Hydrochloride ; Imipenem ; Kanamycin
Sulfate ; Meclocycline ; Minocycline ; Minocycline Hydrochloride ;
Nafcillin Sodium; Norfloxacin ; Ofloxacin ; Oxytetracycline ;
Oxytetracycline Calcium ; Piperacillin Sodium; Pirbenicillin Sodium;
Tetracycline ; Tetracycline Hydrochloride ; Tetracycline Phosphate Complex
; Ticarcillin Cresyl Sodium; Ticarcillin Disodium; Ticarcillin Monosodium;
Tobramycin ; and Tobramycin Sulfate.

As mentioned above, in the subject methods an effective amount of one or
more of the above described active agents is administered to the host,
where "effective amount"means a dosage sufficient to produce a desired
result, where the desired result is at least an amelioration, if not
complete cessation, of the chronic immune disease symptoms. More
specifically, the amount of agent that is an effective amount of an agent
is an amount that inhibits RNase L protein cleavage, i. e., protects
native, high molecular weight RNase L protein from proteolytic attack (e.
g. , by elastase) and subsequent fragmentation specifically in PBMC. By
reducing the amount of RNase L protein fragmentation, the amount of native
RNase L protein is increased by at least about 2 fold, usually by at least
about 3 fold and more usually by at least about 5 fold, as compared to
that observed in a control, e. g. , a PBMC from the host that has not been
contacted by the active agent (s), when contacted with an effective amount
of the inhibitor. While exact amounts may vary depending on the nature of
the agent and delivery vehicle employed, and can be readily determined
empirical by those of skill in the art, in many embodiments, the amount of
agent that is administered in any given dose generally ranges from about
10 micrograms per kilogram total body weight to about 1 gram per kilogram
total body weight, usually from about 1 milligram per kilogram total body
weight to about 100 milligrams per kilogram total body weight. A
particular treatment regimen may include a single dose, or a plurality of
different doses administered over various time intervals, e. g., hourly,
daily, weekly, monthly, etc.

In the subject methods, the active agent (s) may be administered to the
host using any convenient means capable of resulting in the desired
treatment. Thus, the agent can be incorporated into a variety of
formulations for therapeutic administration. More particularly, the agents
of the present invention can be formulated into pharmaceutical
compositions by combination with appropriate, pharmaceutical acceptable
carriers or diluents, and may be formulated into preparations in solid,
semi-solid, liquid or gaseous forms, such as tablets, capsules, powders,
granules, ointments, solutions, suppositories, injections, inhalants and
aerosols.

As such, administration of the agents can be achieved in various ways,
including oral, buccal, rectal, parenteral, intraperitoneal, intradermal,
transdermal, intratracheal, etc. , administration.

In pharmaceutical dosage forms, the agents may be administered in the form
of their pharmaceutically acceptable salts, or they may also be used alone
or in appropriate association, as well as in combination, with other
pharmaceutical active compounds. The following methods and excipients are
merely exemplary and are in no way limiting.

For oral preparations, the agents can be used alone or in combination with
appropriate additives to make tablets, powders, granules or capsules, for
example, with conventional additives, such as lactose, mannitol, corn
starch or potato starch ; with binders, such as crystalline cellulose,
cellulose derivatives, acacia, corn starch or gelatins ; with
disintegrators, such as corn starch, potato starch or sodium
carboxymethylcellulose ; with lubricants, such as talc or magnesium
stearate; and if desired, with diluents, buffering agents, moistening
agents, preservatives and flavoring agents.

The agents can be formulated into preparations for injection by
dissolving, suspending or emulsifying them in an aqueous or nonaqueous
solvent, such as vegetable or other similar oils, synthetic aliphatic acid
glycerides, esters of higher aliphatic acids or propylene glycol ; and if
desired, with conventional additives such as solubilizers, isotonic
agents, suspending agents, emulsifying agents, stabilizers and
preservatives.

The agents can be utilized in aerosol formulation to be administered via
inhalation. The compounds of the present invention can be formulated into
pressurized acceptable propellants such as dichlorodifluoromethane,
propane, nitrogen and the like.

Furthermore, the agents can be made into suppositories by mixing with a
variety of bases such as emulsifying bases or water-soluble bases. The
compounds of the present invention can be administered rectally via a
suppository. The suppository can include vehicles such as cocoa butter,
carbowaxes and polyethylene glycols, which melt at body temperature, yet
are solidified at room temperature.

Unit dosage forms for oral or rectal administration such as syrups,
elixirs, and suspensions may be provided wherein each dosage unit, for
example, teaspoonful, tablespoonful, tablet or suppository, contains a
predetermined amount of the composition containing one or more inhibitors.
Similarly, unit dosage forms for injection or intravenous administration
may comprise the inhibitor (s) in a composition as a solution in sterile
water, normal saline or another pharmaceutical acceptable carrier.

The term"unit dosage form, "as used herein, refers to physically discrete
units suitable as unitary dosages for human and animal subjects, each unit
containing a predetermined quantity of compounds of the present invention
calculated in an amount sufficient to produce the desired effect in
association with a pharmaceutical acceptable diluent, carrier or vehicle.
The specifications for the novel unit dosage forms of the present
invention depend on the particular compound employed and the effect to be
achieved, and the pharmacodynamics associated with each compound in the
host.

The pharmaceutical acceptable excipients, such as vehicles, adjuvants,
carriers or diluents, are readily available to the public. Moreover,
pharmaceutical acceptable auxiliary substances, such as pH adjusting and
buffering agents, tonicity adjusting agents, stabilizers, wetting agents
and the like, are readily available to the public.

Those of skill in the art will readily appreciate that dose levels can
vary as a function of the specific compound, the severity of the symptoms
and the susceptibility of the subject to side effects. Preferred dosages
for a given compound are readily determinable by those of skill in the art
by a variety of means.

As mentioned above, by treatment is meant that at least an amelioration of
the symptoms associated with the chronic immune disease, where
amelioration is used in a broad sense to refer to at least a reduction in
the magnitude of a parameter, e. g. symptom, associated with the condition
being treated. As such, treatment also includes situations where the
pathological condition, or at least symptoms associated therewith, are
completely inhibited, e. g. prevented from happening, or stopped, e. g.
terminated, such that the host no longer suffers from the condition, or at
least the symptoms that characterize the chronic immune disease condition.