Transcript theophanides_theo

Prof.T. Theophanides
[email protected]
J. Anastassopoulou, S. Kella & K. Xenos
IN THE SEARCH OF NEW
USES FOR OLD DRUGS
DRUG DISPOSAL
 PHARMACEUTICALS
 1. Organic : Aspirin, etc.
 2.Inorganic : Boric Acid, etc.
 3. Organometallic : Metal salts, Metalcomplexes
 A lot of materials change their
properties even at ambient
temperature.
 Experimental observation of these
changes is difficult due to their very
low rate of change, which results in so
small physicochemical changes that
are, generally, immeasurable even by
the most sensitive analytical
techniques
 We have checked with FT-IR
Spectroscopy to see if there was a
change in the IR spectrum of an expired
drug compared to the normal drug.
 We found that the FT-IR spectrum did not
change at all and the two spectra were
identical.
 It is accepted that the IR spectrum of a
material is the “finger print” of that
material.
 Then what is the change that takes place
in the expired drug?
FT-IR spectra of Aspirin.
Red: normal Aspirin and
Blue: expired Aspirin
FT-IR spectra of Aspirin.
Red: normal Aspirin and
Blue: expired Aspirin
FT-IR spectra of Aspirin.
Red: normal Aspirin and
Blue: expired Aspirin
 Comparing compounds and diseases will
help find new drugs from a molecular point
of view from the publicly available database.
 A potential compatibility between
numerous drugs and diseases for which
those drugs had never been before
thought to be beneficial has been found.
 This research was performed at Stanford
School of Medicine “Math.com”.
Finding New Uses for Old Drugs
 In
another case, the drugs were
categorized based on genetic background
and not on the affected organs.
 But such leaps do occur in the medical
world, albeit typically by accident
instead of by systematic search.
Notable examples include:
 Sildenafil (Viagra) repositioned from a candidate for




hypertension to a successful drug for erectile
dysfunction
Gemcitabine (Gemzar) switched from use as an
antiviral candidate to a successful anticancer agent
Finasteride expanded use from prostate cancer
(Proscar) to hair loss (Propecia)
Thalidomide (Thalidomid) repositioned from a
discontinued antiemetic drug to a successful cancer
therapeutic
Hydroxychloroquine (Plaquenil). Expanded use from
an antiparasitic to an approved antiarthritic agent
Recycling old drugs in new
appearances
 The chance finding that a drug designed
for one purpose might fit the gap…is
discovering new uses for old drugs or
teaching an old drug new tricks!
 This could be a less costly process of
obtaining pharmaceuticals for other new
diseases.
Pharmaceutical used in this study
 Hydrocortisone : Solu-Cortef
Solu-Cortef(A)
contains
the
active
ingredient
hydrocortisone sodium succinate (B) which is a type of
compound known as a corticosteroid. Corticosteroids are
derivatives of the corticosteroid hormones cortisol and
aldosterone that are produced naturally by the adrenal
glands
Hydrocortisone : Solu-Cortef
 This medication is used to treat various
conditions such as:
 Severe allergic reactions, blood diseases,
breathing problems, certain cancers, eye
diseases, intestinal disorders, and skin
diseases.
 Hydrocortisone is a corticosteroid
hormone (glucocorticoid).
Hydrocortisone Metal-complexes
C25H33O8MCl∙5Η2Ο
Results
 Preliminary experiments showed that these
hydrocortisone metal-complexes could be used
for treating melanoma much better than the
original drug (found from melanoma tests) .
 The metals used were life metal ions, such as
Na+, K+, Mg2+, Ca2+, Fe2+, Mn2+, Zn2+, Sn2+ and
others, which would be mineralized as metal
ions in the electrolytes of the body.
 The transformation of unused drugs to
organometallic adducts could lead to new uses
of old drugs.
Fourier Transform Infrared Spectra of hydrocortisone
and its metal-complexes in the region 4000- 2500 cm-
Fourier Transform Infrared Spectra of
hydrocortisone and its metal-complexes in
the region (2000- 400 cm -1)
Conclusions
 The transformation of unused old drugs to
organometallic-adducts could lead to more active
new drugs (reactivation of old drugs).
 This novel method of recuperation of unused old
drugs could be made with the non-toxic life metals,
such as: Na+, K+, Mg2+, Ca2+, Fe2+, Mn2+, Zn2+,
Sn2+ and others.
 This new way of metallation of non-disposed old
drugs leads to a useful novel recycling method.
Old
drugs
Metallation
Thank You
Reactivated
drugs