FOR THE TREATMENT
OF ALL IRON
DEFICIENCY RELATED
ANEMIAS
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IRON AND ITS FUNCTIONS
Iron is an essential element for living cells, given its ability to gain
and lose electrons.
However, excess iron can be toxic because of its capacity to bind
electrons to oxygen, thus causing the generation of reactive oxygen
species (ROS).
All organisms have developed strategies that allow acquiring,
binding and storing elemental iron in an non-toxic, readily available
form. Absorption of nearly all dietary Iron ( 1-2 mg per day) takes
place in the proximal duodenum.
Excessive iron absorption results in iron-overload in the
parenchymal tissues, while low iron absorption leads to plasma iron
deficiency, which manifests itself as hypoferremia (iron deficiency,
ID) and iron deficiency anemia (IDA).
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IRON AND ITS FUNCTIONS
ID is the most common nutritional deficiency, affecting about two
billion people worldwide. There are three prominent ways to
prevent and control the development of ID and IDA: dietary
diversification, food fortification and individual supplementation. The
preferred treatment of these pathologies is generally the oral
administration of iron as ferrous sulfate.
Oral administration, however, can cause many side effects
including gastro-intestinal discomfort, nausea, vomiting diarrhea,
constipation and may increase the patients susceptibility to
infections.
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DESCRIPTION
SIDERAL FORTE is composed of protected Iron and Vitamin C, useful in case of
deficiency or increased requirements. The iron, included in SIDERAL FORTE is
uniquely coated using a liposomal technology that allows the molecule to pass
through the stomach, avoiding any gastrointestinal irritation, to be directly absorbed
through the lining of the gastrointestinal tract.
REGULATORY STATUS Dietary supplement
MAIN INGREDIENTS
INDICATION
IP
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Liposomal Iron
Dietary support for patients being treated with EPO
Enhances serum iron levels for Chronic Kidney Disease and Dialysis patients
Increases the oxygen carrying ability of blood for radiation and chemotherapy
patients
Prior art 2012 estimate expiration 2032
TENTATIVE LABEL US SiderAL Forte Capsules
Dietary Supplement
Rx Only
Description: SIDERALFORTE is a dietary supplement based on protected liposomal Iron,
Vitamin C.
Contents
Liposomal Iron
Vitamin C
Per 100 g
5.04 g
10,667 g
Per 1 cps
30 mg
64 mg
% RDA
214.3%
80.0%
Indications and Usage: SIDERAL FORTE For the treatment of all anemias responsive to
oral iron therapy, such as hypochromic anemia associated with pregnancy, chronic or acute
blood loss, dietary restriction, metabolic disease and post-surgical convalescence. Useful in
treating iron deficiency anemia or increased requirements of Iron and Vitamin C. The iron
included in SIDERAL FORTE, is uniquely coated with liposomal technology that allows the
molecule to pass through the stomach, avoiding any gastrointestinal irritation, to be directly
through the lining of the gastrointestinal tract.
Dosage: Take one capsule per day with a glass of water.
How Supplied: 20 capsules of 600 mg,
Gluten free
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Net wt. 12 g
IP: Composition Method, Patent Pending
WIPO Patent application WO 2014/009806 A1
SOLID COMPOSITION COMPRISING IRON FOR USE IN IRON DEFICIENT CONDITIONS
Abstract: The present invention relates to an iron-based composition, for use in conditions of total or
relative iron deficiency. In particular, the present invention relates to a solid composition, preferably in
the form of powder or granules, for use in the treatment of disorders or diseases related to or derived
from an iron deficiency. The composition of the present invention is suitable for pediatric subjects,
adolescents, athletes, men, women, pregnant women and elderly. Finally, the present invention relates
to a process for preparing said solid composition.
PATENT CLAIMS I:
1. A solid composition for use in the treatment of disorders or diseases related to an iron deficiency comprising or, alternatively, consisting of an iron (III) salt, sucrose
esters or sucresters E473 and a lecithin.
2. The composition for use according to claim 1, wherein said composition further comprises a gelatinized or pregelatinized starch.
3. The composition for use according to claims 1 or 2, wherein said iron (III) salt is ferric pyrophosphate; said iron (III) salt is in an amount comprised from 30 to 70%,
preferably from 40 to 60% by weight.
4. The composition for use according to claims 1-3, wherein said sucrose esters or sucresters E473 are in an amount comprised from 10 to 30%, preferably from 15
to 25% by weight.
5. The composition for use according to any one of claims 1-4, wherein said lecithin is a lecithin E322 and is selected from the group comprising the maize, sunflower
or soya lecithin; said lecithin is in an amount comprised from 0.1 to 1.5, preferably from 0.4 to 1% by weight.
6. The composition for use according to any one of claims 1-5, wherein said sucrose ester or sucrester and said lecithin are in the composition in a weight ratio
comprised from 25:1 to 20:1; preferably in a weight ratio comprised from 20:1 to 15:1.
7. The composition for use according to any one of claims 1-6, wherein said gelatinized or pregelatinized starch is selected from the group comprising rice starch or
maize starch; said starch is in an amount comprised from 15 to 40%, preferably from 20 to 35% by weight.
PATENT CLAIMS II:
8. The composition for use according to any one of claims 1-7, wherein the iron pyrophosphate is in an amount comprised from 50 to 55% by weight; the sunflower lecithin
is in an amount comprised from 0.5 to 0.8 by weight; sucrester E473 is in an amount comprised from 16 to 20% by weight; the gelatinized or pregelatinized rice starch is in
an amount comprised from 25 to 30% by weight.
9. The composition for use according to any one of claims 1-8, wherein said solid composition for oral use has a particle size comprised from 8 to 16 microns, preferably
from 10 to 14 microns; a bulk density comprised from 0.3 to 0.8 g/ml, preferably from 0.4 to 0.7 g/ml and an iron (III) content comprised from 60 mg/g to 140 mg/g,
preferably from 80 mg/g to 120 mg/g, even more preferably from 90 to 110 mg/g.
10. A supplement product or a medical device or a pharmaceutical composition for oral use comprising the solid composition for oral use according to any one of claims 19 for use in the treatment of disorders or diseases related to an iron deficiency in pediatric subjects, adolescents, athletes, men, women, pregnant women and elderly.
11. A supplement product or a medical device or a pharmaceutical composition according to claim 10, for use in pediatric subjects, adolescents, athletes, men, women and
elderly for preventing anemia and increasing the hemoglobin and ferritin values; or for use in pregnant women for increasing the birth weight of the newborn, preventing
maternal anemia and increasing the hemoglobin and ferritin values both during pregnancy and after birth.
12. A supplement product or a medical device or a pharmaceutical composition according to claims 10 and 11, for use in pediatric subjects, adolescents, athletes, men,
women and elderly over a period comprised from 1 to 5 months, preferably from 2 to 4 months; or for use in pregnant women to be administered throughout the pregnancy
period, in particular from 12th week, until 6 weeks postnatal.
13. A supplement product or a medical device or a pharmaceutical composition according to claims 10-12, for use in pediatric subjects, adolescents, athletes, men,
women, pregnant women and elderly, at a dose comprised from 10 to 40 mg of iron (III)/day, preferably from 14 to 30 mg of iron (III)/day, even more preferably 28 mg of
iron (III)/day.
Clinical Data
International
publications
1 paper submitted
2 in medical writing
2 new studies (oncology,
gastroenterology)
2 new posters
(hematology,
gastroenterology)
Oncology,
Nephrology,
Haematology
6 published studies vs.
ferrous sulfate and I.V.
Iron Posters at EU and
World Congresses
International
publications
1 new study (pregnant
women)
Pregnant women
Study vs. ferrous sulfate
Poster and oral
presentations at EU and
World Congresses
CLINICAL STUDY I
SAFETY AND EFFICACY OF ORAL LIPOSOMAL IRON SUPPLEMENTED IN
ONCOLOGIC PATIENTS WITH CHEMOTHERAPY-RELATED ANEMIA RECEIVING
EPOETIN ALFA
National Congress Medical Oncology, Bologna, Italy, November 2011
57 patients, from 39 to 76 years old with chemotherapy related anemia, treated with
chemotherapy, epoetin alfa plus oral liposomal iron
RESULTS
Significant increase of Hb (Hemoglobin) response (> 2g/dl above baseline)
Improvement in Quality of Life level/ High tolerability
None of the patients required red blood cell transfusion
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CLINICAL STUDY II
SAFETY AND EFFICACY OF ORAL LIPOSOMAL IRON SUPPLEMENTED IN
ONCOLOGIC PATIENTS WITH CHEMOTHERAPY-RELATED ANEMIA RECEIVING
EPOETIN ALPHA, FINAL DATA
ESMO Congress, Wien, 2012
Total of 72 patients, from 39 to 76 years old with chemotherapy related anemia,
treated with chemotherapy, epoetin alpha plus oral liposomal iron 30 mg once daily
for 8 week
RESULTS
Significant increase of Hb (Hemoglobin) response (> 2g/dl above baseline)
Improvement in Quality of Life level/ High tolerability
None of the patients required red blood cell transfusion
CONCLUSIONS
Daily supplementation with LI is safe and produces a significant increase in Hb
This regimen offers an optimal alternative to IV iron supplementation
LI is the best choice to combine the treatment with EPO
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CLINICAL STUDY III
USE OF LIPOSOMAL IRON IN PATIENTS WITH CHRONIC KIDNEY FAILURE
AND LOW TOLERABILITY TO FERROUS SULPHATE UNDER
CONSERVATIVE TREATMENT
Nephrology and Dialysis units, Benevento and SantAndrea (Rome) hospitals
Evaluation of efficacy and adverse effects in 17 patients affected by kidney
failure and using liposomal iron (1 capsule per day) instead of ferrous
sulphate
Evaluation at T0 and T1 (3 months after treatment)
Parameters: hemoglobin, ferritin, transferrin saturation, sideremia, transferrin
RESULTS
Significant increase of all parameters (serum iron, ferritin, hemoglobin)
Liposomal iron therapy is a valid alternative to ferrous sulfate
No adverse events have been reported in using LI (such as gastro intestinal
side effects)
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CLINICAL STUDY IV
EFFICACY OF ORAL LIPOSOMAL IRON VS INTRAVENOUS IRON FOR
THE TREATMENT OF IRON DEFICIT IN PATIENTS WITH CHRONIC
KIDNEY DISEASE NOT IN DIALYSIS, PILOT STUDY
University of Naples and Cardarelli Hospital, Campobasso, Italy
patients (14 patients treated with liposomal iron and 7 treated with intravenous
iron)
8 weeks treatment
Primary end-point: evaluation of the hemoglobin increase at the end of the
therapy
RESULTS
After 8 weeks treatment anemic patients suffering from chronic renal failure
significantly increased their level of hemoglobin vs intravenous iron treated
patients, with minor adverse effects
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CLINICAL STUDY V
EFFICACY OF ORAL LIPOSOMAL IRON VS INTRAVENOUS IRON IN
PATIENTS WITH REFRACTORY ANEMIA, MONOCENTRIC STUDY
University of Messina & Campobasso, Italy
24 patients recruited from June 2008 to December 2010
Randomized study:
o Group A treated with intravenous iron plus erythropoietin alpha
o Group B treated with liposomal iron plus erythropoietin alpha
RESULTS
Therapy with liposomal iron is safe, effective and has demonstrated non
inferiority vs. therapy with intravenous iron (which had minor adverse events,
erythema and hypotension)
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CLINICAL STUDY VI
ERYTHROPOIETIN ALPHA VS BIOSIMILAR ERYTHROPOIETIN ALPHA
PLUS LIPOSOMAL IRON AND B12 FOLATES IN PATIENTS WITH
REFRACTORY ANEMIA, TWO CENTERS PROSPECTIVE STUDY
Poster presented at International Symposium on Supportive Care in Cancer,
New York, June 2012
86 patients affected by refractory anemia
2 groups, one treated with erythropoietin alpha, one with bio similar
erythropoietin alpha
End Point: verify non inferiority of bio similar erythropoietin in terms of
safety, efficacy and costs
RESULTS
Bio similar erythropoietin alpha plus liposomal iron, B12 and folates support
appears to be safe, feasible, cost-effective and non inferior to classical
erythropoietin alpha support in patients affected by refractory anemia.
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Product Positioning
Practice Type
General Practitioner (GP)
Gastroenterologist
Geriatrician
Surgeon
Endocrinologist
Indications
Iron-deficiency anemia (including celiacs)
Patients undergoing gastrointestinal resection or with G.I. lesions
Severe blood loss during surgery
Practice Type
Gynecologist
Obstetrician
Indications
Iron deficiency from menstruation or gynecologic problems
Premenstrual Syndrome
Pregnant women
Female athletes
Practice Type
Oncologist
Hematologist
Nephrologist
Radiologist
Indications
Iron-deficiency anemia, (including celiacs)
Anemia in hematologic patients
Anemia in oncological patients (from chemotherapy/radiotherapy treatment, neoplastic pathology)
Patients with cancer-related fatigue
Nephropathic patients under iron supplementation: conservative treatment or substitution treatment
(hemodialysis and pre-dialysis)
Patients under iron supplementation with Erythropoietin (EPO)
Patients undergoing gastrointestinal resection or with gastrointestinal tract lesions, causing bleed
Iron supplementation supporting or substituting iron intravenous therapy
2008 2012 SiderAL Portfolio sales show a Compound
Annual Growth Rate of 45%(sales performance Italy)
SIDERAL
700.000
600.000
Sales per unit
500.000
400.000
SIDERAL
608.331
300.000
488.597
200.000
312.052
100.000
148.673
198.017
0
2008
2009
2010
2011
2012
Lineare (SIDERAL)
SiderAL sales are 94% of the market increase from 2008
through 2012 (Italy)
SiderAL sells 4 times more than nearest competitor
even if is priced 60% above the average market price
600.000
564.416
500.000
Sales per unit
400.000
300.000
2012
200.000
125.715
100.000
80.884
55.978
53.123
46.442
36.289
31.878
29.144
23.004
22.066
22.045
19.672
19.240
15.322
15.140
14.693
14.394
13.715
11.772
11.320
