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Recent Patents on Endocrine Metabolic
& Immune Drug Discovery
ISSN: 1872-2148

Recent Patents on Endocrine,
Metabolic & Immune Drug Discovery
Volume 4, Number 1, January 2010
Contents
Patented Novelties in Immunoisolation for the Treatment of
Endocrine Disorders Pp. 1-9
Paul de Vos, Barbro Melgert and Marijke M. Faas
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Article]
Medullary Thyroid Cancer: New Targeted
Molecular Therapies Pp. 10-14
Alessandro Antonelli, Silvia Martina Ferrari, Poupak Fallahi,
Michele Minuto, Alda Corrado, Rossella Bruno and
Paolo Miccoli
[Abstract] [Purchase
Article]
Impact of Antihypertensive Drug Use
on Bone Mineral Density and Osteoporotic Fracture - From an
Epidemiological Perspective Pp. 15-33
Naomi Masunari and Saeko Fujiwara
[Abstract] [Purchase
Article]
Recent Methods for Assessing Bone Mineral
Density, Bone Strength, Fracture Risk and Therapeutic Effects
on Osteoporosis Pp. 33-42
Kazuhiro Imai
[Abstract] [Purchase
Article]
Diabetes Vaccinations: An Overview
Pp. 43-46
Sanjay Kalra, Navneet Agrawal, Bharti Kalra, Amit Sharma
and Ritu Kamboj
[Abstract] [Purchase
Article]
Pharmacotherapy for Obesity
Pp. 47-58
Alex H.C. Wong, Stefani S.N. Barg, and Alexander
K.C. Leung
[Abstract] [Purchase
Article]
The Therapeutic Potential of Microencapsulate
Implants: Patents and Clinical Trials Pp. 59-68
Carlos Spuch and Carmen Navarro
[Abstract] [Purchase
Article]
The Possible Use of Terpene Compounds
in DC Immunotherapy against Cancer Pp. 69-74
Masao Takei, Akemi Umeyama and Je-Jung Lee
[Abstract] [Purchase
Article]
The Stomach as an Energy Homeostasis
Regulating Center. An Approach for Obesity Pp. 75-84
Omar Al-Massadi, María Pardo, Felipe F. Casanueva
and Luisa M. Seoane
[Abstract] [Purchase
Article]
Patent
Selections Pp. 85-88
Abstracts

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Patented Novelties in Immunoisolation for the Treatment of
Endocrine Disorders
Paul de Vos, Barbro Melgert and Marijke M. Faas
Immunoisolation is based on the principle that
transplanted tissue is protected for the host immune system
by an artificial membrane. During the past decades a number
of different approaches of immunoisolation have been described.
The approaches include (i) intravascular devices, which are
anatomized to the vascular system, (ii) extravascular macrocapsules,
which are mostly diffusion chambers transplanted at different
sites, and (iii) extravascular microcapsules. Many reviews
describing the advantages and pitfalls of the different approaches
of immunoisolation have been described during recent years.
Almost none of these reviews however describe the technical
advances and (pre)clinical results described in the numerous
patents on the subject. Therefore this review presents the
recent novelties described in patents related to immunoisolation
of tissue.
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Medullary Thyroid Cancer: New Targeted
Molecular Therapies
Alessandro Antonelli, Silvia Martina Ferrari, Poupak Fallahi,
Michele Minuto, Alda Corrado, Rossella Bruno and
Paolo Miccoli
Medullary thyroid carcinoma (MTC) is a rare
tumor arising from neural crest-derived parafollicular C cells.
Metastatic MTC patients are incurable because the cancer does
not respond to radiotherapy or chemotherapy. The elucidation
over the past two decades of multiple genetic abnormalities
in MTC has provided specific targets for therapy. The identification
of activating mutations of the RET tyrosine kinase receptor
(TKR) in both hereditary and sporadic MTC makes this malignancy
an excellent model to examine the effect of a group of small
organic molecule tyrosine kinase inhibitors (TKIs) for treatment
of metastatic MTC. Clinical trials with several TKIs targeting
RET and other TKRs have shown positive results with generally
tolerable toxicity. Approximately one-third to one-half of
MTC patients have a reduction in tumor size up to 50%, with
the longest treatment duration of approximately four years.
The most common treatment-related toxicities are rash, nausea
and diarrhea. Despite promising initial results these studies
are in their early stages; however, the possibility of testing
the sensitivity of primary MTC cells from each subject to
different TKIs could increase the effectiveness of the treatment.
A brief outline on current patents that are the focus on the
treatment of Thyroid Cancer has also been provided in this
review.
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Impact of Antihypertensive Drug Use
on Bone Mineral Density and Osteoporotic Fracture - From an
Epidemiological Perspective
Naomi Masunari and Saeko Fujiwara
Osteoporosis, a common disease today, has serious
impacts on both patients and society, because prognosis can
be complicated and therapy costly. It is therefore important
to identify risk factors for osteoporosis to ensure the prevention
and early detection. Adjustment of confounding factors is
important for accurate evaluation of risk factors. In societies
with long average life spans, the number of people with multiple
chronic diseases has increased in recent years, resulting
in many reports of secondary osteoporosis caused by medication.
In this report, we aim to review the possibility that antihypertensive
drugs impact osteoporosis by investigating epidemiological
research results. As a search strategy, PubMed has been searched
using the keywords “osteoporosis,” “bone
mineral density,” “fracture,” “hypertension,”
and “drug-induced” in April 2009. The abstracts
have been screened and epidemiological studies have been included.
In addition, the authors have also screened reference lists
of relevant papers. The results of the present review seem
to suggest the possibility that thiazide diuretics and ß-blockers
have positive effects on bone, whereas loop diuretics appear
to have adverse effects. In examining effects of drugs on
bone, detailed review is necessary on the duration, time since
suspension of use, and quantity of drugs used. This review
summarizes the impact of antihypertensive drug on bone mineral
density and recent patents for the treatment of osteoporosis.
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Recent Methods for Assessing Bone Mineral
Density, Bone Strength, Fracture Risk and Therapeutic Effects
on Osteoporosis
Kazuhiro Imai
Osteoporosis is a major public health problem
affecting all countries and giving rise to fractures. The
World Health Organization (WHO) published a set of diagnostic
criteria to define osteoporosis in postmenopausal Caucasian
women, using bone mineral density (BMD) values measured by
dual energy X-ray absorptiometry (DXA). Currently, measurement
of BMD by DXA (g/cm2) has
been the standard method for diagnosing osteoporosis, in addition
to assessing fracture risk and therapeutic effects. Quantitative
computed tomography (QCT) can quantify volumetric BMD (mg/cm3),
and cancellous bone can be measured independently of surrounding
cortical bone and aortic calcification. Recently, quantitative
ultrasound (QUS) is emerging as a relatively low-cost and
readily accessible alternative means to identify osteoporosis
and evaluate fracture risk. More recently, finite element
(FE) method based on data from computed tomography (CT) has
been used to assess bone strength, fracture risk, and therapeutic
effects on osteoporosis. In this review, recent patents and
methods for assessing bone mineral density, bone strength,
fracture risk and therapeutic effects on osteoporosis are
outlined.
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Diabetes Vaccinations: An Overview
Sanjay Kalra, Navneet Agrawal, Bharti Kalra, Amit Sharma
and Ritu Kamboj
Recent research interest has focused on the
role of vaccination in preventing type 1 diabetes in high-risk
patients. High-risk subjects are identified on the basis of
genetic and antibody markers. While no single intervention
strategy has been demonstrated to have universal efficacy,
this review focuses on the developments and recent patents
in this field.
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Pharmacotherapy for Obesity
Alex H.C. Wong, Stefani S.N. Barg, and Alexander
K.C. Leung
Obesity is at an epidemic level. All patients
who are overweight and obese should be treated with diet,
exercise, behavioral therapy or a combination thereof; however,
these therapies may not be adequate for a number of patients.
Pharmacotherapy should be considered for patients who are
obese, are overweight with cardiovascular risk factors, or
have failed standard therapy. Several medications, such as
phentermine and diethylpropion for short-term treatment as
well as sibutramine and orlistat for long-term treatment,
are currently available. There are also off-label uses of
other medications such as antidepressants, anticonvulsants,
and anti-diabetic medications, for the management of obesity.
All of these medications provide additional weight loss when
used as an adjunct to the standard therapy of lifestyle modification.
The objective of this review is to summarize different patents
and new approaches in the treatment of obesity.
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The Therapeutic Potential of Microencapsulate
Implants: Patents and Clinical Trials
Carlos Spuch and Carmen Navarro
Cell microencapsulation holds promise for the
treatment of many diseases by the continuous delivery of therapeutic
products. The complexity of many diseases, such as neurological
and metabolic disorders needs the generation of new drugs
and especially new pathways to deliver the drug at proper
concentration and into the correct localization. One hopeful
technology is the developing of new biomaterial components
with the capacity to envelope drugs, cells or tissues, being
able to distribute the therapy; and at the same time, to be
isolated from the immune system. Microcapsules technology
has this capacity: releasing the necessary drug in a precise
location with a long-term efficacy, and keeping the grafts
isolated from the immune system. The objective of this review
is to summarize the last patents and news related with microencapsulation
technology, and the possible therapeutic applications in different
disorders.
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The Possible Use of Terpene Compounds
in DC Immunotherapy against Cancer
Masao Takei, Akemi Umeyama and Je-Jung Lee
Dendritic Cells (DC) play a pivotal role in
the initiation of T-cell-mediated immune responses, making
them an attractive cellular adjuvant for use in cancer vaccines.
The interaction of T cell with DC is crucial for directing
T cell differentiation towards the Th1, Th2 or Th17 type,
and several factors determining the direction of the T cell
polarization. IL-12 plays a central role in the immune system,
not only by augmenting the cytotoxic activity of T cells and
NK cells and regulating IFN-γ
production, but also by the capacity of IL-12 to promote the
development of Th1. Some plant-derived terpenes regulate differentiation
of DC from human monocytes. Terpene compounds-primed DC enhances
the differentiation of naïve
T cell towards the Th1 type, which is dependent on IL-12 secretion.
Some patents on terpene compounds, which may lead to the development
of effective immunotherapy for cancer, are also discussed
in the review.
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The Stomach as an Energy Homeostasis
Regulating Center. An Approach for Obesity
Omar Al-Massadi, María Pardo, Felipe F. Casanueva
and Luisa M. Seoane
Obesity is currently one of the greatest health
problems in industrialized countries, and yet there is no
reliable method to fight this pandemic. Bariatric surgery
is the most effective method to reduce body weight in morbidly
obese patients, suggesting that gastrointestinal tract derived
signals are crucial for energy balance regulation. This would
indicate that homeostatic mechanisms responsible for body
weight maintenance, involving the brain-gut axis are critical
for obesity prevention and development. Several descriptive
studies have proven the presence of gastric endogenous systems
that modulate energetic balance (ghrelin - obestatin system
and endocannabinoid system); however, these systems and their
interactions are still not well known. The present review
describes recent investigations that support the role of the
stomach as an energy balance regulator which exerts its effects
over known and probably unknown gastrointestinal systems.
Additionally, information covering new gastrointestinal derived
peptides patents for obesity treatment is provided as well.
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