Recent
Patents on Anti-Cancer Drug Discovery
ISSN: 1574-8928

Recent Patents on Anti-Cancer
Drug Discovery
Volume 4, Number 3, November 2009
Contents

Recent Patents in Toll-like Receptor Pathways
and Relevance to Cancer Pp. 189-195
Kevin Kimbro and Sabrenia Parker
[Abstract] [Full
text article] [PMID:
19522696 PubMed - indexed for MEDLINE]
Emerging Therapeutic Agents for Cervical Cancer
Pp. 196-206
Daniela B. Cornelio, Rafael Roesler and Gilberto
Schwartsmann
[Abstract] [Full
text article] [PMID:
19522698 PubMed - indexed for MEDLINE]
Use of the Semiconductor Nanotechnologies "Quantum
Dots" for in vivo Cancer Imaging Pp.
207-215
Monica Ciarlo, Patrizia Russo, Alfredo Cesario,
Sara Ramella, Gabriella Baio, Carlo E. Neumaier and
Laura Paleari
[Abstract] [Full
text article] [PMID:
19715554 PubMed - indexed for MEDLINE]
Lapatinib as a Chemotherapeutic Drug Pp.
216-226
Oluwakemi Obajimi
[Abstract] [Full
text article] [PMID:
19522695 PubMed - indexed for MEDLINE]
Recent Advances in Epitope Design for Immunotherapy
of Cancer Pp. 227-240
Pieranna Chiarella, Emanuela Massi, Mariangela
De Robertis, Vito M. Fazio and Emanuela Signori
[Abstract] [Full
text article] [PMID:
19522699 PubMed - indexed for MEDLINE]
Amrubicin: A Synthetic Anthracyclin Analogue
in the Treatment of Extensive Stage Small Cell Lung Cancer
Pp. 241-245
Chirag M. Shah
[Abstract] [Full
text article] [PMID:
19538159 PubMed - indexed for MEDLINE]
Aldo-Keto Reductase Family 1 Member B1 Inhibitors:
Old Drugs with New Perspectives Pp. 246-253
Jianghua Liu, Gebo Wen and Deliang Cao
[Abstract] [Full
text article] [PMID:
19522700 PubMed - indexed for MEDLINE]
Recent Development in Nano-Sized Dosage Forms
of Plant Alkaloid Camptothecin-Derived Drugs Pp.
254-261
Nguyen-Van Cuong, Ming-Fa Hsieh and
Chun-Ming Huang
[Abstract] [Full
text article] [PMID:
19522697 PubMed - indexed for MEDLINE]
Nanoparticle Albumin - Bound (NAB) Technology
is a Promising Method for Anti-Cancer Drug Delivery Pp.
262-272
Qiang Fu, Jin Sun, Wenping Zhang, Xiaofan Sui,
Zhongtian Yan and Zhonggui He
[Abstract] [Full
text article] [PMID:
19538176 PubMed - indexed for MEDLINE]
Patent Selections Pp. 273-276
[Full
text article]
Abstracts

[Back to top]
[Full
text article] [PMID:
19522696 PubMed - indexed for MEDLINE]
Recent Patents in Toll-like Receptor Pathways and Relevance
to Cancer
Kevin Kimbro and Sabrenia Parker
The first lines of defense in the human innate immune
system are membrane receptors called Toll-like receptors (TLRs).
This family of receptors functions as primary sensors to recognize
microbial pathogens. Subsequent binding of ligands to TLRs
lend to the activation of cellular signaling pathways that
regulate expression of genes related to inflammation and immunity.
The discovery and supporting evidence of functional and structural
diversity suggests TLRs are key participants in cellular immunity
and are important to various medical conditions including
the tumor microenvironment. TLR heterogeneity emphasizes the
role of these receptors and suggests a new opportunity to
develop therapies targeting specific or multiple TLRs that
may contribute to the treatment of a myriad of diseases including
various cancers. In this article, we intend to focus on a
number of recently issued patents related to TLRs and to propose
the relevance of these patents to novel treatments for cancers.
[Back to top]
[Full
text article] [PMID:
19522698 PubMed - indexed for MEDLINE]
Emerging Therapeutic Agents for Cervical Cancer
Daniela B. Cornelio, Rafael Roesler and
Gilberto Schwartsmann
Cervical cancer is the second most frequent malignancy
affecting women worldwide. The highest incidences occur in
the developing world, where, in most countries, cervical cancer
is the leading cause of cancer mortality in women. Although
surgery and chemoradiotherapy can cure 80-95% of women with
early stage cancer and 60% of locoregionally advanced cancer,
the recurrent and metastatic disease remains a major cause
of cancer death. The current cytotoxic treatment options for
advanced and metastatic cancer demonstrate modest results,
with response rates of maximum 30% and overall survival of
less than 10 months. Given this limited degree of success
with conventional therapies, interest has increased in other
therapeutic alternatives. In this way, targeted agents are
emerging as potential candidates for improving survival in
cervical cancer patients. In this review we highlight the
main current therapeutic strategies for cervical cancer and
summarize the most relevant patents from the latest five years.
Special attention was given to patents with potential applications
in the clinical practice.
[Back to top]
[Full
text article] [PMID:
19715554 PubMed - indexed for MEDLINE]
Use of the Semiconductor Nanotechnologies "Quantum
Dots" for in vivo Cancer Imaging
Monica Ciarlo, Patrizia Russo, Alfredo Cesario,
Sara Ramella, Gabriella Baio, Carlo E. Neumaier and
Laura Paleari
Non-invasive in vivo imaging offers great potential
to facilitate translational drug development research at the
animal testing phase. The emerging luminescent nanoparticles
or quantum dots provide a new type of biological agents that
can improve these applications. The advantages of luminescent
nanoparticles for biological applications include their high
quantum yield, color availability, good photo-stability, large
surface-to-volume ratio, surface functionality, and small
size. These properties could improve the sensitivity of biological
detection and imaging by at least 10- to 100-fold and make
them an exceptional tool for live-cell imaging. In this review
patents on applications of semiconductor quantum dots for
in vivo imaging are discussed.
[Back to top]
[Full
text article] [PMID:
19522695 PubMed - indexed for MEDLINE]
Lapatinib as a Chemotherapeutic Drug
Oluwakemi Obajimi
Human epidermal growth factor receptor (HER) signaling
is frequently associated with the development and progression
of several types of cancers. Both the MAPK and the PI3K/Akt
pathways have been implicated as effectors of HER signaling
by promoting anti-apoptotic and pro-proliferative effects
in cancer cells. As a result, many anti-HER drugs have been
developed and patented for use in cancer therapy. One such
drug that was recently approved for clinical trials is lapatinib
(Tykerb, GW572016). Lapatinib is a small molecule inhibitor
that is active at the ATP binding site of the tyrosine kinase
involved in HER signaling. Importantly, this drug has dual
specificity acting at the ATP binding sites of both HER-2
and HER-1 (EGFR). This review therefore summarizes the current
knowledge based on pre-clinical and clinical evidence of the
therapeutic effects of lapatinib against cancer and the promising
strategy of combination therapy with the possibility of circumventing
the problems of drug resistance commonly faced by chemotherapeutic
drugs.
[Back to top]
[Full
text article] [PMID:
19522699 PubMed - indexed for MEDLINE]
Recent Advances in Epitope Design for Immunotherapy
of Cancer
Pieranna Chiarella, Emanuela Massi, Mariangela
De Robertis, Vito M. Fazio and Emanuela
Signori
Eradication of cancer cells is imperative for a successful
treatment of tumours. In addition to the existent chemotherapy
or radiation therapy, other novel immunotherapeutic strategies
to fight tumours are currently under investigation. One of
these is cancer vaccination, an approach aimed at inducing
effective immune responses in the host against defined tumour
antigens. Among several classes of cancer vaccines, the subunit
vaccines based on the single and multi epitope-approach are
worthy of note as they offer an exquisite specificity in targeting
only tumour cells. In this review we will focus on the significant
advances made in the development and use of epitope-based
cancer vaccines, reporting a selection of important and recent
patents on tumour antigen discovery and epitope design for
immunotherapy of cancer.
[Back to top]
[Full
text article] [PMID:
19538159 PubMed - indexed for MEDLINE]
Amrubicin: A Synthetic Anthracyclin Analogue
in the Treatment of Extensive Stage Small Cell Lung Cancer
Chirag M. Shah
Amrubicin is a synthetic anthracyclin analogue that has
significant activity in Japanese patients with extensive stage
small cell lung cancer (ES-SCLC). There has not been significant
advances made in the treatment of this disease in last several
years and new therapies are desperately needed to change the
natural history of this disease. Preliminary data has shown
that amrubicin possesses anti-tumor activity in patients with
extensive stage small cell lung cancer in the western population.
Clinical trials are on going to evaluate this agent further
in Europe and US. If effective, it may be an invaluable addition
into the current armamentarium to treat this deadly disease.
The review includes patent coverage on the treatment of small
cell lung cancer.
[Back to top]
[Full
text article] [PMID:
19522700 PubMed - indexed for MEDLINE]
Aldo-Keto Reductase Family 1 Member B1 Inhibitors:
Old Drugs with New Perspectives
Jianghua Liu, Gebo Wen and
Deliang Cao
Aldo-keto reductase 1 member B1 (AKR1B1) is pathogenically
involved in diabetic complications by driving glucose flux
through polyol pathway; a variety of AKR1B1 inhibitors has
been developed for the treatment of diabetic complications
and a body of invaluable preclinical and clinical data have
been collected through decades’ efforts. Recent studies
have shown that some AKR1B1 inhibitors demonstrate strong
inhibitory activity to aldo-keto reductase family 1 member
B10 (AKR1B10), a protein identical to AKR1B1, in vitro
and in cancer cells. AKR1B1 and AKR1B10 are overexpressed
in human tumors, such as liver, breast, and lung cancer, and
may play a critical role in the development and progression
of cancer through carbonyl detoxification, retinoic acid homeostatic
regulation, and lipid metabolic control, as well as the activation
of tobacco smoke carcinogens. Therefore, AKR1B1 inhibitors
may represent a novel class of antitumor agents; and the clinical
data assembled in diabetic clinics would greatly assist the
transition of these inhibitors to cancer clinics. This article
summaries the current understanding of the expression and
function of AKR1B1 and AKR1B10 in human cancers and reviews
the patents and papers of AKR1B1 inhibitors. Authors’
opinions concerning the current and future development of
AKR1B1 and/or AKR1B10-specific inhibitors are discussed.
[Back to top]
[Full
text article] [PMID:
19522697 PubMed - indexed for MEDLINE]
Recent Development in Nano-Sized Dosage Forms
of Plant Alkaloid Camptothecin-Derived Drugs
Nguyen-Van Cuong, Ming-Fa Hsieh and
Chun-Ming Huang
DNA topoisomerase is one of drug targets in cancer therapy.
Camptothecin is a plant alkaloid derived from the Chinese
tree Camptotheca acuminate. It has been demonstrated
that the plant alkaloid camptothecin (CPT) caused DNA damage
by specifically targeting DNA topoisomerase, effectively devastating
a broad spectrum of tumors. Although the anti-tumoral activity
of CPT has been intensively studies for nearly fifty years,
recent advances in drug delivery systems of CPT have considerably
improved this drug’s efficiency. In this review, we
will summarize the current status of CPT-derived anti-cancer
drugs in literatures and patents and highlight their clinical
application.
[Back to top]
[Full
text article] [PMID:
19538176 PubMed - indexed for MEDLINE]
Nanoparticle Albumin - Bound (NAB) Technology
is a Promising Method for Anti-Cancer Drug Delivery
Qiang Fu, Jin Sun, Wenping Zhang, Xiaofan Sui,
Zhongtian Yan and Zhonggui He
Albumin is a versatile drug carrier in anti-cancer drug
delivery system and it also has an actively targeting capacity
to tumors. Recently, nanoparticle albumin-bound (nab™)
paclitaxel (nab-paclitaxel; Abraxane®)
has been approved in 2006 for use in patients with metastatic
breast cancer who have failed in the combination chemotherapy,
and so the nab-technology has attracted much interest in the
anti-cancer drug delivery system. The details about the preparation,
characterization and evaluation of nab-paclitaxel (ABI-007)
are discussed. The pharmacokinetics, pharmacodynamics and
the clinical trials of ABI-007 are also reviewed. Furthermore,
the recent applications of nab-technology in the anti-cancer
drug delivery systems are summarized by virtue of the patents
pertaining to nab-technology. To sum up, nab-technology has
a great potential of being applied extensively in the field
of anti-cancer agents delivery in the future in order to acquire
the good safety and better therapeutical effect.
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