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2012

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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

Environews #2, Nov. 10, 2012, Richard Philp Nov 2012

Environews #2, Nov. 10, 2012, Richard Philp

Richard B. Philp

This issue of Environews covers the astounding infant health problems associated with the residue of radioactivity from depleted uranium artillery shells used in Iraq, the importance of marine microbes to ocean productivity and carbon fixing, and the weakening of environmental protection by the government of Canada through changes to protective legislation.


Reviewing The American University Law Review On Extraterritoriality: A Critical Response To Viki Economides, Note, Tianrui Group Co. V. Itc: The Dubious Status Of Extraterritoriality And The Domestic Industry Requirement Requirement Of Section 337(Link), Jonathan R. K. Stroud Nov 2012

Reviewing The American University Law Review On Extraterritoriality: A Critical Response To Viki Economides, Note, Tianrui Group Co. V. Itc: The Dubious Status Of Extraterritoriality And The Domestic Industry Requirement Requirement Of Section 337(Link), Jonathan R. K. Stroud

Jonathan R. K. Stroud

Recently, the Federal Circuit upheld the Commission’s decision to exclude goods based on a trade secret violation that largely happened abroad. The American University Law Review critiqued that decision on two grounds: First, that a presumption against extraterritorial application of U.S. law applied; and second, that licensing alone could not establish a domestic industry. The American University Law Review's critique remains incomplete, however, as the Federal Circuit correctly decided the case for at least two reasons. first, the Federal Circuit correctly applied the “extraterritorial presumption” canon of construction; and second, the recent Federal Circuit decision in InterDigital Communications LLC v. …


Environews #1, Richard B. Philp Nov 2012

Environews #1, Richard B. Philp

Richard B. Philp

Environews #1 is, hopefuly, the first of a series dealing with current issues of environmental concern. This issue discusses the possible role of climate change in the massive floods that followed hurricane sandy, depletion of the world's fish stocks, the possible role, bothe positive and negative, of aquaculture, and the trend to seek oil in increasingly environmentally dangerous venues.


Target Repurposing For Neglected Diseases, Michael P. Pollastri, Robert K. Campbell Oct 2012

Target Repurposing For Neglected Diseases, Michael P. Pollastri, Robert K. Campbell

Michael Pollastri

Infectious diseases are an enormous burden to global health, and since drug discovery is costly, those infectious diseases that affect the developing world are often not pursued by commercial drug discovery efforts. Therefore, pragmatic means by which new therapeutics can be discovered are needed. One such approach is target repurposing, where pathogen targets are matched with homologous human targets that have been pursued for drug discovery for other indications. In many cases, the medicinal chemistry, structural biology, and biochemistry knowledge around these human targets can be directly repurposed to launch and accelerate new drug discovery efforts against the pathogen targets. …


Library Impact Statement For Bps 555 Protein Molecular Modeling, Michael Vocino Aug 2012

Library Impact Statement For Bps 555 Protein Molecular Modeling, Michael Vocino

michael c vocino

Library Impact Statement for BPS 555 Protein Molecular Modeling. No new resources were required to support this course.


A Mixed-Methods Study To Characterize Pharmaceutical Marketing In The Nursing Home Setting: Off-Label Use Of Atypical Antipsychotics, Camilla Benedicto, Jennifer L. Donovan, Terry S. Field, Jerry H. Gurwitz, Sarah Foy, Leslie R. Harrold, Abir O. Kanaan, Celeste A. Lemay, Kathleen M. Mazor, Jennifer Tjia, Sruthi Valluri, Becky A. Briesacher Jul 2012

A Mixed-Methods Study To Characterize Pharmaceutical Marketing In The Nursing Home Setting: Off-Label Use Of Atypical Antipsychotics, Camilla Benedicto, Jennifer L. Donovan, Terry S. Field, Jerry H. Gurwitz, Sarah Foy, Leslie R. Harrold, Abir O. Kanaan, Celeste A. Lemay, Kathleen M. Mazor, Jennifer Tjia, Sruthi Valluri, Becky A. Briesacher

Jennifer Tjia

Background: Despite FDA warnings that atypical antipsychotic medications are associated with an increased risk of death when used to treat behavioral disorders in older adults with dementia, they are prescribed to nearly one-third of older U.S. nursing home (NH) residents. Reasons for their high use in NHs are poorly understood, but may include pharmaceutical marketing efforts in the NH setting.

Methods: This study is nested within an ongoing cluster randomized trial to improve the use of atypical antipsychotics in NHs. We analyzed semistructured interviews (n = 36) and surveys (n = 139) of administrators, directors of nursing and medical directors …


Computational Analysis Of High Throughput Flow Cytometry Data, Joseph P. Robinson May 2012

Computational Analysis Of High Throughput Flow Cytometry Data, Joseph P. Robinson

Joseph P Robinson

Introduction (significance of area discussed) –Flow cytometry has been around for over 40 years, but only recently has the opportunity arisen to move into the high-throughput domain. The technology is now available and is highly competitive with imaging tools under the right conditions.

Areas Covered (research discussed and literature review) The historical perspective of flow cytometry operation is discussed as well as how the field has changed and what the key changes have been. The authors provide a solid background as well as compelling arguments for moving toward HT flow, where there are many innovative opportunities. These opportunities show strong …


Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters Apr 2012

Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters

Samuel James Matthews

Objectives. To develop a formalized, comprehensive, peer-driven teaching assessment program and a valid and reliable assessment tool. Methods. A volunteer taskforce was formed and a peer-assessment program was developed using a multistep, sequential approach and the Peer Observation and Evaluation Tool (POET). A pilot study was conducted to evaluate the efficiency and practicality of the process and to establish interrater reliability of the tool. Intra-class correlation coefficients (ICC) were calculated. Results. ICCs for 8 separate lectures evaluated by 2-3 observers ranged from 0.66 to 0.97, indicating good interrater reliability of the tool. Conclusion. Our peer assessment program for large classroom …


Pharmacy Student Knowledge And Communication Of Medication Errors, Nathaniel M. Rickles, Carey M. Noland, Anthony Tramontozzi, Michele A. Vinci Apr 2012

Pharmacy Student Knowledge And Communication Of Medication Errors, Nathaniel M. Rickles, Carey M. Noland, Anthony Tramontozzi, Michele A. Vinci

Carey M. Noland

Objectives. To describe and evaluate pharmacy students' knowledge of and comfort in communicating, managing, and preventing medication errors. Methods. Using a cross-sectional design, a survey instrument was administered to fifth-year pharmacy students. The survey instrument included both open-and close-ended questions to describe and examine factors associated with knowledge and comfort in communication of medication errors.Results. Survey instruments were completed by 93 students (90% response rate). Nearly 80% reported not having received training in communicating medication errors. The perception of having more adequate training was related to greater knowledge in the communication of medication errors (p


A Tool For Measuring Active Learning In The Classroom, Jenny A. Van Amburgh, John W. Devlin, Jennifer L. Kirwin, Donna M. Qualters Apr 2012

A Tool For Measuring Active Learning In The Classroom, Jenny A. Van Amburgh, John W. Devlin, Jennifer L. Kirwin, Donna M. Qualters

John W. Devlin

Objectives. To develop a valid and reliable active-learning inventory tool for use in large classrooms and compare faculty perceptions of active-learning using the Active-Learning Inventory Tool.Methods. The Active-Learning Inventory Tool was developed using published literature and validated by national experts in educational research. Reliability was established by trained faculty members who used the Active-Learning Inventory Tool to observe 9 pharmacy lectures. Instructors were then interviewed to elicit perceptions regarding active learning and asked to share their perceptions.Results. Per lecture, 13 ( range: 4-34) episodes of active learning encompassing 3 ( range: 2-5) different types of active learning occurred over 2.2 …


Using Facebook To Facilitate Course-Related Discussion Between Students And Faculty Members, Margarita V. Divall, Jennifer L. Kirwin Apr 2012

Using Facebook To Facilitate Course-Related Discussion Between Students And Faculty Members, Margarita V. Divall, Jennifer L. Kirwin

Jennifer L. Kirwin

Objectives. To use Facebook to facilitate online discussion of the content of a Comprehensive Disease Management course and to evaluate student use and perceptions of this exercise. Design. A Facebook page was created and coordinators encouraged students to "like" the page and to post and view study tips, links, or questions. At the end of the course, students' use and perceptions were evaluated using an anonymous survey tool. Assessment. At the end of week 1, there were 81 followers, 5 wall posts, and 474 visits to the course Facebook page. At peak use, the page had 117 followers, 18 wall …


Service-Learning At A Camp For Children With Asthma As Part Of An Advanced Pharmacy Practice Experience, Jennifer L. Kirwin, Jenny A. Van Amburgh, Kristyn M. Napoli Apr 2012

Service-Learning At A Camp For Children With Asthma As Part Of An Advanced Pharmacy Practice Experience, Jennifer L. Kirwin, Jenny A. Van Amburgh, Kristyn M. Napoli

Jennifer L. Kirwin

Objectives. To describe a service-learning opportunity within an advanced pharmacy practice experience and report satisfaction survey results from 2001 through present. Design. Pharmacy students volunteered to attend asthma camp during an ambulatory care rotation. Students administered and monitored medications and coordinated educational activities for campers. Students set goals for the week and completed reflective journals about the experience. A survey was administered 1 week and 6 months after the experience to assess satisfaction, changes in attitudes toward children with chronic asthma, and empathy towards patients.Assessment. Most students accomplished their goals and were satisfied with the experience. Approximately 40% of students …


Using Facebook To Facilitate Course-Related Discussion Between Students And Faculty Members, Margarita V. Divall, Jennifer L. Kirwin Apr 2012

Using Facebook To Facilitate Course-Related Discussion Between Students And Faculty Members, Margarita V. Divall, Jennifer L. Kirwin

Margarita V. DiVall

Objectives. To use Facebook to facilitate online discussion of the content of a Comprehensive Disease Management course and to evaluate student use and perceptions of this exercise. Design. A Facebook page was created and coordinators encouraged students to "like" the page and to post and view study tips, links, or questions. At the end of the course, students' use and perceptions were evaluated using an anonymous survey tool. Assessment. At the end of week 1, there were 81 followers, 5 wall posts, and 474 visits to the course Facebook page. At peak use, the page had 117 followers, 18 wall …


Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters Apr 2012

Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters

Margarita V. DiVall

Objectives. To develop a formalized, comprehensive, peer-driven teaching assessment program and a valid and reliable assessment tool. Methods. A volunteer taskforce was formed and a peer-assessment program was developed using a multistep, sequential approach and the Peer Observation and Evaluation Tool (POET). A pilot study was conducted to evaluate the efficiency and practicality of the process and to establish interrater reliability of the tool. Intra-class correlation coefficients (ICC) were calculated. Results. ICCs for 8 separate lectures evaluated by 2-3 observers ranged from 0.66 to 0.97, indicating good interrater reliability of the tool. Conclusion. Our peer assessment program for large classroom …


School-Wide Clinical Intervention System To Document Pharmacy Students' Impact On Patient Care, Margarita V. Divall, Brian Zikaras, Debra Copeland, Michael J. Gonyeau Apr 2012

School-Wide Clinical Intervention System To Document Pharmacy Students' Impact On Patient Care, Margarita V. Divall, Brian Zikaras, Debra Copeland, Michael J. Gonyeau

Margarita V. DiVall

Objectives. To implement and evaluate a school wide, Web-based clinical intervention system to document types and impact of pharmacy students' clinical activities during advanced pharmacy practice experiences (APPEs). Methods. A clinical intervention form was developed by pharmacy practice faculty consensus and uploaded to a secure Web site. Prior to APPEs, all pharmacy students were trained on the purpose and use of the system as well as strategies to document interventions appropriately. Results. Over the 3-year period of data collection, 15,393 interventions were documented. Most common intervention types included dosage adjustments, education of patients and providers, and optimization of therapeutic regimens. …


A Vidcasting Project To Promote The Pharmacist's Role In Public Health, Seena L. Haines, Jenny A. Van Amburgh Apr 2012

A Vidcasting Project To Promote The Pharmacist's Role In Public Health, Seena L. Haines, Jenny A. Van Amburgh

Jenny A. Van Amburgh

Objective. To develop, implement, and assess an Internet-based vidcasting project to promote the pharmacist's role in public health. Design. This was a collaborative effort for 2 different courses taught at 2 different schools of pharmacy. Faculty members created a special instructional design for students to follow in planning, producing, and publishing video public service announcements on the Internet.Assessment. Formative and summative assessments, including course examinations, a grading rubric, student survey, and focus group, were implemented to evaluate student learning and public reaction. Students believed Internet video public service announcements served as a useful reference for patients and professionals, aided in …


Status And Recommendations For Self-Care Instruction In Us Colleges And Schools Of Pharmacy, 2006, Seena L. Zierler-Brown, Jenny A. Van Amburgh, Kristin A. Casper, Linda L. Krypel, Amista Lone Salcido, Victor A. Padron, W. Steven Pray, Andrea L. Wall, Jenelle L. Sobotka, Janet P. Engle Apr 2012

Status And Recommendations For Self-Care Instruction In Us Colleges And Schools Of Pharmacy, 2006, Seena L. Zierler-Brown, Jenny A. Van Amburgh, Kristin A. Casper, Linda L. Krypel, Amista Lone Salcido, Victor A. Padron, W. Steven Pray, Andrea L. Wall, Jenelle L. Sobotka, Janet P. Engle

Jenny A. Van Amburgh

Teachers of pharmacy self-care courses have met annually since 1998 at the Nonprescription Medicines Academy (NMA) held in Cincinnati, Ohio. During these meetings, self-care faculty members discuss methods of enhancing the teaching of self-care in US colleges and schools of pharmacy. Self-care courses are taught using a variety of methods and content is woven into pharmacy curricula in many different ways. This manuscript sets forth the current state of self-care instruction in pharmacy curricula including the recommended core curriculum, instructional methodologies, course mechanics, existing standards, and assessment and curricular placement, and makes recommendations for the future.


A Tool For Measuring Active Learning In The Classroom, Jenny A. Van Amburgh, John W. Devlin, Jennifer L. Kirwin, Donna M. Qualters Apr 2012

A Tool For Measuring Active Learning In The Classroom, Jenny A. Van Amburgh, John W. Devlin, Jennifer L. Kirwin, Donna M. Qualters

Jenny A. Van Amburgh

Objectives. To develop a valid and reliable active-learning inventory tool for use in large classrooms and compare faculty perceptions of active-learning using the Active-Learning Inventory Tool.Methods. The Active-Learning Inventory Tool was developed using published literature and validated by national experts in educational research. Reliability was established by trained faculty members who used the Active-Learning Inventory Tool to observe 9 pharmacy lectures. Instructors were then interviewed to elicit perceptions regarding active learning and asked to share their perceptions.Results. Per lecture, 13 ( range: 4-34) episodes of active learning encompassing 3 ( range: 2-5) different types of active learning occurred over 2.2 …


Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters Apr 2012

Development Of A Peer Teaching-Assessment Program And A Peer Observation And Evaluation Tool, Jennifer M. Trujillo, Margarita V. Divall, Judith T. Barr, Michael J. Gonyeau, Jenny A. Van Amburgh, S. James Matthews, Donna M. Qualters

Jenny A. Van Amburgh

Objectives. To develop a formalized, comprehensive, peer-driven teaching assessment program and a valid and reliable assessment tool. Methods. A volunteer taskforce was formed and a peer-assessment program was developed using a multistep, sequential approach and the Peer Observation and Evaluation Tool (POET). A pilot study was conducted to evaluate the efficiency and practicality of the process and to establish interrater reliability of the tool. Intra-class correlation coefficients (ICC) were calculated. Results. ICCs for 8 separate lectures evaluated by 2-3 observers ranged from 0.66 to 0.97, indicating good interrater reliability of the tool. Conclusion. Our peer assessment program for large classroom …


Succession Planning In Us Pharmacy Schools, Jenny A. Van Amburgh, Christopher K. Surratt, James S. Green, Randle M. Gallucci, James Colbert, Shara L. Zatopek, Robert A. Blouin Apr 2012

Succession Planning In Us Pharmacy Schools, Jenny A. Van Amburgh, Christopher K. Surratt, James S. Green, Randle M. Gallucci, James Colbert, Shara L. Zatopek, Robert A. Blouin

Jenny A. Van Amburgh

The deans, associate and assistant deans, and department chairs of a college or school of pharmacy retain historic memories of the institution and share the responsibility for day-to-day operation, sustainability, and future planning. Between the anticipated retirement of baby boomers who are senior administrative faculty members and the steady increase in number of colleges and schools of pharmacy, the academy is facing a shortage of qualified successors. Succession planning involves planning for the effective transition of personnel in leadership positions within an organization. This paper describes the subject of succession planning at a sample population of AACP institutions by obtaining …


Student Participants In Faculty Educational Research, Nathaniel M. Rickles Apr 2012

Student Participants In Faculty Educational Research, Nathaniel M. Rickles

Nathaniel Rickles

No abstract provided.


Pharmacy Student Knowledge And Communication Of Medication Errors, Nathaniel M. Rickles, Carey M. Noland, Anthony Tramontozzi, Michele A. Vinci Apr 2012

Pharmacy Student Knowledge And Communication Of Medication Errors, Nathaniel M. Rickles, Carey M. Noland, Anthony Tramontozzi, Michele A. Vinci

Nathaniel Rickles

Objectives. To describe and evaluate pharmacy students' knowledge of and comfort in communicating, managing, and preventing medication errors. Methods. Using a cross-sectional design, a survey instrument was administered to fifth-year pharmacy students. The survey instrument included both open-and close-ended questions to describe and examine factors associated with knowledge and comfort in communication of medication errors.Results. Survey instruments were completed by 93 students (90% response rate). Nearly 80% reported not having received training in communicating medication errors. The perception of having more adequate training was related to greater knowledge in the communication of medication errors (p


The Impact Of A Standardized Patient Program On Student Learning Of Communication Skills, Nathaniel M. Rickles, Phuong Tieu, Lindsay Myers, Suzanne Galal, Valerie Chung Apr 2012

The Impact Of A Standardized Patient Program On Student Learning Of Communication Skills, Nathaniel M. Rickles, Phuong Tieu, Lindsay Myers, Suzanne Galal, Valerie Chung

Nathaniel Rickles

Objective. Determine the quantitative and qualitative value of a lecture-laboratory course with standardized patients on student communication skills. Methods. A blinded retrospective analysis was conducted on the counseling tapes of 127 students who took a lecture-laboratory course with standardized patients. A Communication Skills Assessment Form (CSAF) was used to evaluate baseline, midpoint and final tapes. Descriptive statistics and repeated measures analysis of variance were used to compare tapes. Students and standardized patients completed written survey instruments evaluating the laboratory at the end of the semester.Results. Students had significant and progressively higher scores on the assessment across baseline, midpoint and final …


Near Infrared Planar Tumor Imaging And Quantification Using Nanosized Alexa 750-Labeled Phospholipid Micelles, Aristarchos Papagiannaros, Amit Kale, Tatyana S. Levchenko, Dmitry Mongayt, William C. Hartner, V. P. Torchilin Apr 2012

Near Infrared Planar Tumor Imaging And Quantification Using Nanosized Alexa 750-Labeled Phospholipid Micelles, Aristarchos Papagiannaros, Amit Kale, Tatyana S. Levchenko, Dmitry Mongayt, William C. Hartner, V. P. Torchilin

Tatyana Levchenko

A novel highly biocompatible near infrared nanosized contrast agent was developed and used for rapid tumor detection and quantification using planar optical imaging and analysis. With this in mind, the near infrared fluorescent dye Alexa 750 was covalently attached to polyethylene glycol-phosphatidylethanolamine (PEG-PE) conjugate, and double labeled (with Alexa and rhodamine) PEG-PE micelles were injected into mice and observed using planar optical imaging. Pixel intensity data from the tumor site were normalized versus the autofluorescence of the animal at the same time point and normalized as signal to noise over the scattered light from the various tissues of the mice. …


Doxorubicin Loaded Polymeric Nanoparticulate Delivery System To Overcome Drug Resistance In Osteosarcoma, Michiro Susa, Arun K. Iyer, Keinosuke Ryu, Francis John Hornicek, Henry J. Mankin, Mansoor M. Amiji, Zhenfeng Duan Apr 2012

Doxorubicin Loaded Polymeric Nanoparticulate Delivery System To Overcome Drug Resistance In Osteosarcoma, Michiro Susa, Arun K. Iyer, Keinosuke Ryu, Francis John Hornicek, Henry J. Mankin, Mansoor M. Amiji, Zhenfeng Duan

Arun Iyer

Background: Drug resistance is a primary hindrance for the efficiency of chemotherapy against osteosarcoma. Although chemotherapy has improved the prognosis of osteosarcoma patients dramatically after introduction of neo-adjuvant therapy in the early 1980's, the outcome has since reached plateau at approximately 70% for 5 year survival. The remaining 30% of the patients eventually develop resistance to multiple types of chemotherapy. In order to overcome both the dose-limiting side effects of conventional chemotherapeutic agents and the therapeutic failure incurred from multidrug resistant (MDR) tumor cells, we explored the possibility of loading doxorubicin onto biocompatible, lipid-modified dextran-based polymeric nanoparticles and evaluated the …


Near Infrared Planar Tumor Imaging And Quantification Using Nanosized Alexa 750-Labeled Phospholipid Micelles, Aristarchos Papagiannaros, Amit Kale, Tatyana S. Levchenko, Dmitry Mongayt, William C. Hartner, V. P. Torchilin Apr 2012

Near Infrared Planar Tumor Imaging And Quantification Using Nanosized Alexa 750-Labeled Phospholipid Micelles, Aristarchos Papagiannaros, Amit Kale, Tatyana S. Levchenko, Dmitry Mongayt, William C. Hartner, V. P. Torchilin

William Hartner

A novel highly biocompatible near infrared nanosized contrast agent was developed and used for rapid tumor detection and quantification using planar optical imaging and analysis. With this in mind, the near infrared fluorescent dye Alexa 750 was covalently attached to polyethylene glycol-phosphatidylethanolamine (PEG-PE) conjugate, and double labeled (with Alexa and rhodamine) PEG-PE micelles were injected into mice and observed using planar optical imaging. Pixel intensity data from the tumor site were normalized versus the autofluorescence of the animal at the same time point and normalized as signal to noise over the scattered light from the various tissues of the mice. …


The Effects Of Laropiprant, A Selective Prostaglandin D₂ Receptor 1 Antagonist, On The Antiplatelet Activity Of Clopidogrel Or Aspirin., Aimee Dallob, Wen-Lin Luo, Julie Mabalot Luk, Lisa Ratcliffe, Amy O Johnson-Levonas, Jules I Schwartz, Victor Dishy, Walter K. Kraft, Jan N De Hoon, Anne Van Hecken, Inge De Lepeleire, Waldemar Radziszewski, John A Wagner, Eseng Lai Mar 2012

The Effects Of Laropiprant, A Selective Prostaglandin D₂ Receptor 1 Antagonist, On The Antiplatelet Activity Of Clopidogrel Or Aspirin., Aimee Dallob, Wen-Lin Luo, Julie Mabalot Luk, Lisa Ratcliffe, Amy O Johnson-Levonas, Jules I Schwartz, Victor Dishy, Walter K. Kraft, Jan N De Hoon, Anne Van Hecken, Inge De Lepeleire, Waldemar Radziszewski, John A Wagner, Eseng Lai

walter k Kraft

Laropiprant (LRPT) is being developed in combination with Merck's extended-release niacin (ERN) formulation for the treatment of dyslipidemia. LRPT, an antagonist of the prostaglandin PGD₂ receptor DP1, reduces flushing symptoms associated with ERN. LRPT also has affinity for the thromboxane A₂ receptor TP (approximately 190-fold less potent at TP compared with DP1). Aspirin and clopidogrel are two frequently used anti-clotting agents with different mechanisms of action. Since LRPT may potentially be co-administered with either one of these agents, these studies were conducted to assess the effects of steady-state LRPT on the antiplatelet activity of steady-state clopidogrel or aspirin. Bleeding time …


A Glycosylated Recombinant Human Granulocyte Colony Stimulating Factor Produced In A Novel Protein Production System (Avi-014) In Healthy Subjects: A First-In Human, Single Dose, Controlled Study., Roslyn Varki, Ed Pequignot, Mark C Leavitt, Andres Ferber, Walter K Kraft Mar 2012

A Glycosylated Recombinant Human Granulocyte Colony Stimulating Factor Produced In A Novel Protein Production System (Avi-014) In Healthy Subjects: A First-In Human, Single Dose, Controlled Study., Roslyn Varki, Ed Pequignot, Mark C Leavitt, Andres Ferber, Walter K Kraft

walter k Kraft

BACKGROUND: AVI-014 is an egg white-derived, recombinant, human granulocyte colony-stimulating factor (G-CSF). This healthy volunteer study is the first human investigation of AVI-014. METHODS: 24 male and female subjects received a single subcutaneous injection of AVI-014 at 4 or 8 mcg/kg. 16 control subjects received 4 or 8 mcg/kg of filgrastim (Neupogen, Amgen) in a partially blinded, parallel fashion. RESULTS: The Geometric Mean Ratio (GMR) (90% CI) of 4 mcg/kg AVI-014/filgrastim AUC(0-72 hr) was 1.00 (0.76, 1.31) and Cmax was 0.86 (0.66, 1.13). At the 8 mcg/kg dose, the AUC(0-72) GMR was 0.89 (0.69, 1.14) and Cmax was 0.76 (0.58, …


Synthesis And Evaluation Of Human Phosphodiesterases (Pde) 5 Inhibitor Analogs As Trypanosomal Pde Inhibitors. 1. Sildenafil Analogs, Cuihua Wang, Trent D. Ashton, Alden Gustafson, Nicholas D. Bland, Stefan O. Ochiana, Robert K. Campbell, Michael P. Pollastri Feb 2012

Synthesis And Evaluation Of Human Phosphodiesterases (Pde) 5 Inhibitor Analogs As Trypanosomal Pde Inhibitors. 1. Sildenafil Analogs, Cuihua Wang, Trent D. Ashton, Alden Gustafson, Nicholas D. Bland, Stefan O. Ochiana, Robert K. Campbell, Michael P. Pollastri

Michael Pollastri

Parasitic diseases, such as African sleeping sickness, have a significant impact on the health and well-being in the poorest regions of the world. Pragmatic drug discovery efforts are needed to find new therapeutic agents. In this report we describe target repurposing efforts focused on trypanosomal phosphodiesterases. We outline the synthesis and biological evaluation of analogs of sildenafil (1), a human PDE5 inhibitor, for activities against trypanosomal PDEB1 (TbrPDEB1). We find that, while low potency analogs can be prepared, this chemical class is a sub-optimal starting point for further development of TbrPDE inhibitors.


Synthesis And Evaluation Of Human Phosphodiesterases (Pde) 5 Inhibitor Analogs As Trypanosomal Pde Inhibitors. 2. Tadalafil Analogs, Stefan O. Ochiana, Alden Gustafson, Nicholas D. Bland, Cuihua Wang, Michael J. Russo, Robert K. Campbell, Michael P. Pollastri Feb 2012

Synthesis And Evaluation Of Human Phosphodiesterases (Pde) 5 Inhibitor Analogs As Trypanosomal Pde Inhibitors. 2. Tadalafil Analogs, Stefan O. Ochiana, Alden Gustafson, Nicholas D. Bland, Cuihua Wang, Michael J. Russo, Robert K. Campbell, Michael P. Pollastri

Michael Pollastri

In this report we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). We outline the synthesis and biological evaluation of analogs of tadalafil, a human PDE5 inhibitor currently utilized for treatment of erectile dysfunction, and report that these analogs are weak inhibitors of TbrPDEB1.