News & Notes

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News & Notes

ImQuest Life Sciences Receives FDA Approval to Initiate Clinical Trials of a Vaginal Gel for the Prevention of HIV Transmission to Women

ImQuest Life Sciences was recently notified by the US Food and Drug Administration of the approval of their Investigational New Drug application (IND) to study the safety in Phase 1 clinical trials of their vaginal gel containing the nonnucleoside reverse transcriptase HIV Inhibitor IQP-0528. Preclinical studies have shown that IQP-0528 is highly effective against virus strains found throughout the world, prevents HIV transmission in cultured cells, causes sterilization of cultures infected with HIV, and acts in concert with other approved HIV inhibitors to inhibit the virus. The IQP-0528 vaginal gel is being developed with the goal of preventing the sexual transmission of HIV to women.

ImQuest plans to evaluate the safety of the IQP-0528 vaginal gel in a Phase I clinical trial at medical centers in the United States and expects to begin recruiting women for the trial by the end of the year.

“The approval of our IND by the FDA is a major and highly significant milestone for ImQuest’s Women’s Health and Prevention programs focused on the protection of susceptible women from infection”, said Dr. Robert Buckheit, Jr., President and Chief Scientific Officer of ImQuest. “We hope that the IQP-0528 containing gel will be a highly successful prevention agent and will be a first step towards development of subsequent products, including our DuoGel™ for protection of both vaginal and rectal virus transmission to men and women and our intravaginal ring which will provide sustained drug delivery for longer periods of time.”  The company plans to submit a second IND to the FDA for approval to test IQP-0528 in a DuoGel™ formulation early next year.

ImQuest Life Sciences developed the HIV inhibitor in partnership with Samjin Pharmaceutical Co. Ltd of Seoul Korea. Preclinical testing was conducted by ImQuest BioSciences of Frederick, Maryland. Development of ImQuest’s prevention products has been supported in part by the National Institutes of Health and the International Partnership for Microbicides, which is funded by The Bill and Melinda Gates Foundation and The United States Agency for International Development (USAID).


ImQuest Receives $14.2 Million Five-Year Grant from NIH to Develop a Dual Compartment Topical Microbicide to Prevent HIV Transmission

ImQuest BioSciences, Inc. announced today the successful acquisition of funding from the National Institutes of Health to support the development of a safe and effective microbicide product that will be designed for both vaginal and rectal use. ImQuest and microbicide researchers from four major US-based universities, along with ImQuest’s Korean partner Samjin Pharmaceutical Co. Ltd., will develop the highly innovative dual use combination product consisting of ImQuest’s highly potent pyrimidinedione inhibitor, IQP-0528, and Gilead’s tenofovir, which has already shown microbicidal activity in human clinical trials.

The $14.2 million award for studies to be performed in the Integrated Preclinical/Clinical Program for HIV Topical Microbicides (IPCP-HTM), which is sponsored by the National Institute of Allergy and Infectious Disease (NIAID), will be led by Principal Investigator Robert W. Buckheit, Jr., Ph.D., President and Chief Executive Officer of ImQuest. Other participating scientific investigators from ImQuest include Anthony Ham, Ph.D., Scot Roberts, Ph.D., and Karen Buckheit, M.S. The project involves a consortium of Universities that contribute critical components to the program, including Johns Hopkins University, Centers for Disease Control, Miriam Hospital/Brown University, Duke University, and University of Pittsburgh. ImQuest and the research team hope to progress its DuoGel and Smart Suppository products to human clinical trials over the next two years, following the clinical evaluation of its IQP-0528 vaginal microbicide gel.


ICAR Presentation: IND-Directed Development of Dual-Acting Pyrimidinediones IQP-0410 and IQP-0528: Enhancement of Solubility and Metabolic Stability

A poster entitled “IND-Directed Development of Dual-Acting Pyrimidinediones IQP-0410 and IQP-0528: Enhancement of Solubility and Metabolic Stability” was presented at the 2012 International Conference for Antiviral Research (ICAR) in Sapporo, Japan.  The data presented identified the pyrimidinedione compound IQP-0528 in the cyclopropyl series as the lead product for both HIV therapy and prevention based on high therapeutic index, dual mechanism of antiviral action, and enhanced genetic barrier to resistance compared to IQP-0410.  Chemical modification efforts to improve solubility and eliminating the sites of rapid metabolism of IQP-0528 identified the new lead compound JDJ01.  The data generated was supported by a NIH Phase II Small Business grant that was won by Dr. Buckheit in 2010.


ICAR Presentation: “Critical Role of a Serum Factor in Facilitating Efficient Synthesis of Hepadnaviral cccDNA”

Dr. Robert Buckheit was recently invited to give an oral presentation about critical role of a serum factor in facilitating efficient synthesis of hepadnaviral cccDNA in 2012 International Conference on Antiviral Research held in Sapporo, Japan, April 16-19. Dr. Buckheit’s presentation was well received and stimulated great interest among audience as the presented data represents a leading clue to understanding how cccDNA synthesis is regulated by the host’ factors, and will facilitate identifying new drug targets for HBV therapy.


ICAR Presentation:  “Muti-Pathway Development of Dual-Acting Pyrimidinedione NNRTIs as HIV Topical Microbicides”

Dr. Robert W. Buckheit Jr., President and CEO presented an oral presentation entitled “Muti-Pathway Development of Dual-Acting Pyrimidinedione NNRTIs as HIV Topical Microbicides” as part of the 25th International Conference on Antiviral Research in Sapporo, Japan.  The presentation summarized the activity of the lead pyrimidinedione IQP-0528 and its development as a gel, film and a component of an intravaginal ring.  In addition to the staff at ImQuest, the work was performed with collaborators Dr. Patrick Kiser at the University of Utah and Dr. Charlene Dezzutti at the University of Pittsburgh as part of a Integrated Preclincial/Clinical U19 grant funded by the NIH.  IQP-0528 was licensed by ImQuest BioSciences in 2005 from Samjin Pharmaceutical Co. LTD in Seoul, Korea.


Microbicides Presentation: “User Experience Shapes Meaning Making & the Acceptability of Intravaginal Rings and Long-Acting Vaginal Gels”

Ms. Karen Buckheit presented an oral presentation entitled “User Experience Shapes Meaning Making & the Acceptability of Intravaginal Rings and Long-Acting Vaginal Gels” as part of the International Microbicides Conference in Sydney, Australia.  The talk focused on recent data from acceptability studies that investigated user’s perceptions and preferences about long-acting vaginal gels and intravaginal rings as microbicide delivery mechanisms.  The talk was presented on behalf of Dr. Kate Morrow at the Miriam Hospital/Brown University where the study was conducted as part of an Integrated Preclinical/Clinical U19 grant funded by the NIH.


Microbicides Presentations:   “Development of a Combination Microbicide Gel Formulation Containing IQP-0528 and Tenofovir for the Prevention of HIV Infection”

At the Microbicides 2012 meeting held in Sydney, Australia, ImQuest BioSciences presented the results of two projects in formulation development for novel microbicides.  The first project entitled “Development of a Combination Microbicide Gel Formulation Containing IQP-0528 and Tenofovir for the Prevention of HIV Infection” presented the results of the formulation of a dual combination gel involving Tenofovir and the ImQuest drug IQP-0528.  The results of the project, also published in the Journal of Pharmaceutical Sciences, showed the quantitative assessment of the various combination gel formulations to identify a lead combination IQP-0528 and tenofovir gel formulation that has significant potential to prevent infection of HIV-1. The promising development of the combination gel formulation warrants further development and is in preparation for animal safety and efficacy trials.  The second presented project entitled “A Nanoparticle Based Targeted Drug Delivery System for a Combination Microbicide Product” detailed the results nanoparticle drug delivery system that can actively target HIV areas of infection and selectively delivery a combination of drugs. Targeted nanoparticles are a potential formulation strategy for combination microbicide delivery.  These results demonstrate that IQP-0528 can be readily encapsulated and ISIS5320 can be conjugated to pH labile tethers onto targeting nanoparticles.   The novel construction of the TDDS also allows for the modular substitution of the targeting ligand and both microbicides suggesting that such controlled targeted delivery system may be advantageous and necessary in microbicide delivery.


Review Manuscript: An Algorithm for the Preclinical Development of Anti-HIV Topical Microbicides

Dr. Robert W. Buckheit Jr., President and CEO and Karen W. Buckheit, Director of Topical Microbicide and STI Research have published a review article on entitled “An Algorithm for the Preclinical Development of Anti-HIV Topical Microbicides” in Current HIV Research (PMID:22264051, January 13, 2012).  The article addressed the current algorithms and the need for more robust and predictive preclinical assays as part of the in vitro algorithms.


Publication in Antimicrobial Agents and Chemotherapy: Development of Dual-Acting Pyrimidinediones as Novel and Highly Potent Topical Anti-HIV Microbicides

Karen W. Buckheit, Director of Topical Microbicide Development and STI Research has published a manuscript with co-authors Dr. Robert W. Buckheit Jr. and Dr. Lu Yang entitled “Development of Dual-Acting Pyrimidinediones as Novel and Highly Potent Topical Anti-HIV Microbicides” which was published in Antimicrobial Agents and Chemotherapy (2011, 55(11), 5243-5254, PMCID:  3195032).  The data presented therein discusses the activity of 12 pyrimindinedione molecules in specific HIV microbicide assays and justifies a rationale for the continued development of IQP-0528 as the lead microbicide candidate.  The data generated was supported by a NIH Phase I Small Business grant that was won by Dr. Buckheit in 2008.


National AAPS Presentation: Transdermal Films for the Delivery of HIV Therapeutics

In 2010, Dr. Ham was awarded a Phase I SBIR grant to develop transdermal films for the delivery of HIV therapeutics. ImQuest Biosciences developed a transdermal patch which releases more than 96 percent of the HIV medication over the course of seven days.  “As we enter the fourth decade of HIV/AIDS, this new delivery method will hopefully reduce the numerous pills most HIV patients have to take daily,” said lead researcher Anthony Ham. “Taking medicines regularly reduces symptoms in HIV patients and extends lives. The transdermal patch offers an easier option for patients to comply with their medication regimes as compared to current treatments.” With an estimated 15 million people living with HIV in developing countries and only 5.3 million people with access to treatment, this offers a more affordable and accessible way to address this unmet medical need. The research was presented at the National AAPS meeting in Washington, D.C.


Publication in Antiviral Research: PYDs in Combination with Approved Anti-HIV Drugs

Tracy Hartman, Director of Anti-Infective Research, has published a manuscript with co-authors Dr. Robert W. Buckheit Jr. and Dr. Lu Yang entitled “Antiviral Interactions of Combinations of Highly Potent 2,4(1H,3H)-pyrimidinedione congeners and Other Anti-HIV Agents” which was published in Antiviral Research (2011, 92, p.505-508).  The data discussed the identification of seven lead pyrimindinedione molecules from a SAR evaluation and suggests excellent potential as candidates for combination therapy with other approved HIV inhibitors of varying mechanism of action.  The data generated was supported by a NIH Phase I Small Business grant that was won by Dr. Buckheit in 2008.


ICAR Presentation: In Vitro Cytoprotection Assay for Identifying Inhibitors of Xenotropic Murine Leukemia-Related Virus

Tracy Hartman, Director of Anti-Infective Research, presented a poster entitled “In Vitro Cytoprotection Assay for Identifying Inhibitors of Xenotropic Murine Leukemia-Related Virus” at the 2011 International Conference for Antiviral Research (ICAR) in Sofia, Bulgaria.  The data presented included the protocol optimization for evaluating inhibitors of Xenotropic Murine Leukemia-Related Virus (XMRV) in a PG-4 cell-based cytoprotection assay and inhibition data for twenty-three drugs approved for use in humans.


ICAR Presentation/MIP V Grant: Development of Antimicrobial Peptides as Topical Microbicides for the Prevention of HIV

Karen Watson, Director of Topical Microbicide and STI Research, presented a poster entitled “Development of Antimicrobial Peptides as Topical Microbicides for the Prevention of HIV” at the 2011 International Conference for Antiviral Research (ICAR) in Sofia, Bulgaria.  The work was performed in collaboration with Dr. Guangshun Wang and the University of Nebraska and details the chemical and biological characterization of lead antimicrobial peptides that are being designed to be used as vaginal and/or rectal microbicides for the prevention of HIV.  The work was funded by a Microbicide Innovation Program grant won by Dr. Robert W. Buckheit, Jr. and Dr. Wang in 2010.  This work is also described in a publication by Wang, Buckheit and Watson titled, “Identification of Novel Human Immunodeficiency Virus Type-1 Inhibitory Peptides Based on the Antimicrobial Peptide Database” which was published in AAC (54 (3), 2010, p 1343-6 It discusses the specificity of chemical modifications to naturally occurring peptides and their effects on HIV activity.


New Hire: Dr. Mansoora Khaliq had joined ImQuest to lead our Microbiology and dengue virus program

Dr. Mansoora Khaliq had joined ImQuest to lead our Microbiology and dengue virus program. Mansoora comes from Purdue University where she did her research on dengue virus.  Her recent publications detail the analysis of inhibitors designed to bind in a hydrophobic pocket of the dengue virus envelope protein, leading to the inhibition of virus entry.  She also has a background in bacteriology and is currently the Manager of Microbiology Research.

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