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Microneedle Delivery of Zanamivir for Treatment of Influenza

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 2R44AI129122-03A1
Agency Tracking Number: R44AI129122
Amount: $2,922,334.00
Phase: Phase II
Program: SBIR
Solicitation Topic Code: NIAID
Solicitation Number: PA18-574
Timeline
Solicitation Year: 2018
Award Year: 2019
Award Start Date (Proposal Award Date): 2019-04-01
Award End Date (Contract End Date): 2022-03-31
Small Business Information
540 AVIS DR STE A
Ann Arbor, MI 48108-7906
United States
DUNS: 156551699
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 ELKE LIPKA
 (734) 223-6862
 elipka@tsrlinc.com
Business Contact
 ELKE LIPKA
Phone: (734) 663-4233
Email: elipka@tsrlinc.com
Research Institution
N/A
Abstract

Abstract
Yearly influenza epidemics strike millions of people, causing up to 500,000 deaths. Fatality caused by most
seasonal influenza viruses is andlt;0.03%, but with significant mortality in the young and the elderly populations.
When a new pathogenic influenza strain enters the population, a pandemic could kill tens of millions of people
with a negative economic impact estimated to be over 150 billion dollars. Influenza virus is a NIAID category C
priority biothreat, characterized as an emerging agent that is readily available and disseminated. Due to the
incomplete efficacy of the current vaccines, effective drug treatment is necessary. Presently, influenza treatment
is only somewhat effective, and some influenza strains are resistant to the currently marketed therapeutics,
adamantanes and the neuraminidase inhibitor Tamiflu®. However, while zanamivir (Relenza®) remains highly
active against oseltamivir-resistant influenza strains, its therapeutic impact is severely limited by its route of
administration, via oral inhalation, which renders it unsuitable for patients with a compromised respiratory
system. Therefore, development of a novel delivery alternative for zanamivir as we propose here, is poised to
address a significant unmet medical need.
Application of a transdermal microneedle (MN) delivery strategy to the anti-viral, and particularly anti-influenza,
market offers a number of solutions to large unmet medical needs, and represents an attractive market entry
strategy. Transdermal delivery systems offer a number of improvements over other delivery systems. Patches
do not require swallowing, eliminating oral side effects. Permeation through the skin allows the drug to directly
enter the systemic circulation and avoid any absorption and first-pass barriers a drug might encounter with oral
delivery. Finally, transdermal delivery avoids skin puncture by syringe needles, eliminating pain and patient visits
to a physician. Transdermal delivery of ZAN is desirable during seasonal and pandemic influenza outbreak, as
large numbers of patients can be treated and the spread of the disease can be controlled.
The Phase II portion of this proposal will involve formulation optimization and scale-up of the ZAN MN formulation
and subsequent pharmacokinetic testing in minipigs and efficacy testing in ferrets. Human dose projections will
be derived from simulation-guided PK/PD modeling and a confirmatory study in the hollow fiber infection model
(HFIM). IND-enabling dermatotoxicology studies will complete the preclinical data package. All preclinical
studies as well as the Phase I clinical development plans will be presented to the FDA during a pre-IND meeting.
The end result of this work will be a novel, transdermal delivery approach for zanamivir with demonstrated
efficacy, PK and preclinical safety data ready to open an IND application. We have assembled a team of expert
advisors and collaborators to ensure successful completion of this research plan.Project Narrative
TSRL and its collaborator F6 Pharma is developing a novel transdermal delivery product of zanamivir for the
treatment if the flu. The proposed research will establish the proof-of-concept that effective treatment of the flu
can be achieved with a patch. Completion of the work in this proposal would render the candidate ready for
clinical development.

* Information listed above is at the time of submission. *

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