Phase 1 study demonstrating ability of intravaginal ring to deliver large molecular weight peptide published

Juniper Pharmaceuticals, Inc., a women's health therapeutics company, has announced that the Journal of Controlled Release has published the results of the first proof of concept study to explore the ability of Juniper's intravaginal ring ("IVR") to successfully deliver larger molecules, including peptides and proteins. The article reports that the unique technology of Juniper's IVR differs from all of the five commercially available transvaginal rings.

"Therapies based on peptides are notoriously difficult to deliver and typically cannot be taken orally," said principal investigator Alexa B. Kimball, MD, MPH, Massachusetts General Hospital and Harvard Medical School. "This study demonstrates the potential of a new delivery route for peptide therapeutics for women. To further explore transvaginal absorption capabilities, future studies will need to examine larger molecules and the administration of these molecules for longer periods of time and in larger numbers of women."

The publication, "A novel approach to administration of peptides in women: Systemic absorption of a GnRH agonist via transvaginal ring delivery system," explored the ability of Juniper's IVR to deliver the nine amino acid peptide leuprolide, a Gonadotropin Releasing Hormone agonist (GnRHa) which is sold commercially as an injectable under the brand names Eligard and Lupron for the treatment of precocious puberty, prostate cancer, infertility, fibroids, and endometriosis.

In this clinical trial, six normal healthy female volunteers underwent administration of 18 or 36mg of leuprolide via Juniper's novel ethylene vinyl acetate intravaginal ring drug delivery system. Consistent with the biologic activity representative of the leuprolide entering the circulation, serum levels rose within eight hours following insertion and was dose dependent. GnRHa biological activity was validated by secretion of gonadotropins and sex steroids.

These results demonstrate that the non-keratinized vaginal epithelium permits a rapid absorption of a biologically active peptide, and that there is significant potential for a novel transvaginal drug delivery system to deliver peptides and possibly other macromolecules, such as proteins, CRISPR therapeutics, siRNA, mRNA, monoclonal antibodies, therapeutically.

"A self-administered vaginal ring provides patients with a simplified drug delivery system and should improve compliance and therefore treatment effectiveness," said Bridget A. Martell, MA, MD, Chief Medical Officer of Juniper Pharmaceuticals.

Co-authors of the paper include renowned scientists Robert Langer, ScD, from the Massachusetts Institute of Technology, William F. Crowley, MD, from Massachusetts General Hospital and Harvard Medical School, and Eyal S. Ron, PhD, who is now chief technology officer of Gelesis; each contributed to the development of the technology.

Peptides cannot typically be given orally because they are broken down in the stomach before they are readily absorbed. While the skin is an attractive way to deliver medications, its superb intrinsic barrier function often makes this route untenable, especially for larger peptides and proteins, and can be a barrier to compliance for some patients since transdermal patches need to be changed more than once weekly. The vaginal epithelium, in contrast, is not keratinized and can allow absorption of other molecules. Juniper's IVR technology also allows sustained delivery over time - from weeks to months. In addition, this vaginal ring can hold one to two orders of magnitude more drug than transdermal patches, greatly expanding the number and types of drugs that can be delivered and extending the duration of use from a single dose.

About Juniper's Intravaginal Ring

Juniper Pharmaceuticals' novel intravaginal ring ("IVR") technology leverages a pathway unique to women, the highly-vascular and non-keratinized tissue of the vaginal wall. Due to its unique polymer composition and segmentation capability, Juniper's IVR is the only single ring that has the ability to allow dosing of small and large molecular weights of multiple drugs at multiple release rates, and multiple dosages. The IVR technology allows delivery of a range molecules of various molecular weights including lipophilic and lipophobic molecules, which may offer the opportunity for this delivery system to be used for a range of therapeutics. The Company expects to file an Investigational New Drug ("IND") application for JNP-0101, its oxybutynin IVR candidate to treat overactive bladder in women, in the second half of 2016.

Article: A novel approach to administration of peptides in women: Systemic absorption of a GnRH agonist via transvaginal ring delivery system, A.B. Kimball, E. Javorsky, E.S. Ron, W. Crowley, Jr., R. Langer, Journal of Controlled Release, doi:10.1016/j.jconrel.2016.04.035, published online 26 April 2016.