Jan 12 2009, 12:01 AM EST

New Interferon Formulations Promise to Eliminate Injections in Multiple Sclerosis Treatment

MARKETWIRE

Jan 12, 2009SAN DIEGO, CAMARKET WIRE

Nerveda Inc. and Aegis Therapeutics LLC today announced preclinical results from their joint collaboration aimed at developing non-injectable formulations of the beta-interferons. The beta interferons, beta-1a (tradename Rebif(R)), and beta 1b (tradenames Betaseron(R) and Betaferon(R)) are closely related injectable protein drugs in the interferon family that are used to treat both the relapsing-remitting and secondary-progressive forms of multiple sclerosis (MS). The beta interferons are currently administered by subcutaneous injection and have been proven clinically to slow the advance of multiple sclerosis and reduce the frequency of attacks. Current worldwide combined annual sales of Rebif(R), Betaseron(R) and Betaferon(R) are approximately $4 Billion.

Because proteins are large and fragile molecules, they cannot be administered orally and are typically administered by injection. They are often subject to instability due to aggregation of the protein molecules -- particularly upon storage and handling at non-refrigerated temperatures. The resulting protein aggregates are more poorly absorbed into the blood stream upon injection due to their increased size, and induce development of circulating antibodies to interferon in patients that reduce the effectiveness of the drug over time.

Leading medical scientists at Johns Hopkins University, expert in the treatment of neurological diseases, in collaboration with Nerveda and Aegis have applied Aegis' Intravail(R) transmucosal absorption enhancement, and ProTek(R) protein stabilization technologies to address these problems and have demonstrated for the first time that the beta interferons can be administered intranasally to prevent nerve damage in preclinical animal models of multiple sclerosis. In addition, the new formulations were shown to reduce or eliminate the immunogenicity of Betaseron(R) and Rebif(R), administered either by injection or intranasally, while substantially increasing stability in a stress test involving constant agitation at elevated temperatures for extended periods of time.

Dr. Edward Maggio, Ph.D., CEO of Aegis Therapeutics, who participated in the research, said, "since interferons will continue to be the foundation of MS therapy, it is critical that non-invasive delivery options for patients be developed." Maggio also indicated, "the reduction in immunogenicity and the increase in stability also address a significant unmet need of the currently available beta-interferon therapies."

Nerveda plans to begin testing the new formulation in clinical trials in early 2009 in collaboration with clinicians and scientists at John Hopkins University Medical Center and other sites.

* Rebif(R) is a registered trademark of Pfizer, Inc.
* Betaseron(R) is a registered trademark of Bayer Healthcare Pharmaceuticals
* Betaferon(R) is a registered trademark of Bayer Schering Pharma AG
* Intravail(R) and ProTek(R) are registered trademarks of Aegis Therapeutics, LLC

continued ...

http://www.genengnews.com/news/bnite...?name=47990820

Cherie

This would be nice to not have to stab myself with the pointy things anymore.

I've been having trouble with the shots. (manual injections and the needle plunger doesnt want to let me inject. Wasting a lot of shots lately.)

I'm with you. I would love to be able to wear shorts and bathing suits without the injection markings....

Niko

I'm on Betaseron, and a lot of my injections have been burning/hurting lately. This would be fantastic for all of us who are on the injectibles.

Thanks Cherie,
I remember when I was on Copaxone and they tried an Oral trial. I was disappointed it didn't work. I hope for all those taking the injections, that they come up with a replacement oral medication.

Here is th Copaxone Trial:

Erratum in:
Lancet Neurol. 2006 May;5(5):383.

Effects of oral glatiramer acetate on clinical and MRI-monitored disease activity in patients with relapsing multiple sclerosis: a multicentre, double-blind, randomised, placebo-controlled study.

Filippi M, Wolinsky JS, Comi G; CORAL Study Group.
Neuroimaging Research Unit, Institute of Experimental Neurology and University Ospedale San Raffaele, Milan, Italy. filippi.massimo@hsr.it

BACKGROUND: Parenterally administered glatiramer acetate reduces the frequency of relapses and the formation of active brain lesions seen with MRI in multiple sclerosis. This study assessed whether two doses of glatiramer acetate given orally could improve clinical and MRI measures of inflammation and neurodegeneration in a large cohort of patients with relapsing-remitting multiple sclerosis.

METHODS: 1912 patients with relapsing-remitting multiple sclerosis were screened and 1651 were randomised to receive 50 mg or 5 mg of glatiramer acetate or placebo by daily oral administration over 14 months. The intention-to-treat cohort consisted of 1644 patients who took at least one dose of study medication (50 mg glatiramer acetate [n=543], 5 mg glatiramer acetate [n=553], placebo [n=548]).

After baseline investigation, clinical assessments were done every 2 months and MRI was obtained for all patients at baseline and at study exit. Additionally, MRI was undertaken every 2 months for a cohort of 486 patients. The primary outcome was the total number of confirmed relapses observed during the study period.

Several prespecified clinical and MRI secondary and tertiary outcomes assessed treatment efficacy on inflammation and neurodegeneration due to multiple sclerosis.

FINDINGS: The cumulative number of confirmed relapses did not differ between the two active treatment groups and the placebo group. Relative to placebo, the rate ratio for the 50 mg glatiramer acetate treated group was 0.92 (95% CI 0.77-1.08, p=0.30) and for the 5 mg glatiramer acetate treated group was 0.98 (0.83-1.15, p=0.76). No drug effect was seen for any of the secondary and tertiary endpoints. The study drug was safe and well tolerated.

INTERPRETATION: 5 mg and 50 mg glatiramer acetate administered orally on a daily basis do not affect relapse rate or other clinical and MRI parameters of disease activity and burden in patients with relapsing-remitting multiple sclerosis.

Treatment with oral formulations of glatiramer acetate at the doses tested cannot be recommended.

http://www.ncbi.nlm.nih.gov/pubmed/1...ubmed_RVDocSum

PMID: 16488376 [PubMed - indexed for MEDLINE]
Lady

Yeah, I remember that . . . but maybe the interferons will fair differently.

Wouldn't it be wonderful for people if it works out though . . .

Cherie

If it does come to be it will be at least 10 years since it is just in early animal studies, but there is hope.

Wonder what it will cost ??

Does anyone else wish they would just spend their time and money finding a formula that works better?