The article reports that in women treated with COL-1077, lidocaine was absorbed through vaginal tissue and into the systemic circulation in a dose-proportional manner, with little systemic accumulation. Plasma concentrations were 10- to 20-fold lower than those seen for intravenous lidocaine when administered for its anti-arrhythmic activity, thus demonstrating a wide safety margin for COL-1077.
"These positive PK and safety studies demonstrate that COL-1077 effectively delivered lidocaine while maintaining relatively low serum levels of the drug," said Bridget A. Martell, MA, MD, Chief Medical Officer of
The publication, "Pharmacokinetics of lidocaine and its metabolites following vaginal administration of lidocaine gel to healthy female subjects," describes single- and multiple-dose double-blind, randomized, placebo-controlled clinical trials conducted to assess the safety profile of COL-1077 and the pharmacokinetics of lidocaine and its metabolites.
In these trials, normal healthy female volunteers were randomly assigned to receive:
- 2.5% lidocaine bioadhesive vaginal gel (n=12), which delivered 37.5 mg lidocaine;
- 5% lidocaine bioadhesive vaginal gel (n=12), which delivered 75 mg lidocaine;
- 10% lidocaine bioadhesive vaginal gel (n=12), which delivered 150 mg lidocaine; or,
- Placebo bioadhesive gel (n=6).
In both studies, safety and tolerability were assessed by evaluating adverse events, vital signs, physical exams, electrocardiography (ECG), and laboratory tests.
The studies demonstrated that lidocaine was effectively absorbed systemically following administration of lidocaine vaginal gel at doses of 2.5%, 5% and 10%. Mean plasma concentrations fell in parallel fashion, with a consistent elimination half-life of approximately 10 hours following peak concentrations achieved in 6 hours.
Plasma concentrations of lidocaine at the 2.5%, 5% and 10% doses were found to be substantially lower than intravenous doses necessary for its anti-arrhythmic properties, suggesting that intravaginal lidocaine could be safely administered at the doses tested without concern for serious systemic adverse effects. In addition, minimal accumulation for lidocaine and its sequential metabolites, monoethylglycinexylidide (MEGX) and glycinexylidide (GX), was detected when lidocaine was administered daily and over four consecutive days.
COL-1077 lidocaine vaginal gel administration was found to be safe and well tolerated, with only mild or moderate adverse events reported. Additionally, there were no clinically significant laboratory, vital sign, physical exam, or ECG findings in the active dose groups of either study.
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Citation for this article: Martell BA et al. Pharmacokinetics of lidocaine and its metabolites following vaginal administration of lidocaine gel to healthy female subjects. Clin Pharmacology in Drug Devel. 2016 June 14. pii: S0168-3659(16)30249-8. doi:10.1002/cpdd.286. [Epub ahead of print]
To view the original version on PR Newswire, visit:http://www.prnewswire.com/news-releases/juniper-pharmaceuticals-announces-phase-1-studies-of-col-1077-lidocaine-vaginal-gel-published-in-peer-reviewed-scientific-journal-300286039.html
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