Collegium Pharmaceutical, Inc., a specialty pharmaceutical company, has released top-line results from its recently completed phase I clinical trial for Oxycodone DETERx, its extended-release, abuse-deterrent, multi-particulate product in a capsule form. The product utilizes Collegium’s DETERx technology and is designed to be more resistant to tampering and abuse than traditional formulations of the drug and is currently in phase III development.

The product’s abuse-deterrent characteristics are being evaluated in laboratory and clinical studies, consistent with the recently-issued FDA Guidance titled “Abuse-Deterrent Opioids - Evaluation and Labeling.”

The objective of the recently-completed study was to assess the safety and pharmacokinetics of Oxycodone DETERx following various tampering methods compared to two controls; Oxycodone DETERx, taken as an intact capsule, and immediate release oxycodone solution. This single dose, open-label, cross-over comparison study was conducted in 44 healthy subjects. The tampering methods used in this study are commonly employed by abusers to destroy the time-release mechanism of tablet and capsule formulations to make the drug more abusable. The two tampering techniques that were studied included opening the capsule and chewing the contents as well as crushing the contents. The selected crushing technique was previously identified in the laboratory as the most effective method of reducing the particle size of the product. In addition, chewing was studied as it a very common method of tampering that has been shown to effective in compromising the time-release of both conventional and newer, abuse-deterrent formulations.

The top-line results of the study demonstrated the following:

Both the crushed and chewed contents of DETERx capsules were bioequivalent to intact DETERx capsules in the fed state, demonstrating that crushing or chewing the contents of DETERx capsules does not alter the pharmacokinetics.

Chewing and crushing the capsule contents in either fed or fasted conditions resulted in mean Cmax values that were lower than the intact capsule when taken fed.

The mean abuse quotient (“AQ” = Cmax/Tmax) was calculated for all manipulated treatment arms. AQ values for the chewed and crushed Oxycodone DETERx were similar to when taking the product intact. The AQ for immediate release oxycodone solution was seven to 12 times higher than the AQ values for chewed or crushed Oxycodone DETERx.

The company intends to release detailed study results in the coming weeks. "The results of this study confirm the superior abuse-deterrent properties of our DETERx Technology,” said Michael Heffernan CEO, Collegium Pharmaceutical. “We are not aware of any other product that has demonstrated bioequivalent pharmacokinetics when comparing tampered with intact product. We believe this data differentiates Oxycodone DETERx from other abuse-deterrent formulations on the market and in development.”

The DETERx drug delivery platform consists of a multi-particulate matrix formulation in a capsule. While developed primarily to provide tamper-resistant properties to protect against common methods of tampering such as chewing, crushing, insufflation and extraction for IV injection, the multi-particulate design is expected to enable patients with difficulty swallowing to open the capsule and administer the contents on food or via a gastronomy tube, while maintaining the extended-release properties of the product. DETERx technology can be used with drugs that are commonly abused such as opioids and amphetamines, as well as drugs that have narrow therapeutic windows that would benefit from protection against misuse such as breaking, crushing, grinding or dissolving the product. The formulation platform is covered by US and international patents and patent applications. COL-003 is the first of a number of product candidates using the DETERx platform.

Collegium Pharmaceutical, Inc. is focused on developing a portfolio of products that incorporate its patent-protected DETERx formulation platform for the treatment of chronic pain.