Oxycodone DETERx® ER Capsules: A Review in Severe, Chronic Pain

Abstract

Oxycodone DETERx extended-release (ER) capsules (Xtampza ER), an abuse-deterrent formulation of oxycodone as the myristate salt, are approved in the USA for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate. This narrative review discusses the clinical efficacy and tolerability of the oxycodone DETERx ER capsule formulation in the management of severe pain, and provides an overview of pharmacokinetics, abuse-deterrent properties and alternative administration options. The microsphere-in-capsule DETERx drug delivery platform allows administration via sprinkle-dosing or enteral tubes. The physicochemical properties of the formulation make it difficult to manipulate and its ER pharmacokinetic profile is retained after crushing or chewing. Clinical abuse-potential studies suggest these properties may translate to reduced intranasal abuse, with implications for abuse via the oral route less certain. The efficacy of oxycodone DETERx ER in the management of moderate to severe, chronic pain was demonstrated in a well designed, phase III trial, in which it was more effective than placebo at reducing pain intensity. The formulation was generally well tolerated in this trial; the most common treatment-emergent adverse events were nausea and constipation. As an opioid, oxycodone DETERx ER carries risks of addiction, abuse and misuse. Post-marketing epidemiological studies will be necessary in determining the impact of oxycodone DETERx on oxycodone abuse liability. Nevertheless, oxycodone DETERx ER is a useful treatment option for patients with severe, chronic pain, particularly when comorbid dysphagia or difficulty swallowing is a concern.

In Vitro Drug Release After Crushing: Evaluation of Xtampza® ER and Other ER Opioid Formulations

“…Xtampza ® ER (Collegium Pharmaceutical, Inc., Canton, MA, USA) is an ER oxycodone formulation that uses the DETERx ® (Collegium Pharmaceutical, Inc., Canton, MA, USA) technology [ 15 – 17 ]. Xtampza ER is a microsphere-in-capsule formulation in which each microsphere contains oxycodone homogeneously dispersed within a hydrophobic matrix of fatty acids and waxes.…”

“…Xtampza ER is a microsphere-in-capsule formulation in which each microsphere contains oxycodone homogeneously dispersed within a hydrophobic matrix of fatty acids and waxes. Xtampza ER is designed to be abuse deterrent, with each microsphere functioning as an individual abuse-deterrent, ER, drug-delivery system [ 15 – 17 ]. Xtampza ER is the only opioid formulation available without a boxed warning against crushing or chewing [ 16 ].…”

Extended-Release Delivery Systems of Opioids: Analgesia and Dependence

“…Por otro lado, Xtampza ER® fue aprobado en 2016 y consiste en cápsulas que incorporan microesferas de liberación prolongada de hidrocodona. Xtampza ER® está formulado con la tecnología antiabuso DETERx, que se caracteriza porque cada microesfera contiene oxicodona homogéneamente dispersa dentro de una matriz hidrofóbica formada por ácidos grasos y ceras que permiten controlar la liberación de oxicodona y además son capaces de resistir el aplastamiento, la masticación, el calentamiento y la disolución, lo que dificultará la administración por vías alternativas a la oral en caso de abuso (51). Estudios in vitro han demostrado que, tras manipulación de la formulación, Xtampza ER® es capaz de mantener las propiedades de liberación prolongada en mayor medida que otras formulaciones con tecnologías antiabuso como OxyContin® (52) (63,64).…”

Oral Drug Delivery Technologies—A Decade of Developments

“…In this section of the review, we focused on 1) the innovation of the materials used to make capsules and 2) the fillings of drug complex/drug/drug conjugate/micro-or nanoformulation used for better bioavailability of the drug in the body. Scientists have scrutinized the literature for various aspects of capsule formation, such as the use of polymers (Ma, 2014;Lamb et al, 2016), and for the target delivery of drugs and for surgical treatments, such as medical robot capsules…”