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. Author manuscript; available in PMC: 2021 Feb 24.
Published in final edited form as: Expert Opin Drug Metab Toxicol. 2020 Feb 24;16(2):125–141. doi: 10.1080/17425255.2020.1721458

Table 4: Abuse deterrent formulations and mechanisms of action.

Abuse-Deterrent Technique: 1. Physical or 2. chemical barrier to resist mechanical alternation of medication. 3. Agonist/antagonist combination to reduce opioid-induced euphoria if the orally administered medication is used via nasal/IV route; 4. Aversive substances that decrease drug appeal for unintended uses. 5. Novel delivery system that makes manipulation difficult once administered. 6. New prodrug formulation.

Works Cited Pharmaceutical Formulation Medication component FDA approval ADF label US availability Abuse-Deterrent Technique Comment
1 2 3 4 5 6
7 Egalet Corporation / Acura Pharmaceuticals Oxaydo Oxycodone IR 2015 ✓ ✓ ✓ viscous gel forming agent deter IV abuse. Aversive agent cause nasal irritation to deter IN abuse
5 SpecGx / Mallinckrodt plc Roxicodone Oxycodone IR none ✓ ✓ ✓ ✓ Physical manipulation resistant. viscous gel forming agent deter IV abuse. Aversive agent cause nasal irritation to deter IN abuse
18 Daiichi Sankyo Company, Limited RoxyBond Oxycodone IR 2017 N/A ✓ ✓ Physical manipulation resistant. Chemical extraction and dosage dumping hindered.
8,9 Acura Pharmaceuticals, Inc LTX01 & LTX 02 Oxycodone IR none N/A When ingest in large quantities, micro-particle ingredients bind tablet matrix to slow the release of active ingredients. Insoluble nasally.
19 Acura Pharmaceuticals Acuracet Oxycodone IR + niacin + APAP none N/A ✓ ✓ viscous gel forming agent deter IV abuse. Aversive agent cause nasal irritation to deter IN abuse
20 Acura Pharmaceuticals / King Pharmaceuticals Acurox with niacin Oxycodone IR + niacin none N/A ✓ ✓ viscous gel forming agent deter IV abuse. Aversive agent cause nasal irritation to deter IN abuse
1, 2, 3, 21 Purdue Pharma OxyContin Oxycodone ER 2010 ✓ ✓ ✓ Physical manipulation resistant. viscous gel forming agent deter IV abuse.
2, 21 Collegium pharmacetuical Xtampza ER Oxycodone ER 2016 ✓ ✓ ✓ Microspheres with physical manipulation resistance. Chemical extraction and dosage dumping hindered.
21 Pain Therapeutics Remoxy Oxycodone ER none N/A ✓ ✓ Hard gelatin capsule containing viscous liquid
21 Pfizer Troxyca ER Oxycodone ER + naltrexone 2016 N/A ✓ naltrexone is released to counteract the effects of oxycodone.
2, 21 Purdue Pharma Targiniq ER Oxycodone ER + naloxone 2014 N/A ✓ ✓ Physical manipulation resistant and naltrexone is released to counteract the effects of oxycodone.
21 Labopharm/Paladin DDS-08B Oxycodone ER + APAP none N/A ✓ Drug still is released slowly even after manipulation
21 Collegium Pharmaceuticals COL-003 Oxycodone SR none N/A ✓ Deters multiparticulate matrix with partcles in waxy excipient base
21 Collegium Pharmaceuticals COL-172 Oxycodone SR none N/A ✓ Multiparticulate matrix with partcles in waxy excipient base
21 Intellipharmaceutics ReXista Oxycodone SR none N/A ✓ No further description
21 Albert Einstein College of Medicine oxytrex Oxycodone + naltrexone none N/A ✓ Ultra-low dose naltrexone
21 Elite Pharmaceuticals OxyNal Oxycodone SR + naltrexone none N/A ✓ naltrexone release when crushed
12 New River Pharmaceuticals NRP 369 Oxycodone none N/A ✓ conditional bioreversible derivative. Lysine-modified
8,9 Acura Pharmaceuticals, Inc LTX-03 Hydorcodone IR + APAP none N/A ✓ When ingest in large quantities, micro-particle ingredients bind tablet matrix to slow the release of active ingredients. Insoluble nasally.
21 Acura Pharmaceuticals, Inc Vycavert Hydrocodone IR + APAP none N/A ✓ No further description
2 Purdue Pharma Hysingla ER Hydrocodone ER 2014 ✓ ✓ ✓ Physical manipulation resistant. Chemical extraction and dosage dumping hindered.
2 Teva Pharmaceuticals Vantrela ER Hydrocodone ER 2017 N/A ✓ ✓ Physical manipulation resistant. Chemical extraction and dosage dumping hindered.
21 Egalet Corporation Egalet Hydrocodone Hydrocodone ER none N/A ✓ Non-erodible shell that is water-impermeable with erodible matrix cover
11 New River Pharmaceuticals NRP 290 Hydrocodone none N/A ✓ conditional bioreversible derivative. Lysine-modified
2 Alpharma Embeda Morphine ER + naltrexone 2014 ✓ ✓ ✓ Sequesttered naltrexone core surrounded by morphine
2 Daiichi Sankyo Company, Limited MorphaBond Morphine ER 2015 ✓ ✓ ✓ Physical manipulation resistant. Chemical extraction and dosage dumping hindered.
2 Egalet Corporation Arymo ER Morphine ER 2017 N/A ✓ ✓ Physical manipulation resistant. viscous gel forming agent deter IV abuse.
10 Egalet Corporation ADPREM Morphine none N/A ✓ Non-erodible shell water-impermeable with erodible matrix cover
21 TheraQuest Biosciences TQ-1017 Tramadol ER none N/A ✓ Hydration creates viscous substance
21 TheraQuest Biosciences TQ-1015 Oxycodone ER none N/A ✓ Physical manipulation resistant.
13 Collegium Pharmaceuticals Nucynta ER Tapentadol ER 2011 ✓ ✓ Physical manipulation resistant.
21 Neuromed/Covidien Exalgo ER Hydromorphone ER 2010 ✓ ✓ Osmotic delivery system / OROS push-pull technology
8,9 Acura Pharmaceuticals, Inc LTX-04 Hydromorphone IR none N/A When ingest in large quantities, micro-particle ingredients bind tablet matrix to slow the release of active ingredients. Insoluble nasally.
16 Titan Pharmaceuticals Inc Probuphine Buprenorphine 2016 ✓ ✓ Subcutaneous implant
17 neuromed/Covidien Sublocade Buprenorphine 2017 ✓ ✓ Subcutaneous implant
15 Reckitt Benckiser Suboxone Film Buprenorphine + naloxone none N/A ✓ Injection with suboxone will cause withdrawal signs and symptoms from naloxone
4 Endo Pharmaceuticals Opana ER Oxymorphone none ✓ ✓ ✓ Physical manipulation resistant. Gelling agent resist IV abuse.
21 TheraQuest Biosciences TQ1020 Levorphanol ER none N/A ✓ No further description
21 Sanofi-Aventis Talwin Pentazocine + naloxone none N/A ✓ naltrexone release with IV administration
6 Nektar Therapeutics NKTR-181 none N/A ✓ Long acting selective mu-opioid agonist with reduced rate of CNS permeability. FDA rejected its NDA application on 1/2020.
22 Trevena TRV250 Ongoing study N/A G-protein selective agonist at delta receptor.
22 Trevena TRV734 Ongoing study N/A G-protein selective agonist at delta receptor.
22 Trevena TRV045 Ongoing study N/A Novel non-opioid S1P receptor stimulation in modulating neurotransmission and membrane excitability without immune-suppression

Note: IR: Immediate release. ER: Extended release. SR: Sustained release. APAP: acetaminophen.

Reference:

1

Timeline of Selected FDA Activities and Significant Events Addressing Opioid Misuse and Abuse. (2019, September 25). In U.S. Food & Drug Administration. Retrieved from https://www.fda.gov/drugs/information-drug-class/timeline-selected-fda-activities-and-significant-events-addressing-opioid-misuse-and-abuse

2

Litman, R. S., Pagan, O. H., & Cicero, T. J. (2018, May). Abuse-deterrent Opioid Formulations. Anesthesiology, 128(5), 1015–1026.

3

U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). (2017, November). In U.S. Food & Drug Administration. Retrieved from https://www.fda.gov/media/96643/download

13

Nucynta ER abuse profile: an evaluation of abuse and route of administration among individuals receiving substance abuse treatment.

14

NECEPAC ADF Draft

21

Raffa, R.B. Designing Opioids That Deter Abuse.