Opioid Receptor Antagonist Market: Competitive Landscape, Pipeline, and Market Analysis 2024

Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are 40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain, spinal cord, peripheral neurons, and digestive tract. Four different opioid receptor systems, Mu (μ), Delta (δ), Kappa (κ), opioid receptor like-1 (ORL1), and the most commonly used opioids for pain management act on μ opioid receptor (MOR) systems. Mechanism of action (MOA) of the Opioid Receptor Antagonist is by competitive displacement of opioid molecules at receptors, as well as the blocking of opioid access to the receptor sites. The binding of opioid receptor antagonists does not activate the receptors or produce any opioid-like effects. Instead, they act as neutral antagonists, effectively preventing the activation of the receptors by agonists.

Opioid Receptor Antagonists are used in the treatment of pain management, opioid-related disorders, psychotic disorders, CNS disorders, constipation, mood disorder, neuralgia, arthritis, diabetes mellitus, spinal stenosis, fractures, migraine,  etc. Increased prevalence of chronic pain disorders and changing lifestyles, rising aging population,etc, are the key drivers for the Opioid Receptor Antagonist market. For instance, according to the Centers for Disease Control and Prevention 2023, around there were an estimated 20.9% of U.S. adults (51.6 million persons) experienced chronic pain, and 6.9% (17.1 million persons) experienced high-impact chronic pain. The introduction of newer products by market players may look for opportunities that greatly impact comprehensive research and development in Opioid Receptor Antagonists. For instance, AbbVie’s Viberzi (Eluxadoline) was launched to treat irritable bowel syndrome with diarrhea. Moreover, numerous market participants are developing innovative compounds to address the difficulties in therapy. For instance, Innoviva’s TD-1211 for the indication of constipation is under the various stages of clinical studies.

Key Market Developments:

• In March 2023, Adapt’s first Narcan (naloxone hydrochloride nasal spray) received FDA approval for over-the-counter (OTC), nonprescription use.
• In May 2023, Braeburn received FDA approval for its Brixadi (Buprenorphine) Extended Release Subcutaneous Injection for the treatment of moderate to severe opioid use disorder.

Approved Drug Molecules and Brand Names for Opioid Receptor Antagonist:

• Brixadi (Buprenorphine) Extended Release Subcutaneous Injection
• Lybalvi (Olanzapine And Samidorphan)
• Narcan (Naloxone Hydrochloride)
• Viberzi (Eluxadoline)
• Targiniq ER (Oxycodone Hydrochloride + Naloxone Hydrochloride) Extended-Release
• Tablets
• Movantik (Naloxegol)
• Symproic (Naldemedine)
• Zubsolv (Buprenorphine And Naloxone) Sublingual Tablet
• Belbuca (Buprenorphine) Buccal Film
• Entereg (Alvimopan)
• Contrave (Naltrexone Hcl And Bupropion Hcl)
• Lazanda (Fentanyl Citrate) Nasal Spray
• Troxyca ER (Oxycodone/Naltrexone)

Drugs under the Pipeline for Opioid Receptor Antagonist:

• Embeda (Morphine & Sequestered Naltrexone)
• TD-1211
• Moxduo IR (Morphine + Oxycodone)
• Bevenopran (CB-5945)
• Naltrexone Implant (OLANI)
• Naltrexone (JKB-122)
• Acetaminophen/Naltrexone (ALLOD-2)
• Baclofen/Naltrexone/Sorbitol (PXT3003)
• Evzio (Naloxone Auto-Injector)
• Kloxxado (Naloxone Intranasal Spray)
• Numorphan (Oxymorphone)
• Oxynal (Oxycodone/Naltrexone)
• Nalbuphine (PHN-131)
• Naltrexone Low Dose Delayed Burst Release (SP-104)
• Noribogaine (DMX-NB1)
• IPT-803
• Ibogaine (DMX-IB1)
• Naloxone Multidose Nasal Spray (AP003)
• Naltrexone SR Implant (BICX104)
• Naltrexone Low Dose (STAT-205)
• Sustained Release Naltrexone Implant (DLP-160)

Clinical Activity and Developments of Opioid Receptor Antagonist:

Up until July 2023, there will be about 34 companies with over 34 compounds that focus on various forms of pain and digestive disorders. For these molecules, more than 125 of  clinical trials are being conducted and majority are in phase-2, phase-3 clinical trials by the players across the globe. For instance,

• In April 2019, Pfizer has completed phase 4 study, to quantify misuse, abuse, dependence, and health resource use of extended-release Morphine Sulfate With Sequestered Naltrexone Hydrochloride (ER-MSN; EMBEDA), compared with non-abuse-deterrent extended-release Morphine (ERM) products in medicaid non-cancer patients.
• In January 2020, Adolor Corporation has completed phase 2, randomized, double-blind, placebo-controlled, study to evaluate the efficacy and safety of ADL5945 Once Daily for the treatment of opioid-induced constipation in adults taking opioid therapy for chronic noncancer pain.