The µ-opioid receptor (Mu opioid receptor- MOR) is an inhibitory G-protein coupled receptor, which activates the G1 alpha subunit, inhibiting adenylate cyclase activity, and lowering cAMP levels. These classes of opioid receptors have a high affinity for enkephalins and beta-endorphin. The µ-opioid receptor induces acute changes in neuronal excitability by suppressing the presynaptic release of GABA. Activation of the µ-opioid receptor by an agonist causes analgesia, sedation, nausea, euphoria, respiratory depression, miosis, and others. µ-opioid agonists are primarily used for the management of moderate to severe pain, chronic pain, post-operative pain, pain induced by cancer, and others. Takeda Pharmaceutical, Tris Pharm, AbbVie, Assertio Therapeutics, Gilead Sciences, and Ensysce Biosciences are some of the major market players in the mu-opioid agonists market, Moreover, there are drug molecules under the pipeline of various companies for other disease conditions.
Key Market Developments:
- In Oct 2022, Jiangsu Hengrui Medicine applied for preregistration for postoperative pain in China for SHR-8554, an opioid mu receptor agonist.
- In Dec 2022, Tris Pharma received a Fast Track status for Cebranopadol (TRN-228) from the US FDA.
- In Apr 2023, Trevena received patent protection for compositions and methods of use of TRV-734, an opioid mu receptor agonist, for treating drug abuse in Israel, Japan, South Korea, and Macau.
Approved Drug Molecules and Brand Names for Mu-opioid Receptor Agonists:
- Morphine sulfate
- Methadone
- Tramadol hydrochloride
- Oxycodone controlled release
- Loperamide
- Oxycodone/Acetaminophen
- Alfenta (Alfentanil)
- Pethidine
- Instanyl (Fentanyl)
- Oxycodone/Naloxone ER
- Palexia RP (Tapentadol extended release)
- Morphine extended release
- Nucynta (Tapentadol)
- 3-day Fentanyl transdermal patch
- OxiFast (Oxycodone immediate release)
- Oxytrex (Oxycodone & Naltrexone)
- Olinvyk (Oliceridine)
- Remoxy ER (extended-release Oxycodone capsules CII)
- Troxyca ER (Oxycodone/Naltrexone)
- Brixadi once-monthly depot (Buprenorphine once-monthly depot)
- Viberzi (Eluxadoline)
- Oxecta (Oxycodone)
- Xtampza ER (Oxycodone)
- Hydrocodone bitartrate
- sustained-release Oxycodone transdermal patch (TPM Oxycodone patch)
- Omnitram (Desmetramadol)
- Xartemis XR (Oxycodone and Acetaminophen CR)
- Fentanyl transdermal patch
- Oxycodone hydrochloride/aspirin
- Oxycodone hydrochloride
- ConZip (Tramadol ER)
- Ibuprofen/Oxycodone
Drugs under the Pipeline for µ-Opioid Agonists:
- Cebranopadol (TRN-228)
- AeroLEF (Fentanyl)
- Oxycodone ER (PF614)
- SHR8554
- Loxicodegol (NKTR-181)
- TRV734
- Methionine Enkephalin (STAT-401)
- nebulized Fentanyl citrate
- Oxycodone ER (Egalet-002)
- Staccato Fentanyl (AZ-003)
- Tramadol (AVE-901)
- Arymo (Morphine)
- E-58425
- JI-101
- LY03014
- TussiCaps (Hydrocodone/Chlorpheniramine)
- Celecoxib/Tramadol (YYC301)
- Etoricoxib/Tramadol
- Imrecoxib/Tramadol (HR18042)
- CEP-37440
- ETR028
- ETR029
- Fentanyl Ethypharm (Fentanyl citrate)
- MEB-1170
- ORP-101
- Viotra (Tramadol ER)
- deuterated Mitragynine (KUR-101)
- Hydromorphone once daily (CEP-33236)
Clinical Activity and Developments of Mu-opioid Receptor Agonists:
Currently, there are 62 products in the opioid mu receptor agonists, including more than 30 approved drugs in the market, and the rest of the drug molecules are in the clinical development phases.
- In Jul 2022, Kowa Pharmaceuticals America released the efficacy and adverse events data from a phase-III trial in acute pain for the drug combination Celecoxib/Tramadol.
- In Dec 2022, Tris Pharma conducted phase-III clinical trials for acute pain and back pain in the USA for Cebranopandol (TRN-228).
|
Molecule Name |
Number of Studies |
|
Cebranopadol (TRN-228) |
15 |
|
AeroLEF (Fentanyl) |
7 |
|
Oxycodone ER (PF614) |
5 |
|
SHR8554 |
5 |
|
Loxicodegol (NKTR-181) |
4 |
|
TRV734 |
4 |
|
Methionine Enkephalin (STAT-401) |
3 |
|
nebulized Fentanyl citrate |
3 |
|
Oxycodone ER (Egalet-002) |
3 |
|
Staccato Fentanyl (AZ-003) |
3 |
|
Tramadol (AVE-901) |
2 |
|
Arymo (Morphine) |
2 |
|
E-58425 |
2 |
|
JI-101 |
2 |
|
LY03014 |
2 |
|
TussiCaps (Hydrocodone/Chlorpheniramine) |
2 |
|
Celecoxib/Tramadol (YYC301) |
2 |
|
Etoricoxib/Tramadol |
2 |
|
Imrecoxib/Tramadol (HR18042) |
2 |
|
CEP-37440 |
2 |
|
ETR028 |
1 |
|
ETR029 |
1 |
|
Fentanyl Ethypharm (Fentanyl citrate) |
1 |
|
MEB-1170 |
1 |
|
ORP-101 |
1 |
|
Viotra (Tramadol ER) |
1 |
|
deuterated Mitragynine (KUR-101) |
1 |
|
Hydromorphone once daily (CEP-33236) |
1 |
Target Indication Analysis of Mu-opioid Receptor Agonists
The µ-opioid agonists such as morphine, methadone, tramadol, oxycodone, and others are primarily used in the treatment of cancer pain, opioid-related disorders, postoperative pain, and acute pain. Drug molecules like cebranopadol are in the clinical phase-III for acute pain and back pain, and in phase-II for cancer pain and neuropathic pain. Methionine Enkephalin is in phase-II for HIV infections, liver cancer, ovarian cancer, and pancreatic cancer. Celecoxib/tramadol combination drug is in phase-III for osteoarthritis. OrphoMed’s ORP-101, a buprenorphine dimer is in phase-II for irritable bowel syndrome.
Regional Analysis of Mu-opioid Receptor Agonists
Mu-opioid Receptor Agonists Market
Collegium Pharmaceuticals’s Xtampza and Nucynta ER had total sales of US$ 1,38,804 million, and 1,12,058 million respectively in 2022. Mallinckrodt Pharmaceuticals’s Xartemis XR will see all of its patent expiration by 2032. According to a report, consumption of Morphine in the year 2021 was the highest in Europe (39.4%), followed by the USA (33.4%), Australia and New Zealand (7.9%), Canada (4.5%), Japan (0.5%), and others (14.3%). According to World Drug Report 2019, about 9.3 million people in the USA misused pharmaceutical opioids which included hydrocodone (5.1 million people), oxycodone (3.2 million), and fentanyl products (0.26 million).
Latin America
Europe
Asia Pacific
Middle East
North America
Key Features of the Reports
- The report provides granular level information about the market size, regional market share, historic market (2019-2023), and forecast (2024-2030)
- The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
- The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
- The report tracks recent innovations, key developments, and start-up details that are actively working in the market
- The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
Frequently Asked Questions
Morphine sulfate, Methadone, Tramadol hydrochloride, Oxycodone controlled release, Loperamide are the few approved µ-Opioid agonists in the market.
Takeda Pharmaceutical, Tris Pharm, AbbVie, Assertio Therapeutics, Gilead Sciences, and Ensysce Biosciences are the major market players in the µ-Opioid agonists.
Major indications for µ-Opioid agonists are cancer pain, opioid-related disorders, postoperative pain, and acute pain.
There are more than 30 molecules in clinical development for µ-Opioid agonists.
- Samaritan Pharmaceutical
- Mallinckrodt Pharmaceuticals
- Takeda Pharmaceutical
- Collegium Pharmaceutical
- Tris Pharma
- AbbVie
- Assertio Therapeutics
- Gilead Sciences
- Ensysce Biosciences
- Mallinckrodt
- Immune Therapeutics
- Statera BioPharma
- Boehringer Ingelheim
- Fortress Pharmaceutical
- Elysium Therapeuctics