IP Library › Granted Patent US 12,268,679
Granted Patent B1
US 12,268,679 · App. 17/851,175 · Granted Apr 8, 2025

Compositions and methods for epidural administration of MCOPPB for pain relief

Inventor: James N. Campbell (Baltimore, MD)
Assignee: Centrexion Therapeutics Corporation
A61K31/444A61K9/0021
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,268,679
App. No.
17/851,175
Granted
Apr 8, 2025
Kind
B1
Abstract

The invention provides compositions and methods for epidural administration of the compound MCOPPB or a pharmaceutically acceptable salt thereof for treating pain, such as nociceptive pain suffered by an adult human.

Claims (30)

1. A method of treating a patient suffering from pain, comprising epidurally administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (i) MCOPPB or a pharmaceutically acceptable salt thereof and (ii) a pharmaceutically acceptable carrier, to thereby treat the pain.

2. The method of claim 1 , wherein the pain is chronic pain.

3. The method of claim 1 , wherein the pain is acute pain.

4. The method of claim 1 , wherein the pain is nociceptive pain.

5. The method of claim 1 , wherein the pain is neuropathic pain.

6. The method of claim 1 , wherein the pain is inflammatory pain.

7. The method of claim 1 , wherein the pain is trauma pain.

8. The method of claim 1 , wherein the pain is due to surgery.

9. The method of claim 1 , wherein the pain is postoperative pain.

10. The method of claim 1 , wherein the pain is complex regional pain syndrome.

11. The method of claim 10 , wherein the complex regional pain syndrome is reflex sympathetic dystrophy pain.

12. The method of claim 1 , wherein the pain is due to cancer.

13. The method of claim 1 , wherein the pain is due to a cancer selected from the group consisting of a solid tumor, leukemia, and lymphoma.

14. The method of claim 1 , wherein the pain is due to a cancer selected from the group consisting of a bladder cancer, breast cancer, cervical cancer, colon cancer, colorectal cancer, endometrial cancer, esophageal cancer, leukemia, lung cancer, liver cancer, skin cancer, ovarian cancer, pancreatic cancer, prostate cancer, rectal cancer, renal cancer, stomach cancer, testicular cancer, and uterine cancer.

15. The method of claim 1 , wherein the pain is arthritis pain.

16. The method of claim 1 , wherein the pain is arthritis pain selected from osteoarthritis pain and rheumatoid arthritis pain.

17. The method of claim 1 , wherein the pain is located in the patient's hand, wrist, arm, shoulder, back, hip, leg, knee, ankle, foot, or toe.

18. The method of claim 1 , wherein the pain is postoperative pain following surgery to remove prostate cancer tissue.

19. The method of claim 1 , wherein the pain is pain due to a pinched nerve, a herniated disc, or spinal stenosis.

20. The method of claim 1 , wherein the pain is back pain.

21. The method of claim 1 , wherein the pain is low back pain.

22. The method of claim 1 , wherein the pain is leg pain.

23. The method of claim 1 , wherein the pain is abdominal pain.

24. The method of claim 1 , wherein the pain is a neuropathic pain selected from the group consisting of low back pain, hip pain, leg pain, non-herpetic neuralgia, post-herpetic neuralgia, diabetic neuropathy pain, lumbosacral radiculopathy pain, nerve injury-induced pain, acquired immune deficiency syndrome (AIDS) related neuropathic pain, head trauma pain, phantom limb pain, multiple sclerosis pain, root avulsion pain, painful traumatic mononeuropathy, painful polyneuropathy, thalamic pain syndrome, post-stroke pain, central nervous system injury pain, post-surgical pain, carpal tunnel syndrome pain, trigeminal neuralgia pain, post mastectomy syndrome pain, post-thoracotomy syndrome pain, stump pain, repetitive motion pain, neuropathic pain associated hyperalgesia and allodynia, drug-induced pain, toxin-caused nerve injury pain, chemotherapy-caused nerve injury pain, and combinations thereof.

25. The method of claim 1 , wherein the method is characterized by achieving at least a 60% reduction in pain intensity relative to pain observed without administering said pharmaceutical composition.

26. The method of claim 1 , wherein the method is characterized by achieving at least an 80% reduction in pain intensity relative to pain observed without administering said pharmaceutical composition.

27. A method of locally administering MCOPPB or a pharmaceutically acceptable salt thereof to a patient, comprising epidurally administering to a patient in need thereof a pharmaceutical composition comprising (i) MCOPPB or a pharmaceutically acceptable salt thereof and (ii) a pharmaceutically acceptable carrier.

28. The method of claim 1 , wherein the administering delivers a dose of MCOPPB in the range of about 0.1 mg to 15 mg.

29. The method of claim 1 , wherein the administering delivers a dose of MCOPPB in the range of about 1 mg to 10 mg.

30. The method of claim 1 , wherein the patient is an adult human.

Assignments (2)
SECURITY INTEREST Recorded Nov 21, 2025
From: CENTREXION THERAPEUTICS CORPORATION
To: ANKURA TRUST COMPANY, LLC, AS ADMINISTRATIVE AND COLLATERAL AGENT
Reel/Frame 073683/0108 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 3, 2025
From: CAMPBELL, JAMES N.
To: CENTREXION THERAPEUTICS CORPORATION
Reel/Frame 070380/0091 →
Continuity (1)
Provisional Application 63215581 · Jun 28, 2021
References Cited (31)
US 11045459B1 · Campbell et al. · 2021 [cited by applicant]
US 20140171466A1 · Zaveri et al. · 2014 [cited by applicant]
US 20150290211A1 · Bosse et al. · 2015 [cited by applicant]
US 20150322066A1 · Tanaka et al. · 2015 [cited by applicant]
US 20160052913A1 · Bannister et al. · 2016 [cited by applicant]
US 20180228797A1 · Bosse et al. · 2018 [cited by applicant]
US 20210386728A1 · Campbell et al. · 2021 [cited by applicant]
WO WO2017066488A1 · 2017 [cited by applicant]
WO WO2019197564A1 · 2019 [cited by applicant]
Morgan, Anaesth. Intens, Care, vol. 15, pp. 60-67 (Year: 1987). [cited by examiner]
Farquhar-Smith et al, British Journal of Pain, vol. 6, No. 1, pp. 25-35, Feb. 2012. [cited by examiner]
Adler and Lotz, “Intrathecal pain management: a team-based approach,” J Pain Res. Nov. 3, 2017;10:2565-2575. [cited by applicant]
Chang et al., “Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor,” Mol Pharmacol. Sep. 2015;88(3):502-11. [cited by applicant]
Courteix et al., “Evidence for an exclusive antinociceptive effect of nociceptin/orphanin FQ, an endogenous ligand for the ORL1 receptor, in two animal models of neuropathic pain,” Pain. Jul. 2004;110(1-2):236-45. [cited by applicant]
Cowen et al., “Assessing pain objectively: the use of physiological markers,” Anaesthesia. Jul. 2015;70(7):828-47. [cited by applicant]
Dougherty and Staats, “Intrathecal drug therapy for chronic pain: from basic science to clinical practice,” Anesthesiology. Dec. 1999;91(6):1891-918. [cited by applicant]
Ferrari et al., “In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403,” Pharmacol Res Perspect. Aug. 2017;5(4):e00333. [cited by applicant]
Hayashi et al., “Discovery of 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: integrated drug-design and structure-activity relationships for orally potent, metabolically stable and pot… [cited by applicant]
Hayashi et al., “Discovery of 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: integrated drug-design and structure-activity relationships for orally potent, metabolically stable and pot… [cited by applicant]
Hayashi et al., “Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor a… [cited by applicant]
Hayashi et al., “Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of ora… [cited by applicant]
Hayashi et al., “Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of ora… [cited by applicant]
Hirao et al., “Pharmacological characterization of the newly synthesized nociceptin/orphanin FQ-receptor agonist 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole as an anxiolytic agent,” … [cited by applicant]
Kiguchi et al., “Central N/OFQ-NOP Receptor System in Pain Modulation,” Adv Pharmacol. 2016;75:217-43. [cited by applicant]
National Institutes of Health, “Complex Regional Pain Syndrome,” National Insitute of Neurological Disorders and Stroke. Jan. 2017; NIH Pub. No. 17-4173. [cited by applicant]
Pope and Deer, “Intrathecal drug delivery for pain: a clinical guide and future directions,” Pain Manag. 2015;5(3):175-83. [cited by applicant]
Rauck et al., “Intrathecal gabapentin to treat chronic intractable noncancer pain,” Anesthesiology. Sep. 2013;119(3):675-86. [cited by applicant]
U.S. Food & Drug Administration, “Clinical Outcome Assessment (COA) Compendium,” Center for Drug Evanuation and Research. Aug. 2019. [cited by applicant]
Vranken et al., “Severe toxic damage to the rabbit spinal cord after intrathecal administration of preservative-free S(+)-ketamine,” Anesthesiology. Oct. 2006;105(4):813-8. [cited by applicant]
Yaksh et al., “Toxicology profile of N-methyl-D-aspartate antagonists delivered by intrathecal infusion in the canine model,” Anesthesiology. May 2008;108(5):938-49. [cited by applicant]
Younger et al., “Pain outcomes: a brief review of instruments and techniques,” Curr Pain Headache Rep. Feb. 2009;13(1):39-43. [cited by applicant]