Monlunabant

Monlunabant
Clinical data
Other namesINV-202, MRI-1891
Legal status
Legal status
  • Investigational
Identifiers
  • N-[(E)-N′-[(Z)-C-[(4S)-5-(4-Chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-N-[4-(trifluoromethyl)phenyl]sulfonylcarbonimidoyl]carbamimidoyl]acetamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC26H22ClF3N6O3S
Molar mass591.01 g·mol−1
3D model (JSmol)
  • CC(=O)N/C(=N/C(=N/S(=O)(=O)C1=CC=C(C=C1)C(F)(F)F)/N2C[C@@H](C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4)/N
  • InChI=1S/C26H22ClF3N6O3S/c1-16(37)32-24(31)33-25(35-40(38,39)21-13-9-19(10-14-21)26(28,29)30)36-15-22(17-5-3-2-4-6-17)23(34-36)18-7-11-20(27)12-8-18/h2-14,22H,15H2,1H3,(H3,31,32,33,35,37)/t22-/m1/s1
  • Key:GYJPQNPVIJXXTA-JOCHJYFZSA-N

Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is a peripherally selective cannabinoid receptor 1 inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by Dr George Kunos, Dr Resat Cinar, and Dr Malliga Iyer at the National Institutes of Health. It was developed as a weight loss drug by Inversago Pharma.

Novo Nordisk’s obesity drug monlunabant showed only modest weight loss in a Phase 2a trial. The drug was associated with higher rates of mild to moderate neuropsychiatric side effects like anxiety and sleep disturbances. Suicidal ideations were not reported.

See also

References

  1. ↑ Liu, Ziyi; Iyer, Malliga R.; Godlewski, Grzegorz; Jourdan, Tony; Liu, Jie; Coffey, Nathan J.; Zawatsky, Charles N.; Puhl, Henry L.; Wess, Jürgen; Meister, Jaroslawna; Liow, Jeih-San; Innis, Robert B.; Hassan, Sergio A.; Lee, Yong Sok; Kunos, George; Cinar, Resat (11 June 2021). "Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB 1 R) Antagonist". ACS Pharmacology & Translational Science. 4 (3): 1175–1187. doi:10.1021/acsptsci.1c00048. PMC 8204328. PMID 34151207.</
  2. ↑ Crater, Glenn D.; Ravenelle, Francois; Lalonde, Karine; DespréS, Jean-Pierre (20 June 2023). "431-P: Effects of CB1 Antagonist INV-202 in Patients with Metabolic Syndrome—A Randomized, Placebo-Controlled, Double-Blind Phase 1B Study". Diabetes. 72 (Supplement_1) 431-P. doi:10.2337/db23-431-P. S2CID 259384475.
  3. ↑ Morris, C.R.; Chandrasekaran, R.; Butzirius, I.; Daphtary, N.; Aliyeva, M.; Bates, J.H.T.; Anathy, V.; Crater, G.D.; Gaucher, G.; Dixon, A.E. (May 2023). "Cannabinoid Receptor 1 Inverse Agonist, INV-202, Induces Weight Loss and Reduces Airway Hyperreactivity in a Mouse Model of Obese Asthma". B15. Asthma: Hot off the Press from the Bench to the Clinic. pp. A2759. doi:10.1164/ajrccm-conference.2023.207.1_MeetingAbstracts.A2759. S2CID 258446002.
  4. ↑ Crater, Glenn D.; Lalonde, Karine; Ravenelle, François; Harvey, Michael; Després, Jean-Pierre (8 November 2023). "Effects of CB1R inverse agonist, INV -202, in patients with features of metabolic syndrome. A randomized, placebo-controlled, double-blind phase 1b study". Diabetes, Obesity and Metabolism. 26 (2): 642–649. doi:10.1111/dom.15353. PMID 37941317.
  5. ↑ Chen, Elaine (2024-09-20). "Novo's new obesity drug shows modest results, raises concerns of psychiatric side effects". STAT. Retrieved 2024-09-21.
  6. ↑ "News Details". Novo Nordisk. Retrieved 2024-09-21.