Monlunabant Explained

Legal Status:	Investigational
Synonyms:	INV-202, MRI-1891
Cas Number:	2712480-46-9
Pubchem:	164888943
Unii:	4G8X27X87A
Chemspiderid:	128942559
Iupac Name:	N-[(''E'')-''{{prime|N}}''-[(''Z'')-''C''-[(4''S'')-5-(4-Chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-N-[4-(trifluoromethyl)phenyl]sulfonylcarbonimidoyl]carbamimidoyl]acetamide
C:	26
H:	22
Cl:	1
F:	3
N:	6
O:	3
S:	1
Stdinchi:	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
Stdinchikey:	GYJPQNPVIJXXTA-JOCHJYFZSA-N
Smiles:	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

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.^[1] It was developed as a weight loss drug by Inversago Pharma.^{[2] [3] [4]}

Novo Nordisk’s obesity drug monlunabant showed only modest weight loss in a Phase 2a trial.^[5] The drug was associated with higher rates of mild to moderate neuropsychiatric side effects like anxiety and sleep disturbances.^[6] Suicidal ideations were not reported.

See also

• Zevaquenabant

Notes and 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 . Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB 1 R) Antagonist . ACS Pharmacology & Translational Science . 11 June 2021 . 4 . 3 . 1175–1187 . 10.1021/acsptsci.1c00048. free . 34151207 . 8204328 .
2. Crater . Glenn D. . Ravenelle . Francois . Lalonde . Karine . DespréS . Jean-Pierre . 431-P: Effects of CB1 Antagonist INV-202 in Patients with Metabolic Syndrome—A Randomized, Placebo-Controlled, Double-Blind Phase 1B Study . Diabetes . 20 June 2023 . 72 . Supplement_1 . 10.2337/db23-431-P. 259384475 .
3. Book: 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. . B15. Asthma: Hot off the Press from the Bench to the Clinic . Cannabinoid Receptor 1 Inverse Agonist, INV-202, Induces Weight Loss and Reduces Airway Hyperreactivity in a Mouse Model of Obese Asthma . May 2023 . A2759 . 10.1164/ajrccm-conference.2023.207.1_MeetingAbstracts.A2759. 258446002 .
4. Crater . Glenn D. . Lalonde . Karine . Ravenelle . François . Harvey . Michael . Després . Jean-Pierre . 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 . 8 November 2023 . 26 . 2 . 642–649 . 10.1111/dom.15353. 37941317 . free .
5. Web site: Chen . Elaine . 2024-09-20 . Novo's new obesity drug shows modest results, raises concerns of psychiatric side effects . 2024-09-21 . STAT . en-US.
6. Web site: News Details . 2024-09-21 . Novo Nordisk . en.