Movatterモバイル変換

Samelisant

From Wikipedia, the free encyclopedia

Experimental drug to treat narcolepsy

Pharmaceutical compound

Samelisant
Clinical data

Other names	SUVN-G3031
Drug class	Histamine H₃ receptor inverse agonist;Wakefulness-promoting agent
Pharmacokinetic data
Eliminationhalf-life	23-34 hours
Identifiers
IUPAC name N-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-morpholin-4-ylacetamide
CAS Number	1394808-82-2
PubChemCID	60151477
IUPHAR/BPS	10232
DrugBank	DB14835
ChemSpider	64854818
UNII	65V47O9NOP
ChEMBL	ChEMBL4297328
Chemical and physical data
Formula	C₂₁H₃₁N₃O₃
Molar mass	373.497 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1CC(C1)N2CCC(CC2)OC3=CC=C(C=C3)NC(=O)CN4CCOCC4
InChI InChI=1S/C21H31N3O3/c25-21(16-23-12-14-26-15-13-23)22-17-4-6-19(7-5-17)27-20-8-10-24(11-9-20)18-2-1-3-18/h4-7,18,20H,1-3,8-16H2,(H,22,25) Key:LNXDUSQEXVQFGP-UHFFFAOYSA-N

Samelisant (INNTooltip International Nonproprietary Name; developmental code nameSUVN-G3031) is anexperimental wakefulness-promoting agent acting as aselective histamine H₃ receptor inverse agonist which is under development for the treatment ofnarcolepsy.^[1]^[2]^[3]^[4] It was also under development for the treatment ofcognition disorders andParkinson's disease, but no recent development has been reported for these indications.^[1]^[3] As of June 2024, samelisant is inphase 2 clinical trials for the treatment of narcolepsy.^[1]^[5]

^^a ^b ^c"Samelisant - Suven Life Sciences".AdisInsight. 12 June 2024. Retrieved22 September 2024.
^Alhusaini M, Eissa N, Saad AK, Beiram R, Sadek B (2022)."Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep-Wake Cycle Disorder".Frontiers in Pharmacology.13 861094.doi:10.3389/fphar.2022.861094.PMC 9198498.PMID 35721194.
^^a ^bKonofal E (August 2024)."From past to future: 50 years of pharmacological interventions to treat narcolepsy".Pharmacology, Biochemistry, and Behavior.241 173804.doi:10.1016/j.pbb.2024.173804.PMID 38852786.
^Nirogi R, Jayarajan P, Benade V, Abraham R, Goyal VK (June 2024). "Hits and misses with animal models of narcolepsy and the implications for drug discovery".Expert Opinion on Drug Discovery.19 (6):755–768.doi:10.1080/17460441.2024.2354293.PMID 38747534.
^Nirogi R, Mudigonda K, Bhyrapuneni G, Muddana NR, Shinde A, Goyal VK, et al. (July 2020). "Safety, Tolerability, and Pharmacokinetics of SUVN-G3031, a Novel Histamine-3 Receptor Inverse Agonist for the Treatment of Narcolepsy, in Healthy Human Subjects Following Single and Multiple Oral Doses".Clinical Drug Investigation.40 (7):603–615.doi:10.1007/s40261-020-00920-8.PMID 32399853.

v t e Wakefulness-promoting agents
Catecholaminergic agents	Dopamine reuptake inhibitors (DRIs):Adrafinil^‡ Armodafinil Mesocarb^‡ Modafinil Phenylpiracetam (fonturacetam) Norepinephrine reuptake inhibitors (NRIs):Atomoxetine Desipramine Reboxetine Viloxazine Norepinephrine–dopamine reuptake inhibitors (NDRIs):Amineptine^‡ Bupropion Dexmethylphenidate Methylphenidate Nomifensine^‡ Serdexmethylphenidate Solriamfetol Serotonin–norepinephrine–dopamine reuptake inhibitors (SNDRIs):Mazindol Norepinephrine releasing agents (NRAs):Ephedrine Pseudoephedrine Selegiline (via metabolites) Norepinephrine–dopamine releasing agents (NDRAs):Amphetamine Dextroamphetamine Levoamphetamine^‡ Lisdexamfetamine Methamphetamine Mixed amphetamine salts Pemoline^‡
Orexin receptor agonists	Alixorexton^§ Danavorexton^§ Firazorexton^§ Oveporexton^†
Histamine H₃ receptor antagonists	Pitolisant Samelisant^§
Adenosine receptor antagonists	Caffeine Istradefylline Paraxanthine
Others	GABA_A receptor antagonists andnegative allosteric modulators (e.g.,clarithromycin,flumazenil,pentylenetetrazol (pentetrazol)) GABA_B receptor agonists (e.g.,sodium oxybate/γ-hydroxybutyrate (GHB)) (viaimproved nightly sleep) Nicotinic acetylcholine receptor agonists (e.g.,nicotine)
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III
See also:Stimulants List of investigational narcolepsy and hypersomnia drugs

Agonists

Antagonists

Agonists	Amthamine Betazole Dimaprit Histamine HTMT Impromidine L-Histidine UR-AK49
Antagonists	Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine (loxtidine) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine (quisultidine) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine

Agonists	α-Methylhistamine BP 2.94 Cipralisant (GT-2331) GT-2203 (VUF-5296) Histamine Imetit Immepip Immethridine (BP-1-5375) L-Histidine Methimepip Proxyfan SCH-50971 VUF-5297
Antagonists	A-349821 A-423579 ABT-239 ABT-652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK-189254 Impentamine Iodophenpropit Irdabisant JNJ-5207852 NNC 38-1049 PF-03654746 Pitolisant SCH-79687 Thioperamide VUF-5681

Agonists	4-Methylhistamine α-Methylhistamine Histamine L-Histidine OUP-16 VUF-8430
Antagonists	JNJ-7777120 Mianserin Seliforant Thioperamide Toreforant VUF-6002

See also: Receptor/signaling modulators; Monoamine metabolism modulators; Monoamine reuptake inhibitors

Thispharmacology-related article is astub. You can help Wikipedia byexpanding it.

Hidden categories: