General Information of Drug (ID: DM9KB8A)

Drug Name
SERGOLEXOLE MALEATE Drug Info
Synonyms
LY-281067; Sergolexole maleate < Rec INNM; [trans-(8beta)]-1-Isopropyl-6-methylergoline-8-carboxylic acid 4-methoxycyclohexyl ester maleate; (9S)-4-Isopropyl-7-methyl-4,6,6abeta,7,8,9,10,10aalpha-octahydroindolo[3,4-fg]quinoline-9beta-carboxylic acid trans-4-methoxycyclohexyl ester maleate
Indication
Disease Entry ICD 11 Status REF
Migraine 8A80 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
6435752
CAS Number
CAS 108674-87-9
TTD Drug ID
DM9KB8A

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT 2A receptor (HTR2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [3]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [4]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [5]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [6]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [7]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [8]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [9]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [10]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [11]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [12]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Antagonist [2]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000706)
2 5-Hydroxytryptamine2 receptor antagonist activity of the acid metabolite (1-isopropyl dihydrolysergic acid) of the ergoline ester, sergolexole (LY281067). J Pharmacol Exp Ther. 1989 Dec;251(3):1006-11.
3 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
4 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
5 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
6 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
7 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
8 Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
10 Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
11 Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
12 Clinical pipeline report, company report or official report of Lundbeck.