General Information of Drug (ID: DMBRH0Q)

Drug Name
PMID7629799C2e Drug Info
Synonyms GTPL3064; BDBM50031843
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
10339001
TTD Drug ID
DMBRH0Q

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Discontinued Drug(s)
Investigative Drug(s)
Drug(s) Targeting Squalene synthetase (FDFT1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lapaquistat acetate DMJY9CW Hyperlipidaemia 5C80 Discontinued in Phase 3 [2]
SQ-32709 DMSQRXW Arteriosclerosis BD40 Discontinued in Phase 2 [3]
BMS-187745 DMP8SIV Hyperlipidaemia 5C80 Discontinued in Phase 2 [4]
Squalestatin 1 DM4JZPT Arteriosclerosis BD40 Terminated [5]
A-87049 DMUID46 N. A. N. A. Terminated [6]
RPR-101821 DM21Y75 Arteriosclerosis BD40 Terminated [7]
SQ-34919 DMT7O9V N. A. N. A. Terminated [8]
L-735021 DM8BVJQ Discovery agent N.A. Investigative [9]
PMID19191557C32 DMH8QRI Discovery agent N.A. Investigative [4]
PMID9871507C14 DMY28QM Discovery agent N.A. Investigative [10]
⏷ 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
Squalene synthetase (FDFT1) TTFQEO5 FDFT_HUMAN Inhibitor [1]

References

1 1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate. J Med Chem. 1995 Jul 7;38(14):2596-605.
2 Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous le... Br J Pharmacol. 2008 Jul;154(5):949-57.
3 Clinical pharmacokinetics and pharmacodynamics of a new squalene synthase inhibitor, BMS-188494, in healthy volunteers. J Clin Pharmacol. 1998 Dec;38(12):1116-21.
4 Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in Staphylococcus aureus. J Med Chem. 2009 Feb 26;52(4):976-88.
5 Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo. J Biol Chem. 1992 Jun 15;267(17):11705-8.
6 (1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent ... J Med Chem. 1997 Jul 4;40(14):2123-5.
7 RPR 101821, a new potent cholesterol-lowering agent: inhibition of squalene synthase and 7-dehydrocholesterol reductase. Naunyn Schmiedebergs Arch Pharmacol. 1996 Jan;353(2):233-40.
8 Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine, Bioorg. Med. Chem. Lett. 6(12):1291-1296 (1996).
9 Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives. J Med Chem. 1994 Nov 11;37(23):4031-51.
10 Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation. Bioorg Med Chem Lett. 1998 Apr 21;8(8):891-6.