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Chemical compound
Lorundrostat
Other names MLS 101
Legal status
N -(4-Acetamidocyclohexyl)-2-[4-[5-(4-methylphenyl)-1,2,4-triazin-3-yl]piperazin-1-yl]acetamide
CAS Number
PubChem
CID
ChemSpider
UNII
KEGG
ChEMBL
Formula C 24 H 33 N 7 O 2
Molar mass 451.575 g·mol−1 3D model (
JSmol )
CC1=CC=C(C=C1)C2=CN=NC(=N2)N3CCN(CC3)CC(=O)NC4CCC(CC4)NC(=O)C
InChI=1S/C24H33N7O2/c1-17-3-5-19(6-4-17)22-15-25-29-24(28-22)31-13-11-30(12-14-31)16-23(33)27-21-9-7-20(8-10-21)26-18(2)32/h3-6,15,20-21H,7-14,16H2,1-2H3,(H,26,32)(H,27,33)
Key:YHGVDZULVMINCJ-UHFFFAOYSA-N
Lorundrostat (developmental name MLS 101 ) is an
aldosterone synthase inhibitor developed by Mineralys Therapeutics for high blood pressure. In clinical trials as an add-on medication for people with uncontrolled hypertension, decreased
renin and elevated
aldosterone it significantly reduced blood pressure.
Hyperkalemia occurred in some trial participants.
[1]
[2]
[3]
[4]
^ Laffin, Luke J.; Rodman, David; Luther, James M.; Vaidya, Anand; Weir, Matthew R.; Rajicic, Natasa; Slingsby, B. T.; Nissen, Steven E.; Beasley, Richard; Budoff, Matthew; Carr, George; Carroll, Michael; Cevallos Yepez, Jose; Chhabra, Anil; Cole, Frank; Dunn, Leonard; Eaves, William; Ebuh, Valentine; Estevez, Roger; Gould, Glenn; Hong, Matthew; Iteld, Bruce; Jain, Mahendra; Kemp, Charles; Kennelly, Christina; Kleiner, Mark; Kutner, Mark; Laffin, Luke; Lambert, Joseph; Ledesma, Gilbert; Lee, Keung; Lentz, John; Lupovitch, Steven; Luther, James; Lynn, Lon; Marquez, Obadias; Mazhar, Mobeen; Morin, David; Neutel, Joel; Oppong, Yaa; Osorio, Merlin; Patron, Andres; Pharr, Walter; Ponce de Leon, Mercedes; Rodriguez-Ables, Lilia; Rosen, Jeffrey; Sachmechi, Issac; Surowitz, Ronald; Wadsworth, Larkin; Wayne, Jeffrey; Zafar, Zahid (26 September 2023).
"Aldosterone Synthase Inhibition With Lorundrostat for Uncontrolled Hypertension: The Target-HTN Randomized Clinical Trial" . JAMA . 330 (12): 1140–1150.
doi :
10.1001/jama.2023.16029 .
ISSN
0098-7484 .
PMC
10493865 .
PMID
37690061 .
^ Rodman, David; Weir, Matthew R.; Slingsby, Bt; Laffin, Luke; Nissen, Steven E. (March 2023).
"Highly Effective Blood Pressure Lowering with MLS-101, A New Aldosterone Synthase Inhibitor, in Individuals with Obesity and Raas Dysregulation" . Journal of the American College of Cardiology . 81 (8): 306.
doi :
10.1016/S0735-1097(23)00750-7 .
S2CID
257347846 .
^ Fujii, Aya; Hiraga, Yuki; Kawai, Mizue; Ogawa, Kei; Ohta, Yoshiyasu; Rahman, Sheikh Mohammed Ashfaq; Shimizu, Hidetoshi; Sugimoto-Kawabata, Kanami; Van Iersel, Mattheus (Thijs); Van Lier, Jan Jaap; Slingsby, Bt; Rodman, David (March 2023).
"First-In-Human Study of MLS-101, A Potent and Highly Selective Aldosterone Synthase Inhibitor" . Journal of the American College of Cardiology . 81 (8): 616.
doi :
10.1016/S0735-1097(23)01060-4 .
S2CID
257350703 .
^ Irfan, Hamza; Ahmed, Aliza; Nawani, Komal Devi (January 2024). "Hypertension and Lorundrostat: Key Discoveries From the TARGET-HTN Trial". Current Problems in Cardiology . 49 (1): 102144.
doi :
10.1016/j.cpcardiol.2023.102144 .
PMID
37858848 .
S2CID
264334619 .